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18 results

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Page 1
Structural basis of TRPC4 regulation by calmodulin and pharmacological agents.
Vinayagam D, Quentin D, Yu-Strzelczyk J, Sitsel O, Merino F, Stabrin M, Hofnagel O, Yu M, Ledeboer MW, Nagel G, Malojcic G, Raunser S. Vinayagam D, et al. Among authors: ledeboer mw. Elife. 2020 Nov 25;9:e60603. doi: 10.7554/eLife.60603. Elife. 2020. PMID: 33236980 Free PMC article.
Discovery of a Potent and Selective TRPC5 Inhibitor, Efficacious in a Focal Segmental Glomerulosclerosis Model.
Yu M, Ledeboer MW, Daniels M, Malojcic G, Tibbitts TT, Coeffet-Le Gal M, Pan-Zhou XR, Westerling-Bui A, Beconi M, Reilly JF, Mundel P, Harmange JC. Yu M, et al. Among authors: ledeboer mw. ACS Med Chem Lett. 2019 Oct 22;10(11):1579-1585. doi: 10.1021/acsmedchemlett.9b00430. eCollection 2019 Nov 14. ACS Med Chem Lett. 2019. PMID: 31749913 Free PMC article.
Discovery and Optimization of Highly Selective Inhibitors of CDK5.
Daniels MH, Malojcic G, Clugston SL, Williams B, Coeffet-Le Gal M, Pan-Zhou XR, Venkatachalan S, Harmange JC, Ledeboer M. Daniels MH, et al. J Med Chem. 2022 Feb 24;65(4):3575-3596. doi: 10.1021/acs.jmedchem.1c02069. Epub 2022 Feb 10. J Med Chem. 2022. PMID: 35143203
Transplanted organoids empower human preclinical assessment of drug candidate for the clinic.
Westerling-Bui AD, Fast EM, Soare TW, Venkatachalan S, DeRan M, Fanelli AB, Kyrychenko S, Hoang H, Corriea GM, Zhang W, Yu M, Daniels M, Malojcic G, Pan-Zhou XR, Ledeboer MW, Harmange JC, Emani M, Tibbitts TT, Reilly JF, Mundel P. Westerling-Bui AD, et al. Among authors: ledeboer mw. Sci Adv. 2022 Jul 8;8(27):eabj5633. doi: 10.1126/sciadv.abj5633. Epub 2022 Jul 6. Sci Adv. 2022. PMID: 35857479 Free PMC article.
Discovery of VX-509 (Decernotinib): A Potent and Selective Janus Kinase 3 Inhibitor for the Treatment of Autoimmune Diseases.
Farmer LJ, Ledeboer MW, Hoock T, Arnost MJ, Bethiel RS, Bennani YL, Black JJ, Brummel CL, Chakilam A, Dorsch WA, Fan B, Cochran JE, Halas S, Harrington EM, Hogan JK, Howe D, Huang H, Jacobs DH, Laitinen LM, Liao S, Mahajan S, Marone V, Martinez-Botella G, McCarthy P, Messersmith D, Namchuk M, Oh L, Penney MS, Pierce AC, Raybuck SA, Rugg A, Salituro FG, Saxena K, Shannon D, Shlyakter D, Swenson L, Tian SK, Town C, Wang J, Wang T, Wannamaker MW, Winquist RJ, Zuccola HJ. Farmer LJ, et al. Among authors: ledeboer mw. J Med Chem. 2015 Sep 24;58(18):7195-216. doi: 10.1021/acs.jmedchem.5b00301. Epub 2015 Sep 10. J Med Chem. 2015. PMID: 26230873
Discovery of Novel, Orally Bioavailable β-Amino Acid Azaindole Inhibitors of Influenza PB2.
Farmer LJ, Clark MP, Boyd MJ, Perola E, Jones SM, Tsai A, Jacobs MD, Bandarage UK, Ledeboer MW, Wang T, Deng H, Ledford B, Gu W, Duffy JP, Bethiel RS, Shannon D, Byrn RA, Leeman JR, Rijnbrand R, Bennett HB, O'Brien C, Memmott C, Nti-Addae K, Bennani YL, Charifson PS. Farmer LJ, et al. Among authors: ledeboer mw. ACS Med Chem Lett. 2017 Jan 20;8(2):256-260. doi: 10.1021/acsmedchemlett.6b00486. eCollection 2017 Feb 9. ACS Med Chem Lett. 2017. PMID: 28197322 Free PMC article.
Discovery of a novel, first-in-class, orally bioavailable azaindole inhibitor (VX-787) of influenza PB2.
Clark MP, Ledeboer MW, Davies I, Byrn RA, Jones SM, Perola E, Tsai A, Jacobs M, Nti-Addae K, Bandarage UK, Boyd MJ, Bethiel RS, Court JJ, Deng H, Duffy JP, Dorsch WA, Farmer LJ, Gao H, Gu W, Jackson K, Jacobs DH, Kennedy JM, Ledford B, Liang J, Maltais F, Murcko M, Wang T, Wannamaker MW, Bennett HB, Leeman JR, McNeil C, Taylor WP, Memmott C, Jiang M, Rijnbrand R, Bral C, Germann U, Nezami A, Zhang Y, Salituro FG, Bennani YL, Charifson PS. Clark MP, et al. Among authors: ledeboer mw. J Med Chem. 2014 Aug 14;57(15):6668-78. doi: 10.1021/jm5007275. Epub 2014 Jul 24. J Med Chem. 2014. PMID: 25019388
2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2.
Ledeboer MW, Pierce AC, Duffy JP, Gao H, Messersmith D, Salituro FG, Nanthakumar S, Come J, Zuccola HJ, Swenson L, Shlyakter D, Mahajan S, Hoock T, Fan B, Tsai WJ, Kolaczkowski E, Carrier S, Hogan JK, Zessis R, Pazhanisamy S, Bennani YL. Ledeboer MW, et al. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6529-33. doi: 10.1016/j.bmcl.2009.10.053. Epub 2009 Oct 24. Bioorg Med Chem Lett. 2009. PMID: 19857967
Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase γ.
Collier PN, Messersmith D, Le Tiran A, Bandarage UK, Boucher C, Come J, Cottrell KM, Damagnez V, Doran JD, Griffith JP, Khare-Pandit S, Krueger EB, Ledeboer MW, Ledford B, Liao Y, Mahajan S, Moody CS, Roday S, Wang T, Xu J, Aronov AM. Collier PN, et al. Among authors: ledeboer mw. J Med Chem. 2015 Jul 23;58(14):5684-8. doi: 10.1021/acs.jmedchem.5b00498. Epub 2015 Jul 6. J Med Chem. 2015. PMID: 26121481
Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole.
Wang T, Duffy JP, Wang J, Halas S, Salituro FG, Pierce AC, Zuccola HJ, Black JR, Hogan JK, Jepson S, Shlyakter D, Mahajan S, Gu Y, Hoock T, Wood M, Furey BF, Frantz JD, Dauffenbach LM, Germann UA, Fan B, Namchuk M, Bennani YL, Ledeboer MW. Wang T, et al. Among authors: ledeboer mw. J Med Chem. 2009 Dec 24;52(24):7938-41. doi: 10.1021/jm901383u. J Med Chem. 2009. PMID: 20014869
18 results