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Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα.
Hanan EJ, Braun MG, Heald RA, MacLeod C, Chan C, Clausen S, Edgar KA, Eigenbrot C, Elliott R, Endres N, Friedman LS, Gogol E, Gu XH, Thibodeau RH, Jackson PS, Kiefer JR, Knight JD, Nannini M, Narukulla R, Pace A, Pang J, Purkey HE, Salphati L, Sampath D, Schmidt S, Sideris S, Song K, Sujatha-Bhaskar S, Ultsch M, Wallweber H, Xin J, Yeap S, Young A, Zhong Y, Staben ST. Hanan EJ, et al. Among authors: macleod c. J Med Chem. 2022 Dec 22;65(24):16589-16621. doi: 10.1021/acs.jmedchem.2c01422. Epub 2022 Dec 1. J Med Chem. 2022. PMID: 36455032
Mitigation of Acetylcholine Esterase Activity in the 1,7-Diazacarbazole Series of Inhibitors of Checkpoint Kinase 1.
Gazzard L, Williams K, Chen H, Axford L, Blackwood E, Burton B, Chapman K, Crackett P, Drobnick J, Ellwood C, Epler J, Flagella M, Gancia E, Gill M, Goodacre S, Halladay J, Hewitt J, Hunt H, Kintz S, Lyssikatos J, Macleod C, Major S, Médard G, Narukulla R, Ramiscal J, Schmidt S, Seward E, Wiesmann C, Wu P, Yee S, Yen I, Malek S. Gazzard L, et al. Among authors: macleod c. J Med Chem. 2015 Jun 25;58(12):5053-74. doi: 10.1021/acs.jmedchem.5b00464. Epub 2015 Jun 4. J Med Chem. 2015. PMID: 25988399
Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model.
Liang J, Van Abbema A, Balazs M, Barrett K, Berezhkovsky L, Blair WS, Chang C, Delarosa D, DeVoss J, Driscoll J, Eigenbrot C, Goodacre S, Ghilardi N, MacLeod C, Johnson A, Bir Kohli P, Lai Y, Lin Z, Mantik P, Menghrajani K, Nguyen H, Peng I, Sambrone A, Shia S, Smith J, Sohn S, Tsui V, Ultsch M, Williams K, Wu LC, Yang W, Zhang B, Magnuson S. Liang J, et al. Among authors: macleod c. Bioorg Med Chem Lett. 2017 Sep 15;27(18):4370-4376. doi: 10.1016/j.bmcl.2017.08.022. Epub 2017 Aug 12. Bioorg Med Chem Lett. 2017. PMID: 28830649
Structure-guided design of a selective inhibitor of the methyltransferase KMT9 with cellular activity.
Wang S, Klein SO, Urban S, Staudt M, Barthes NPF, Willmann D, Bacher J, Sum M, Bauer H, Peng L, Rennar GA, Gratzke C, Schüle KM, Zhang L, Einsle O, Greschik H, MacLeod C, Thomson CG, Jung M, Metzger E, Schüle R. Wang S, et al. Among authors: macleod c. Nat Commun. 2024 Jan 2;15(1):43. doi: 10.1038/s41467-023-44243-6. Nat Commun. 2024. PMID: 38167811 Free PMC article.
A restricted role for TYK2 catalytic activity in human cytokine responses revealed by novel TYK2-selective inhibitors.
Sohn SJ, Barrett K, Van Abbema A, Chang C, Kohli PB, Kanda H, Smith J, Lai Y, Zhou A, Zhang B, Yang W, Williams K, Macleod C, Hurley CA, Kulagowski JJ, Lewin-Koh N, Dengler HS, Johnson AR, Ghilardi N, Zak M, Liang J, Blair WS, Magnuson S, Wu LC. Sohn SJ, et al. Among authors: macleod c. J Immunol. 2013 Sep 1;191(5):2205-16. doi: 10.4049/jimmunol.1202859. Epub 2013 Jul 26. J Immunol. 2013. PMID: 23894201 Free PMC article.
841 results