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Page 1
Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases.
Harris PA, Berger SB, Jeong JU, Nagilla R, Bandyopadhyay D, Campobasso N, Capriotti CA, Cox JA, Dare L, Dong X, Eidam PM, Finger JN, Hoffman SJ, Kang J, Kasparcova V, King BW, Lehr R, Lan Y, Leister LK, Lich JD, MacDonald TT, Miller NA, Ouellette MT, Pao CS, Rahman A, Reilly MA, Rendina AR, Rivera EJ, Schaeffer MC, Sehon CA, Singhaus RR, Sun HH, Swift BA, Totoritis RD, Vossenkämper A, Ward P, Wisnoski DD, Zhang D, Marquis RW, Gough PJ, Bertin J. Harris PA, et al. Among authors: dare l. J Med Chem. 2017 Feb 23;60(4):1247-1261. doi: 10.1021/acs.jmedchem.6b01751. Epub 2017 Feb 10. J Med Chem. 2017. PMID: 28151659
DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors.
Harris PA, King BW, Bandyopadhyay D, Berger SB, Campobasso N, Capriotti CA, Cox JA, Dare L, Dong X, Finger JN, Grady LC, Hoffman SJ, Jeong JU, Kang J, Kasparcova V, Lakdawala AS, Lehr R, McNulty DE, Nagilla R, Ouellette MT, Pao CS, Rendina AR, Schaeffer MC, Summerfield JD, Swift BA, Totoritis RD, Ward P, Zhang A, Zhang D, Marquis RW, Bertin J, Gough PJ. Harris PA, et al. Among authors: dare l. J Med Chem. 2016 Mar 10;59(5):2163-78. doi: 10.1021/acs.jmedchem.5b01898. Epub 2016 Feb 23. J Med Chem. 2016. PMID: 26854747
Cutting Edge: RIP1 kinase activity is dispensable for normal development but is a key regulator of inflammation in SHARPIN-deficient mice.
Berger SB, Kasparcova V, Hoffman S, Swift B, Dare L, Schaeffer M, Capriotti C, Cook M, Finger J, Hughes-Earle A, Harris PA, Kaiser WJ, Mocarski ES, Bertin J, Gough PJ. Berger SB, et al. Among authors: dare l. J Immunol. 2014 Jun 15;192(12):5476-80. doi: 10.4049/jimmunol.1400499. Epub 2014 May 12. J Immunol. 2014. PMID: 24821972 Free PMC article.
Discovery of Small Molecule RIP1 Kinase Inhibitors for the Treatment of Pathologies Associated with Necroptosis.
Harris PA, Bandyopadhyay D, Berger SB, Campobasso N, Capriotti CA, Cox JA, Dare L, Finger JN, Hoffman SJ, Kahler KM, Lehr R, Lich JD, Nagilla R, Nolte RT, Ouellette MT, Pao CS, Schaeffer MC, Smallwood A, Sun HH, Swift BA, Totoritis RD, Ward P, Marquis RW, Bertin J, Gough PJ. Harris PA, et al. Among authors: dare l. ACS Med Chem Lett. 2013 Nov 4;4(12):1238-43. doi: 10.1021/ml400382p. eCollection 2013 Dec 12. ACS Med Chem Lett. 2013. PMID: 24900635 Free PMC article.
Characterization of GSK'963: a structurally distinct, potent and selective inhibitor of RIP1 kinase.
Berger SB, Harris P, Nagilla R, Kasparcova V, Hoffman S, Swift B, Dare L, Schaeffer M, Capriotti C, Ouellette M, King BW, Wisnoski D, Cox J, Reilly M, Marquis RW, Bertin J, Gough PJ. Berger SB, et al. Among authors: dare l. Cell Death Discov. 2015 Jul 27;1:15009. doi: 10.1038/cddiscovery.2015.9. eCollection 2015. Cell Death Discov. 2015. PMID: 27551444 Free PMC article.
MALT1 Protease Activity Is Required for Innate and Adaptive Immune Responses.
Yu JW, Hoffman S, Beal AM, Dykon A, Ringenberg MA, Hughes AC, Dare L, Anderson AD, Finger J, Kasparcova V, Rickard D, Berger SB, Ramanjulu J, Emery JG, Gough PJ, Bertin J, Foley KP. Yu JW, et al. Among authors: dare l. PLoS One. 2015 May 12;10(5):e0127083. doi: 10.1371/journal.pone.0127083. eCollection 2015. PLoS One. 2015. PMID: 25965667 Free PMC article.
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.
Kumar S, Dare L, Vasko-Moser JA, James IE, Blake SM, Rickard DJ, Hwang SM, Tomaszek T, Yamashita DS, Marquis RW, Oh H, Jeong JU, Veber DF, Gowen M, Lark MW, Stroup G. Kumar S, et al. Among authors: dare l. Bone. 2007 Jan;40(1):122-31. doi: 10.1016/j.bone.2006.07.015. Epub 2006 Sep 7. Bone. 2007. PMID: 16962401
Potent and selective inhibition of human cathepsin K leads to inhibition of bone resorption in vivo in a nonhuman primate.
Stroup GB, Lark MW, Veber DF, Bhattacharyya A, Blake S, Dare LC, Erhard KF, Hoffman SJ, James IE, Marquis RW, Ru Y, Vasko-Moser JA, Smith BR, Tomaszek T, Gowen M. Stroup GB, et al. Among authors: dare lc. J Bone Miner Res. 2001 Oct;16(10):1739-46. doi: 10.1359/jbmr.2001.16.10.1739. J Bone Miner Res. 2001. PMID: 11585335 Free article.
47 results