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A randomized, placebo-controlled experimental medicine study of RIPK1 inhibitor GSK2982772 in patients with moderate to severe rheumatoid arthritis.
Weisel K, Berger S, Thorn K, Taylor PC, Peterfy C, Siddall H, Tompson D, Wang S, Quattrocchi E, Burriss SW, Walter J, Tak PP. Weisel K, et al. Among authors: berger s. Arthritis Res Ther. 2021 Mar 16;23(1):85. doi: 10.1186/s13075-021-02468-0. Arthritis Res Ther. 2021. PMID: 33726834 Free PMC article. Clinical Trial.
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. 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.
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: berger sb. 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
Discovery of a First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific Clinical Candidate, 2-((4-(Benzo[d]thiazol-5-ylamino)-6-(tert-butylsulfonyl)quinazolin-7-yl)oxy)ethyl Dihydrogen Phosphate, for the Treatment of Inflammatory Diseases.
Haile PA, Casillas LN, Votta BJ, Wang GZ, Charnley AK, Dong X, Bury MJ, Romano JJ, Mehlmann JF, King BW, Erhard KF, Hanning CR, Lipshutz DB, Desai BM, Capriotti CA, Schaeffer MC, Berger SB, Mahajan MK, Reilly MA, Nagilla R, Rivera EJ, Sun HH, Kenna JK, Beal AM, Ouellette MT, Kelly M, Stemp G, Convery MA, Vossenkämper A, MacDonald TT, Gough PJ, Bertin J, Marquis RW. Haile PA, et al. J Med Chem. 2019 Jul 25;62(14):6482-6494. doi: 10.1021/acs.jmedchem.9b00575. Epub 2019 Jul 2. J Med Chem. 2019. PMID: 31265286
RIPK1 ensures intestinal homeostasis by protecting the epithelium against apoptosis.
Takahashi N, Vereecke L, Bertrand MJ, Duprez L, Berger SB, Divert T, Gonçalves A, Sze M, Gilbert B, Kourula S, Goossens V, Lefebvre S, Günther C, Becker C, Bertin J, Gough PJ, Declercq W, van Loo G, Vandenabeele P. Takahashi N, et al. Among authors: berger sb. Nature. 2014 Sep 4;513(7516):95-9. doi: 10.1038/nature13706. Nature. 2014. PMID: 25186904
2,739 results