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Publikationer i urvalet

39 träffar

Bibliografisk träff 2025-07-25

Lamin variants cause cardiac arrhythmogenicity in Drosophila.

van Wijk SW, Vree P, Huiskes FG, van der Palen RL, Liutkute A, Voigt N, Wallrath LL, Brundel BJJM.

Dis Model Mech · research support, non-u.s. gov't; research-article; journal article · DOI 10.1242/dmm.052424

Bibliografisk träff 2024-01-31

Structure-Guided Design and Synthesis of Pyridinone-Based Selective Bromodomain and Extra-Terminal Domain (BET)-First Bromodomain (BD1) Inhibitors.

Li Y, Shen Z, Ratia K, Zhao J, Huang F, Dubrovyskyii O, Indukuri D, Fu J, Lozano Ramos O, Thatcher GRJ, Xiong R.

J Med Chem · journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.3c01837

Bibliografisk träff 2024-01-04

Discovery of Novel Phenoxyaryl Pyridones as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with High Selectivity for the Second Bromodomain (BD2) to Potentially Treat Acute Myeloid Leukemia.

Jiang W, Hou Q, Xu H, Yang K, Wang X, Zhang K, Zeng Y, Li W, Wang B, Luo G, Zhao X, Shen H, Xu Y, Wu X.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.3c02104

Bibliografisk träff 2023-11-07

Discovery of (R)-4-(8-methoxy-2-methyl-1-(1-phenylethy)-1H-imidazo[4,5-c]quinnolin-7-yl)-3,5-dimethylisoxazole as a potent and selective BET inhibitor for treatment of acute myeloid leukemia (AML) guided by FEP calculation.

Yu S, Zhang Y, Yang J, Xu H, Lan S, Zhao B, Luo M, Ma X, Zhang H, Wang S, Shen H, Zhang Y, Xu Y, Li R.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2023.115924

Bibliografisk träff 2023-07-21

Discovery of a Bromodomain and Extra Terminal Domain (BET) Inhibitor with the Selectivity for the Second Bromodomain (BD2) and the Capacity for the Treatment of Inflammatory Diseases.

Wang Z, Yin L, Xiong Z, Huang F, Yang N, Jiang F, Li H, Cui Y, Ren J, Cheng Z, Jia K, Lu T, Zhu J, Hu Q, Chen Y.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.3c01028

Bibliografisk träff 2022-11-29

Design, synthesis and anti-ovarian cancer activities of thieno[2,3-d]pyrimidine based chimeric BRD4 inhibitor/nitric oxide-donator.

Zhang Y, Pan Z, Chen C, Tan Y, Wang X, Wang L, Zhang L, Chen Y, He G.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2022.114970

Bibliografisk träff 2022-05-08

Discovery of 2-((2-methylbenzyl)thio)-6-oxo-4-(3,4,5-trimethoxyphenyl)-1,6-dihydropyrimidine-5-carbonitrile as a novel and effective bromodomain and extra-terminal (BET) inhibitor for the treatment of sepsis.

Chen X, Meng F, Zhang J, Zhang Z, Ye X, Zhang W, Tong Y, Ji X, Xu R, Xu XL, You QD, Jiang ZY.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2022.114423

Bibliografisk träff 2022-03-29

CRCM5484: A BET-BDII Selective Compound with Differential Anti-leukemic Drug Modulation.

Carrasco K, Montersino C, Derviaux C, Saez-Ayala M, Hoffer L, Restouin A, Castellano R, Casassa J, Roche P, Pasquier E, Combes S, Morelli X, Collette Y, Betzi S.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.1c02168

Bibliografisk träff 2022-01-04

Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site.

Liu Z, Li Y, Chen H, Lai HT, Wang P, Wu SY, Wold EA, Leonard PG, Joseph S, Hu H, Chiang CM, Brasier AR, Tian B, Zhou J.

J Med Chem · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.1c01851

Bibliografisk träff 2021-12-30

Dual-target inhibitors of poly (ADP-ribose) polymerase-1 for cancer therapy: Advances, challenges, and opportunities.

Hu X, Zhang J, Zhang Y, Jiao F, Wang J, Chen H, Ouyang L, Wang Y.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2021.114094

Bibliografisk träff 2021-10-29

Discovery of 1-(5-(1H-benzo[d]imidazole-2-yl)-2,4-dimethyl-1H-pyrrol-3-yl)ethan-1-one derivatives as novel and potent bromodomain and extra-terminal (BET) inhibitors with anticancer efficacy.

Kong B, Zhu Z, Li H, Hong Q, Wang C, Ma Y, Zheng W, Jiang F, Zhang Z, Ran T, Bian Y, Yang N, Lu T, Zhu J, Tang W, Chen Y.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2021.113953

Bibliografisk träff 2021-09-13

Progress in the development of domain selective inhibitors of the bromo and extra terminal domain family (BET) proteins.

Fu Y, Zhang Y, Sun H.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2021.113853

Bibliografisk träff 2021-03-10

Synergistic effects of type I PRMT and PARP inhibitors against non-small cell lung cancer cells.

Dominici C, Sgarioto N, Yu Z, Sesma-Sanz L, Masson JY, Richard S, Raynal NJ.

Clin Epigenetics · research support, non-u.s. gov't; research-article; journal article · DOI 10.1186/s13148-021-01037-1

Bibliografisk träff 2021-01-23

HIV latency reversal agents: A potential path for functional cure?

Lopes JR, Chiba DE, Dos Santos JL.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2021.113213

Bibliografisk träff 2020-12-29

Targeting MYC: From understanding its biology to drug discovery.

Ross J, Miron CE, Plescia J, Laplante P, McBride K, Moitessier N, Möröy T.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2020.113137

Bibliografisk träff 2020-08-20

Design and Synthesis of a Highly Selective and In Vivo-Capable Inhibitor of the Second Bromodomain of the Bromodomain and Extra Terminal Domain Family of Proteins.

Preston A, Atkinson S, Bamborough P, Chung CW, Craggs PD, Gordon L, Grandi P, Gray JRJ, Jones EJ, Lindon M, Michon AM, Mitchell DJ, Prinjha RK, Rianjongdee F, Rioja I, Seal J, Taylor S, Wall I, Watson RJ, Woolven J, Demont EH.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.0c00605

Bibliografisk träff 2020-05-07

Discovery of N-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain.

Sheppard GS, Wang L, Fidanze SD, Hasvold LA, Liu D, Pratt JK, Park CH, Longenecker K, Qiu W, Torrent M, Kovar PJ, Bui M, Faivre E, Huang X, Lin X, Wilcox D, Zhang L, Shen Y, Albert DH, Magoc TJ, Rajaraman G, Kati WM, McDaniel KF.

J Med Chem · research support, u.s. gov't, non-p.h.s.; journal article · DOI 10.1021/acs.jmedchem.0c00628

Bibliografisk träff 2020-04-30

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.

Gordon DE, Jang GM, Bouhaddou M, Xu J, Obernier K, White KM, O'Meara MJ, Rezelj VV, Guo JZ, Swaney DL, Tummino TA, Hüttenhain R, Kaake RM, Richards AL, Tutuncuoglu B, Foussard H, Batra J, Haas K, Modak M, Kim M, Haas P, Polacco BJ, Braberg H, Fabius JM, Eckhardt M, Soucheray M, Bennett MJ, Cakir M, McGregor MJ, Li Q, Meyer B, Roesch F, Vallet T, Mac Kain A, Miorin L, Moreno E, Naing ZZC, Zhou Y, Peng S, Shi Y, Zhang Z, Shen W, Kirby IT, Melnyk JE, Chorba JS, Lou K, Dai SA, Barrio-Hernandez I, Memon D, Hernandez-Armenta C, Lyu J, Mathy CJP, Perica T, Pilla KB, Ganesan SJ, Saltzberg DJ, Rakesh R, Liu X, Rosenthal SB, Calviello L, Venkataramanan S, Liboy-Lugo J, Lin Y, Huang XP, Liu Y, Wankowicz SA, Bohn M, Safari M, Ugur FS, Koh C, Savar NS, Tran QD, Shengjuler D, Fletcher SJ, O'Neal MC, Cai Y, Chang JCJ, Broadhurst DJ, Klippsten S, Sharp PP, Wenzell NA, Kuzuoglu-Ozturk D, Wang HY, Trenker R, Young JM, Cavero DA, Hiatt J, Roth TL, Rathore U, Subramanian A, Noack J, Hubert M, Stroud RM, Frankel AD, Rosenberg OS, Verba KA, Agard DA, Ott M, Emerman M, Jura N, von Zastrow M, Verdin E, Ashworth A, Schwartz O, d'Enfert C, Mukherjee S, Jacobson M, Malik HS, Fujimori DG, Ideker T, Craik CS, Floor SN, Fraser JS, Gross JD, Sali A, Roth BL, Ruggero D, Taunton J, Kortemme T, Beltrao P, Vignuzzi M, García-Sastre A, Shokat KM, Shoichet BK, Krogan NJ.

Nature · research support, non-u.s. gov't; research-article; research support, u.s. gov't, non-p.h.s.; journal article; research support, n.i.h., extramural · DOI 10.1038/s41586-020-2286-9

Bibliografisk träff 2020-04-22

Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.

Liu Z, Chen H, Wang P, Li Y, Wold EA, Leonard PG, Joseph S, Brasier AR, Tian B, Zhou J.

J Med Chem · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.0c00035

Bibliografisk träff 2020-03-18

Discovery of Thieno[2,3-d]pyrimidine-Based Hydroxamic Acid Derivatives as Bromodomain-Containing Protein 4/Histone Deacetylase Dual Inhibitors Induce Autophagic Cell Death in Colorectal Carcinoma Cells.

Pan Z, Li X, Wang Y, Jiang Q, Jiang L, Zhang M, Zhang N, Wu F, Liu B, He G.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.9b02178

Bibliografisk träff 2019-12-13

Discovery of Benzo[cd]indol-2(1H)-ones and Pyrrolo[4,3,2-de]quinolin-2(1H)-ones as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the First Bromodomain with Potential High Efficiency against Acute Gouty Arthritis.

Jiang F, Hu Q, Zhang Z, Li H, Li H, Zhang D, Li H, Ma Y, Xu J, Chen H, Cui Y, Zhi Y, Zhang Y, Xu J, Zhu J, Lu T, Chen Y.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.9b01010

Bibliografisk träff 2019-11-14

A concise review of recent advances in anti-heart failure targets and its small molecules inhibitors in recent years.

Li X, Liao J, Jiang Z, Liu X, Chen S, He X, Zhu L, Duan X, Xu Z, Qi B, Guo X, Tong R, Shi J.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2019.111852

Bibliografisk träff 2019-07-25

Design, synthesis and biological evaluation of 3,5-dimethylisoxazole and pyridone derivatives as BRD4 inhibitors.

Rong J, Feng ZZ, Shi YJ, Ren J, Xu Y, Wang NY, Xue Q, Liu KL, Zhou SY, Wei W, Yu LT.

Bioorg Med Chem Lett · research support, non-u.s. gov't; evaluation study; journal article · DOI 10.1016/j.bmcl.2019.07.036

Bibliografisk träff 2019-06-20

Design, synthesis and biological evaluation of hypolipidemic compounds based on BRD4 inhibitor RVX-208.

Yu P, Liu W, Ren J, Wang Y, Ning Y, Huang M, Hu X, Wei L, Ji M, Cai J.

Bioorg Med Chem Lett · letter; research support, non-u.s. gov't · DOI 10.1016/j.bmcl.2019.06.028

Bibliografisk träff 2019-03-22

Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors.

Ma J, Chen H, Yang J, Yu Z, Huang P, Yang H, Zheng B, Liu R, Li Q, Hu G, Chen Z.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2019.03.037

Bibliografisk träff 2018-11-16

Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.

Xing J, Zhang R, Jiang X, Hu T, Wang X, Qiao G, Wang J, Yang F, Luo X, Chen K, Shen J, Luo C, Jiang H, Zheng M.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2018.11.018

Bibliografisk träff 2018-10-16

Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.

Divakaran A, Talluri SK, Ayoub AM, Mishra NK, Cui H, Widen JC, Berndt N, Zhu JY, Carlson AS, Topczewski JJ, Schonbrunn EK, Harki DA, Pomerantz WCK.

J Med Chem · research support, non-u.s. gov't; research-article; research support, u.s. gov't, non-p.h.s.; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.8b01248

Bibliografisk träff 2018-05-03

Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.

Law RP, Atkinson SJ, Bamborough P, Chung CW, Demont EH, Gordon LJ, Lindon M, Prinjha RK, Watson AJB, Hirst DJ.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.7b01666

Bibliografisk träff 2018-04-03

Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.

Liu Z, Tian B, Chen H, Wang P, Brasier AR, Zhou J.

Eur J Med Chem · research-article; journal article · DOI 10.1016/j.ejmech.2018.04.006

Bibliografisk träff 2017-12-07

Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer.

Ouyang L, Zhang L, Liu J, Fu L, Yao D, Zhao Y, Zhang S, Wang G, He G, Liu B.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.7b00275

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Publikationer i urvalet

Lamin variants cause cardiac arrhythmogenicity in Drosophila.

Structure-Guided Design and Synthesis of Pyridinone-Based Selective Bromodomain and Extra-Terminal Domain (BET)-First Bromodomain (BD1) Inhibitors.

Discovery of Novel Phenoxyaryl Pyridones as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with High Selectivity for the Second Bromodomain (BD2) to Potentially Treat Acute Myeloid Leukemia.

Discovery of (R)-4-(8-methoxy-2-methyl-1-(1-phenylethy)-1H-imidazo[4,5-c]quinnolin-7-yl)-3,5-dimethylisoxazole as a potent and selective BET inhibitor for treatment of acute myeloid leukemia (AML) guided by FEP calculation.

Discovery of a Bromodomain and Extra Terminal Domain (BET) Inhibitor with the Selectivity for the Second Bromodomain (BD2) and the Capacity for the Treatment of Inflammatory Diseases.

Design, synthesis and anti-ovarian cancer activities of thieno[2,3-d]pyrimidine based chimeric BRD4 inhibitor/nitric oxide-donator.

Discovery of 2-((2-methylbenzyl)thio)-6-oxo-4-(3,4,5-trimethoxyphenyl)-1,6-dihydropyrimidine-5-carbonitrile as a novel and effective bromodomain and extra-terminal (BET) inhibitor for the treatment of sepsis.

CRCM5484: A BET-BDII Selective Compound with Differential Anti-leukemic Drug Modulation.

Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site.

Dual-target inhibitors of poly (ADP-ribose) polymerase-1 for cancer therapy: Advances, challenges, and opportunities.

Discovery of 1-(5-(1H-benzo[d]imidazole-2-yl)-2,4-dimethyl-1H-pyrrol-3-yl)ethan-1-one derivatives as novel and potent bromodomain and extra-terminal (BET) inhibitors with anticancer efficacy.

Progress in the development of domain selective inhibitors of the bromo and extra terminal domain family (BET) proteins.

Synergistic effects of type I PRMT and PARP inhibitors against non-small cell lung cancer cells.

HIV latency reversal agents: A potential path for functional cure?

Targeting MYC: From understanding its biology to drug discovery.

Design and Synthesis of a Highly Selective and <i>In Vivo</i>-Capable Inhibitor of the Second Bromodomain of the Bromodomain and Extra Terminal Domain Family of Proteins.

Discovery of <i>N</i>-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1<i>H</i>-pyrrolo[2,3-<i>c</i>]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain.

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.

Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.

Discovery of Thieno[2,3-<i>d</i>]pyrimidine-Based Hydroxamic Acid Derivatives as Bromodomain-Containing Protein 4/Histone Deacetylase Dual Inhibitors Induce Autophagic Cell Death in Colorectal Carcinoma Cells.

Discovery of Benzo[<i>cd</i>]indol-2(1<i>H</i>)-ones and Pyrrolo[4,3,2-<i>de</i>]quinolin-2(1<i>H</i>)-ones as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the First Bromodomain with Potential High Efficiency against Acute Gouty Arthritis.

A concise review of recent advances in anti-heart failure targets and its small molecules inhibitors in recent years.

Design, synthesis and biological evaluation of 3,5-dimethylisoxazole and pyridone derivatives as BRD4 inhibitors.

Design, synthesis and biological evaluation of hypolipidemic compounds based on BRD4 inhibitor RVX-208.

Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors.

Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.

Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.

Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.

Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.

Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer.