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Page 1
Design of amidobenzimidazole STING receptor agonists with systemic activity.
Ramanjulu JM, Pesiridis GS, Yang J, Concha N, Singhaus R, Zhang SY, Tran JL, Moore P, Lehmann S, Eberl HC, Muelbaier M, Schneck JL, Clemens J, Adam M, Mehlmann J, Romano J, Morales A, Kang J, Leister L, Graybill TL, Charnley AK, Ye G, Nevins N, Behnia K, Wolf AI, Kasparcova V, Nurse K, Wang L, Puhl AC, Li Y, Klein M, Hopson CB, Guss J, Bantscheff M, Bergamini G, Reilly MA, Lian Y, Duffy KJ, Adams J, Foley KP, Gough PJ, Marquis RW, Smothers J, Hoos A, Bertin J. Ramanjulu JM, et al. Among authors: singhaus r. Nature. 2018 Dec;564(7736):439-443. doi: 10.1038/s41586-018-0705-y. Epub 2018 Nov 7. Nature. 2018. PMID: 30405246
Author Correction: Design of amidobenzimidazole STING receptor agonists with systemic activity.
Ramanjulu JM, Pesiridis GS, Yang J, Concha N, Singhaus R, Zhang SY, Tran JL, Moore P, Lehmann S, Eberl HC, Muelbaier M, Schneck JL, Clemens J, Adam M, Mehlmann J, Romano J, Morales A, Kang J, Leister L, Graybill TL, Charnley AK, Ye G, Nevins N, Behnia K, Wolf AI, Kasparcova V, Nurse K, Wang L, Puhl AC, Li Y, Klein M, Hopson CB, Guss J, Bantscheff M, Bergamini G, Reilly MA, Lian Y, Duffy KJ, Adams J, Foley KP, Gough PJ, Marquis RW, Smothers J, Hoos A, Bertin J. Ramanjulu JM, et al. Among authors: singhaus r. Nature. 2019 Jun;570(7761):E53. doi: 10.1038/s41586-019-1265-5. Nature. 2019. PMID: 31142845
Identification of Quinoline-Based RIP2 Kinase Inhibitors with an Improved Therapeutic Index to the hERG Ion Channel.
Haile PA, Casillas LN, Bury MJ, Mehlmann JF, Singhaus R Jr, Charnley AK, Hughes TV, DeMartino MP, Wang GZ, Romano JJ, Dong X, Plotnikov NV, Lakdawala AS, Convery MA, Votta BJ, Lipshutz DB, Desai BM, Swift B, Capriotti CA, Berger SB, Mahajan MK, Reilly MA, Rivera EJ, Sun HH, Nagilla R, LePage C, Ouellette MT, Totoritis RD, Donovan BT, Brown BS, Chaudhary KW, Gough PJ, Bertin J, Marquis RW. Haile PA, et al. Among authors: singhaus r jr. ACS Med Chem Lett. 2018 Sep 26;9(10):1039-1044. doi: 10.1021/acsmedchemlett.8b00344. eCollection 2018 Oct 11. ACS Med Chem Lett. 2018. PMID: 30344914 Free PMC article.
The Identification and Pharmacological Characterization of 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine (GSK583), a Highly Potent and Selective Inhibitor of RIP2 Kinase.
Haile PA, Votta BJ, Marquis RW, Bury MJ, Mehlmann JF, Singhaus R Jr, Charnley AK, Lakdawala AS, Convery MA, Lipshutz DB, Desai BM, Swift B, Capriotti CA, Berger SB, Mahajan MK, Reilly MA, Rivera EJ, Sun HH, Nagilla R, Beal AM, Finger JN, Cook MN, King BW, Ouellette MT, Totoritis RD, Pierdomenico M, Negroni A, Stronati L, Cucchiara S, Ziółkowski B, Vossenkämper A, MacDonald TT, Gough PJ, Bertin J, Casillas LN. Haile PA, et al. Among authors: singhaus r jr. J Med Chem. 2016 May 26;59(10):4867-80. doi: 10.1021/acs.jmedchem.6b00211. Epub 2016 May 4. J Med Chem. 2016. PMID: 27109867
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: singhaus rr. 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
Correction to Identification of Quinoline-Based RIP2 Kinase Inhibitors with an Improved Therapeutic Index to the hERG Ion Channel.
Haile PA, Casillas LN, Bury MJ, Mehlmann JF, Singhaus R Jr, Charnley AK, Hughes TV, DeMartino MP, Wang GZ, Romano JJ, Dong X, Plotnikov NV, Lakdawala AS, Duraiswami C, Convery MA, Votta BJ, Lipshutz DB, Desai BM, Swift B, Capriotti CA, Berger SB, Mahajan MK, Reilly MA, Rivera EJ, Sun HH, Nagilla R, LePage C, Ouellette MT, Totoritis RD, Donovan BT, Brown BS, Chaudhary KW, Gough PJ, Bertin J, Marquis RW. Haile PA, et al. Among authors: singhaus r jr. ACS Med Chem Lett. 2020 Jun 2;11(6):1353. doi: 10.1021/acsmedchemlett.0c00260. eCollection 2020 Jun 11. ACS Med Chem Lett. 2020. PMID: 32551024 Free PMC article.
Biarylether amide quinolines as liver X receptor agonists.
Bernotas RC, Singhaus RR, Kaufman DH, Ullrich J, Fletcher H 3rd, Quinet E, Nambi P, Unwalla R, Wilhelmsson A, Goos-Nilsson A, Farnegardh M, Wrobel J. Bernotas RC, et al. Among authors: singhaus rr. Bioorg Med Chem. 2009 Feb 15;17(4):1663-70. doi: 10.1016/j.bmc.2008.12.048. Epub 2008 Dec 27. Bioorg Med Chem. 2009. PMID: 19162487
4-(3-aryloxyaryl)quinoline alcohols are liver X receptor agonists.
Bernotas RC, Kaufman DH, Singhaus RR, Ullrich J, Unwalla R, Quinet E, Nambi P, Wilhelmsson A, Goos-Nilsson A, Wrobel J. Bernotas RC, et al. Among authors: singhaus rr. Bioorg Med Chem. 2009 Dec 1;17(23):8086-92. doi: 10.1016/j.bmc.2009.10.001. Epub 2009 Oct 4. Bioorg Med Chem. 2009. PMID: 19853462
4-(3-Aryloxyaryl)quinoline sulfones are potent liver X receptor agonists.
Bernotas RC, Singhaus RR, Kaufman DH, Travins JM, Ullrich JW, Unwalla R, Quinet E, Evans M, Nambi P, Olland A, Kauppi B, Wilhelmsson A, Goos-Nilsson A, Wrobel J. Bernotas RC, et al. Among authors: singhaus rr. Bioorg Med Chem Lett. 2010 Jan 1;20(1):209-12. doi: 10.1016/j.bmcl.2009.10.132. Epub 2009 Oct 31. Bioorg Med Chem Lett. 2010. PMID: 19932617
14 results