J
James R. Kiefer
Researcher at Genentech
Publications - 52
Citations - 1606
James R. Kiefer is an academic researcher from Genentech. The author has contributed to research in topics: Medicine & Bromodomain. The author has an hindex of 19, co-authored 47 publications receiving 1250 citations. Previous affiliations of James R. Kiefer include Pharmacia & Pfizer.
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Journal ArticleDOI
An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells
Maia Vinogradova,Victor S. Gehling,Amy Gustafson,Shilpi Arora,Charles Tindell,Catherine Wilson,Kaylyn E. Williamson,Gulfem D. Guler,Pranoti Gangurde,Wanda Manieri,Jennifer Busby,E. Megan Flynn,Fei Lan,Hyojin Kim,Shobu Odate,Andrea G. Cochran,Yichin Liu,Matthew Wongchenko,Yibin Yang,Tommy K. Cheung,Tobias M. Maile,Ted Lau,Michael R. Costa,Ganapati V. Hegde,Erica L. Jackson,Robert M. Pitti,David Arnott,Christopher M. Bailey,Steve Bellon,Richard T. Cummings,Brian K. Albrecht,Jean-Christophe Harmange,James R. Kiefer,Patrick Trojer,Marie Classon +34 more
TL;DR: Findings show that pretreatment of cancer cells with a KDM5-specific inhibitor results in the ablation of a subpopulation of cancers cells that can serve as the founders for therapeutic relapse.
Journal ArticleDOI
Cyclooxygenase enzymes: catalysis and inhibition
TL;DR: Crystal structures of fatty acid substrate and prostaglandin product complexes have been elucidated, and novel substrates of cyclooxygenase-2 have been identified.
Journal ArticleDOI
Structural basis for dual-mode inhibition of the ABC transporter MsbA
Hoangdung Ho,Anh Miu,Mary Kate Alexander,Natalie K. Garcia,Angela Oh,Inna Zilberleyb,Mike Reichelt,Cary D. Austin,Christine Tam,Stephanie Shriver,Huiyong Hu,Sharada Labadie,Jun Liang,Lan Wang,Jian Wang,Yan Lu,Hans E. Purkey,John G. Quinn,Yvonne Franke,Kevin R Clark,Maureen Beresini,Man-Wah Tan,Benjamin D. Sellers,Till Maurer,Michael F. T. Koehler,Aaron T. Wecksler,James R. Kiefer,Vishal Verma,Yiming Xu,Mireille Nishiyama,Jian Payandeh,Christopher M. Koth +31 more
TL;DR: A framework for the selective modulation of ABC transporters is established and provides rational avenues for the design of new antibiotics and other therapeutics targeting this protein family.
Journal ArticleDOI
Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains
Terry Crawford,Vickie Tsui,E. Megan Flynn,Shumei Wang,Alexander M. Taylor,Alexandre Côté,James E. Audia,Maureen Beresini,Daniel J. Burdick,Richard D. Cummings,Les A. Dakin,Martin Duplessis,Andrew C. Good,Michael C. Hewitt,Hon-Ren Huang,Hariharan Jayaram,James R. Kiefer,Ying Jiang,Jeremy Murray,Christopher G. Nasveschuk,Eneida Pardo,Florence Poy,F. Anthony Romero,Yong Tang,Jian Wang,Zhaowu Xu,Laura Zawadzke,Xiaoyu Zhu,Brian K. Albrecht,Steven Magnuson,Steve Bellon,Andrea G. Cochran +31 more
TL;DR: The preference of distinct substituents for individual bromodomains provided selectivity handles useful for future lead optimization efforts for selective BRD9, CECR2, and TAF1(2) inhibitors.
Journal ArticleDOI
Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637).
Alexander M. Taylor,Alexandre Côté,Michael C. Hewitt,Richard Pastor,Yves Leblanc,Christopher G. Nasveschuk,F. Anthony Romero,Terry Crawford,Nico Cantone,Hariharan Jayaram,Jeremy W. Setser,Jeremy Murray,Maureen Beresini,Gladys de Leon Boenig,Zhongguo Chen,Andrew R. Conery,Richard T. Cummings,Leslie A. Dakin,E. Megan Flynn,Oscar W. Huang,Susan Kaufman,Patricia J. Keller,James R. Kiefer,Tommy Lai,Yingjie Li,Jiangpeng Liao,Wenfeng Liu,Henry Lu,Eneida Pardo,Vickie Tsui,Jian Wang,Yongyun Wang,Zhaowu Xu,Fen Yan,Dong Yu,Laura Zawadzke,Xiaoqin Zhu,Xiaoyu Zhu,Robert J. Sims,Andrea G. Cochran,Steve Bellon,James E. Audia,Steven Magnuson,Brian K. Albrecht +43 more
TL;DR: A series of cell-potent and selective probes of the CBP/EP300 bromodomains, derived from the fragment screening hit 4-methyl-1,3,4,5-tetrahydro-2H-benzo[b][1,4]diazepin-2-one are reported here.