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Page 1
Therapeutic Ligands Antagonize Estrogen Receptor Function by Impairing Its Mobility.
Guan J, Zhou W, Hafner M, Blake RA, Chalouni C, Chen IP, De Bruyn T, Giltnane JM, Hartman SJ, Heidersbach A, Houtman R, Ingalla E, Kategaya L, Kleinheinz T, Li J, Martin SE, Modrusan Z, Nannini M, Oeh J, Ubhayakar S, Wang X, Wertz IE, Young A, Yu M, Sampath D, Hager JH, Friedman LS, Daemen A, Metcalfe C. Guan J, et al. Among authors: kleinheinz t. Cell. 2019 Aug 8;178(4):949-963.e18. doi: 10.1016/j.cell.2019.06.026. Epub 2019 Jul 25. Cell. 2019. PMID: 31353221 Free article.
USP7 small-molecule inhibitors interfere with ubiquitin binding.
Kategaya L, Di Lello P, Rougé L, Pastor R, Clark KR, Drummond J, Kleinheinz T, Lin E, Upton JP, Prakash S, Heideker J, McCleland M, Ritorto MS, Alessi DR, Trost M, Bainbridge TW, Kwok MCM, Ma TP, Stiffler Z, Brasher B, Tang Y, Jaishankar P, Hearn BR, Renslo AR, Arkin MR, Cohen F, Yu K, Peale F, Gnad F, Chang MT, Klijn C, Blackwood E, Martin SE, Forrest WF, Ernst JA, Ndubaku C, Wang X, Beresini MH, Tsui V, Schwerdtfeger C, Blake RA, Murray J, Maurer T, Wertz IE. Kategaya L, et al. Among authors: kleinheinz t. Nature. 2017 Oct 26;550(7677):534-538. doi: 10.1038/nature24006. Epub 2017 Oct 18. Nature. 2017. PMID: 29045385
Discovery of Small-Molecule Inhibitors of Ubiquitin Specific Protease 7 (USP7) Using Integrated NMR and in Silico Techniques.
Di Lello P, Pastor R, Murray JM, Blake RA, Cohen F, Crawford TD, Drobnick J, Drummond J, Kategaya L, Kleinheinz T, Maurer T, Rougé L, Zhao X, Wertz I, Ndubaku C, Tsui V. Di Lello P, et al. Among authors: kleinheinz t. J Med Chem. 2017 Dec 28;60(24):10056-10070. doi: 10.1021/acs.jmedchem.7b01293. Epub 2017 Dec 8. J Med Chem. 2017. PMID: 29166018
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: kleinheinz t. 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
Discovery of a C-8 hydroxychromene as a potent degrader of estrogen receptor alpha with improved rat oral exposure over GDC-0927.
Labadie SS, Li J, Blake RA, Chang JH, Goodacre S, Hartman SJ, Liang W, Kiefer JR, Kleinheinz T, Lai T, Liao J, Ortwine DF, Mody V, Ray NC, Roussel F, Vinogradova M, Yeap SK, Zhang B, Zheng X, Zbieg JR, Liang J, Wang X. Labadie SS, et al. Among authors: kleinheinz t. Bioorg Med Chem Lett. 2019 Aug 15;29(16):2090-2093. doi: 10.1016/j.bmcl.2019.07.013. Epub 2019 Jul 6. Bioorg Med Chem Lett. 2019. PMID: 31311734
Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity.
Pillow TH, Adhikari P, Blake RA, Chen J, Del Rosario G, Deshmukh G, Figueroa I, Gascoigne KE, Kamath AV, Kaufman S, Kleinheinz T, Kozak KR, Latifi B, Leipold DD, Sing Li C, Li R, Mulvihill MM, O'Donohue A, Rowntree RK, Sadowsky JD, Wai J, Wang X, Wu C, Xu Z, Yao H, Yu SF, Zhang D, Zang R, Zhang H, Zhou H, Zhu X, Dragovich PS. Pillow TH, et al. Among authors: kleinheinz t. ChemMedChem. 2020 Jan 7;15(1):17-25. doi: 10.1002/cmdc.201900497. Epub 2019 Nov 14. ChemMedChem. 2020. PMID: 31674143
Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα).
Dragovich PS, Adhikari P, Blake RA, Blaquiere N, Chen J, Cheng YX, den Besten W, Han J, Hartman SJ, He J, He M, Rei Ingalla E, Kamath AV, Kleinheinz T, Lai T, Leipold DD, Li CS, Liu Q, Lu J, Lu Y, Meng F, Meng L, Ng C, Peng K, Lewis Phillips G, Pillow TH, Rowntree RK, Sadowsky JD, Sampath D, Staben L, Staben ST, Wai J, Wan K, Wang X, Wei B, Wertz IE, Xin J, Xu K, Yao H, Zang R, Zhang D, Zhou H, Zhao Y. Dragovich PS, et al. Among authors: kleinheinz t. Bioorg Med Chem Lett. 2020 Feb 15;30(4):126907. doi: 10.1016/j.bmcl.2019.126907. Epub 2019 Dec 18. Bioorg Med Chem Lett. 2020. PMID: 31902710
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: kleinheinz 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.
Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties.
Dragovich PS, Pillow TH, Blake RA, Sadowsky JD, Adaligil E, Adhikari P, Bhakta S, Blaquiere N, Chen J, Dela Cruz-Chuh J, Gascoigne KE, Hartman SJ, He M, Kaufman S, Kleinheinz T, Kozak KR, Liu L, Liu L, Liu Q, Lu Y, Meng F, Mulvihill MM, O'Donohue A, Rowntree RK, Staben LR, Staben ST, Wai J, Wang J, Wei B, Wilson C, Xin J, Xu Z, Yao H, Zhang D, Zhang H, Zhou H, Zhu X. Dragovich PS, et al. Among authors: kleinheinz t. J Med Chem. 2021 Mar 11;64(5):2534-2575. doi: 10.1021/acs.jmedchem.0c01845. Epub 2021 Feb 17. J Med Chem. 2021. PMID: 33596065
Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy.
Dragovich PS, Pillow TH, Blake RA, Sadowsky JD, Adaligil E, Adhikari P, Chen J, Corr N, Dela Cruz-Chuh J, Del Rosario G, Fullerton A, Hartman SJ, Jiang F, Kaufman S, Kleinheinz T, Kozak KR, Liu L, Lu Y, Mulvihill MM, Murray JM, O'Donohue A, Rowntree RK, Sawyer WS, Staben LR, Wai J, Wang J, Wei B, Wei W, Xu Z, Yao H, Yu SF, Zhang D, Zhang H, Zhang S, Zhao Y, Zhou H, Zhu X. Dragovich PS, et al. Among authors: kleinheinz t. J Med Chem. 2021 Mar 11;64(5):2576-2607. doi: 10.1021/acs.jmedchem.0c01846. Epub 2021 Feb 17. J Med Chem. 2021. PMID: 33596073
23 results