Paul Brennan

I am an industry trained, innovative and successful medicinal chemistry with diverse experience, a history of clinical candidate delivery and a strong background in synthetic organic and medicinal chemistry. I have led and delivered advanced compounds in projects targeting major disease targets: kinase inhibitors, GPCR agonists and antagonists, metabolic enzymes, ion channels and chromatin modifiers. As the principal investigator of medicinal chemistry at the Structural Genomics Consortium in Oxford University, I lead the chemistry team dedicated to designing and synthesizing open-access small molecule probes for epigenetic proteins in order to elucidate the mechanism of epigenetic regulation, one of the most exciting new areas of human biology.

Informações coletadas do Lattes em 04/11/2022

Acadêmico

Formação acadêmica

Doutorado em Organic Synthesis

1995 - 2000

University of California, Berkeley
Título: I. Phosphinate Inhibitors of Peptidoglycan Biosynthesis. II. Development of a New Ring System for Combinatorial Chemistry
Orientador: Paul A. Bartlett

Graduação em Science in Chemistry

1991 - 1995

University of California Davis
Orientador: Professor Mark J. Kurth, PhD

Idiomas

Inglês

Compreende Bem, Fala Bem, Lê Bem, Escreve Bem.

Áreas de atuação

Grande área: Ciências Exatas e da Terra / Área: Química / Subárea: Medicinal Chemistry.

Produções bibliográficas

BRENNAN, PAUL E. . Discovery and Optimization of Small-Molecule Ligands for the CBP/p300 Bromodomains. Journal of the American Chemical Society (Print) , v. 136, p. 9308-9319, 2014.
STORER, R. IAN ; BRENNAN, PAUL E. ; BROWN, ALAN D. ; BUNGAY, PETER J. ; CONLON, KELLY M. ; CORBETT, MATTHEW S. ; DEPIANTA, ROBERT P. ; FISH, PAUL V. ; HEIFETZ, ALEXANDER ; HO, DANNY K. H. ; JESSIMAN, ALAN S. ; MCMURRAY, GORDON ; DE OLIVEIRA, CESAR AUGUSTO F. ; ROBERTS, LEE R. ; ROOT, JAMES A. ; SHANMUGASUNDARAM, VEERABAHU ; SHAPIRO, MICHAEL J. ; SKERTEN, MELANIE ; WESTBROOK, DOMINIQUE ; WHEELER, SIMON ; WHITLOCK, GAVIN A. ; WRIGHT, JOHN . Multiparameter Optimization in CNS Drug Discovery: Design of Pyrimido[4,5- ]azepines as Potent 5-Hydroxytryptamine 2C (5-HT ) Receptor Agonists with Exquisite Functional Selectivity over 5-HT and 5-HT Receptors. Journal of Medicinal Chemistry , v. 57, p. 5258-5269, 2014.
FEDOROV, OLEG ; LINGARD, HANNAH ; WELLS, CHRIS ; MONTEIRO, OCTOVIA P. ; PICAUD, SARAH ; KEATES, TRACY ; YAPP, CLARENCE ; PHILPOTT, MARTIN ; MARTIN, SARAH J. ; FELLETAR, ILDIKO ; MARSDEN, BRIAN D. ; FILIPPAKOPOULOS, PANAGIS ; MÜLLER, SUSANNE ; KNAPP, STEFAN ; BRENNAN, PAUL E. . [1,2,4]Triazolo[4,3- ]phthalazines: Inhibitors of Diverse Bromodomains. Journal of Medicinal Chemistry , v. 57, p. 462-476, 2014.
PICAUD, S. ; WELLS, C. ; FELLETAR, I. ; BROTHERTON, D. ; MARTIN, S. ; SAVITSKY, P. ; DIEZ-DACAL, B. ; PHILPOTT, M. ; BOUNTRA, C. ; LINGARD, H. ; FEDOROV, O. ; MULLER, S. ; BRENNAN, P. E. ; 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 , v. 110, p. 19754-19759, 2013.
HEWINGS, DAVID S. ; FEDOROV, OLEG ; FILIPPAKOPOULOS, PANAGIS ; MARTIN, SARAH ; PICAUD, SARAH ; TUMBER, ANTHONY ; WELLS, CHRISTOPHER ; OLCINA, MONICA M. ; FREEMAN, KATHERINE ; GILL, ANDREW ; RITCHIE, ALISON J. ; SHEPPARD, DAVID W. ; RUSSELL, ANGELA J. ; HAMMOND, ESTER M. ; KNAPP, STEFAN ; BRENNAN, PAUL E. ; CONWAY, STUART J. . Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands. Journal of Medicinal Chemistry , v. 56, p. 3217-3227, 2013.
FISH, PAUL V. ; FILIPPAKOPOULOS, PANAGIS ; BISH, GERWYN ; BRENNAN, PAUL E. ; BUNNAGE, MARK E. ; COOK, ANDREW S. ; FEDEROV, OLEG ; GERSTENBERGER, BRIAN S. ; JONES, HANNAH ; KNAPP, STEFAN ; MARSDEN, BRIAN ; NOCKA, KARL ; OWEN, DAFYDD R. ; PHILPOTT, MARTIN ; PICAUD, SARAH ; PRIMIANO, MICHAEL J. ; RALPH, MICHAEL J. ; SCIAMMETTA, NUNZIO ; TRZUPEK, JOHN D. . Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit. Journal of Medicinal Chemistry , v. 55, p. 9831-9837, 2012.
HEWINGS, DAVID S. ; ROONEY, TIMOTHY P. C. ; JENNINGS, LAURA E. ; HAY, DUNCAN A. ; SCHOFIELD, CHRISTOPHER J. ; BRENNAN, PAUL E. ; KNAPP, STEFAN ; CONWAY, STUART J. . Progress in the Development and Application of Small Molecule Inhibitors of Bromodomain-Acetyl-lysine Interactions. Journal of Medicinal Chemistry , v. 55, p. 9393-9413, 2012.
ROSE, NATHAN R. WOON, ESTHER C. Y. TUMBER, ANTHONY WALPORT, LOUISE J. CHOWDHURY, RASHEDUZZAMAN LI, XUAN SHIRLEY KING, OLIVER N. F. LEJEUNE, CLARISSE NG, STANLEY S. KROJER, TOBIAS CHAN, MUN CHIANG RYDZIK, ANNA M. HOPKINSON, RICHARD J. CHE, KA HING DANIEL, MICHELLE STRAIN-DAMERELL, CLAIRE GILEADI, CARINA KOCHAN, GRAZYNA LEUNG, IVANHOE K. H. DUNFORD, JAMES YEOH, KAR KHENG RATCLIFFE, PETER J. BURGESS-BROWN, NICOLA VON DELFT, FRANK MULLER, SUSANNE , et al. MARSDEN, BRIAN BRENNAN, PAUL E. MCDONOUGH, MICHAEL A. OPPERMANN, UDO KLOSE, ROBERT J. SCHOFIELD, CHRISTOPHER J. KAWAMURA, AKANE ; Plant Growth Regulator Daminozide Is a Selective Inhibitor of Human KDM2/7 Histone Demethylases. Journal of Medicinal Chemistry , v. 55, p. 6639-6643, 2012.
BRENNAN, PAUL E. ; WHITLOCK, GAVIN A. ; HO, DANNY K.H. ; CONLON, KELLY ; MCMURRAY, GORDON . Discovery of a novel azepine series of potent and selective 5-HT2C agonists as potential treatments for urinary incontinence. Bioorganic & Medicinal Chemistry Letters (Print) , v. 19, p. 4999-5003, 2009.
WHITLOCK, GAVIN A. ; BRENNAN, PAUL E. ; ROBERTS, LEE R. ; STOBIE, ALAN . Potent and selective α1A adrenoceptor partial agonists-Novel imidazole frameworks. Bioorganic & Medicinal Chemistry Letters (Print) , v. 19, p. 3118-3121, 2009.
LEY, STEVEN'V. ; TACKETT, MILES'N. ; MADDESS, MATTHEW'L. ; ANDERSON, JAMES'C. ; BRENNAN, PAUL'E. ; CAPPI, MICHAEL'W. ; HEER, JAG'P. ; HELGEN, CÉLINE ; KORI, MASAKUNI ; KOUKLOVSKY, CYRILLE ; MARSDEN, STEPHEN'P. ; NORMAN, JOANNE ; OSBORN, DAVID'P. ; PALOMERO, MARÍA'Á. ; PAVEY, JOHN'B.'J. ; PINEL, CATHERINE ; ROBINSON, LESLEY'A. ; SCHNAUBELT, JÜRGEN ; SCOTT, JAMES'S. ; SPILLING, CHRISTOPHER'D. ; WATANABE, HIDENORI ; WESSON, KIERON'E. ; WILLIS, MICHAEL'C. . Total Synthesis of Rapamycin. Chemistry - A European Journal , v. 15, p. 2874-2914, 2009.
ROONEY, TIMOTHY P. C. ; FILIPPAKOPOULOS, PANAGIS ; FEDOROV, OLEG ; PICAUD, SARAH ; CORTOPASSI, WILIAN A. ; HAY, DUNCAN A. ; MARTIN, SARAH ; TUMBER, ANTHONY ; ROGERS, CATHERINE M. ; PHILPOTT, MARTIN ; WANG, MINGHUA ; THOMPSON, AMBER L. ; HEIGHTMAN, TOM D. ; PRYDE, DAVID C. ; COOK, ANDREW ; PATON, ROBERT S. ; MÜLLER, SUSANNE ; KNAPP, STEFAN ; BRENNAN, PAUL E. ; CONWAY, STUART J. . A Series of Potent CREBBP Bromodomain Ligands Reveals an Induced-Fit Pocket Stabilized by a Cation-π Interaction. Angewandte Chemie (International ed. Print) , 2014.

Histórico profissional

Endereço profissional

University of Oxford. , NDMRB, Roosevelt Drive, OX3 7FZ, Headington, 0000000 - Oxford, - Inglaterra, Telefone: (44) 1865612932

Experiência profissional

2011 - Atual

University of Oxford

Vínculo: Formal labor contract, Enquadramento Funcional: Principal Investigator

2005 - 2011

Pfizer UK

Vínculo: Formal labor contract, Enquadramento Funcional: Senior Principal Scientist

2003 - 2005

Amgen

Vínculo: Formal labor contract, Enquadramento Funcional: Research Scientist

2000 - 2003

University Of Cambridge

Vínculo: Formal labor contract, Enquadramento Funcional: Post doc

1989 - 1991

Genta Inc.

Vínculo: Formal labor contract, Enquadramento Funcional: Research Associate