Widespread potential for growth-factor-driven resistance to anticancer kinase inhibitors TR Wilson, J Fridlyand, Y Yan, E Penuel, L Burton, E Chan, J Peng, E Lin, ... Nature 487 (7408), 505-509, 2012 | 1334 | 2012 |
GDC-0449—A potent inhibitor of the hedgehog pathway KD Robarge, SA Brunton, GM Castanedo, Y Cui, MS Dina, R Goldsmith, ... Bioorganic & medicinal chemistry letters 19 (19), 5576-5581, 2009 | 463 | 2009 |
Small molecule inhibition of GDC-0449 refractory smoothened mutants and downstream mechanisms of drug resistance GJP Dijkgraaf, B Alicke, L Weinmann, T Januario, K West, Z Modrusan, ... Cancer research 71 (2), 435-444, 2011 | 422 | 2011 |
Synthesis and application of functionally diverse 2, 6, 9-trisubstituted purine libraries as CDK inhibitors YT Chang, NS Gray, GR Rosania, DP Sutherlin, S Kwon, TC Norman, ... Chemistry & biology 6 (6), 361-375, 1999 | 390 | 1999 |
Structural basis of Nav1. 7 inhibition by an isoform-selective small-molecule antagonist S Ahuja, S Mukund, L Deng, K Khakh, E Chang, H Ho, S Shriver, C Young, ... Science 350 (6267), aac5464, 2015 | 330 | 2015 |
GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway JJ Wallin, KA Edgar, J Guan, M Berry, WW Prior, L Lee, JD Lesnick, ... Molecular cancer therapeutics 10 (12), 2426-2436, 2011 | 296 | 2011 |
Myoseverin, a microtubule-binding molecule with novel cellular effects GR Rosania, YT Chang, O Perez, D Sutherlin, H Dong, DJ Lockhart, ... Nature biotechnology 18 (3), 304-308, 2000 | 267 | 2000 |
Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the … DP Sutherlin, L Bao, M Berry, G Castanedo, I Chuckowree, J Dotson, ... Journal of medicinal chemistry 54 (21), 7579-7587, 2011 | 231 | 2011 |
A method for directed evolution and functional cloning of enzymes H Pedersen, S Hölder, DP Sutherlin, U Schwitter, DS King, PG Schultz Proceedings of the National Academy of Sciences 95 (18), 10523-10528, 1998 | 229 | 1998 |
Selective inhibition of fibroblast activation protein protease based on dipeptide substrate specificity CY Edosada, C Quan, C Wiesmann, T Tran, D Sutherlin, M Reynolds, ... Journal of Biological Chemistry 281 (11), 7437-7444, 2006 | 182 | 2006 |
Fibroblast activation protein cleaves and inactivates fibroblast growth factor 21 DR Dunshee, TW Bainbridge, NM Kljavin, J Zavala-Solorio, ... Journal of Biological Chemistry 291 (11), 5986-5996, 2016 | 151 | 2016 |
Discovery of (thienopyrimidin-2-yl) aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer DP Sutherlin, D Sampath, M Berry, G Castanedo, Z Chang, I Chuckowree, ... Journal of medicinal chemistry 53 (3), 1086-1097, 2010 | 148 | 2010 |
Generation of C-glycoside peptide ligands for cell surface carbohydrate receptors using a four-component condensation on solid support DP Sutherlin, TM Stark, R Hughes, RW Armstrong The Journal of organic chemistry 61 (23), 8350-8354, 1996 | 131 | 1996 |
In vitro sulfotransferase activity of NodH, a nodulation protein of Rhizobium meliloti required for host-specific nodulation DW Ehrhardt, EM Atkinson, KF Faull, DI Freedberg, DP Sutherlin, ... Journal of Bacteriology 177 (21), 6237-6245, 1995 | 122 | 1995 |
Synthesis of tetrasubstituted thiophenes on solid-support using the Gewald reaction GM Castanedo, DP Sutherlin Tetrahedron Letters 42 (41), 7181-7184, 2001 | 100 | 2001 |
Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor TP Heffron, M Berry, G Castanedo, C Chang, I Chuckowree, J Dotson, ... Bioorganic & medicinal chemistry letters 20 (8), 2408-2411, 2010 | 97 | 2010 |
Inhibition and reversal of myogenic differentiation by purine-based microtubule assembly inhibitors OD Perez, YT Chang, G Rosania, D Sutherlin, PG Schultz Chemistry & biology 9 (4), 475-483, 2002 | 95 | 2002 |
Rational design of phosphoinositide 3-kinase α inhibitors that exhibit selectivity over the phosphoinositide 3-kinase β isoform TP Heffron, BQ Wei, A Olivero, ST Staben, V Tsui, S Do, J Dotson, ... Journal of medicinal chemistry 54 (22), 7815-7833, 2011 | 83 | 2011 |
Discovery and preclinical development of vismodegib SE Gould, JA Low, JC Marsters Jr, K Robarge, LL Rubin, FJ de Sauvage, ... Expert opinion on drug discovery 9 (8), 969-984, 2014 | 79 | 2014 |
Discovery of Aryl Sulfonamides as Isoform-Selective Inhibitors of NaV1.7 with Efficacy in Rodent Pain Models T Focken, S Liu, N Chahal, M Dauphinais, ME Grimwood, S Chowdhury, ... ACS medicinal chemistry letters 7 (3), 277-282, 2016 | 78 | 2016 |