Publications

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  2025 (3)
Drug repurposing in amyotrophic lateral sclerosis (ALS). Carroll, E.; Scaber, J.; Huber, K. V. M.; Brennan, P. E.; Thompson, A. G.; Turner, M. R.; and Talbot, K. EXPERT OPINION ON DRUG DISCOVERY, 20(4): 447-464. APR 3 2025.
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Structural Dynamics of the Ubiquitin Specific Protease USP30 in Complex with a Cyanopyrrolidine-Containing Covalent Inhibitor. O'Brien, D. P.; Jones, H. B. L.; Shi, Y.; Guenther, F.; Vendrell, I.; Viner, R.; Brennan, P. E.; Mead, E.; Zarganes-Tzitzikas, T.; Davis, J. B.; Pinto-Fernandez, A.; England, K. S.; Murphy, E. J.; Turnbull, A. P.; and Kessler, B. M. JOURNAL OF PROTEOME RESEARCH, 24(2): 479-490. JAN 13 2025.
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Luminescence-based complementation assay to assess target engagement and cell permeability of glycolate oxidase (HAO1) inhibitors. Mackinnon, S. R.; Zarganes-Tzitzikas, T.; Adams, C. J.; Brennan, P. E.; and Yue, W. W. BIOCHIMIE, 228: 71-81. JAN 2025.
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  2024 (7)
Identification and characterization of human KALRN mRNA and Kalirin protein isoforms. Mould, A. W.; Wright, D. J.; Bornemann, K. D.; Hengerer, B.; Pinnock, R.; Drydale, E.; Bancroft, J.; Hall, N. A. L.; von Delft, A.; Brennan, P. E.; Harrison, P. J.; Haerty, W.; and Tunbridge, E. M. CEREBRAL CORTEX, 34(12). DEC 4 2024.
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The Chemical Probes Portal-2024: update on this public resource to support best-practice selection and use of small molecules in biomedical research. Sanfelice, D.; Antolin, A. A.; Crisp, A.; Chen, Y.; Bellenie, B.; Brennan, P. E.; Edwards, A.; Mueller, S.; Al-Lazikani, B.; and Workman, P. NUCLEIC ACIDS RESEARCH, 53(D1): D1663-D1669. NOV 18 2024.
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Covalent Inhibitors of S100A4 Block the Formation of a Pro-Metastasis Non-Muscle Myosin 2A Complex. Giroud, C.; Szommer, T.; Coxon, C.; Monteiro, O.; Grimes, T.; Zarganes-Tzitzikas, T.; Christott, T.; Bennett, J.; Buchan, K.; Brennan, P. E.; and Fedorov, O. JOURNAL OF MEDICINAL CHEMISTRY, 67(21): 18943-18956. OCT 19 2024.
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Unexpected Noncovalent Off-Target Activity of Clinical BTK Inhibitors Leads to Discovery of a Dual NUDT5/14 Antagonist. Balikci, E.; Marques, A. M. C.; Bauer, L. G.; Seupel, R.; Bennett, J.; Raux, B.; Buchan, K.; Simelis, K.; Singh, U.; Rogers, C.; Ward, J.; Cheng, C.; Szommer, T.; Schutzenhofer, K.; Elkins, J. M.; Sloman, D. L.; Ahel, I.; Fedorov, O.; Brennan, P. E.; and Huber, K. V. M. JOURNAL OF MEDICINAL CHEMISTRY, 67(9): 7245-7259. APR 18 2024.
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Regulation of inositol 5-phosphatase activity by the C2 domain of SHIP1 and SHIP2. Bradshaw, W. J.; Kennedy, E. C.; Moreira, T.; Smith, L. A.; Chalk, R.; Katis, V. L.; Benesch, J. L. P.; Brennan, P. E.; Murphy, E. J.; and Gileadi, O. STRUCTURE, 32(4). APR 4 2024.
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Discovery of a Potent, Selective, and Cell-Active SPIN1 Inhibitor. Xiong, Y.; Greschik, H.; Johansson, C.; Seifert, L.; Gamble, V.; Park, K.; Fagan, V.; Li, F.; Chau, I.; Vedadi, M.; Arrowsmith, C. H.; Brennan, P.; Fedorov, O.; Jung, M.; Farnie, G.; Liu, J.; Oppermann, U.; Schuele, R.; and Jin, J. JOURNAL OF MEDICINAL CHEMISTRY, 67(7): 5837-5853. MAR 27 2024.
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Characterization of covalent inhibitors that disrupt the interaction between the tandem SH2 domains of SYK and FCER1G phospho-ITAM. Bashore, F. M.; Katis, V. L.; Du, Y.; Sikdar, A.; Wang, D.; Bradshaw, W. J.; Rygiel, K. A.; Leisner, T. M.; Chalk, R.; Mishra, S.; Williams, C. A.; Gileadi, O.; Brennan, P. E.; Wiley, J. C.; Gockley, J.; Cary, G. A.; Carter, G. W.; Young, J. E.; Pearce, K. H.; Fu, H.; Axtman, A. D.; and Ctr, E. S. S. A. PLOS ONE, 19(2). FEB 15 2024.
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  2023 (5)
Discovery of FERM domain protein-protein interaction inhibitors for MSN and CD44 as a potential therapeutic approach for Alzheimer's disease. Du, Y.; Bradshaw, W. J.; Leisner, T. M.; Annor-Gyamfi, J. K.; Qian, K.; Bashore, F. M.; Sikdar, A.; Nwogbo, F. O.; Ivanov, A. A.; Frye, V; Gileadi, O.; Brennan, P. E.; Levey, A. I.; Axtman, A. D.; Pearce, K. H.; Fu, H.; Katis, V. L.; and Ctr, E. S. S. T. A. JOURNAL OF BIOLOGICAL CHEMISTRY, 299(12). DEC 2023.
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The X-linked histone demethylases KDM5C and KDM6A as regulators of T cell-driven autoimmunity in the central nervous system. Fazazi, M. R.; Ruda, G. F.; Brennan, P. E.; and Rangachari, M. BRAIN RESEARCH BULLETIN, 202. OCT 1 2023.
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Structural Premise of Selective Deubiquitinase USP30 Inhibition by Small-Molecule Benzosulfonamides. O'Brien, D. P.; Jones, H. B. L.; Guenther, F.; Murphy, E. J.; England, K. S.; Vendrell, I.; Anderson, M.; Brennan, P. E.; Davis, J. B.; Turnbull, A. P.; Kessler, B. M.; and Pinto-Fernandez, A. MOLECULAR & CELLULAR PROTEOMICS, 22(8). AUG 2023.
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Open drug discovery in Alzheimer's disease. Axtman, A. D. E.; Brennan, P. E.; Frappier-Brinton, T.; Betarbet, R. W.; Carter, G. W.; Fu, H.; Gileadi, O. K.; Greenwood, A. K.; Leal, K. M.; Longo, F. M. M.; Mangravite, L. M. M.; Edwards, A. M. I.; Levey, I; and Ctr, E. T. ALZHEIMERS & DEMENTIA-TRANSLATIONAL RESEARCH & CLINICAL INTERVENTIONS, 9(2). APR 2023.
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Development of Selective ADAMTS-5 Peptide Substrates to Monitor Proteinase Activity. Fowkes, M. M.; Troeberg, L.; Brennan, P. E.; Vincent, T. L.; Meldal, M.; and Lim, N. H. JOURNAL OF MEDICINAL CHEMISTRY, 66(5): 3522-3539. MAR 9 2023.
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  2022 (5)
Synthesis of meta-substituted arene bioisosteres from [3.1.1]propellane. Frank, N.; Nugent, J.; Shire, B. R.; Pickford, H. D.; Rabe, P.; Sterling, A. J.; Zarganes-Tzitzikas, T.; Grimes, T.; Thompson, A. L.; Smith, R. C.; Schofield, C. J.; Brennan, P. E.; Duarte, F.; and Anderson, E. A. NATURE, 611(7937): 721+. NOV 24 2022.
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Novel Starting Points for Human Glycolate Oxidase Inhibitors, Revealed by Crystallography-Based Fragment Screening. Mackinnon, S. R.; Bezerra, G. A.; Krojer, T.; Szommer, T.; von Delft, F.; Brennan, P. E.; and Yue, W. W. FRONTIERS IN CHEMISTRY, 10. MAY 4 2022.
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Covalent fragment-based ligand screening approaches for identification of novel ubiquitin proteasome system modulators. Rothweiler, E. M.; Brennan, P. E.; and Huber, K. V. M. BIOLOGICAL CHEMISTRY, 403(4): 391-402. MAR 28 2022.
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Kalirin as a Novel Treatment Target for Cognitive Dysfunction in Schizophrenia. Mould, A. W.; Al-Juffali, N.; von Delft, A.; Brennan, P. E.; and Tunbridge, E. M. CNS DRUGS, 36(1): 1-16. JAN 2022.
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Target 2035-update on the quest for a probe for every protein. Mueller, S.; Ackloo, S.; Al Chawaf, A.; Al-Lazikani, B.; Antolin, A.; Baell, J. B.; Beck, H.; Beedie, S.; Betz, U. A. K.; Bezerra, G. A.; Brennan, P. E.; Brown, D.; Brown, P. J.; Bullock, A. N.; Carter, A. J.; Chaikuad, A.; Chaineau, M.; Ciulli, A.; Collins, I.; Dreher, J.; Drewry, D.; Edfeldt, K.; Edwards, A. M.; Egner, U.; Frye, V; Fuchs, S. M.; Hall, M. D.; Hartung, V; Hillisch, A.; Hitchcock, S. H.; Homan, E.; Kannan, N.; Kiefer, J. R.; Knapp, S.; Kostic, M.; Kubicek, S.; Leach, A. R.; Lindemann, S.; Marsden, B. D.; Matsui, H.; Meier, J. L.; Merk, D.; Michel, M.; Morgan, M. R.; Mueller-Fahrnow, A.; Owen, D. R.; Perry, B. G.; Rosenberg, S. H.; Saikatendu, K. S.; Schapira, M.; Scholten, C.; Sharma, S.; Simeonov, A.; Sundstrom, M.; Superti-Furga, G.; Todd, M. H.; Tredup, C.; Vedadi, M.; von Delft, F.; Willson, T. M.; Winter, G. E.; Workman, P.; and Arrowsmith, C. H. RSC MEDICINAL CHEMISTRY, 13(1): 13-21. JAN 27 2022.
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  2021 (8)
A phenotypic high-content, high-throughput screen identifies inhibitors of NLRP3 inflammasome activation (vol 11, 15319, 2021). Nizami, S.; Millar, V.; Arunasalam, K.; Zarganes-Tzitzikas, T.; Brough, D.; Tresadern, G.; Brennan, P. E.; Davis, J. B.; Ebner, D.; and Di Daniel, E. SCIENTIFIC REPORTS, 11(1). OCT 11 2021.
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A phenotypic high-content, high-throughput screen identifies inhibitors of NLRP3 inflammasome activation. Nizami, S.; Millar, V.; Arunasalam, K.; Zarganes-Tzitzikas, T.; Brough, D.; Tresadern, G.; Brennan, P. E.; Davis, J. B.; Ebner, D.; and Di Daniel, E. SCIENTIFIC REPORTS, 11(1). JUL 28 2021.
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The structural basis of fatty acid elongation by the ELOVL elongases. Nie, L.; Pascoa, T. C.; Pike, A. C. W.; Bushell, S. R.; Quigley, A.; Ruda, G. F.; Chu, A.; Cole, V.; Speedman, D.; Moreira, T.; Shrestha, L.; Mukhopadhyay, S. M. M.; Burgess-Brown, N. A.; Love, J. D.; Brennan, P. E.; and Carpenter, E. P. NATURE STRUCTURAL & MOLECULAR BIOLOGY, 28(6): 512+. JUN 2021.
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Chemogenomics for drug discovery: clinical molecules from open access chemical probes. Quinlan, R. B. A.; and Brennan, P. E. RSC CHEMICAL BIOLOGY, 2(3): 759-795. JUN 1 2021.
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Fragment Screening Reveals Starting Points for Rational Design of Galactokinase 1 Inhibitors to Treat Classic Galactosemia. Mackinnon, S. R.; Krojer, T.; Foster, W. R.; Diaz-Saez, L.; Tang, M.; Huber, K. V. M.; von Delft, F.; Lai, K.; Brennan, P. E.; Bezerra, G. A.; and Yue, W. W. ACS CHEMICAL BIOLOGY, 16(4): 586-595. APR 16 2021.
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Male sex chromosomal complement exacerbates the pathogenicity of Th17 cells in a chronic model of central nervous system autoimmunity. Doss, P. M. I. A.; Umair, M.; Baillargeon, J.; Fazazi, R.; Fudge, N.; Akbar, I.; Yeola, A. P.; Williams, J. B.; Leclercq, M.; Joly-Beauparlant, C.; Beauchemin, P.; Ruda, G. F.; Alpaugh, M.; Anderson, A. C.; Brennan, P. E.; Droit, A.; Lassmann, H.; Moore, C. S.; and Rangachari, M. CELL REPORTS, 34(10). MAR 9 2021.
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The Discovery and Utility of Chemical Probes in Target Discovery Preface. Brennan, P.; and Rodriguez, S. V. In Brennan, P; and Rodriguez, S., editor(s), DISCOVERY AND UTILITY OF CHEMICAL PROBES IN TARGET DISCOVERY, volume 16, of Chemical Biology, pages V-VII. 2021.
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RHO to the DOCK for GDP disembarking: Structural insights into the DOCK GTPase nucleotide exchange factors. Thompson, A. P.; Bitsina, C.; Gray, J. L.; von Delft, F.; and Brennan, P. E. JOURNAL OF BIOLOGICAL CHEMISTRY, 296. JAN-JUN 2021.
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  2020 (7)
Inhibition of the SUV4-20 H1 histone methyltransferase increases frataxin expression in Friedreich's ataxia patient cells. Vilema-Enriquez, G.; Quinlan, R.; Kilfeather, P.; Mazzone, R.; Saqlain, S.; del Molino del Barrio, I.; Donato, A.; Corda, G.; Li, F.; Vedadi, M.; Nemeth, A. H.; Brennan, P. E.; and Wade-Martins, R. JOURNAL OF BIOLOGICAL CHEMISTRY, 295(52): 17973-17985. DEC 25 2020.
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Inhibition of Histone H3K27 Demethylases Inactivates Brachyury (TBXT) and Promotes Chordoma Cell Death. Cottone, L.; Cribbs, A. P.; Khandelwal, G.; Wells, G.; Ligammari, L.; Philpott, M.; Tumber, A.; Lombard, P.; Hookway, E. S.; Szommer, T.; Johansson, C.; Brennan, P. E.; Pillay, N.; Jenner, R. G.; Oppermann, U.; and Flanagan, A. M. CANCER RESEARCH, 80(20): 4540-4551. OCT 15 2020.
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Deliberately Losing Control of C-H Activation Processes in the Design of Small-Molecule-Fragment Arrays Targeting Peroxisomal Metabolism. Khan Tareque, R.; Hassell-Hart, S.; Krojer, T.; Bradley, A.; Velupillai, S.; Talon, R.; Fairhead, M.; Day, I. J.; Bala, K.; Felix, R.; Kemmitt, P. D.; Brennan, P.; von Delft, F.; Diaz Saez, L.; Huber, K.; and Spencer, J. CHEMMEDCHEM, 15(24): 2513-2520. DEC 15 2020.
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TargetDB: A target information aggregation tool and tractability predictor. De Cesco, S.; Davis, J. B.; and Brennan, P. E. PLOS ONE, 15(9). SEP 2 2020.
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Targeting the Small GTPase Superfamily through Their Regulatory Proteins. Gray, J. L.; von Delft, F.; and Brennan, P. E. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 59(16): 6342-6366. APR 16 2020.
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Synthesis and Biological Investigation of (+)-JD1, an Organometallic BET Bromodomain Inhibitor. Hassell-Hart, S.; Runcie, A.; Krojer, T.; Doyle, J.; Lineham, E.; Ocasio, C. A.; Neto, B. A. D.; Fedorov, O.; Marsh, G.; Maple, H.; Felix, R.; Banks, R.; Ciulli, A.; Picaud, S.; Filippakopoulos, P.; von Delft, F.; Brennan, P. E.; Stewart, H. J. S.; Chevassut, T. J.; Walker, M.; Austin, C.; Morley, S.; and Spencer, J. ORGANOMETALLICS, 39(3): 408-416. FEB 10 2020.
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Chemical Strategies for Evaluating New Drug Targets. Carter, A. J.; Seupel, R.; Brennan, P. E.; Sundstrom, M.; Introini, A.; and Mueller-Fahrnow, A. In Plowright, A., editor(s), TARGET DISCOVERY AND VALIDATION: METHODS AND STRATEGIES FOR DRUG DISCOVERY, of Methods and Principles in Medicinal Chemistry, pages 1-24. 2020.
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  2019 (13)
Structural Insights into Interaction Mechanisms of Alternative Piperazine-urea YEATS Domain Binders in MLLT1. Ni, X.; Heidenreich, D.; Christott, T.; Bennet, J.; Moustakim, M.; Brennan, P. E.; Fedorov, O.; Knapp, S.; and Chaikuad, A. ACS MEDICINAL CHEMISTRY LETTERS, 10(12): 1661+. DEC 2019.
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Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1). Xiong, Y.; Greschik, H.; Johansson, C.; Seifert, L.; Bacher, J.; Park, K.; Babault, N.; Martini, M.; Fagan, V.; Li, F.; Chau, I.; Christott, T.; Dilworth, D.; Barsyte-Lovejoy, D.; Vedadi, M.; Arrowsmith, C. H.; Brennan, P.; Fedorov, O.; Jung, M.; Farnie, G.; Liu, J.; Oppermann, U.; Schuele, R.; and Jin, J. JOURNAL OF MEDICINAL CHEMISTRY, 62(20): 8996-9007. OCT 24 2019.
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A Chemical Probe for Tudor Domain Protein Spindlin1 to Investigate Chromatin Function. Fagan, V.; Johansson, C.; Gileadi, C.; Monteiro, O.; Dunford, J. E.; Nibhani, R.; Philpott, M.; Malzahn, J.; Wells, G.; Faram, R.; Cribbs, A. P.; Halidi, N.; Li, F.; Chau, I.; Greschik, H.; Velupillai, S.; Allali-Hassani, A.; Bennett, J.; Christott, T.; Giroud, C.; Lewis, A. M.; Huber, K. V. M.; Athanasou, N.; Bountrat, C.; Jung, M.; Schuele, R.; Vedadi, M.; Arrowsmith, C.; Xion, Y.; Jin, J.; Fedorov, O.; Farnie, G.; Brennan, P. E.; and Oppermann, U. JOURNAL OF MEDICINAL CHEMISTRY, 62(20): 9008-9025. OCT 24 2019.
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C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays. Le Bihan, Y.; Lanigan, R. M.; Atrash, B.; McLaughlin, M. G.; Velupillai, S.; Malcolm, A. G.; England, K. S.; Ruda, G. F.; Mok, N. Y.; Tumber, A.; Tomlin, K.; Saville, H.; Shehu, E.; McAndrew, C.; Carmichael, L.; Bennett, J. M.; Jeganathan, F.; Eve, P.; Donovan, A.; Hayes, A.; Wood, F.; Raynaud, F. I.; Fedorov, O.; Brennan, P. E.; Burke, R.; van Montfort, R. L. M.; Rossanese, O. W.; Blagg, J.; and Bavetsias, V. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 177: 316-337. SEP 1 2019.
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A genetics-led approach defines the drug target landscape of 30 immune-related traits. Fang, H.; Beckmann, G.; Bountra, C.; Bowness, P.; Burgess-Brown, N.; Carpenter, L.; Chen, L.; Damerell, D.; Egner, U.; Fujii, R.; Howe, T.; Jakobsson, P.; Katopodis, A.; Knight, J. C.; Marsden, B. D.; De Martino, J.; Matthias, G.; McVean, G.; Mueller-Fahrnow, A.; Malarstig, A.; O'Callaghan, C. A.; Ostermann, N.; Paez-cortez, J. R.; Peeters, P. J.; Prinz, F.; Soulard, P.; Sundstrom, M.; Yabuki, C.; Vlach, J.; De Wolf, H.; Knezevic, B.; Burnham, K. L.; Osgood, J.; Sanniti, A.; Lara, A. L.; Kasela, S.; De Cesco, S.; Wegner, J. K.; Handunnetthi, L.; McCann, F. E.; Sekine, T.; Brennan, P. E.; Sundstrom, Y.; Milani, L.; Berg, L.; Gohlmann, H. W.; Fairfax, B. P.; and Consortium, U. NATURE GENETICS, 51(7): 1082+. JUL 2019.
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Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening. Resnick, E.; Bradley, A.; Gan, J.; Douangamath, A.; Krojer, T.; Sethi, R.; Geurink, P. P.; Aimon, A.; Amitai, G.; Bellini, D.; Bennett, J.; Fairhead, M.; Fedorov, O.; Gabizon, R.; Gan, J.; Gu, J.; Plotnikov, A.; Reznik, N.; Ruda, G. F.; Diaz-Saez, L.; Straub, V. M.; Szommer, T.; Velupillai, S.; Zaidman, D.; Zhang, Y.; Coker, A. R.; Dowson, C. G.; Barr, H. M.; Wang, C.; Huber, K. V. M.; Brennan, P. E.; Ovaa, H.; von Delft, F.; and London, N. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 141(22): 8951-8968. JUN 5 2019.
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ALK2 inhibitors display beneficial effects in preclinical models of ACVR1 mutant diffuse intrinsic pontine glioma. Carvalho, D.; Taylor, K. R.; Olaciregui, N. G.; Molinari, V.; Clarke, M.; Mackay, A.; Ruddle, R.; Henley, A.; Valenti, M.; Hayes, A.; Brandon, A. D. H.; Eccles, S. A.; Raynaud, F.; Boudhar, A.; Monje, M.; Popov, S.; Moore, A. S.; Mora, J.; Cruz, O.; Vinci, M.; Brennan, P. E.; Bullock, A. N.; Carcaboso, A. M.; and Jones, C. COMMUNICATIONS BIOLOGY, 2. MAY 9 2019.
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Discovery of Pyrrolo[3,2-d]pyrimidin-4-one Derivatives as a New Class of Potent and Cell-Active Inhibitors of P300/CBP-Associated Factor Bromodomain. Huang, L.; Li, H.; Li, L.; Niu, L.; Seupel, R.; Wu, C.; Cheng, W.; Chen, C.; Ding, B.; Brennan, P. E.; and Yang, S. JOURNAL OF MEDICINAL CHEMISTRY, 62(9): 4526-4542. MAY 9 2019.
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A chemical toolbox for the study of bromodomains and epigenetic signaling. Wu, Q.; Heidenreich, D.; Zhou, S.; Ackloo, S.; Kraemer, A.; Nakka, K.; Lima-Fernandes, E.; Deblois, G.; Duan, S.; Vellanki, R. N.; Li, F.; Vedadi, M.; Dilworth, J.; Lupien, M.; Brennan, P. E.; Arrowsmith, C. H.; Mueller, S.; Fedorov, O.; Filippakopoulos, P.; and Knapp, S. NATURE COMMUNICATIONS, 10. APR 23 2019.
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SuCOS: A pharmacophoric-shape overlap metric for comparing binding modes. Leung, S.; Bodkin, M.; von Delft, F.; Brennan, P.; and Morris, G. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 257. MAR 31 2019. National Meeting of the American-Chemical-Society (ACS), Orlando, FL, MAR 31-APR 04, 2019
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An Activity-Based Probe Targeting Non-Catalytic, Highly Conserved Amino Acid Residues within Bromodomains. D'Ascenzio, M.; Pugh, K. M.; Konietzny, R.; Berridge, G.; Tallant, C.; Hashem, S.; Monteiro, O.; Thomas, J. R.; Schirle, M.; Knapp, S.; Marsden, B.; Fedorov, O.; Bountra, C.; Kessler, B. M.; and Brennan, P. E. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 58(4): 1007-1012. JAN 21 2019.
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Design, Synthesis and Characterization of Covalent KDM5 Inhibitors. Vazquez-Rodriguez, S.; Wright, M.; Rogers, C. M.; Cribbs, A. P.; Velupillai, S.; Philpott, M.; Lee, H.; Dunford, J. E.; Huber, K. V. M.; Robers, M. B.; Vasta, J. D.; Thezenas, M.; Bonham, S.; Kessler, B.; Bennett, J.; Fedorov, O.; Raynaud, F.; Donovan, A.; Blagg, J.; Bavetsias, V.; Oppermann, U.; Bountra, C.; Kawamura, A.; and Brennan, P. E. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 58(2): 515-519. JAN 8 2019.
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Chemical Probes. Donner, A.; King, H.; Brennan, P. E.; Moustakim, M.; and Zuercher, W. J. In Sippl, W; and Jung, M, editor(s), EPIGENETIC DRUG DISCOVERY, pages 133-152. 2019.
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  2018 (9)
Structure-Based Approach toward Identification of Inhibitory Fragments for Eleven-Nineteen-Leukemia Protein (ENL). Heidenreich, D.; Moustakim, M.; Schmidt, J.; Merk, D.; Brennan, P. E.; Fedorov, O.; Chaikuad, A.; and Knapp, S. JOURNAL OF MEDICINAL CHEMISTRY, 61(23): 10929-10934. DEC 13 2018.
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Discovery of an MLLT1/3 YEATS Domain Chemical Probe. Moustakim, M.; Christott, T.; Monteiro, O. P.; Bennett, J.; Giroud, C.; Ward, J.; Rogers, C. M.; Smith, P.; Panagakou, I.; Diaz-Saez, L.; Felce, S. L.; Gamble, V.; Gileadi, C.; Halidi, N.; Heidenreich, D.; Chaikuad, A.; Knapp, S.; Huber, K. V. M.; Farnie, G.; Heer, J.; Manevski, N.; Poda, G.; Al-awar, R.; Dixon, D. J.; Brennan, P. E.; and Fedorov, O. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 57(50): 16302-16307. DEC 10 2018.
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Bench-Stable Transfer Reagent Facilitates the Generation of Trifluoromethyl-sulfonimidamides. Wright, M.; Martinez-Lamenca, C.; Leenaerts, J. E.; Brennan, P. E.; Trabanco, A. A.; and Oehlrich, D. JOURNAL OF ORGANIC CHEMISTRY, 83(16): 9510-9516. AUG 17 2018.
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Discovery of a novel allosteric inhibitor scaffold for polyadenosine-diphosphate-ribose polymerase 14 (PARP14) macrodomain 2. Moustakim, M.; Riedel, K.; Schuller, M.; Gehring, A. P.; Monteiro, O. P.; Martin, S. P.; Fedorov, O.; Heer, J.; Dixon, D. J.; Elkins, J. M.; Knapp, S.; Bracher, F.; and Brennan, P. E. BIOORGANIC & MEDICINAL CHEMISTRY, 26(11): 2965-2972. JUL 15 2018.
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Halogen-Aromatic Interactions Modulate Inhibitor Residence Times. Heroven, C.; Georgi, V.; Ganotra, G. K.; Brennan, P.; Wolfreys, F.; Wade, R. C.; Fernandez-Montalvan, A. E.; Chaikuad, A.; and Knapp, S. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 57(24): 7220-7224. JUN 11 2018.
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Identifying Small-Molecule Binding Sites for Epigenetic Proteins at Domain-Domain Interfaces. Bowkett, D.; Talon, R.; Tallant, C.; Schofield, C.; von Delft, F.; Knapp, S.; Bruton, G.; and Brennan, P. E. CHEMMEDCHEM, 13(10): 1051-1057. MAY 23 2018.
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Mild, calcium catalysed Beckmann rearrangements. Kiely-Collins, H. J.; Sechi, I.; Brennan, P. E.; and McLaughlin, M. G. CHEMICAL COMMUNICATIONS, 54(6): 654-657. JAN 18 2018.
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Target Identification Using Chemical Probes. Moustakim, M.; Felce, S. L.; Zaarour, N.; Farnie, G.; McCann, F. E.; and Brennan, P. E. In Lesburg, C., editor(s), MODERN APPROACHES IN DRUG DISCOVERY, volume 610, of Methods in Enzymology, pages 27-58. 2018.
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Principles and Applications of Fragment-based Drug Discovery for Chemical Probes. Moustakim, M.; and Brennan, P. E. In Westwood, N.; and Nelson, A, editor(s), CHEMICAL AND BIOLOGICAL SYNTHESIS: ENABLING APPROACHES FOR UNDERSTANDING BIOLOGY, volume 10, of Chemical Biology, pages 114-137. 2018.
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  2017 (12)
Discovery of a Highly Selective Cell-Active Inhibitor of the Histone Lysine Demethylases KDM2/7. Gerken, P. A.; Wolstenhulme, J. R.; Tumber, A.; Hatch, S. B.; Zhang, Y.; Mueller, S.; Chandler, S. A.; Mair, B.; Li, F.; Nijman, S. M. B.; Konietzny, R.; Szommer, T.; Yapp, C.; Fedorov, O.; Benesch, J. L. P.; Vedadi, M.; Kessler, B. M.; Kawamura, A.; Brennan, P. E.; and Smith, M. D. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 56(49): 15555-15559. DEC 4 2017.
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Selective Targeting of Bromodomains of the Bromodomain-PHD Fingers Family Impairs Osteoclast Differentiation. Meier, J. C.; Tallant, C.; Fedorov, O.; Witwicka, H.; Hwang, S.; van Stiphout, R. G.; Lambert, J.; Rogers, C.; Yapp, C.; Gerstenberger, B. S.; Fedele, V.; Savitsky, P.; Heidenreich, D.; Daniels, D. L.; Owen, D. R.; Fish, P. V.; Igoe, N. M.; Bayle, E. D.; Haendler, B.; Oppermann, U. C. T.; Buffa, F.; Brennan, P. E.; Mueller, S.; Gingras, A. C.; Odgren, P. R.; Birnbaum, M. J.; and Knapp, S. ACS CHEMICAL BIOLOGY, 12(10): 2619-2630. OCT 2017.
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Design of a Chemical Probe for the Bromodomain and Plant Homeodomain Finger-Containing (BRPF) Family of Proteins. Igoe, N.; Bayle, E. D.; Tallant, C.; Fedorov, O.; Meier, J. C.; Savitsky, P.; Rogers, C.; Morias, Y.; Scholze, S.; Boyd, H.; Cunoosarny, D.; Andrews, D. M.; Cheasty, A.; Brennan, P. E.; Mueller, S.; Knapp, S.; and Fish, P. V. JOURNAL OF MEDICINAL CHEMISTRY, 60(16): 6998-7011. AUG 24 2017.
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BRD3 and BRD4 BET Bromodomain Proteins Differentially Regulate Skeletal Myogenesis. Roberts, T. C.; Etxaniz, U.; Dall'Agnese, A.; Wu, S.; Chiang, C.; Brennan, P. E.; Wood, M. J. A.; and Puri, P. L. SCIENTIFIC REPORTS, 7. JUL 21 2017.
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Structure-Based Design of Highly Selective Inhibitors of the CREB Binding Protein Bromodomain. Denny, R. A.; Flick, A. C.; Coe, J.; Langille, J.; Basak, A.; Liu, S.; Stock, I.; Sahasrabudhe, P.; Bonin, P.; Hay, D. A.; Brennan, P. E.; Pletcher, M.; Jones, L. H.; and Chekler, E. L. P. JOURNAL OF MEDICINAL CHEMISTRY, 60(13): 5349-5363. JUL 13 2017.
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Di-iodotyrosinated peptide imaging of cartilage (DIPIC). Fowkes, M. M.; Borges, P. d. N.; Brennan, P. E.; Vincent, T. L.; and Lim, N. H. INTERNATIONAL JOURNAL OF EXPERIMENTAL PATHOLOGY, 98(3): A7. JUN 2017. Spring Meeting of the British-Society-for-Matrix-Biology (BSMB), Univ Oxford, Oxford, ENGLAND, APR 03-04, 2017
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Highly selective inhibition of histone demethylases by de novo macrocyclic peptides. Kawamura, A.; Muenzel, M.; Kojima, T.; Yapp, C.; Bhushan, B.; Goto, Y.; Tumber, A.; Katoh, T.; King, O. N. F.; Passioura, T.; Walport, L. J.; Hatch, S. B.; Madden, S.; Mueller, S.; Brennan, P. E.; Chowdhury, R.; Hopkinson, R. J.; Suga, H.; and Schofield, C. J. NATURE COMMUNICATIONS, 8. APR 6 2017.
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Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells. Tumber, A.; Nuzzi, A.; Hookway, E. S.; Hatch, S. B.; Velupillai, S.; Johansson, C.; Kawamura, A.; Savitsky, P.; Yapp, C.; Szykowska, A.; Wu, N.; Bountra, C.; Strain-Damerell, C.; Burgess-Brown, N. A.; Ruda, G. F.; Fedorov, O.; Munro, S.; England, K. S.; Nowak, R. P.; Schofield, C. J.; La Thangue, N. B.; Pawlyn, C.; Davies, F.; Morgan, G.; Athanasou, N.; Mueller, S.; Oppermann, U.; and Brennan, P. E. CELL CHEMICAL BIOLOGY, 24(3): 371-380. MAR 16 2017.
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Assessing histone demethylase inhibitors in cells: lessons learned. Hatch, S. B.; Yapp, C.; Montenegro, R. C.; Savitsky, P.; Gamble, V.; Tumber, A.; Ruda, G. F.; Bavetsias, V.; Fedorov, O.; Atrash, B.; Raynaud, F.; Lanigan, R.; Carmichael, L.; Tomlin, K.; Burke, R.; Westaway, S. M.; Brown, J. A.; Prinjha, R. K.; Martinez, E. D.; Oppermann, U.; Schofield, C. J.; Bountra, C.; Kawamura, A.; Blagg, J.; Brennan, P. E.; Rossanese, O.; and Mueller, S. EPIGENETICS & CHROMATIN, 10. MAR 1 2017.
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Design of a Biased Potent Small Molecule Inhibitor of the Bromodonnain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies. Igoe, N.; Bayle, E. D.; Fedorov, O.; Tallant, C.; Savitsky, P.; Rogers, C.; Owen, D. R.; Deb, G.; Somervaille, T. C. P.; Andrews, D. M.; Jones, N.; Cheasty, A.; Ryder, H.; Brennan, P. E.; Mueller, S.; Knapp, S.; and Fish, P. V. JOURNAL OF MEDICINAL CHEMISTRY, 60(2): 668-680. JAN 26 2017.
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Discovery of a PCAF Bromodomain Chemical Probe. Moustakim, M.; Clark, P. G. K.; Trulli, L.; de Arriba, A. L. F.; Ehebauer, M. T.; Chaikuad, A.; Murphy, E. J.; Mendez-Johnson, J.; Daniels, D.; Hou, C. D.; Lin, Y.; Walker, J. R.; Hui, R.; Yang, H.; Dorrell, L.; Rogers, C. M.; Monteiro, O. P.; Fedorov, O.; Huber, K. V. M.; Knapp, S.; Heer, J.; Dixon, D. J.; and Brennan, P. E. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 56(3): 827-831. JAN 16 2017.
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The SGC beyond structural genomics: redefining the role of 3D structures by coupling genomic stratification with fragment-based discovery. Bradley, A. R.; Echalier, A.; Fairhead, M.; Strain-Damerell, C.; Brennan, P.; Bullock, A. N.; Burgess-Brown, N. A.; Carpenter, E. P.; Gileadi, O.; Marsden, B. D.; Lee, W. H.; Yue, W.; Bountra, C.; and von Delft, F. In VanMontfort, R.; and Workman, P, editor(s), STRUCTURE-BASED DRUG DESIGN: INSIGHTS FROM ACADEMIA AND INDUSTRY, volume 61, of Essays in Biochemistry, pages 495-503. 2017.
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  2016 (16)
Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors. Popp, T. A.; Tallant, C.; Rogers, C.; Fedorov, O.; Brennan, P. E.; Mueller, S.; Knapp, S.; and Bracher, F. JOURNAL OF MEDICINAL CHEMISTRY, 59(19): 8889-8912. OCT 13 2016.
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Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia. Picaud, S.; Leonards, K.; Lambert, J.; Dovey, O.; Wells, C.; Fedorov, O.; Monteiro, O.; Fujisawa, T.; Wang, C.; Lingard, H.; Tallant, C.; Nikbin, N.; Guetzoyan, L.; Ingham, R.; Ley, S. V.; Brennan, P.; Muller, S.; Samsonova, A.; Gingras, A.; Schwaller, J.; Vassiliou, G.; Knapp, S.; and Filippakopoulos, P. SCIENCE ADVANCES, 2(10). OCT 2016.
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Exploring the role of water in molecular recognition: predicting protein ligandability using a combinatorial search of surface hydration sites. Vukovic, S.; Brennan, P. E.; and Huggins, D. J. JOURNAL OF PHYSICS-CONDENSED MATTER, 28(34). SEP 1 2016.
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Advances and challenges in understanding histone demethylase biology. Nowak, R. P.; Tumber, A.; Johansson, C.; Che, K. H.; Brennan, P.; Owen, D.; and Oppermann, U. CURRENT OPINION IN CHEMICAL BIOLOGY, 33: 151-159. AUG 2016.
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BET inhibition as a new strategy for the treatment of gastric cancer. Montenegro, R. C.; Clark, P. G. K.; Howarth, A.; Wan, X.; Ceroni, A.; Siejka, P.; Nunez-Alonso, G. A.; Monteiro, O.; Rogers, C.; Gamble, V.; Burbano, R.; Brennan, P. E.; Tallant, C.; Ebner, D.; Fedorov, O.; O'Neill, E.; Knapp, S.; Dixon, D.; and Muller, S. ONCOTARGET, 7(28): 43997-44012. JUL 12 2016.
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Structural analysis of human KDM5B guides histone demethylase inhibitor development. Johansson, C.; Velupillai, S.; Tumber, A.; Szykowska, A.; Hookway, E. S.; Nowak, R. P.; Strain-Damerell, C.; Gileadi, C.; Philpott, M.; Burgess-Brown, N.; Wu, N.; Kopec, J.; Nuzzi, A.; Steuber, H.; Egner, U.; Badock, V.; Munro, S.; LaThangue, N. B.; Westaway, S.; Brown, J.; Athanasou, N.; Prinjha, R.; Brennan, P. E.; and Oppermann, U. NATURE CHEMICAL BIOLOGY, 12(7): 539+. JUL 2016.
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Structure of the Human Protein Kinase ZAK in Complex with Vemurafenib. Mathea, S.; Azeez, K. R. A.; Salah, E.; Tallant, C.; Wolfreys, F.; Konietzny, R.; Fischer, R.; Lou, H. J.; Brennan, P. E.; Schnapp, G.; Pautsch, A.; Kessler, B. M.; Turk, B. E.; and Knapp, S. ACS CHEMICAL BIOLOGY, 11(6): 1595-1602. JUN 2016.
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Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. Gerstenberger, B. S.; Trzupek, J. D.; Tallant, C.; Fedorov, O.; Filippakopoulos, P.; Brennan, P. E.; Fedele, V.; Martin, S.; Picaud, S.; Rogers, C.; Parikh, M.; Taylor, A.; Samas, B.; O'Mahony, A.; Berg, E.; Pallares, G.; Torrey, A. D.; Treiber, D. K.; Samardjiev, I. J.; Nasipak, B. T.; Padilla-Benavides, T.; Wu, Q.; Imbalzano, A. N.; Nickerson, J. A.; Bunnage, M. E.; Muller, S.; Knapp, S.; and Owen, D. R. JOURNAL OF MEDICINAL CHEMISTRY, 59(10): 4800-4811. MAY 26 2016.
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Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex. Sutherell, C. L.; Tallant, C.; Monteiro, O. P.; Yapp, C.; Fuchs, J. E.; Fedorov, O.; Siejka, P.; Muller, S.; Knapp, S.; Brenton, J. D.; Brennan, P. E.; and Ley, S. V. JOURNAL OF MEDICINAL CHEMISTRY, 59(10): 5095-5101. MAY 26 2016.
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Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF. Bennett, J.; Fedorov, O.; Tallant, C.; Monteiro, O.; Meier, J.; Gamble, V.; Savitsky, P.; Nunez-Alonso, G. A.; Haendler, B.; Rogers, C.; Brennan, P. E.; Mueller, S.; and Knapp, S. JOURNAL OF MEDICINAL CHEMISTRY, 59(4, SI): 1642-1647. FEB 25 2016.
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Structure-Based Identification of Inhibitory Fragments Targeting the p300/CBP-Associated Factor Bromodomain. Chaikuad, A.; Lang, S.; Brennan, P. E.; Temperini, C.; Fedorov, O.; Hollander, J.; Nachane, R.; Abell, C.; Mueller, S.; Siegal, G.; and Knapp, S. JOURNAL OF MEDICINAL CHEMISTRY, 59(4, SI): 1648-1653. FEB 25 2016.
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Recent Progress in Histone Demethylase Inhibitors. McAllister, T. E.; England, K. S.; Hopkinson, R. J.; Brennan, P. E.; Kawamura, A.; and Schofield, C. J. JOURNAL OF MEDICINAL CHEMISTRY, 59(4, SI): 1308-1329. FEB 25 2016.
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8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors. Bavetsias, V.; Lanigan, R. M.; Ruda, G. F.; Atrash, B.; McLaughlin, M. G.; Tumber, A.; Mok, N. Y.; Le Bihan, Y.; Dempster, S.; Boxall, K. J.; Jeganathan, F.; Hatch, S. B.; Savitsky, P.; Velupillai, S.; Krojer, T.; England, K. S.; Sejberg, J.; Thai, C.; Donovan, A.; Pal, A.; Scozzafava, G.; Bennett, J. M.; Kawamura, A.; Johansson, C.; Szykowska, A.; Gileadi, C.; Burgess-Brown, N. A.; von Delft, F.; Oppermann, U.; Walters, Z.; Shipley, J.; Raynaud, F. I.; Westaway, S. M.; Prinjha, R. K.; Fedorov, O.; Burke, R.; Schofield, C. J.; Westwood, I. M.; Bountra, C.; Mueller, S.; van Montfort, R. L. M.; Brennan, P. E.; and Blagg, J. JOURNAL OF MEDICINAL CHEMISTRY, 59(4, SI): 1388-1409. FEB 25 2016.
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Deciphering the true antiproliferative target of an MK2 activation inhibitor in glioblastoma. Brennan, P. E. CELL DEATH & DISEASE, 7. JAN 2016.
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A poised fragment library enables rapid synthetic expansion yielding the first reported inhibitors of PHIP(2), an atypical bromodomain. Cox, O. B.; Krojer, T.; Collins, P.; Monteiro, O.; Talon, R.; Bradley, A.; Fedorov, O.; Amin, J.; Marsden, B. D.; Spencer, J.; von Delft, F.; and Brennan, P. E. CHEMICAL SCIENCE, 7(3): 2322-2330. 2016.
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Chemical probes and inhibitors of bromodomains outside the BET family. Moustakim, M.; Clark, P. G. K.; Hay, D. A.; Dixon, D. J.; and Brennan, P. E. MEDCHEMCOMM, 7(12): 2246-2264. 2016.
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  2015 (9)
Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy. Picaud, S.; Fedorov, O.; Thanasopoulou, A.; Leonards, K.; Jones, K.; Meier, J.; Olzscha, H.; Monteiro, O.; Martin, S.; Philpott, M.; Tumber, A.; Filippakopoulos, P.; Yapp, C.; Wells, C.; Che, K. H.; Bannister, A.; Robson, S.; Kumar, U.; Parr, N.; Lee, K.; Lugo, D.; Jeffrey, P.; Taylor, S.; Vecellio, M. L.; Bountra, C.; Brennan, P. E.; O'Mahony, A.; Velichko, S.; Mueller, S.; Hay, D.; Daniels, D. L.; Urh, M.; La Thangue, N. B.; Kouzarides, T.; Prinjha, R.; Schwaller, J.; and Knapp, S. CANCER RESEARCH, 75(23): 5106-5119. DEC 1 2015.
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Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance. Fedorov, O.; Castex, J.; Tallant, C.; Owen, D. R.; Martin, S.; Aldeghi, M.; Monteiro, O.; Filippakopoulos, P.; Picaud, S.; Trzupek, J. D.; Gerstenberger, B. S.; Bountra, C.; Willmann, D.; Wells, C.; Philpott, M.; Rogers, C.; Biggin, P. C.; Brennan, P. E.; Bunnage, M. E.; Schuele, R.; Guenther, T.; Knapp, S.; and Mueller, S. SCIENCE ADVANCES, 1(10). NOV 2015.
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Inflammatory Signaling by NOD-RIPK2 Is Inhibited by Clinically Relevant Type II Kinase Inhibitors. Canning, P.; Ruan, Q.; Schwerd, T.; Hrdinka, M.; Maki, J. L.; Saleh, D.; Suebsuwong, C.; Ray, S.; Brennan, P. E.; Cuny, G. D.; Uhlig, H. H.; Gyrd-Hansen, M.; Degterev, A.; and Bullock, A. N. CHEMISTRY & BIOLOGY, 22(9): 1174-1184. SEP 17 2015.
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CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses. Hammitzsch, A.; Tallant, C.; Fedorov, O.; O'Mahony, A.; Brennan, P. E.; Hay, D. A.; Martinez, F. O.; Al-Mossawi, M. H.; de Wit, J.; Vecellio, M.; Wells, C.; Wordsworth, P.; Mueller, S.; Knapp, S.; and Bowness, P. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 112(34): 10768-10773. AUG 25 2015.
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The promise and peril of chemical probes. Arrowsmith, C. H.; Audia, J. E.; Austin, C.; Baell, J.; Bennett, J.; Blagg, J.; Bountra, C.; Brennan, P. E.; Brown, P. J.; Bunnage, M. E.; Buser-Doepner, C.; Campbell, R. M.; Carter, A. J.; Cohen, P.; Copeland, R. A.; Cravatt, B.; Dahlin, J. L.; Dhanak, D.; Edwards, A. M.; Frye, S. V.; Gray, N.; Grimshaw, C. E.; Hepworth, D.; Howe, T.; Huber, K. V. M.; Jin, J.; Knapp, S.; Kotz, J. D.; Kruger, R. G.; Lowe, D.; Mader, M. M.; Marsden, B.; Mueller-Fahrnow, A.; Mueller, S.; O'Hagan, R. C.; Overington, J. P.; Owen, D. R.; Rosenberg, S. H.; Roth, B.; Ross, R.; Schapira, M.; Schreiber, S. L.; Shoichet, B.; Sundstrom, M.; Superti-Furga, G.; Taunton, J.; Toledo-Sherman, L.; Walpole, C.; Walters, M. A.; Willson, T. M.; Workman, P.; Young, R. N.; and Zuercher, W. J. NATURE CHEMICAL BIOLOGY, 11(8): 536-541. AUG 2015.
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LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor. Clark, P. G. K.; Vieira, L. C. C.; Tallant, C.; Fedorov, O.; Singleton, D. C.; Rogers, C. M.; Monteiro, O. P.; Bennett, J. M.; Baronio, R.; Mueller, S.; Daniels, D. L.; Mendez, J.; Knapp, S.; Brennan, P. E.; and Dixon, D. J. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 54(21): 6217-6221. MAY 18 2015.
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K2P channel gating mechanisms revealed by structures of TREK-2 and a complex with Prozac. Dong, Y. Y.; Pike, A. C. W.; Mackenzie, A.; McClenaghan, C.; Aryal, P.; Dong, L.; Quigley, A.; Grieben, M.; Goubin, S.; Mukhopadhyay, S.; Ruda, G. F.; Clausen, M. V.; Cao, L.; Brennan, P. E.; Burgess-Brown, N. A.; Sansom, M. S. P.; Tucker, S. J.; and Carpenter, E. P. SCIENCE, 347(6227): 1256-1259. MAR 13 2015.
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Betti reaction enables efficient synthesis of 8-hydroxyquinoline inhibitors of 2-oxoglutarate oxygenases. Thinnes, C. C.; Tumber, A.; Yapp, C.; Scozzafava, G.; Yeh, T.; Chan, M. C.; Tran, T. A.; Hsu, K.; Tarhonskaya, H.; Walport, L. J.; Wilkins, S. E.; Martinez, E. D.; Mueller, S.; Pugh, C. W.; Ratcliffe, P. J.; Brennan, P. E.; Kawamura, A.; and Schofield, C. J. CHEMICAL COMMUNICATIONS, 51(84): 15458-15461. 2015.
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Design and synthesis of potent and selective inhibitors of BRD7 and BRD9 bromodomains. Hay, D. A.; Rogers, C. M.; Fedorov, O.; Tallant, C.; Martin, S.; Monteiro, O. P.; Mueller, S.; Knapp, S.; Schofield, C. J.; and Brennan, P. E. MEDCHEMCOMM, 6(7): 1381-1386. 2015.
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  2014 (7)
Optimizing in vivo probes for the BET bromodomains. Jennings, L. E.; Hewings, D. S.; Humphreys, P. G.; Brennan, P. E.; and Conway, S. J. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 248. AUG 10 2014. 248th National Meeting of the American-Chemical-Society (ACS), San Francisco, CA, AUG 10-14, 2014
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Discovery and Optimization of Small-Molecule Ligands for the CBP/p300 Bromodomains. Hay, D. A.; Fedorov, O.; Martin, S.; Singleton, D. C.; Tallant, C.; Wells, C.; Picaud, S.; Philpott, M.; Monteiro, O. P.; Rogers, C. M.; Conway, S. J.; Rooney, T. P. C.; Tumber, A.; Yapp, C.; Filippakopoulos, P.; Bunnage, M. E.; Mueller, S.; Knapp, S.; Schofield, C. J.; and Brennan, P. E. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 136(26): 9308-9319. JUL 2 2014.
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A Series of Potent CREBBP Bromodomain Ligands Reveals an Induced-Fit Pocket Stabilized by a Cation-π Interaction. Rooney, T. P. C.; Filippakopoulos, P.; Fedorov, O.; Picaud, S.; Cortopassi, W. A.; Hay, D. A.; Martin, S.; Tumber, A.; Rogers, C. M.; Philpott, M.; Wang, M.; Thompson, A. L.; Heightman, T. D.; Pryde, D. C.; Cook, A.; Paton, R. S.; Mueller, S.; Knapp, S.; Brennan, P. E.; and Conway, S. J. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 53(24): 6126-6130. JUN 2014.
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Machine-assisted synthesis of modulators of the histone reader BRD9 using flow methods of chemistry and frontal affinity chromatography. Guetzoyan, L.; Ingham, R. J.; Nikbin, N.; Rossignol, J.; Wolling, M.; Baumert, M.; Burgess-Brown, N. A.; Strain-Damerell, C. M.; Shrestha, L.; Brennan, P. E.; Fedorov, O.; Knapp, S.; and Ley, S. V. MEDCHEMCOMM, 5(4): 540-546. APR 2014.
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[1,2,4]Triazolo[4,3-a]phthalazines: Inhibitors of Diverse Bromodomains. Fedorov, O.; Lingard, H.; Wells, C.; Monteiro, O. P.; Picaud, S.; Keates, T.; Yapp, C.; Philpott, M.; Martin, S. J.; Felletar, I.; Marsden, B. D.; Filippakopoulos, P.; Mueller, S.; Knapp, S.; and Brennan, P. E. JOURNAL OF MEDICINAL CHEMISTRY, 57(2): 462-476. JAN 23 2014.
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The Role of Protein Structural Analysis in the Next Generation Sequencing Era. Yue, W. W.; Froese, D. S.; and Brennan, P. E. In Tang, N.; and Poon, T, editor(s), CHEMICAL DIAGNOSTICS: FROM BENCH TO BEDSIDE, volume 336, of Topics in Current Chemistry-Series, pages 67-98. 2014.
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Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor. England, K. S.; Tumber, A.; Krojer, T.; Scozzafava, G.; Ng, S. S.; Daniel, M.; Szykowska, A.; Che, K.; von Delft, F.; Burgess-Brown, N. A.; Kawamura, A.; Schofield, C. J.; and Brennan, P. E. MEDCHEMCOMM, 5(12): 1879-1886. 2014.
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  2013 (7)
RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Picaud, S.; Wells, C.; Felletar, I.; Brotherton, D.; Martin, S.; Savitsky, P.; Diez-Dacal, B.; Philpott, M.; Bountra, C.; Lingard, H.; Fedorov, O.; Mueller, S.; Brennan, P. E.; Knapp, S.; and Filippakopoulos, P. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 110(49): 19754-19759. DEC 3 2013.
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Fragment-based hit identification: thinking in 3D. Morley, A. D.; Pugliese, A.; Birchall, K.; Bower, J.; Brennan, P.; Brown, N.; Chapman, T.; Drysdale, M.; Gilbert, I. H.; Hoelder, S.; Jordan, A.; Ley, S. V.; Merritt, A.; Miller, D.; Swarbrick, M. E.; and Wyatt, P. G. DRUG DISCOVERY TODAY, 18(23-24): 1221-1227. DEC 2013.
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Chemical probes for bromodomains outside the BET family. Brennan, P. E.; Martin, S. J.; Monteiro, O.; Fedorov, O.; Knapp, S.; Hay, D.; Wells, C.; Filippakopoulos, P.; Picaud, S.; Muller-Knapp, S.; Keates, T.; Yapp, C.; Philpott, M.; Schofield, C.; Burgess-Brown, N.; Shrestha, L.; and Strain-Damerell, C. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 246. SEP 8 2013. 246th National Meeting of the American-Chemical-Society (ACS), Indianapolis, IN, SEP 08-12, 2013
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PFI-1, a Highly Selective Protein Interaction Inhibitor, Targeting BET Bromodomains. Picaud, S.; Da Costa, D.; Thanasopoulou, A.; Filippakopoulos, P.; Fish, P. V.; Philpott, M.; Fedorov, O.; Brennan, P.; Bunnage, M. E.; Owen, D. R.; Bradner, J. E.; Taniere, P.; O'Sullivan, B.; Mueller, S.; Schwaller, J.; Stankovic, T.; and Knapp, S. CANCER RESEARCH, 73(11): 3336-3346. JUN 1 2013.
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Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands. Hewings, D. S.; Fedorov, O.; Filippakopoulos, P.; Martin, S.; Picaud, S.; Tumber, A.; Wells, C.; Olcina, M. M.; Freeman, K.; Gill, A.; Ritchie, A. J.; Sheppard, D. W.; Russell, A. J.; Hammond, E. M.; Knapp, S.; Brennan, P. E.; and Conway, S. J. JOURNAL OF MEDICINAL CHEMISTRY, 56(8): 3217-3227. APR 25 2013.
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The design and synthesis of 5-and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains. Hay, D.; Fedorov, O.; Filippakopoulos, P.; Martin, S.; Philpott, M.; Picaud, S.; Hewings, D. S.; Uttakar, S.; Heightman, T. D.; Conway, S. J.; Knapp, S.; and Brennan, P. E. MEDCHEMCOMM, 4(1): 140-144. JAN 2013.
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5-Carboxy-8-hydroxyquinoline is a broad spectrum 2-oxoglutarate oxygenase inhibitor which causes iron translocation. Hopkinson, R. J.; Tumber, A.; Yapp, C.; Chowdhury, R.; Aik, W.; Che, K. H.; Li, X. S.; Kristensen, J. B. L.; King, O. N. F.; Chan, M. C.; Yeoh, K. K.; Choi, H.; Walport, L. J.; Thinnes, C. C.; Bush, J. T.; Lejeune, C.; Rydzik, A. M.; Rose, N. R.; Bagg, E. A.; McDonough, M. A.; Krojer, T. J.; Yue, W. W.; Ng, S. S.; Olsen, L.; Brennan, P. E.; Oppermann, U.; Mueller, S.; Klose, R. J.; Ratcliffe, P. J.; Schofield, C. J.; and Kawamura, A. CHEMICAL SCIENCE, 4(8): 3110-3117. 2013.
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  2012 (6)
Progress in the Development and Application of Small Molecule Inhibitors of Bromodomain-Acetyl-lysine Interactions. Hewings, D. S.; Rooney, T. P. C.; Jennings, L. E.; Hay, D. A.; Schofield, C. J.; Brennan, P. E.; Knapp, S.; and Conway, S. J. JOURNAL OF MEDICINAL CHEMISTRY, 55(22): 9393-9413. NOV 22 2012.
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Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit. Fish, P. V.; Filippakopoulos, P.; Bish, G.; Brennan, P. E.; Bunnage, M. E.; Cook, A. S.; Federov, O.; Gerstenberger, B. S.; Jones, H.; Knapp, S.; Marsden, B.; Nocka, K.; Owen, D. R.; Philpott, M.; Picaud, S.; Primiano, M. J.; Ralph, M. J.; Sciammetta, N.; and Trzupek, J. D. JOURNAL OF MEDICINAL CHEMISTRY, 55(22): 9831-9837. NOV 22 2012.
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Developing small molecule inhibitors of the CREBBP bromodomain-histone interaction. Rooney, T. P. C.; Fedorov, O.; Filippakopoulos, P.; Wang, M.; Philpott, M.; Cook, A.; Heightman, T. D.; Knapp, S.; Pryde, D.; Brennan, P. E.; and Conway, S. J. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 244. AUG 19 2012. 244th National Fall Meeting of the American-Chemical-Society (ACS), Philadelphia, PA, AUG 19-23, 2012
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Plant Growth Regulator Daminozide Is a Selective Inhibitor of Human KDM2/7 Histone Demethylases. Rose, N. R.; Woon, E. C. Y.; Tumber, A.; Walport, L. J.; Chowdhury, R.; Li, X. S.; King, O. N. F.; Lejeune, C.; Ng, S. S.; Krojer, T.; Chan, M. C.; Rydzik, A. M.; Hopkinson, R. J.; Che, K. H.; Daniel, M.; Strain-Damerell, C.; Gileadi, C.; Kochan, G.; Leung, I. K. H.; Dunford, J.; Yeoh, K. K.; Ratcliffe, P. J.; Burgess-Brown, N.; von Delft, F.; Muller, S.; Marsden, B.; Brennan, P. E.; McDonough, M. A.; Oppermann, U.; Klose, R. J.; Schofield, C. J.; and Kawamura, A. JOURNAL OF MEDICINAL CHEMISTRY, 55(14): 6639-6643. JUL 26 2012.
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3,5-Dimethylisoxazoles inhibit the bromodomain-histone protein-protein interaction. Hewings, D. S.; Wang, M.; Philpott, M.; Fedorov, O.; Uttarkar, S.; Filippakopoulos, P.; Picaud, S.; Vuppusetty, C.; Marsden, B.; Heightman, T. D.; Knapp, S.; Brennan, P.; and Conway, S. J. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 243. MAR 25 2012. 243rd National Spring Meeting of the American-Chemical-Society, San Diego, CA, MAR 25-29, 2012
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Developing chemical probes for the BET bromodomains. Hewings, D. S.; Wang, M.; Philpott, M.; Fedorov, O.; Uttarkar, S.; Filippakopoulos, P.; Picaud, S.; Vuppusetty, C.; Marsden, B.; Heightman, T. D.; Knapp, S.; Brennan, P.; and Conway, S. J. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 243. MAR 25 2012. 243rd National Spring Meeting of the American-Chemical-Society, San Diego, CA, MAR 25-29, 2012
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  2011 (2)
Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: Design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. Andrews, M. D.; Fish, P. V.; Blagg, J.; Brabham, T. K.; Brennan, P. E.; Bridgeland, A.; Brown, A. D.; Bungay, P. J.; Conlon, K. M.; Edmunds, N. J.; af Forselles, K.; Gibbons, C. P.; Green, M. P.; Hanton, G.; Holbrook, M.; Jessiman, A. S.; McIntosh, K.; McMurray, G.; Nichols, C. L.; Root, J. A.; Storer, R. I.; Sutton, M. R.; Ward, R. V.; Westbrook, D.; and Whitlock, G. A. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 21(9): 2715-2720. MAY 1 2011.
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A tandem asymmetric synthesis approach for the efficient preparation of enantiomerically pure 9-(hydroxyethyl) anthracene. Ball, J. C.; Brennan, P.; Elsunaki, T. M.; Jaunet, A.; and Jones, S. TETRAHEDRON-ASYMMETRY, 22(3): 253-255. FEB 10 2011.
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  2009 (1)
Potent and selective α1A adrenoceptor partial agonists-Novel imidazole frameworks. Whitlock, G. A.; Brennan, P. E.; Roberts, L. R.; and Stobie, A. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 19(11): 3118-3121. JUN 1 2009.
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  2003 (3)
Palladium-containing perovskites: recoverable and reuseable catalysts for Suzuki couplings. Smith, M.; Stepan, A.; Ramarao, C; Brennan, P.; and Ley, S. CHEMICAL COMMUNICATIONS, (21): 2652-2653. NOV 7 2003.
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Studies toward a total synthesis of bengazole A utilizing BDA-protected building blocks. Balskus, E.; Brennan, P.; and Ley, S. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 225(2): U350-U351. MAR 2003. 225th National Meeting of the American-Chemical-Society, NEW ORLEANS, LOUISIANA, MAR 23-27, 2003
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Synthesis of carbohydrate derivatives using solid-phase work-up and scavenging techniques. MacCoss, R.; Brennan, P.; and Ley, S. ORGANIC & BIOMOLECULAR CHEMISTRY, 1(12): 2029-2031. 2003.
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