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An allosteric pan-TEAD inhibitor blocks oncogenic YAP/TAZ signaling and overcomes KRAS G12C inhibitor resistance.
Hagenbeek TJ, Zbieg JR, Hafner M, Mroue R, Lacap JA, Sodir NM, Noland CL, Afghani S, Kishore A, Bhat KP, Yao X, Schmidt S, Clausen S, Steffek M, Lee W, Beroza P, Martin S, Lin E, Fong R, Di Lello P, Kubala MH, Yang MN, Lau JT, Chan E, Arrazate A, An L, Levy E, Lorenzo MN, Lee HJ, Pham TH, Modrusan Z, Zang R, Chen YC, Kabza M, Ahmed M, Li J, Chang MT, Maddalo D, Evangelista M, Ye X, Crawford JJ, Dey A. Hagenbeek TJ, et al. Among authors: zbieg jr. Nat Cancer. 2023 Jun;4(6):812-828. doi: 10.1038/s43018-023-00577-0. Epub 2023 Jun 5. Nat Cancer. 2023. PMID: 37277530 Free PMC article.
Discovery of GNE-502 as an orally bioavailable and potent degrader for estrogen receptor positive breast cancer.
Zbieg JR, Liang J, Li J, Blake RA, Chang J, Friedman L, Goodacre S, Hartman SJ, Rei Ingalla E, Kiefer JR, Kleinheinz T, Labadie S, Lai T, Liao J, McLean N, Metcalfe C, Mody V, Nannini M, Ortwine DF, Ran Y, Ray N, Roussel F, Sambrone A, Sampath D, Vinogradova M, Wai J, Wang T, Yeap K, Zhang B, Zheng X, Zhong Y, Wang X. Zbieg JR, et al. Bioorg Med Chem Lett. 2021 Oct 15;50:128335. doi: 10.1016/j.bmcl.2021.128335. Epub 2021 Aug 20. Bioorg Med Chem Lett. 2021. PMID: 34425201
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: zbieg jr. 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
Small Molecule Dysregulation of TEAD Lipidation Induces a Dominant-Negative Inhibition of Hippo Pathway Signaling.
Holden JK, Crawford JJ, Noland CL, Schmidt S, Zbieg JR, Lacap JA, Zang R, Miller GM, Zhang Y, Beroza P, Reja R, Lee W, Tom JYK, Fong R, Steffek M, Clausen S, Hagenbeek TJ, Hu T, Zhou Z, Shen HC, Cunningham CN. Holden JK, et al. Among authors: zbieg jr. Cell Rep. 2020 Jun 23;31(12):107809. doi: 10.1016/j.celrep.2020.107809. Cell Rep. 2020. PMID: 32579935 Free article.
28 results