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Page 1
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: casimiro garcia 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
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. Among authors: casimiro garcia a. 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 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. 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
Identification of Morpholino-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-ones as Nonsteroidal Mineralocorticoid Antagonists.
Piotrowski DW, Futatsugi K, Casimiro-Garcia A, Wei L, Sammons MF, Herr M, Jiao W, Lavergne SY, Coffey SB, Wright SW, Song K, Loria PM, Banker ME, Petersen DN, Bauman J. Piotrowski DW, et al. Among authors: casimiro garcia a. J Med Chem. 2018 Feb 8;61(3):1086-1097. doi: 10.1021/acs.jmedchem.7b01515. Epub 2018 Jan 23. J Med Chem. 2018. PMID: 29300474
Identification of (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-methoxynicotinic acid, a highly potent and selective nonsteroidal mineralocorticoid receptor antagonist.
Casimiro-Garcia A, Piotrowski DW, Ambler C, Arhancet GB, Banker ME, Banks T, Boustany-Kari CM, Cai C, Chen X, Eudy R, Hepworth D, Hulford CA, Jennings SM, Loria PM, Meyers MJ, Petersen DN, Raheja NK, Sammons M, She L, Song K, Vrieze D, Wei L. Casimiro-Garcia A, et al. J Med Chem. 2014 May 22;57(10):4273-88. doi: 10.1021/jm500206r. Epub 2014 Apr 30. J Med Chem. 2014. PMID: 24738581
Discovery of a Series of Pyrimidine Carboxamides as Inhibitors of Vanin-1.
Casimiro-Garcia A, Allais C, Brennan A, Choi C, Dower G, Farley KA, Fleming M, Flick A, Frisbie RK, Hall J, Hepworth D, Jones H, Knafels JD, Kortum S, Lovering FE, Mathias JP, Mohan S, Morgan PM, Parng C, Parris K, Pullen N, Schlerman F, Stansfield J, Strohbach JW, Vajdos FF, Vincent F, Wang H, Wang X, Webster R, Wright SW. Casimiro-Garcia A, et al. J Med Chem. 2022 Jan 13;65(1):757-784. doi: 10.1021/acs.jmedchem.1c01849. Epub 2021 Dec 30. J Med Chem. 2022. PMID: 34967602
Selective, Small-Molecule Co-Factor Binding Site Inhibition of a Su(var)3-9, Enhancer of Zeste, Trithorax Domain Containing Lysine Methyltransferase.
Taylor AP, Swewczyk M, Kennedy S, Trush VV, Wu H, Zeng H, Dong A, Ferreira de Freitas R, Tatlock J, Kumpf RA, Wythes M, Casimiro-Garcia A, Denny RA, Parikh MD, Li F, Barsyte-Lovejoy D, Schapira M, Vedadi M, Brown PJ, Arrowsmith CH, Owen DR. Taylor AP, et al. Among authors: casimiro garcia a. J Med Chem. 2019 Sep 12;62(17):7669-7683. doi: 10.1021/acs.jmedchem.9b00112. Epub 2019 Sep 3. J Med Chem. 2019. PMID: 31415173
PF-07059013: A Noncovalent Modulator of Hemoglobin for Treatment of Sickle Cell Disease.
Gopalsamy A, Aulabaugh AE, Barakat A, Beaumont KC, Cabral S, Canterbury DP, Casimiro-Garcia A, Chang JS, Chen MZ, Choi C, Dow RL, Fadeyi OO, Feng X, France SP, Howard RM, Janz JM, Jasti J, Jasuja R, Jones LH, King-Ahmad A, Knee KM, Kohrt JT, Limberakis C, Liras S, Martinez CA, McClure KF, Narayanan A, Narula J, Novak JJ, O'Connell TN, Parikh MD, Piotrowski DW, Plotnikova O, Robinson RP, Sahasrabudhe PV, Sharma R, Thuma BA, Vasa D, Wei L, Wenzel AZ, Withka JM, Xiao J, Yayla HG. Gopalsamy A, et al. Among authors: casimiro garcia a. J Med Chem. 2021 Jan 14;64(1):326-342. doi: 10.1021/acs.jmedchem.0c01518. Epub 2020 Dec 24. J Med Chem. 2021. PMID: 33356244
25 results