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Page 1
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: gascoigne ke. ChemMedChem. 2020 Jan 7;15(1):17-25. doi: 10.1002/cmdc.201900497. Epub 2019 Nov 14. ChemMedChem. 2020. PMID: 31674143
Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300.
Crawford TD, Romero FA, Lai KW, Tsui V, Taylor AM, de Leon Boenig G, Noland CL, Murray J, Ly J, Choo EF, Hunsaker TL, Chan EW, Merchant M, Kharbanda S, Gascoigne KE, Kaufman S, Beresini MH, Liao J, Liu W, Chen KX, Chen Z, Conery AR, Côté A, Jayaram H, Jiang Y, Kiefer JR, Kleinheinz T, Li Y, Maher J, Pardo E, Poy F, Spillane KL, Wang F, Wang J, Wei X, Xu Z, Xu Z, Yen I, Zawadzke L, Zhu X, Bellon S, Cummings R, Cochran AG, Albrecht BK, Magnuson S. Crawford TD, et al. Among authors: gascoigne ke. J Med Chem. 2016 Dec 8;59(23):10549-10563. doi: 10.1021/acs.jmedchem.6b01022. Epub 2016 Sep 28. J Med Chem. 2016. PMID: 27682507
GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP).
Romero FA, Murray J, Lai KW, Tsui V, Albrecht BK, An L, Beresini MH, de Leon Boenig G, Bronner SM, Chan EW, Chen KX, Chen Z, Choo EF, Clagg K, Clark K, Crawford TD, Cyr P, de Almeida Nagata D, Gascoigne KE, Grogan JL, Hatzivassiliou G, Huang W, Hunsaker TL, Kaufman S, Koenig SG, Li R, Li Y, Liang X, Liao J, Liu W, Ly J, Maher J, Masui C, Merchant M, Ran Y, Taylor AM, Wai J, Wang F, Wei X, Yu D, Zhu BY, Zhu X, Magnuson S. Romero FA, et al. Among authors: gascoigne ke. J Med Chem. 2017 Nov 22;60(22):9162-9183. doi: 10.1021/acs.jmedchem.7b00796. Epub 2017 Sep 21. J Med Chem. 2017. PMID: 28892380
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: gascoigne ke. 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
Therapeutic Targeting of the CBP/p300 Bromodomain Blocks the Growth of Castration-Resistant Prostate Cancer.
Jin L, Garcia J, Chan E, de la Cruz C, Segal E, Merchant M, Kharbanda S, Raisner R, Haverty PM, Modrusan Z, Ly J, Choo E, Kaufman S, Beresini MH, Romero FA, Magnuson S, Gascoigne KE. Jin L, et al. Among authors: gascoigne ke. Cancer Res. 2017 Oct 15;77(20):5564-5575. doi: 10.1158/0008-5472.CAN-17-0314. Epub 2017 Aug 17. Cancer Res. 2017. PMID: 28819026
An Antibody-Drug Conjugate Directed against Lymphocyte Antigen 6 Complex, Locus E (LY6E) Provides Robust Tumor Killing in a Wide Range of Solid Tumor Malignancies.
Asundi J, Crocker L, Tremayne J, Chang P, Sakanaka C, Tanguay J, Spencer S, Chalasani S, Luis E, Gascoigne K, Desai R, Raja R, Friedman BA, Haverty PM, Polakis P, Firestein R. Asundi J, et al. Clin Cancer Res. 2015 Jul 15;21(14):3252-62. doi: 10.1158/1078-0432.CCR-15-0156. Epub 2015 Apr 10. Clin Cancer Res. 2015. PMID: 25862760
Correction: Bromodomain inhibition of the transcriptional coactivators CBP/EP300 as a therapeutic strategy to target the IRF4 network in multiple myeloma.
Conery AR, Centore RC, Neiss A, Keller PJ, Joshi S, Spillane KL, Sandy P, Hatton C, Pardo E, Zawadzke L, Bommi-Reddy A, Gascoigne KE, Bryant BM, Mertz JA, Sims RJ. Conery AR, et al. Among authors: gascoigne ke. Elife. 2016 Jul 14;5:e19432. doi: 10.7554/eLife.19432. Elife. 2016. PMID: 27411486 Free PMC article. No abstract available.
Enhancer Activity Requires CBP/P300 Bromodomain-Dependent Histone H3K27 Acetylation.
Raisner R, Kharbanda S, Jin L, Jeng E, Chan E, Merchant M, Haverty PM, Bainer R, Cheung T, Arnott D, Flynn EM, Romero FA, Magnuson S, Gascoigne KE. Raisner R, et al. Among authors: gascoigne ke. Cell Rep. 2018 Aug 14;24(7):1722-1729. doi: 10.1016/j.celrep.2018.07.041. Cell Rep. 2018. PMID: 30110629 Free article.
24 results