Paul E. Brennan, Ph.D. - Publications

Affiliations: 
2000 University of California, Berkeley, Berkeley, CA 
Area:
Bio-Organic and Synthetic Chemistry

37 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
2016 Popp TA, Tallant C, Rogers C, Fedorov O, Brennan PE, Müller S, Knapp S, Bracher F. Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors. Journal of Medicinal Chemistry. PMID 27673482 DOI: 10.1021/acs.jmedchem.6b00774  0.68
2016 Montenegro RC, Clark PG, Howarth A, Wan X, Ceroni A, Siejka P, Nunez-Alonso GA, Monteiro O, Rogers C, Gamble V, Burbano R, Brennan PE, Tallant C, Ebner D, Fedorov O, et al. BET inhibition as a new strategy for the treatment of gastric cancer. Oncotarget. PMID 27259267 DOI: 10.18632/oncotarget.9766  0.68
2016 Johansson C, Velupillai S, Tumber A, Szykowska A, Hookway ES, Nowak RP, Strain-Damerell C, Gileadi C, Philpott M, Burgess-Brown N, Wu N, Kopec J, Nuzzi A, Steuber H, Egner U, ... ... Brennan PE, et al. Structural analysis of human KDM5B guides histone demethylase inhibitor development. Nature Chemical Biology. PMID 27214403 DOI: 10.1038/nchembio.2087  0.68
2016 Sutherell CL, Tallant C, Monteiro OP, Yapp C, Fuchs JE, Fedorov O, Siejka P, Müller S, Knapp S, Brenton JD, Brennan PE, Ley SV. Identification and development of 2,3-dihydropyrrolo[1,2-a]quinazolin-5(1H)-one inhibitors targeting bromodomains within the Switch/Sucrose Non-Fermenting complex. Journal of Medicinal Chemistry. PMID 27119626 DOI: 10.1021/acs.jmedchem.5b01997  0.68
2016 Gerstenberger BS, Trzupek JD, Tallant C, Fedorov O, Filippakopoulos P, Brennan PE, Fedele V, Martin S, Picaud S, Rogers CM, Parikh MD, Taylor A, Samas BM, O'Mahony A, Berg EL, et al. Identification of a chemical probe for family VIII bromodomains through optimization of a fragment hit. Journal of Medicinal Chemistry. PMID 27115555 DOI: 10.1021/acs.jmedchem.6b00012  0.68
2016 Mathea S, Abdul Azeez KR, Salah E, Tallant C, Wolfreys F, Konietzny R, Fischer R, Lou HJ, Brennan PE, Schnapp G, Pautsch A, Kessler BM, Turk BE, Knapp S. Structure of the Human Protein Kinase ZAK in Complex with Vemurafenib. Acs Chemical Biology. PMID 26999302 DOI: 10.1021/acschembio.6b00043  0.68
2016 Bavetsias V, Lanigan RM, Ruda GF, Atrash B, McLaughlin MG, Tumber A, Mok NY, Le Bihan YV, Dempster S, Boxall KJ, Jeganathan F, Hatch SB, Savitsky P, Velupillai S, Krojer T, ... ... Brennan PE, et al. 8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors. Journal of Medicinal Chemistry. PMID 26741168 DOI: 10.1021/acs.jmedchem.5b01635  0.68
2016 Chaikuad A, Lang S, Brennan PE, Temperini C, Fedorov O, Hollander J, Nachane R, Abell C, Müller S, Siegal G, Knapp S. Structure-based identification of inhibitory fragments targeting the p300/CBP-associated factor bromodomain. Journal of Medicinal Chemistry. PMID 26731131 DOI: 10.1021/acs.jmedchem.5b01719  0.68
2015 McAllister TE, England KS, Hopkinson RJ, Brennan PE, Kawamura A, Schofield CJ. Recent Progress in Histone Demethylase Inhibitors. Journal of Medicinal Chemistry. PMID 26710088 DOI: 10.1021/acs.jmedchem.5b01758  0.68
2015 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, Hing Che K, ... ... Brennan P, et al. Generation of a selective small molecule inhibitor of the CBP/p300 bromodomain for leukemia therapy. Cancer Research. PMID 26552700 DOI: 10.1158/0008-5472.CAN-15-0236  0.68
2015 Thinnes CC, Tumber A, Yapp C, Scozzafava G, Yeh T, Chan MC, Tran TA, Hsu K, Tarhonskaya H, Walport LJ, Wilkins SE, Martinez ED, Müller S, Pugh CW, Ratcliffe PJ, ... Brennan PE, et al. Betti reaction enables efficient synthesis of 8-hydroxyquinoline inhibitors of 2-oxoglutarate oxygenases. Chemical Communications (Cambridge, England). 51: 15458-61. PMID 26345662 DOI: 10.1039/c5cc06095h  0.68
2015 Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, et al. The promise and peril of chemical probes. Nature Chemical Biology. 11: 536-41. PMID 26196764 DOI: 10.1038/nchembio.1867  0.68
2015 Bennett J, Fedorov O, Tallant C, Monteiro O, Meier J, Gamble V, Savitsky P, Nunez-Alonso GA, Haendler B, Rogers C, Brennan PE, Müller S, Knapp S. Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF. Journal of Medicinal Chemistry. PMID 25974391 DOI: 10.1021/acs.jmedchem.5b00458  0.68
2015 Clark PG, Vieira LC, Tallant C, Fedorov O, Singleton DC, Rogers CM, Monteiro OP, Bennett JM, Baronio R, Müller S, Daniels DL, Méndez J, Knapp S, Brennan PE, Dixon DJ. LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor. Angewandte Chemie (International Ed. in English). 54: 6217-21. PMID 25864491 DOI: 10.1002/anie.201501394  0.68
2015 Dong YY, Pike AC, Mackenzie A, McClenaghan C, Aryal P, Dong L, Quigley A, Grieben M, Goubin S, Mukhopadhyay S, Ruda GF, Clausen MV, Cao L, Brennan PE, Burgess-Brown NA, et al. K2P channel gating mechanisms revealed by structures of TREK-2 and a complex with Prozac. Science (New York, N.Y.). 347: 1256-9. PMID 25766236 DOI: 10.1126/science.1261512  0.68
2015 Hammitzsch A, Tallant C, Fedorov O, O'Mahony A, Brennan PE, Hay DA, Martinez FO, Al-Mossawi MH, De Wit J, Vecellio M, Wells C, Wordsworth P, Müller S, Knapp S, Bowness P. CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses Proceedings of the National Academy of Sciences of the United States of America. 112: 10768-10773. DOI: 10.1073/pnas.1501956112  0.68
2015 Hay DA, Rogers CM, Fedorov O, Tallant C, Martin S, Monteiro OP, Müller S, Knapp S, Schofield CJ, Brennan PE. Design and synthesis of potent and selective inhibitors of BRD7 and BRD9 bromodomains Medchemcomm. 6: 1381-1386. DOI: 10.1039/c5md00152h  0.68
2014 Hay DA, Fedorov O, Martin S, Singleton DC, Tallant C, Wells C, Picaud S, Philpott M, Monteiro OP, Rogers CM, Conway SJ, Rooney TP, Tumber A, Yapp C, Filippakopoulos P, ... ... Brennan PE, et al. Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains. Journal of the American Chemical Society. 136: 9308-19. PMID 24946055 DOI: 10.1021/ja412434f  0.68
2014 Storer RI, Brennan PE, Brown AD, Bungay PJ, Conlon KM, Corbett MS, DePianta RP, Fish PV, Heifetz A, Ho DK, Jessiman AS, McMurray G, de Oliveira CA, Roberts LR, Root JA, et al. Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HTâ‚‚C) receptor agonists with exquisite functional selectivity over 5-HTâ‚‚A and 5-HTâ‚‚B receptors. Journal of Medicinal Chemistry. 57: 5258-69. PMID 24878222 DOI: 10.1021/jm5003292  0.68
2014 Rooney TP, Filippakopoulos P, Fedorov O, Picaud S, Cortopassi WA, Hay DA, Martin S, Tumber A, Rogers CM, Philpott M, Wang M, Thompson AL, Heightman TD, Pryde DC, Cook A, ... ... Brennan PE, et al. A series of potent CREBBP bromodomain ligands reveals an induced-fit pocket stabilized by a cation-π interaction. Angewandte Chemie (International Ed. in English). 53: 6126-30. PMID 24821300 DOI: 10.1002/anie.201402750  0.68
2014 Fedorov O, Lingard H, Wells C, Monteiro OP, Picaud S, Keates T, Yapp C, Philpott M, Martin SJ, Felletar I, Marsden BD, Filippakopoulos P, Müller S, Knapp S, Brennan PE. [1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains. Journal of Medicinal Chemistry. 57: 462-76. PMID 24313754 DOI: 10.1021/jm401568s  0.68
2014 Yue WW, Froese DS, Brennan PE. The role of protein structural analysis in the next generation sequencing era. Topics in Current Chemistry. 336: 67-98. PMID 22610134 DOI: 10.1007/128_2012_326  0.68
2014 England KS, Tumber A, Krojer T, Scozzafava G, Ng SS, Daniel M, Szykowska A, Che K, Von Delft F, Burgess-Brown NA, Kawamura A, Schofield CJ, Brennan PE. Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor Medchemcomm. 5: 1879-1886. DOI: 10.1039/c4md00291a  0.68
2014 Guetzoyan L, Ingham RJ, Nikbin N, Rossignol J, Wolling M, Baumert M, Burgess-Brown NA, Strain-Damerell CM, Shrestha L, Brennan PE, Fedorov O, Knapp S, Ley SV. Machine-assisted synthesis of modulators of the histone reader BRD9 using flow methods of chemistry and frontal affinity chromatography Medchemcomm. 5: 540-546. DOI: 10.1039/c4md00007b  0.68
2013 Picaud S, Wells C, Felletar I, Brotherton D, Martin S, Savitsky P, Diez-Dacal B, Philpott M, Bountra C, Lingard H, Fedorov O, Müller S, Brennan PE, Knapp S, Filippakopoulos P. RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proceedings of the National Academy of Sciences of the United States of America. 110: 19754-9. PMID 24248379 DOI: 10.1073/pnas.1310658110  0.68
2013 Hewings DS, Fedorov O, Filippakopoulos P, Martin S, Picaud S, Tumber A, Wells C, Olcina MM, Freeman K, Gill A, Ritchie AJ, Sheppard DW, Russell AJ, Hammond EM, Knapp S, ... Brennan PE, et al. Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands. Journal of Medicinal Chemistry. 56: 3217-27. PMID 23517011 DOI: 10.1021/jm301588r  0.68
2013 Hopkinson RJ, Tumber A, Yapp C, Chowdhury R, Aik W, Che KH, Li XS, Kristensen JBL, King ONF, Chan MC, Yeoh KK, Choi H, Walport LJ, Thinnes CC, Bush JT, ... ... Brennan PE, et al. 5-Carboxy-8-hydroxyquinoline is a broad spectrum 2-oxoglutarate oxygenase inhibitor which causes iron translocation Chemical Science. 4: 3110-3117. DOI: 10.1039/c3sc51122g  0.68
2013 Hay D, Fedorov O, Filippakopoulos P, Martin S, Philpott M, Picaud S, Hewings DS, Uttakar S, Heightman TD, Conway SJ, Knapp S, Brennan PE. The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains Medchemcomm. 4: 140-144. DOI: 10.1039/c2md20189e  0.68
2012 Fish PV, Filippakopoulos P, Bish G, Brennan PE, Bunnage ME, Cook AS, Federov O, Gerstenberger BS, Jones H, Knapp S, Marsden B, Nocka K, Owen DR, Philpott M, Picaud S, et al. Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit. Journal of Medicinal Chemistry. 55: 9831-7. PMID 23095041 DOI: 10.1021/jm3010515  0.68
2012 Hewings DS, Rooney TP, Jennings LE, Hay DA, Schofield CJ, Brennan PE, Knapp S, Conway SJ. Progress in the development and application of small molecule inhibitors of bromodomain-acetyl-lysine interactions. Journal of Medicinal Chemistry. 55: 9393-413. PMID 22924434 DOI: 10.1021/jm300915b  0.68
2012 Rose NR, Woon EC, Tumber A, Walport LJ, Chowdhury R, Li XS, King ON, Lejeune C, Ng SS, Krojer T, Chan MC, Rydzik AM, Hopkinson RJ, Che KH, Daniel M, ... ... Brennan PE, et al. Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases. Journal of Medicinal Chemistry. 55: 6639-43. PMID 22724510 DOI: 10.1021/jm300677j  0.68
2011 Andrews MD, Fish PV, Blagg J, Brabham TK, Brennan PE, Bridgeland A, Brown AD, Bungay PJ, Conlon KM, Edmunds NJ, af Forselles K, Gibbons CP, Green MP, Hanton G, Holbrook M, et al. 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. Bioorganic & Medicinal Chemistry Letters. 21: 2715-20. PMID 21195614 DOI: 10.1016/j.bmcl.2010.11.120  0.68
2009 Ley SV, Tackett MN, Maddess ML, Anderson JC, Brennan PE, Cappi MW, Heer JP, Helgen C, Kori M, Kouklovsky C, Marsden SP, Norman J, Osborn DP, Palomero MA, Pavey JB, et al. Total synthesis of rapamycin. Chemistry (Weinheim An Der Bergstrasse, Germany). 15: 2874-914. PMID 19204960 DOI: 10.1002/chem.200801656  0.68
2007 Maddess ML, Tackett MN, Watanabe H, Brennan PE, Spilling CD, Scott JS, Osborn DP, Ley SV. Total synthesis of rapamycin. Angewandte Chemie (International Ed. in English). 46: 591-7. PMID 17154218 DOI: 10.1002/anie.200604053  0.68
2003 Smith MD, Stepan AF, Ramarao C, Brennan PE, Ley SV. Palladium-containing perovskites: recoverable and reuseable catalysts for Suzuki couplings. Chemical Communications (Cambridge, England). 2652-3. PMID 14649794  0.68
2002 Spaller MR, Thielemann WT, Brennan PE, Bartlett PA. Combinatorial synthetic design. Solution and polymer-supported synthesis of heterocycles via intramolecular aza Diels-Alder and imino alcohol cyclizations. Journal of Combinatorial Chemistry. 4: 516-22. PMID 12217025 DOI: 10.1021/cc020027+  0.68
2001 Scholl M, Ding S, Lee CW, Grubbs RH, Brennan PE, Ley SV, Chatterjee AK, Morgan JP. New catalysts for olefin metathesis Chemtracts. 14: 88-93.  0.68
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