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Page 1
Structural and thermodynamic characterization of the TYK2 and JAK3 kinase domains in complex with CP-690550 and CMP-6.
Chrencik JE, Patny A, Leung IK, Korniski B, Emmons TL, Hall T, Weinberg RA, Gormley JA, Williams JM, Day JE, Hirsch JL, Kiefer JR, Leone JW, Fischer HD, Sommers CD, Huang HC, Jacobsen EJ, Tenbrink RE, Tomasselli AG, Benson TE. Chrencik JE, et al. Among authors: hirsch jl. J Mol Biol. 2010 Jul 16;400(3):413-33. doi: 10.1016/j.jmb.2010.05.020. Epub 2010 May 15. J Mol Biol. 2010. PMID: 20478313
Expression, purification, characterization and crystallization of non- and phosphorylated states of JAK2 and JAK3 kinase domain.
Hall T, Emmons TL, Chrencik JE, Gormley JA, Weinberg RA, Leone JW, Hirsch JL, Saabye MJ, Schindler JF, Day JE, Williams JM, Kiefer JR, Lightle SA, Harris MS, Guru S, Fischer HD, Tomasselli AG. Hall T, et al. Among authors: hirsch jl. Protein Expr Purif. 2010 Jan;69(1):54-63. doi: 10.1016/j.pep.2009.09.011. Epub 2009 Sep 23. Protein Expr Purif. 2010. PMID: 19781647
Expression, purification, and characterization of TYK-2 kinase domain, a member of the Janus kinase family.
Korniski B, Wittwer AJ, Emmons TL, Hall T, Brown S, Wrightstone AD, Hirsch JL, Gormley JA, Weinberg RA, Leone JW, Day JE, Chrencik JE, Sommers CD, Fischer HD, Tomasselli AG. Korniski B, et al. Among authors: hirsch jl. Biochem Biophys Res Commun. 2010 May 28;396(2):543-8. doi: 10.1016/j.bbrc.2010.04.141. Epub 2010 May 8. Biochem Biophys Res Commun. 2010. PMID: 20435017
Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase.
Selness SR, Devraj RV, Devadas B, Walker JK, Boehm TL, Durley RC, Shieh H, Xing L, Rucker PV, Jerome KD, Benson AG, Marrufo LD, Madsen HM, Hitchcock J, Owen TJ, Christie L, Promo MA, Hickory BS, Alvira E, Naing W, Blevis-Bal R, Messing D, Yang J, Mao MK, Yalamanchili G, Vonder Embse R, Hirsch J, Saabye M, Bonar S, Webb E, Anderson G, Monahan JB. Selness SR, et al. Bioorg Med Chem Lett. 2011 Jul 1;21(13):4066-71. doi: 10.1016/j.bmcl.2011.04.121. Epub 2011 May 11. Bioorg Med Chem Lett. 2011. PMID: 21641211
Design, synthesis and activity of a potent, selective series of N-aryl pyridinone inhibitors of p38 kinase.
Selness SR, Boehm TL, Walker JK, Devadas B, Durley RC, Kurumbail R, Shieh H, Xing L, Hepperle M, Rucker PV, Jerome KD, Benson AG, Marrufo LD, Madsen HM, Hitchcock J, Owen TJ, Christie L, Promo MA, Hickory BS, Alvira E, Naing W, Blevis-Bal R, Devraj RV, Messing D, Schindler JF, Hirsch J, Saabye M, Bonar S, Webb E, Anderson G, Monahan JB. Selness SR, et al. Bioorg Med Chem Lett. 2011 Jul 1;21(13):4059-65. doi: 10.1016/j.bmcl.2011.04.120. Epub 2011 May 13. Bioorg Med Chem Lett. 2011. PMID: 21640588
SD0006: a potent, selective and orally available inhibitor of p38 kinase.
Burnette BL, Selness S, Devraj R, Jungbluth G, Kurumbail R, Stillwell L, Anderson G, Mnich S, Hirsch J, Compton R, De Ciechi P, Hope H, Hepperle M, Keith RH, Naing W, Shieh H, Portanova J, Zhang Y, Zhang J, Leimgruber RM, Monahan J. Burnette BL, et al. Pharmacology. 2009;84(1):42-60. doi: 10.1159/000227286. Epub 2009 Jul 4. Pharmacology. 2009. PMID: 19590255 Free PMC article. Clinical Trial.
A benzothiophene inhibitor of mitogen-activated protein kinase-activated protein kinase 2 inhibits tumor necrosis factor alpha production and has oral anti-inflammatory efficacy in acute and chronic models of inflammation.
Mourey RJ, Burnette BL, Brustkern SJ, Daniels JS, Hirsch JL, Hood WF, Meyers MJ, Mnich SJ, Pierce BS, Saabye MJ, Schindler JF, South SA, Webb EG, Zhang J, Anderson DR. Mourey RJ, et al. Among authors: hirsch jl. J Pharmacol Exp Ther. 2010 Jun;333(3):797-807. doi: 10.1124/jpet.110.166173. Epub 2010 Mar 17. J Pharmacol Exp Ther. 2010. PMID: 20237073
54 results