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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: zhong y. 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
Preclinical and translational pharmacology of afucosylated anti-CCR8 antibody for depletion of tumour-infiltrating regulatory T cells.
Gampa G, Spinosa P, Getz J, Zhong Y, Halpern W, Esen E, Davies J, Chou C, Kwong M, Wang Y, Arenzana TL, Shivva V, Huseni M, Hsieh R, Schartner J, Koerber JT, Rutz S, Hosseini I. Gampa G, et al. Among authors: zhong y. Br J Pharmacol. 2024 Jul;181(13):2033-2052. doi: 10.1111/bph.16326. Epub 2024 Mar 14. Br J Pharmacol. 2024. PMID: 38486310
GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer.
Liang J, Zbieg JR, Blake RA, Chang JH, Daly S, DiPasquale AG, Friedman LS, Gelzleichter T, Gill M, Giltnane JM, Goodacre S, Guan J, Hartman SJ, Ingalla ER, Kategaya L, Kiefer JR, Kleinheinz T, Labadie SS, Lai T, Li J, Liao J, Liu Z, Mody V, McLean N, Metcalfe C, Nannini MA, Oeh J, O'Rourke MG, Ortwine DF, Ran Y, Ray NC, Roussel F, Sambrone A, Sampath D, Schutt LK, Vinogradova M, Wai J, Wang T, Wertz IE, White JR, Yeap SK, Young A, Zhang B, Zheng X, Zhou W, Zhong Y, Wang X. Liang J, et al. Among authors: zhong y. J Med Chem. 2021 Aug 26;64(16):11841-11856. doi: 10.1021/acs.jmedchem.1c00847. Epub 2021 Jul 12. J Med Chem. 2021. PMID: 34251202
Unexpected equivalent potency of a constrained chromene enantiomeric pair rationalized by co-crystal structures in complex with estrogen receptor alpha.
Zhang B, Kiefer JR, Blake RA, Chang JH, Hartman S, Ingalla ER, Kleinheinz T, Mody V, Nannini M, Ortwine DF, Ran Y, Sambrone A, Sampath D, Vinogradova M, Zhong Y, Nwachukwu JC, Nettles KW, Lai T, Liao J, Zheng X, Chen H, Wang X, Liang J. Zhang B, et al. Among authors: zhong y. Bioorg Med Chem Lett. 2019 Apr 1;29(7):905-911. doi: 10.1016/j.bmcl.2019.01.036. Epub 2019 Feb 1. Bioorg Med Chem Lett. 2019. PMID: 30732944
First-in-human phase 1 trial evaluating safety, pharmacokinetics, and pharmacodynamics of NLRP3 inflammasome inhibitor, GDC-2394, in healthy volunteers.
Tang F, Kunder R, Chu T, Hains A, Nguyen A, McBride JM, Zhong Y, Santagostino S, Wilson M, Trenchak A, Chen L, Ly J, Moein A, Lewin-Koh N, Raghavan V, Osaghae U, Wynne C, Owen R, Place D. Tang F, et al. Among authors: zhong y. Clin Transl Sci. 2023 Sep;16(9):1653-1666. doi: 10.1111/cts.13576. Epub 2023 Jul 23. Clin Transl Sci. 2023. PMID: 37350225 Free PMC article. Clinical Trial.
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