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Page 1
Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer.
Liang J, Blake R, Chang J, Friedman LS, Goodacre S, Hartman S, Ingalla ER, Kiefer JR, Kleinheinz T, Labadie S, Li J, Lai KW, Liao J, Mody V, McLean N, Metcalfe C, Nannini M, Otwine D, Ran Y, Ray N, Roussel F, Sambrone A, Sampath D, Vinogradova M, Wai J, Wang T, Yeap K, Young A, Zbieg J, Zhang B, Zheng X, Zhong Y, Wang X. Liang J, et al. Among authors: wang x, wang t. ACS Med Chem Lett. 2020 May 26;11(6):1342-1347. doi: 10.1021/acsmedchemlett.0c00224. eCollection 2020 Jun 11. ACS Med Chem Lett. 2020. PMID: 32551022 Free PMC article.
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: wang x, wang t. 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
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. Among authors: wang x, wang t. 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
Structure-Based Design of GNE-495, a Potent and Selective MAP4K4 Inhibitor with Efficacy in Retinal Angiogenesis.
Ndubaku CO, Crawford TD, Chen H, Boggs JW, Drobnick J, Harris SF, Jesudason R, McNamara E, Nonomiya J, Sambrone A, Schmidt S, Smyczek T, Vitorino P, Wang L, Wu P, Yeung S, Chen J, Chen K, Ding CZ, Wang T, Xu Z, Gould SE, Murray LJ, Ye W. Ndubaku CO, et al. Among authors: wang l, wang t. ACS Med Chem Lett. 2015 Jun 29;6(8):913-8. doi: 10.1021/acsmedchemlett.5b00174. eCollection 2015 Aug 13. ACS Med Chem Lett. 2015. PMID: 26288693 Free PMC article.
Linker Immolation Determines Cell Killing Activity of Disulfide-Linked Pyrrolobenzodiazepine Antibody-Drug Conjugates.
Zhang D, Pillow TH, Ma Y, Cruz-Chuh JD, Kozak KR, Sadowsky JD, Lewis Phillips GD, Guo J, Darwish M, Fan P, Chen J, He C, Wang T, Yao H, Xu Z, Chen J, Wai J, Pei Z, Hop CE, Khojasteh SC, Dragovich PS. Zhang D, et al. Among authors: wang t. ACS Med Chem Lett. 2016 Aug 26;7(11):988-993. doi: 10.1021/acsmedchemlett.6b00233. eCollection 2016 Nov 10. ACS Med Chem Lett. 2016. PMID: 27882196 Free PMC article.
Discovery of Peptidomimetic Antibody-Drug Conjugate Linkers with Enhanced Protease Specificity.
Wei B, Gunzner-Toste J, Yao H, Wang T, Wang J, Xu Z, Chen J, Wai J, Nonomiya J, Tsai SP, Chuh J, Kozak KR, Liu Y, Yu SF, Lau J, Li G, Phillips GD, Leipold D, Kamath A, Su D, Xu K, Eigenbrot C, Steinbacher S, Ohri R, Raab H, Staben LR, Zhao G, Flygare JA, Pillow TH, Verma V, Masterson LA, Howard PW, Safina B. Wei B, et al. Among authors: wang j, wang t. J Med Chem. 2018 Feb 8;61(3):989-1000. doi: 10.1021/acs.jmedchem.7b01430. Epub 2017 Dec 21. J Med Chem. 2018. PMID: 29227683
Antibody-Drug Conjugates Derived from Cytotoxic seco-CBI-Dimer Payloads Are Highly Efficacious in Xenograft Models and Form Protein Adducts In Vivo.
Su D, Chen J, Cosino E, Dela Cruz-Chuh J, Davis H, Del Rosario G, Figueroa I, Goon L, He J, Kamath AV, Kaur S, Kozak KR, Lau J, Lee D, Lee MV, Leipold D, Liu L, Liu P, Lu GL, Nelson C, Ng C, Pillow TH, Polakis P, Polson AG, Rowntree RK, Saad O, Safina B, Stagg NJ, Tercel M, Vandlen R, Vollmar BS, Wai J, Wang T, Wei B, Xu K, Xue J, Xu Z, Yan G, Yao H, Yu SF, Zhang D, Zhong F, Dragovich PS. Su D, et al. Among authors: wang t. Bioconjug Chem. 2019 May 15;30(5):1356-1370. doi: 10.1021/acs.bioconjchem.9b00133. Epub 2019 Apr 22. Bioconjug Chem. 2019. PMID: 30966735
Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists.
Shi J, Gu Z, Jurica EA, Wu X, Haque LE, Williams KN, Hernandez AS, Hong Z, Gao Q, Dabros M, Davulcu AH, Mathur A, Rampulla RA, Gupta AK, Jayaram R, Apedo A, Moore DB, Liu H, Kunselman LK, Brady EJ, Wilkes JJ, Zinker BA, Cai H, Shu YZ, Sun Q, Dierks EA, Foster KA, Xu C, Wang T, Panemangalore R, Cvijic ME, Xie C, Cao GG, Zhou M, Krupinski J, Whaley JM, Robl JA, Ewing WR, Ellsworth BA. Shi J, et al. Among authors: wang t. J Med Chem. 2018 Feb 8;61(3):681-694. doi: 10.1021/acs.jmedchem.7b00982. Epub 2018 Jan 27. J Med Chem. 2018. PMID: 29316397
Discovery of a Hydroxypyridinone APJ Receptor Agonist as a Clinical Candidate.
Johnson JA, Kim SH, Jiang J, Phillips M, Schumacher WA, Bostwick JS, Gargalovic PS, Onorato JM, Luk CE, Generaux C, He Y, Chen XQ, Xu C, Galella MA, Wang T, Gordon DA, Wexler RR, Finlay HJ. Johnson JA, et al. Among authors: wang t. J Med Chem. 2021 Mar 25;64(6):3086-3099. doi: 10.1021/acs.jmedchem.0c01878. Epub 2021 Mar 9. J Med Chem. 2021. PMID: 33689340
Improving Metabolic Stability with Deuterium: The Discovery of BMT-052, a Pan-genotypic HCV NS5B Polymerase Inhibitor.
Parcella K, Eastman K, Yeung KS, Grant-Young KA, Zhu J, Wang T, Zhang Z, Yin Z, Parker D, Mosure K, Fang H, Wang YK, Lemm J, Zhuo X, Hanumegowda U, Liu M, Rigat K, Donoso M, Tuttle M, Zvyaga T, Haarhoff Z, Meanwell NA, Soars MG, Roberts SB, Kadow JF. Parcella K, et al. Among authors: wang yk, wang t. ACS Med Chem Lett. 2017 Jun 29;8(7):771-774. doi: 10.1021/acsmedchemlett.7b00211. eCollection 2017 Jul 13. ACS Med Chem Lett. 2017. PMID: 28740615 Free PMC article.
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