Thomas Hunsaker

genentech inc

H指数:20

被引数:2,057

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Discovery and Optimization of a Potent; Efficacious; and Brain-Penetrant Inhibitor of KRAS G12C

发现和优化一种强效、高效且能穿透血脑屏障的KRAS G12C抑制剂

Journal of Medicinal Chemistry

IF6.8

2026-03-020

PRE

Matthew L. Landry; Sushant Malhotra; Maureen Beresini; Connie Chan; Emily Chan; Cecile C. de la Cruz; Nicholas F. Endres; Marie Evangelista; Amy Gustafson; Dennis Hu; Thomas Hunsaker; Peter Hsu; Yevgeniy Izrayelit; Hank La; Pablo Saenz-Lopez Larrocha; Qihui Lian; Mark Merchant; Jialin Mao; Rana Mroue; Angela Oh; Emile Plise; Cheng Shao; Michael Siu; John C. Tran; Yanguang Wang; Weiru Wang; Binqing Wei; Susan Wong; Chun-Wan Yen; Yuhui Zhou; Hans E. Purkey; Timothy P. Heffron; Laurent Salphati

Discovery and Characterization of Divarasib (GDC-6036); a Potent Covalent Inhibitor of KRAS G12C

Divarasib (GDC-6036)的发现与表征：一种强效的KRAS G12C共价抑制剂

Journal of Medicinal Chemistry

IF6.8

2026-03-020

PRE

Nicholas F. Endres; Steven Do; Rana Mroue; Jack A. Terrett; Matt Saabye; Angela Oh; Thomas Hunsaker; Emily Chan; John C. Tran; Lan K. Nguyen; Qihui Lian; Taylur P. Ma; Thomas Garner; Luca Gerosa; Maureen Beresini; Aaron Boudreau; Sarah M. Bronner; Patrick Cyr; Noriko Ishisoko; Yevgeniy Izrayelit; Fan Jiang; Terry Kellar; Hank La; Sharada Labadie; Matthew Lardy; Liling Liu; Wendy Liu; Sarah Miller; Joachim Rudolph; Emile Plise; Benjamin D. Sellers; Cheng Shao; Weiru Wang; Yanguang Wang; Wentao Wei; Susan Wong; Christine Yu; Kebing Yu; Po-Wai Yuen; Richard Zang; Chenghong Zhang; Yuhui Zhou; Xiaoyu Zhu; John G. Quinn; Xin Ye; James R. Kiefer; Jialin Mao; Marie Evangelista; Mark Merchant; Matthew L. Landry; Sushant Malhotra; Hans E. Purkey

Identification of GDC-1971 (RLY-1971), a SHP2 Inhibitor Designed for the Treatment of Solid Tumors

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2023-09-2916

PRE

Taylor, Alexander M.; Williams, Bret R.; Giordanetto, Fabrizio; Kelley, Elizabeth H.; Lescarbeau, Andre; Shortsleeves, Kelley; Tang, Yong; Walters, W. Patrick; Arrazate, Alfonso; Bowman, Christine; Brophy, Erin; Chan, Emily W.; Deshmukh, Gauri; Greisman, Jack B.; Hunsaker, Thomas L.; Kipp, D. Randal; Lopez-Larrocha, Pablo Saenz; Maddalo, Danilo; Martin, Iain J.; Maragakis, Paul; Merchant, Mark; Murcko, Mark; Nisonoff, Hunter; Nguyen, Vi; Nguyen, Vy; Orozco, Olivia; Owen, Christopher; Pierce, Levi; Schmidt, Molly; Shaw, David E.; Smith, Sherri; Therrien, Eric; Tran, John C.; Watters, Jim; Waters, Nigel J.; Wilbur, Jeremy; Willmore, Lindsay

Quantifying KRAS G12C Covalent Drug Inhibitor Activity in Mouse Tumors Using Mass Spectrometry

ANALYTICAL CHEMISTRY

IF6.7

2023-03-064

PRE

Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3H)-quinazolinone Aryl Urea pan-RAF Kinase Inhibitor

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2021-03-2920

PRE

Entrectinib, a TRK/ROS1 inhibitor with anti-CNS tumor activity: differentiation from other inhibitors in its class due to weak interaction with P-glycoprotein

NEURO-ONCOLOGY

IF13.4

2020-05-0866

OAAI

Determination of the efficacious Entrectinib exposures required for pathway inhibition and anti-tumor activity in a subcutaneous and intracranialTPM3-NTRK1mutant tumor model

CANCER RESEARCH

IF16.6

2019-07-013

PRE

Pan-Cancer Metabolic Signature Predicts Co-Dependency on Glutaminase and De Novo Glutathione Synthesis Linked to a High-Mesenchymal Cell State

CELL METABOLISM

IF30.9

2018-09-0163

OAAI

Pharmacologically induced RAS-GTP levels and CRAF-BRAF hetero-dimerization drive sensitization to Type II pan-RAF inhibitors in KRAS mutant cancer

CANCER RESEARCH

IF16.6

2018-07-010

PRE

GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP)

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2017-09-2199

PREAI

Romero, F. Anthony; Murray, Jeremy; Lai, Kwong Wah; Tsui, Vickie; Albrecht, Brian K.; An, Le; Beresini, Maureen H.; Boenig, Gladys de Leon; Bronner, Sarah M.; Chan, Emily W.; Chen, Kevin X.; Chen, Zhongguo; Choo, Edna F.; Clagg, Kyle; Clark, Kevin; Crawford, Terry D.; Cyr, Patrick; Nagata, Denise de Almeida; Gascoigne, Karen E.; Grogan, Jane L.; Hatzivassiliou, Georgia; Huang, Wei; Hunsaker, Thomas L.; Kaufman, Susan; Koenig, Stefan G.; Li, Ruina; Li, Yingjie; Liang, Xiaorong; Liao, Jiangpeng; Liu, Wenfeng; Ly, Justin; Maher, Jonathan; Masui, Colin; Merchant, Mark; Ran, Yingqing; Taylor, Alexander M.; Wai, John; Wang, Fei; Wei, Xiaocang; Yu, Dong; Zhu, Bing-Yan; Zhu, Xiaoyu; Magnuson, Steven

RAF kinase inhibition synergizes with MEK inhibitors in KRAS mutant tumors

CANCER RESEARCH

IF16.6

2017-07-010

PRE

Preclinical validation of ERK inhibition via GDC-0994 as a potent therapeutic strategy in BRAFV600E mutant colorectal cancers

EUROPEAN JOURNAL OF CANCER

IF7.1

2016-12-010

PREAI

Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2016-09-2883

PREAI

Crawford, Terry D.; Romero, F. Anthony; Lai, Kwong Wah; Tsui, Vickie; Taylor, Alexander M.; Boenig, Gladys de Leon; Noland, Cameron L.; Murray, Jeremy; Ly, Justin; Choo, Edna F.; Hunsaker, Thomas L.; Chan, Emily W.; Merchant, Mark; Kharbanda, Samir; Gascoigne, Karen E.; Kaufman, Susan; Beresini, Maureen H.; Liao, Jiangpeng; Liu, Wenfeng; Chen, Kevin X.; Chen, Zhongguo; Conery, Andrew R.; Cote, Alexandre; Jayaram, Hariharan; Jiang, Ying; Kiefer, James R.; Kleinheinz, Tracy; Li, Yingjie; Maher, Jonathan; Pardo, Eneida; Poy, Florence; Spillane, Kerry L.; Wang, Fei; Wang, Jian; Wei, Xiaocang; Xu, Zhaowu; Xu, Zhongya; Yen, Ivana; Zawadzke, Laura; Zhu, Xiaoyu; Bellon, Steven; Cummings, Richard; Cochran, Andrea G.; Albrecht, Brian K.; Magnuson, Steven

Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2016-06-07128

OAAI

Blake, James F.; Burkard, Michael; Chan, Jocelyn; Chen, Huifen; Chou, Kang-Jye; Diaz, Dolores; Dudley, Danette A.; Gaudino, John J.; Gould, Stephen E.; Grina, Jonas; Hunsaker, Thomas; Liu, Lichuan; Martinson, Matthew; Moreno, David; Mueller, Lars; Orr, Christine; Pacheco, Patricia; Qin, Ann; Rasor, Kevin; Ren, Li; Robarse, Kirk; Shahidi-Latham, Sheerin; Stults, Jeffrey; Sullivan, Francis; Wang, Weiru; Yin, Jianping; Zhou, Aihe; Belvin, Marcia; Merchant, Mark; Moffat, John; Schwarz, Jacob B.

Combination of the ERK inhibitor GDC-0994 with the MEK inhibitor cobimetinib significantly enhances anti-tumor activity in KRAS and BRAF mutant tumor models

EUROPEAN JOURNAL OF CANCER

IF7.1

2014-11-017

PREAI

A high-content cellular senescence screen identifies candidate tumor suppressors, including EPHA3

CELL CYCLE

IF3.4

2014-10-3118

OAAI

An Integrated Genomic Screen Identifies LDHB as an Essential Gene for Triple-Negative Breast Cancer

CANCER RESEARCH