Dorjsuren, Dorjbal; Eastman, Richard T.; Wicht, Kathryn J.; Jansen, Daniel; Talley, Daniel C.; Sigmon, Benjamin A.; Zakharov, Alexey V.; Roncal, Norma; Girvin, Andrew T.; Antonova-Koch, Yevgeniya; Will, Paul M.; Shah, Pranav; Sun, Hongmao; Klumpp-Thomas, Carleen; Mok, Sachel; Yeo, Tomas; Meister, Stephan; Marugan, Juan Jose; Ross, Leila S.; Xu, Xin; Maloney, David J.; Jadhav, Ajit; Mott, Bryan T.; Sciotti, Richard J.; Winzeler, Elizabeth A.; Waters, Norman C.; Campbell, Robert F.; Huang, Wenwei; Simeonov, Anton; Fidock, David A.

Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2020-09-0933

OAAI

Rai, Ganesha; Urban, Daniel J.; Mott, Bryan T.; Hu, Xin; Yang, Shyh-Ming; Benavides, Gloria A.; Johnson, Michelle S.; Squadrito, Giuseppe L.; Brimacombe, Kyle R.; Lee, Tobie D.; Cheff, Dorian M.; Zhu, Hu; Henderson, Mark J.; Pohida, Katherine; Sulikowski, Gary A.; Dranow, David M.; Kabir, Md; Shah, Pranav; Padilha, Elias; Tao, Dingyin; Fang, Yuhong; Christov, Plamen P.; Kim, Kwangho; Jana, Somnath; Muttil, Pavan; Anderson, Tamara; Kunda, Nitesh K.; Hathaway, Helen J.; Kusewitt, Donna F.; Oshima, Nobu; Cherukuri, Murali; Davies, Douglas R.; Norenberg, Jeffrey P.; Sklar, Larry A.; Moore, William J.; Dang, Chi, V; Stott, Gordon M.; Neckers, Leonard; Flint, Andrew J.; Darley-Usmar, Victor M.; Simeonov, Anton; Waterson, Alex G.; Jadhav, Ajit; Hall, Matthew D.; Maloney, David J.

Dynamic Imaging of LDH Inhibition in Tumors Reveals Rapid In Vivo Metabolic Rewiring and Vulnerability to Combination Therapy

肿瘤中LDH抑制的动态成像揭示了快速的体内代谢重组和对联合治疗的脆弱性

CELL REPORTS

IF6.9

2020-02-0181

OAAI

Oshima, Nobu; Ishida, Ryo; Kishimoto, Shun; Beebe, Kristin; Brender, Jeffrey R.; Yamamoto, Kazutoshi; Urban, Daniel; Rai, Ganesha; Johnson, Michelle S.; Benavides, Gloria; Squadrito, Giuseppe L.; Crooks, Dan; Jackson, Joseph; Joshi, Abhinav; Mott, Bryan T.; Shrimp, Jonathan H.; Moses, Michael A.; Lee, Min-Jung; Yuno, Akira; Lee, Tobie D.; Hu, Xin; Anderson, Tamara; Kusewitt, Donna; Hathaway, Helen H.; Jadhav, Ajit; Picard, Didier; Trepel, Jane B.; Mitchell, James B.; Stott, Gordon M.; Moore, William; Simeonov, Anton; Sklar, Larry A.; Norenberg, Jeffrey P.; Linehan, W. Marston; Maloney, David J.; Dang, Chi V.; Waterson, Alex G.; Hall, Matthew; Darley-Usmar, Victor M.; Krishna, Murali C.; Neckers, Leonard M.

Structure-Based Engineering of Irreversible Inhibitors against Histone Lysine Demethylase KDM5A

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2018-11-0326

OAAI

Room-Temperature, Copper-Free Sonogashira Reactions Facilitated by Air-Stable, Monoligated Precatalyst [DTBNpP] Pd(crotyl)Cl

ACS OMEGA

IF4.3

2018-10-105

OAAI

Insights into the Action of Inhibitor Enantiomers against Histone Lysine Demethylase 5A

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2018-03-149

OAAI

Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH)

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2017-11-09107

OAAI

Rai, Ganesha; Brimacombe, Kyle R.; Mott, Bryan T.; Urban, Daniel J.; Hu, Xin; Yang, Shyh-Ming; Lee, Tobie D.; Cheff, Dorian M.; Kouznetsova, Jennifer; Benavides, Gloria A.; Pohida, Katie; Kuenstner, Eric J.; Luci, Diane K.; Lukacs, Christine M.; Davies, Douglas R.; Dranow, David M.; Zhu, Hu; Sulikowski, Gary; Moore, William J.; Stott, Gordon M.; Flint, Andrew J.; Hall, Matthew D.; Darley-Usmar, Victor M.; Neckers, Leonard M.; Dang, Chi V.; Waterson, Alex G.; Simeonov, Anton; Jadhav, Ajit; Maloney, David J.

Monitoring the impact on metabolic flux in vivo of a newly developed LDH inhibitor using hyperpolarized 13C magnetic resonance spectroscopic imaging

CANCER RESEARCH

IF16.6

2017-07-010

PRE

mQC: A Heuristic Quality-Control Metric for High-Throughput Drug Combination Screening

SCIENTIFIC REPORTS

IF3.9

2016-11-248

OAAI

Structural Basis for KDM5A Histone Lysine Demethylase Inhibition by Diverse Compounds

CELL CHEMICAL BIOLOGY