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Page 1
Filling a nick in NIK: Extending the half-life of a NIK inhibitor through structure-based drug design.
Crawford JJ, Feng J, Brightbill HD, Johnson AR, Wright M, Kolesnikov A, Lee W, Castanedo GM, Do S, Blaquiere N, Staben ST, Chiang PC, Fan PW, Baumgardner M, Wong S, Godemann R, Grabbe A, Wiegel C, Sujatha-Bhaskar S, Hymowitz SG, Liau N, Hsu PL, McEwan PA, Ismaili MHA, Landry ML. Crawford JJ, et al. Among authors: ismaili mha. Bioorg Med Chem Lett. 2023 Jun 1;89:129277. doi: 10.1016/j.bmcl.2023.129277. Epub 2023 Apr 25. Bioorg Med Chem Lett. 2023. PMID: 37105490
Inhibition of the kinase ITK in a mouse model of asthma reduces cell death and fails to inhibit the inflammatory response.
Sun Y, Peng I, Webster JD, Suto E, Lesch J, Wu X, Senger K, Francis G, Barrett K, Collier JL, Burch JD, Zhou M, Chen Y, Chan C, Eastham-Anderson J, Ngu H, Li O, Staton T, Havnar C, Jaochico A, Jackman J, Jeet S, Riol-Blanco L, Wu LC, Choy DF, Arron JR, McKenzie BS, Ghilardi N, Ismaili MH, Pei Z, DeVoss J, Austin CD, Lee WP, Zarrin AA. Sun Y, et al. Sci Signal. 2015 Dec 1;8(405):ra122. doi: 10.1126/scisignal.aab0949. Sci Signal. 2015. PMID: 26628680
Oral enzyme therapy for maple syrup urine disease (MSUD) suppresses plasma leucine levels in intermediate MSUD mice and healthy nonhuman primates.
Skvorak K, Liu J, Kruse N, Mehmood R, Das S, Jenne S, Chng C, Lao UL, Duan D, Asfaha J, Du F, Teadt L, Sero A, Ching C, Riggins J, Pope L, Yan P, Mashiana H, Ismaili MHA, McCluskie K, Huisman G, Silverman AP. Skvorak K, et al. Among authors: ismaili mha. J Inherit Metab Dis. 2023 Nov;46(6):1089-1103. doi: 10.1002/jimd.12662. Epub 2023 Aug 9. J Inherit Metab Dis. 2023. PMID: 37494004
An orally administered enzyme therapeutic for homocystinuria that suppresses homocysteine by metabolizing methionine in the gastrointestinal tract.
Skvorak K, Mitchell V, Teadt L, Franklin KA, Lee HO, Kruse N, Huitt-Roehl C, Hang J, Du F, Galanie S, Guan S, Aijaz H, Zhang N, Rajkovic G, Kruger WD, Ismaili MHA, Huisman G, McCluskie K, Silverman AP. Skvorak K, et al. Among authors: ismaili mha. Mol Genet Metab. 2023 Aug;139(4):107653. doi: 10.1016/j.ymgme.2023.107653. Epub 2023 Jul 12. Mol Genet Metab. 2023. PMID: 37463544 Free article.
Optimizing human α-galactosidase for treatment of Fabry disease.
Hallows WC, Skvorak K, Agard N, Kruse N, Zhang X, Zhu Y, Botham RC, Chng C, Shukla C, Lao J, Miller M, Sero A, Viduya J, Ismaili MHA, McCluskie K, Schiffmann R, Silverman AP, Shen JS, Huisman GW. Hallows WC, et al. Among authors: ismaili mha. Sci Rep. 2023 Mar 23;13(1):4748. doi: 10.1038/s41598-023-31777-4. Sci Rep. 2023. PMID: 36959353 Free PMC article.
Tetrahydroindazoles as Interleukin-2 Inducible T-Cell Kinase Inhibitors. Part II. Second-Generation Analogues with Enhanced Potency, Selectivity, and Pharmacodynamic Modulation in Vivo.
Burch JD, Barrett K, Chen Y, DeVoss J, Eigenbrot C, Goldsmith R, Ismaili MH, Lau K, Lin Z, Ortwine DF, Zarrin AA, McEwan PA, Barker JJ, Ellebrandt C, Kordt D, Stein DB, Wang X, Chen Y, Hu B, Xu X, Yuen PW, Zhang Y, Pei Z. Burch JD, et al. J Med Chem. 2015 May 14;58(9):3806-16. doi: 10.1021/jm501998m. Epub 2015 Apr 16. J Med Chem. 2015. PMID: 25844760
Design, synthesis and structure-activity relationships of a novel class of sulfonylpyridine inhibitors of Interleukin-2 inducible T-cell kinase (ITK).
Trani G, Barker JJ, Bromidge SM, Brookfield FA, Burch JD, Chen Y, Eigenbrot C, Heifetz A, Ismaili MHA, Johnson A, Krülle TM, MacKinnon CH, Maghames R, McEwan PA, Montalbetti CAGN, Ortwine DF, Pérez-Fuertes Y, Vaidya DG, Wang X, Zarrin AA, Pei Z. Trani G, et al. Among authors: ismaili mha. Bioorg Med Chem Lett. 2014 Dec 15;24(24):5818-5823. doi: 10.1016/j.bmcl.2014.10.020. Epub 2014 Oct 12. Bioorg Med Chem Lett. 2014. PMID: 25455497
Property- and structure-guided discovery of a tetrahydroindazole series of interleukin-2 inducible T-cell kinase inhibitors.
Burch JD, Lau K, Barker JJ, Brookfield F, Chen Y, Chen Y, Eigenbrot C, Ellebrandt C, Ismaili MH, Johnson A, Kordt D, MacKinnon CH, McEwan PA, Ortwine DF, Stein DB, Wang X, Winkler D, Yuen PW, Zhang Y, Zarrin AA, Pei Z. Burch JD, et al. J Med Chem. 2014 Jul 10;57(13):5714-27. doi: 10.1021/jm500550e. Epub 2014 Jun 27. J Med Chem. 2014. PMID: 24918870