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Page 1
Inhibiting complex IL-17A and IL-17RA interactions with a linear peptide.
Liu S, Desharnais J, Sahasrabudhe PV, Jin P, Li W, Oates BD, Shanker S, Banker ME, Chrunyk BA, Song X, Feng X, Griffor M, Jimenez J, Chen G, Tumelty D, Bhat A, Bradshaw CW, Woodnutt G, Lappe RW, Thorarensen A, Qiu X, Withka JM, Wood LD. Liu S, et al. Among authors: thorarensen a. Sci Rep. 2016 May 17;6:26071. doi: 10.1038/srep26071. Sci Rep. 2016. PMID: 27184415 Free PMC article.
Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists.
Liu S, Dakin LA, Xing L, Withka JM, Sahasrabudhe PV, Li W, Banker ME, Balbo P, Shanker S, Chrunyk BA, Guo Z, Chen JM, Young JA, Bai G, Starr JT, Wright SW, Bussenius J, Tan S, Gopalsamy A, Lefker BA, Vincent F, Jones LH, Xu H, Hoth LR, Geoghegan KF, Qiu X, Bunnage ME, Thorarensen A. Liu S, et al. Among authors: thorarensen a. Sci Rep. 2016 Aug 16;6:30859. doi: 10.1038/srep30859. Sci Rep. 2016. PMID: 27527709 Free PMC article.
Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition.
Telliez JB, Dowty ME, Wang L, Jussif J, Lin T, Li L, Moy E, Balbo P, Li W, Zhao Y, Crouse K, Dickinson C, Symanowicz P, Hegen M, Banker ME, Vincent F, Unwalla R, Liang S, Gilbert AM, Brown MF, Hayward M, Montgomery J, Yang X, Bauman J, Trujillo JI, Casimiro-Garcia A, Vajdos FF, Leung L, Geoghegan KF, Quazi A, Xuan D, Jones L, Hett E, Wright K, Clark JD, Thorarensen A. Telliez JB, et al. Among authors: thorarensen a. ACS Chem Biol. 2016 Dec 16;11(12):3442-3451. doi: 10.1021/acschembio.6b00677. Epub 2016 Nov 10. ACS Chem Biol. 2016. PMID: 27791347
The advantages of describing covalent inhibitor in vitro potencies by IC50 at a fixed time point. IC50 determination of covalent inhibitors provides meaningful data to medicinal chemistry for SAR optimization.
Thorarensen A, Balbo P, Banker ME, Czerwinski RM, Kuhn M, Maurer TS, Telliez JB, Vincent F, Wittwer AJ. Thorarensen A, et al. Bioorg Med Chem. 2021 Jan 1;29:115865. doi: 10.1016/j.bmc.2020.115865. Epub 2020 Nov 18. Bioorg Med Chem. 2021. PMID: 33285410
Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors.
Casimiro-Garcia A, Trujillo JI, Vajdos F, Juba B, Banker ME, Aulabaugh A, Balbo P, Bauman J, Chrencik J, Coe JW, Czerwinski R, Dowty M, Knafels JD, Kwon S, Leung L, Liang S, Robinson RP, Telliez JB, Unwalla R, Yang X, Thorarensen A. Casimiro-Garcia A, et al. Among authors: thorarensen a. J Med Chem. 2018 Dec 13;61(23):10665-10699. doi: 10.1021/acs.jmedchem.8b01308. Epub 2018 Nov 30. J Med Chem. 2018. PMID: 30423248
Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans.
Thorarensen A, Dowty ME, Banker ME, Juba B, Jussif J, Lin T, Vincent F, Czerwinski RM, Casimiro-Garcia A, Unwalla R, Trujillo JI, Liang S, Balbo P, Che Y, Gilbert AM, Brown MF, Hayward M, Montgomery J, Leung L, Yang X, Soucy S, Hegen M, Coe J, Langille J, Vajdos F, Chrencik J, Telliez JB. Thorarensen A, et al. J Med Chem. 2017 Mar 9;60(5):1971-1993. doi: 10.1021/acs.jmedchem.6b01694. Epub 2017 Feb 16. J Med Chem. 2017. PMID: 28139931
Identification of type-II inhibitors using kinase structures.
Lovering F, McDonald J, Whitlock GA, Glossop PA, Phillips C, Bent A, Sabnis Y, Ryan M, Fitz L, Lee J, Chang JS, Han S, Kurumbail R, Thorarensen A. Lovering F, et al. Among authors: thorarensen a. Chem Biol Drug Des. 2012 Nov;80(5):657-64. doi: 10.1111/j.1747-0285.2012.01443.x. Epub 2012 Sep 3. Chem Biol Drug Des. 2012. PMID: 22759374
Investigation of the binding pocket of human hematopoietic prostaglandin (PG) D2 synthase (hH-PGDS): a tale of two waters.
Trujillo JI, Kiefer JR, Huang W, Day JE, Moon J, Jerome GM, Bono CP, Kornmeier CM, Williams ML, Kuhn C, Rennie GR, Wynn TA, Carron CP, Thorarensen A. Trujillo JI, et al. Among authors: thorarensen a. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3795-9. doi: 10.1016/j.bmcl.2012.04.004. Epub 2012 Apr 13. Bioorg Med Chem Lett. 2012. PMID: 22546671
43 results