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Page 1
Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.
Lee KL, Ambler CM, Anderson DR, Boscoe BP, Bree AG, Brodfuehrer JI, Chang JS, Choi C, Chung S, Curran KJ, Day JE, Dehnhardt CM, Dower K, Drozda SE, Frisbie RK, Gavrin LK, Goldberg JA, Han S, Hegen M, Hepworth D, Hope HR, Kamtekar S, Kilty IC, Lee A, Lin LL, Lovering FE, Lowe MD, Mathias JP, Morgan HM, Murphy EA, Papaioannou N, Patny A, Pierce BS, Rao VR, Saiah E, Samardjiev IJ, Samas BM, Shen MWH, Shin JH, Soutter HH, Strohbach JW, Symanowicz PT, Thomason JR, Trzupek JD, Vargas R, Vincent F, Yan J, Zapf CW, Wright SW. Lee KL, et al. Among authors: gavrin lk. J Med Chem. 2017 Jul 13;60(13):5521-5542. doi: 10.1021/acs.jmedchem.7b00231. Epub 2017 Jun 14. J Med Chem. 2017. PMID: 28498658
Small molecules that target protein misfolding.
Gavrin LK, Denny RA, Saiah E. Gavrin LK, et al. J Med Chem. 2012 Dec 27;55(24):10823-43. doi: 10.1021/jm301182j. Epub 2012 Nov 1. J Med Chem. 2012. PMID: 23075044
Recent developments in targeting protein misfolding diseases.
Denny RA, Gavrin LK, Saiah E. Denny RA, et al. Among authors: gavrin lk. Bioorg Med Chem Lett. 2013 Apr 1;23(7):1935-44. doi: 10.1016/j.bmcl.2013.01.089. Epub 2013 Feb 4. Bioorg Med Chem Lett. 2013. PMID: 23454013 Free article. Review.
Discovery of WAY-260022, a Potent and Selective Inhibitor of the Norepinephrine Transporter.
Gavrin LK, Mahaney PE, Jenkins D, Nogle LM, Mugford CA, Huselton C, Leiter J, Johnston GH, Bray JA, Burroughs KD, Cosmi SA, Alfinito P, Ho DM, Deecher DC, Trybulski EJ. Gavrin LK, et al. ACS Med Chem Lett. 2010 Mar 25;1(3):91-5. doi: 10.1021/ml100009p. eCollection 2010 Jun 10. ACS Med Chem Lett. 2010. PMID: 24900182 Free PMC article.
Synthesis of pyrazolo[1,5-alpha]pyrimidinone regioisomers.
Gavrin LK, Lee A, Provencher BA, Massefski WW, Huhn SD, Ciszewski GM, Cole DC, McKew JC. Gavrin LK, et al. J Org Chem. 2007 Feb 2;72(3):1043-6. doi: 10.1021/jo062120g. J Org Chem. 2007. PMID: 17253833
Structure-activity relationships of the cycloalkanol ethylamine scaffold: discovery of selective norepinephrine reuptake inhibitors.
Mahaney PE, Gavrin LK, Trybulski EJ, Stack GP, Vu TA, Cohn ST, Ye F, Belardi JK, Santilli AA, Sabatucci JP, Leiter J, Johnston GH, Bray JA, Burroughs KD, Cosmi SA, Leventhal L, Koury EJ, Zhang Y, Mugford CA, Ho DM, Rosenzweig-Lipson SJ, Platt B, Smith VA, Deecher DC. Mahaney PE, et al. Among authors: gavrin lk. J Med Chem. 2008 Jul 10;51(13):4038-49. doi: 10.1021/jm8002262. Epub 2008 Jun 17. J Med Chem. 2008. PMID: 18557608