Results 121 to 130 of about 128,101 (191)

Design, Synthesis, and Characterization of I‑BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate

Through regulation of the epigenome, the bromodomain and extra terminal (BET) family of proteins represent important therapeutic targets for the treatment of human disease. Through mimicking the endogenous N-acetyl-lysine group and disrupting the protein–
Thomas G. Hayhow (3624884), David Lugo (2803279), Peter D. Craggs (7180412), Inmaculada Rioja (8539), Alan Ferrie (11920186), Simon Taylor (441637), Ian D. Holyer (11920195), Nicholas Smithers (487233), Andrea Haynes (1399255), Leanne Cutler (1738141), Nick Henley (11920192), Rino A. Bit (1357536), Jonathan T. Seal (2119816), Alex Preston (9105252), Natalie H. Theodoulou (1508650), Paul Bamborough (1343466), Chris Patten (8232804), Qendresa Osmani (11920201), Dalin Tang (835554), Robert J. Watson (1343463), Linrong Zhu (11920207), Fenglai Sun (11920204), Christopher R. Wellaway (7148462), GangLi Gong (11920189), Philip G. Humphreys (1357530), Laurie J. Gordon (1343442), Cerys Lovatt (11920198), Nicholas C. O. Tomkinson (7417448), Rob Davis (9204195), Lee A. Harrison (2160145), Chun-wa Chung (1343454), David J. Hirst (1399282), Matthew Gray (2402251), Scott McCleary (8232795), Clare Thomas (7943747), Rab K. Prinjha (449759), Stephen J. Atkinson (1297362), Judit Molnar (1357521), Matthew J. Lindon (8232792)   +38 more
core   +2 more sources

BET bromodomain inhibition rescues PD-1-mediated T-cell exhaustion in acute myeloid leukemia. [PDF]

Cell Death Dis, 2022
Zhong M, Gao R, Zhao R, Huang Y, Chen C, Li K, Yu X, Nie D, Chen Z, Liu X, Liu Z, Chen S, Lu Y, Yu Z, Wang L, Li P, Zeng C, Li Y.   +17 more
europepmc   +1 more source

Discovery of potent BET bromodomain 1 stereoselective inhibitors using DNA-encoded chemical library selections. [PDF]

Proc Natl Acad Sci U S A, 2022
Modukuri RK, Yu Z, Tan Z, Ta HM, Ucisik MN, Jin Z, Anglin JL, Sharma KL, Nyshadham P, Li F, Riehle K, Faver JC, Duong K, Nagarajan S, Simmons N, Palmer SS, Teng M, Young DW, Yi JS, Kim C, Matzuk MM.   +20 more
europepmc   +1 more source

Combined inhibition of BET bromodomain and mTORC1/2 provides therapeutic advantage for rhabdomyosarcoma by switching cell death mechanism. [PDF]

Mol Carcinog, 2022
Srivastava RK, Guroji P, Jin L, Mukhtar MS, Athar M.   +4 more
europepmc   +1 more source

Correction to: BET bromodomain inhibition rescues PD-1-mediated T-cell exhaustion in acute myeloid leukemia. [PDF]

Cell Death Dis, 2022
Zhong M, Gao R, Zhao R, Huang Y, Chen C, Li K, Yu X, Nie D, Chen Z, Liu X, Liu Z, Chen S, Lu Y, Yu Z, Wang L, Li P, Zeng C, Li Y.   +17 more
europepmc   +1 more source

Bridging BET bromodomain and immune checkpoint inhibitors through generative bioorganic frameworks for next-generation cancer immunotherapy. [PDF]

RSC Med Chem
Diab MK, Yassen ASA, Fahmy SA, Ashour HF, Nafie MS.   +4 more
europepmc   +1 more source

Combined BET bromodomain and DNA methyltransferase inhibition targets critical survival pathways in transdifferentiated prostate cancer. [PDF]

JCI Insight
Storck WK, Flores D, Kumaraswamy A, Duan Z, Chakraborty S, Zhang C, Rodansky E, Khokhani D, Swaim OA, Bedi K, Cavalcante RG, Chen C, Zhao F, Hu YM, Xia Z, Rebernick RJ, Cieslik M, Mannan R, Mahapatra S, Chinnaiyan AM, Udager AM, Kuleape JA, Alumkal CR, Beck HN, Nelson PS, Morrissey C, Haffner MC, Ellis L, Wang Y, Yates JA, Alumkal JJ.   +30 more
europepmc   +1 more source

Therapeutically targeting oncogenic CRCs facilitates induced differentiation of NB by RA and the BET bromodomain inhibitor. [PDF]

Mol Ther Oncolytics, 2021
Alleboina S, Aljouda N, Miller M, Freeman KW.   +3 more
europepmc   +1 more source

Single-Cell Computational Frameworks for Quantifying BET Bromodomain Inhibitor Resistance and Screening Re-Sensitizer Drugs in Triple-Negative Breast Cancer. [PDF]

Adv Sci (Weinh)
Liu H, Yuan M, Shang Y, Chen J, Hou F, Wang L, Jiang W.   +6 more
europepmc   +1 more source

Combined noncanonical NF-κB agonism and targeted BET bromodomain inhibition reverse HIV latency ex vivo. [PDF]

J Clin Invest, 2022
Falcinelli SD, Peterson JJ, Turner AW, Irlbeck D, Read J, Raines SL, James KS, Sutton C, Sanchez A, Emery A, Sampey G, Ferris R, Allard B, Ghofrani S, Kirchherr JL, Baker C, Kuruc JD, Gay CL, James LI, Wu G, Zuck P, Rioja I, Furze RC, Prinjha RK, Howell BJ, Swanstrom R, Browne EP, Strahl BD, Dunham RM, Archin NM, Margolis DM.   +30 more
europepmc   +1 more source