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MLKL compromises plasma membrane integrity by binding to phosphatidylinositol phosphates Y Dondelinger, W Declercq, S Montessuit, R Roelandt, A Goncalves, ... Cell reports 7 (4), 971-981, 2014 | 815 | 2014 |
RIP3 induces apoptosis independent of pronecrotic kinase activity P Mandal, SB Berger, S Pillay, K Moriwaki, C Huang, H Guo, JD Lich, ... Molecular cell 56 (4), 481-495, 2014 | 569 | 2014 |
Design of amidobenzimidazole STING receptor agonists with systemic activity JM Ramanjulu, GS Pesiridis, J Yang, N Concha, R Singhaus, SY Zhang, ... Nature 564 (7736), 439-443, 2018 | 563 | 2018 |
Novel peroxisome proliferator-activated receptor (PPAR) γ and PPARδ ligands produce distinct biological effects J Berger, MD Leibowitz, TW Doebber, A Elbrecht, B Zhang, G Zhou, ... Journal of Biological Chemistry 274 (10), 6718-6725, 1999 | 555 | 1999 |
Activation of PPARδ alters lipid metabolism in db/db mice MD Leibowitz, C Fiévet, N Hennuyer, J Peinado-Onsurbe, H Duez, ... FEBS letters 473 (3), 333-336, 2000 | 431 | 2000 |
N-((1S)-1-{[4-((2S)-2-{[(2, 4-dichlorophenyl) sulfonyl] amino}-3-hydroxypropanoyl)-1-piperazinyl] carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), a novel … KS Thorneloe, AC Sulpizio, Z Lin, DJ Figueroa, AK Clouse, GP McCafferty, ... Journal of Pharmacology and Experimental Therapeutics 326 (2), 432-442, 2008 | 419 | 2008 |
Discovery of a first-in-class receptor interacting protein 1 (RIP1) kinase specific clinical candidate (GSK2982772) for the treatment of inflammatory diseases PA Harris, SB Berger, JU Jeong, R Nagilla, D Bandyopadhyay, ... Journal of medicinal chemistry 60 (4), 1247-1261, 2017 | 416 | 2017 |
An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure KS Thorneloe, M Cheung, W Bao, H Alsaid, S Lenhard, MY Jian, ... Science translational medicine 4 (159), 159ra148-159ra148, 2012 | 334 | 2012 |
Systemic activation of the transient receptor potential vanilloid subtype 4 channel causes endothelial failure and circulatory collapse: Part 2 RN Willette, W Bao, S Nerurkar, T Yue, CP Doe, G Stankus, GH Turner, ... Journal of Pharmacology and Experimental Therapeutics 326 (2), 443-452, 2008 | 319 | 2008 |
DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors PA Harris, BW King, D Bandyopadhyay, SB Berger, N Campobasso, ... Journal of medicinal chemistry 59 (5), 2163-2178, 2016 | 246 | 2016 |
Potent and selective inhibition of human cathepsin K leads to inhibition of bone resorption in vivo in a nonhuman primate GB Stroup, MW Lark, DF Veber, A Bhattacharyya, S Blake, LC Dare, ... Journal of Bone and Mineral Research 16 (10), 1739-1746, 2001 | 183 | 2001 |
Discovery of small molecule RIP1 kinase inhibitors for the treatment of pathologies associated with necroptosis PA Harris, D Bandyopadhyay, SB Berger, N Campobasso, CA Capriotti, ... ACS medicinal chemistry letters 4 (12), 1238-1243, 2013 | 148 | 2013 |
A highly potent inhibitor of cathepsin K (relacatib) reduces biomarkers of bone resorption both in vitro and in an acute model of elevated bone turnover in vivo in monkeys S Kumar, L Dare, JA Vasko-Moser, IE James, SM Blake, DJ Rickard, ... Bone 40 (1), 122-131, 2007 | 143 | 2007 |
Characterization of GSK′ 963: a structurally distinct, potent and selective inhibitor of RIP1 kinase SB Berger, P Harris, R Nagilla, V Kasparcova, S Hoffman, B Swift, L Dare, ... Cell death discovery 1 (1), 1-7, 2015 | 136 | 2015 |
Azepanone-based inhibitors of human and rat cathepsin K RW Marquis, Y Ru, SM LoCastro, J Zeng, DS Yamashita, HJ Oh, ... Journal of medicinal chemistry 44 (9), 1380-1395, 2001 | 136 | 2001 |
The Identification and Pharmacological Characterization of 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine (GSK583), a Highly Potent and … PA Haile, BJ Votta, RW Marquis, MJ Bury, JF Mehlmann, R Singhaus Jr, ... Journal of medicinal chemistry 59 (10), 4867-4880, 2016 | 106 | 2016 |
An orally active calcium-sensing receptor antagonist that transiently increases plasma concentrations of PTH and stimulates bone formation S Kumar, CJ Matheny, SJ Hoffman, RW Marquis, M Schultz, X Liang, ... Bone 46 (2), 534-542, 2010 | 94 | 2010 |
A potent small molecule, nonpeptide inhibitor of cathepsin K (SB 331750) prevents bone matrix resorption in the ovariectomized rat MW Lark, GB Stroup, IE James, RA Dodds, SM Hwang, SM Blake, ... Bone 30 (5), 746-753, 2002 | 93 | 2002 |
Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors DS Yamashita, RW Marquis, R Xie, SD Nidamarthy, HJ Oh, JU Jeong, ... Journal of medicinal chemistry 49 (5), 1597-1612, 2006 | 81 | 2006 |