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Page 1
Design, Synthesis, and Preclinical Characterization of Selective Factor D Inhibitors Targeting the Alternative Complement Pathway.
Karki RG, Powers J, Mainolfi N, Anderson K, Belanger DB, Liu D, Ji N, Jendza K, Gelin CF, Mac Sweeney A, Solovay C, Delgado O, Crowley M, Liao SM, Argikar UA, Flohr S, La Bonte LR, Lorthiois EL, Vulpetti A, Brown A, Long D, Prentiss M, Gradoux N, de Erkenez A, Cumin F, Adams C, Jaffee B, Mogi M. Karki RG, et al. Among authors: gelin cf. J Med Chem. 2019 May 9;62(9):4656-4668. doi: 10.1021/acs.jmedchem.9b00271. Epub 2019 Apr 30. J Med Chem. 2019. PMID: 30995036
A Dipolar Cycloaddition Reaction To Access 6-Methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate.
Chrovian CC, Soyode-Johnson A, Peterson AA, Gelin CF, Deng X, Dvorak CA, Carruthers NI, Lord B, Fraser I, Aluisio L, Coe KJ, Scott B, Koudriakova T, Schoetens F, Sepassi K, Gallacher DJ, Bhattacharya A, Letavic MA. Chrovian CC, et al. Among authors: gelin cf. J Med Chem. 2018 Jan 11;61(1):207-223. doi: 10.1021/acs.jmedchem.7b01279. Epub 2017 Dec 20. J Med Chem. 2018. PMID: 29211470
4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate.
Letavic MA, Savall BM, Allison BD, Aluisio L, Andres JI, De Angelis M, Ao H, Beauchamp DA, Bonaventure P, Bryant S, Carruthers NI, Ceusters M, Coe KJ, Dvorak CA, Fraser IC, Gelin CF, Koudriakova T, Liang J, Lord B, Lovenberg TW, Otieno MA, Schoetens F, Swanson DM, Wang Q, Wickenden AD, Bhattacharya A. Letavic MA, et al. Among authors: gelin cf. J Med Chem. 2017 Jun 8;60(11):4559-4572. doi: 10.1021/acs.jmedchem.7b00408. Epub 2017 May 25. J Med Chem. 2017. PMID: 28493698
Development of small molecule inhibitors of natural killer group 2D receptor (NKG2D).
Wang J, Nakafuku KM, Ziff J, Gelin CF, Gholami H, Thompson AA, Karpowich NK, Limon L, Coate HR, Damm-Ganamet KL, Shih AY, Grant JC, Côte M, Mak PA, Pascual HA, Rives ML, Edwards JP, Venable JD, Venkatesan H, Shi Z, Allen SJ, Sharma S, Kung PP, Shireman BT. Wang J, et al. Among authors: gelin cf. Bioorg Med Chem Lett. 2023 Nov 15;96:129492. doi: 10.1016/j.bmcl.2023.129492. Epub 2023 Sep 29. Bioorg Med Chem Lett. 2023. PMID: 37778428
Discovery of a Series of Substituted 1H-((1,2,3-Triazol-4-yl)methoxy)pyrimidines as Brain Penetrants and Potent GluN2B-Selective Negative Allosteric Modulators.
Gelin CF, Stenne B, Coate H, Hiscox A, Soyode-Johnson A, Wall JL, Lord B, Schoellerman J, Coe KJ, Wang K, Alcázar J, Chrovian CC, Dvorak CA, Carruthers NI, Koudriakova T, Balana B, Letavic MA. Gelin CF, et al. J Med Chem. 2023 Feb 23;66(4):2877-2892. doi: 10.1021/acs.jmedchem.2c01916. Epub 2023 Feb 9. J Med Chem. 2023. PMID: 36757100
Identification of small-molecule protein-protein interaction inhibitors for NKG2D.
Thompson AA, Harbut MB, Kung PP, Karpowich NK, Branson JD, Grant JC, Hagan D, Pascual HA, Bai G, Zavareh RB, Coate HR, Collins BC, Côte M, Gelin CF, Damm-Ganamet KL, Gholami H, Huff AR, Limon L, Lumb KJ, Mak PA, Nakafuku KM, Price EV, Shih AY, Tootoonchi M, Vellore NA, Wang J, Wei N, Ziff J, Berger SB, Edwards JP, Gardet A, Sun S, Towne JE, Venable JD, Shi Z, Venkatesan H, Rives ML, Sharma S, Shireman BT, Allen SJ. Thompson AA, et al. Among authors: gelin cf. Proc Natl Acad Sci U S A. 2023 May 2;120(18):e2216342120. doi: 10.1073/pnas.2216342120. Epub 2023 Apr 25. Proc Natl Acad Sci U S A. 2023. PMID: 37098070 Free PMC article.
Identification of a novel small molecule HIF-1alpha translation inhibitor.
Narita T, Yin S, Gelin CF, Moreno CS, Yepes M, Nicolaou KC, Van Meir EG. Narita T, et al. Among authors: gelin cf. Clin Cancer Res. 2009 Oct 1;15(19):6128-36. doi: 10.1158/1078-0432.CCR-08-3180. Epub 2009 Sep 29. Clin Cancer Res. 2009. PMID: 19789328 Free PMC article.
11 results