Oncometabolite 2-hydroxyglutarate is a competitive inhibitor of α-ketoglutarate-dependent dioxygenases W Xu, H Yang, Y Liu, Y Yang, P Wang, SH Kim, S Ito, C Yang, P Wang, ... Cancer cell 19 (1), 17-30, 2011 | 3012 | 2011 |
The promise and peril of chemical probes CH Arrowsmith, JE Audia, C Austin, J Baell, J Bennett, J Blagg, C Bountra, ... Nature chemical biology 11 (8), 536-541, 2015 | 833 | 2015 |
Dynamic reprogramming of the kinome in response to targeted MEK inhibition in triple-negative breast cancer JS Duncan, MC Whittle, K Nakamura, AN Abell, AA Midland, ... Cell 149 (2), 307-321, 2012 | 828 | 2012 |
A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells M Vedadi, D Barsyte-Lovejoy, F Liu, S Rival-Gervier, A Allali-Hassani, ... Nature chemical biology 7 (8), 566-574, 2011 | 547 | 2011 |
An orally bioavailable chemical probe of the lysine methyltransferases EZH2 and EZH1 KD Konze, A Ma, F Li, D Barsyte-Lovejoy, T Parton, CJ MacNevin, F Liu, ... ACS chemical biology 8 (6), 1324-1334, 2013 | 480 | 2013 |
The art of the chemical probe SV Frye Nature chemical biology 6 (3), 159-161, 2010 | 443 | 2010 |
Too many roads not taken AM Edwards, R Isserlin, GD Bader, SV Frye, TM Willson, FH Yu Nature 470 (7333), 163-165, 2011 | 435 | 2011 |
Discovery of β-arrestin–biased dopamine D2 ligands for probing signal transduction pathways essential for antipsychotic efficacy JA Allen, JM Yost, V Setola, X Chen, MF Sassano, M Chen, S Peterson, ... Proceedings of the National Academy of Sciences 108 (45), 18488-18493, 2011 | 380 | 2011 |
Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis HN Bramson, J Corona, ST Davis, SH Dickerson, M Edelstein, SV Frye, ... Journal of medicinal chemistry 44 (25), 4339-4358, 2001 | 317 | 2001 |
The discovery of potent cRaf1 kinase inhibitors K Lackey, M Cory, R Davis, SV Frye, PA Harris, RN Hunter, DK Jung, ... Bioorganic & medicinal chemistry letters 10 (3), 223-226, 2000 | 293 | 2000 |
Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP F Liu, D Barsyte-Lovejoy, F Li, Y Xiong, V Korboukh, XP Huang, ... Journal of medicinal chemistry 56 (21), 8931-8942, 2013 | 264 | 2013 |
Structure and inhibition of microbiome β-glucuronidases essential to the alleviation of cancer drug toxicity BD Wallace, AB Roberts, RM Pollet, JD Ingle, KA Biernat, SJ Pellock, ... Chemistry & biology 22 (9), 1238-1249, 2015 | 250 | 2015 |
Discovery of a 2, 4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a F Liu, X Chen, A Allali-Hassani, AM Quinn, GA Wasney, A Dong, ... Journal of medicinal chemistry 52 (24), 7950-7953, 2009 | 246 | 2009 |
Prevention of chemotherapy-induced alopecia in rats by CDK inhibitors ST Davis, BG Benson, HN Bramson, DE Chapman, SH Dickerson, ... Science 291 (5501), 134-137, 2001 | 245 | 2001 |
Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia B Xu, DM On, A Ma, T Parton, KD Konze, SG Pattenden, DF Allison, L Cai, ... Blood, The Journal of the American Society of Hematology 125 (2), 346-357, 2015 | 234 | 2015 |
Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2, 4-diamino-7-aminoalkoxy-quinazolines. F Liu, X Chen, A Allali-Hassani, AM Quinn, TJ Wigle, GA Wasney, A Dong, ... Journal of medicinal chemistry 53 (15), 5844-5857, 2010 | 218 | 2010 |
Unique preclinical characteristics of GG745, a potent dual inhibitor of 5AR HN Bramson, D Hermann, KW Batchelor, FW Lee, MK James, SV Frye Journal of Pharmacology and Experimental Therapeutics 282 (3), 1496-1502, 1997 | 203 | 1997 |
Chelates as intermediates in nucleophilic additions to alkoxy ketones according to Cram's rule (cyclic model) X Chen, ER Hortelano, EL Eliel, SV Frye Journal of the American Chemical Society 114 (5), 1778-1784, 1992 | 194 | 1992 |
Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain LI James, D Barsyte-Lovejoy, N Zhong, L Krichevsky, VK Korboukh, ... Nature chemical biology 9 (3), 184-191, 2013 | 188 | 2013 |
Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines F Liu, D Barsyte-Lovejoy, A Allali-Hassani, Y He, JM Herold, X Chen, ... Journal of medicinal chemistry 54 (17), 6139-6150, 2011 | 162 | 2011 |