人类溴结构域化学抑制剂的发现。 - Suppr

Discovery of Chemical Inhibitors of Human Bromodomains.

作者信息

Zhang Guangtao, Smith Steven G, Zhou Ming-Ming

机构信息

Department of Structural and Chemical Biology, Icahn School of Medicine at Mount Sinai , 1425 Madison Avenue, New York, New York 10029, United States.

出版信息

Chem Rev. 2015 Nov 11;115(21):11625-68. doi: 10.1021/acs.chemrev.5b00205. Epub 2015 Oct 23.

DOI:10.1021/acs.chemrev.5b00205

PMID:26492937

Abstract

摘要

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Discovery of Chemical Inhibitors of Human Bromodomains.

作者信息

Zhang Guangtao, Smith Steven G, Zhou Ming-Ming

机构信息

Department of Structural and Chemical Biology, Icahn School of Medicine at Mount Sinai , 1425 Madison Avenue, New York, New York 10029, United States.

出版信息

Chem Rev. 2015 Nov 11;115(21):11625-68. doi: 10.1021/acs.chemrev.5b00205. Epub 2015 Oct 23.

DOI:10.1021/acs.chemrev.5b00205

PMID:26492937

Abstract

摘要

相似文献

Discovery of Chemical Inhibitors of Human Bromodomains.

Chem Rev. 2015 Nov 11;115(21):11625-68. doi: 10.1021/acs.chemrev.5b00205. Epub 2015 Oct 23.

An Overview on Small Molecule Inhibitors of BRD4.

Mini Rev Med Chem. 2016;16(17):1403-1414. doi: 10.2174/1389557516666160611014130.

Selective small molecules blocking HIV-1 Tat and coactivator PCAF association.

J Am Chem Soc. 2005 Mar 2;127(8):2376-7. doi: 10.1021/ja044885g.

Straightforward hit identification approach in fragment-based discovery of bromodomain-containing protein 4 (BRD4) inhibitors.

Bioorg Med Chem. 2018 Jul 23;26(12):3399-3405. doi: 10.1016/j.bmc.2018.05.010. Epub 2018 May 9.

DNA-binding small molecules as inhibitors of transcription factors.

Med Res Rev. 2013 Jul;33(4):823-46. doi: 10.1002/med.21266. Epub 2012 Apr 30.

The "Gatekeeper" Residue Influences the Mode of Binding of Acetyl Indoles to Bromodomains.

J Med Chem. 2016 Apr 14;59(7):3087-97. doi: 10.1021/acs.jmedchem.5b01757. Epub 2016 Mar 30.

Truncated norzoanthamine exhibiting similar collagen protection activity, toward a promising anti-osteoporotic drug.

Bioorg Med Chem Lett. 2014 Jan 15;24(2):508-9. doi: 10.1016/j.bmcl.2013.12.032. Epub 2013 Dec 16.

Composing compound libraries for hit discovery--rationality-driven preselection or random choice by structural diversity?

Future Med Chem. 2014;6(18):2057-72. doi: 10.4155/fmc.14.142.

Toward the comprehensive systematic enumeration and synthesis of novel kinase inhibitors based on a 4-anilinoquinazoline binding mode.

J Chem Inf Model. 2010 Apr 26;50(4):525-33. doi: 10.1021/ci9004767.

Phenotypic screening and fragment-based approaches to the discovery of small-molecule bromodomain ligands.

Future Med Chem. 2014 Feb;6(2):179-204. doi: 10.4155/fmc.13.197.

引用本文的文献

Targeting lysine acetylation readers and writers.

Nat Rev Drug Discov. 2025 Feb;24(2):112-133. doi: 10.1038/s41573-024-01080-6. Epub 2024 Nov 21.

Development and Evaluation of [C]I-58: A Novel PET Radiotracer Targeting BRD4 BD2 for Advanced Epigenetic Imaging.

ACS Omega. 2024 Aug 12;9(34):36177-36184. doi: 10.1021/acsomega.4c01495. eCollection 2024 Aug 27.

Bromodomain and extraterminal (BET) proteins: biological functions, diseases, and targeted therapy.

Signal Transduct Target Ther. 2023 Nov 6;8(1):420. doi: 10.1038/s41392-023-01647-6.

Bromodomain inhibitors and therapeutic applications.

Curr Opin Chem Biol. 2023 Aug;75:102323. doi: 10.1016/j.cbpa.2023.102323. Epub 2023 May 17.

Drugging the epigenome in the age of precision medicine.

Clin Epigenetics. 2023 Jan 11;15(1):6. doi: 10.1186/s13148-022-01419-z.

Mapping oncogenic protein interactions for precision medicine.

Int J Cancer. 2022 Jul 1;151(1):7-19. doi: 10.1002/ijc.33954. Epub 2022 Feb 14.

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

J Med Chem. 2022 Feb 10;65(3):2388-2408. doi: 10.1021/acs.jmedchem.1c01851. Epub 2022 Jan 4.

Design and Synthesis of LM146, a Potent Inhibitor of PB1 with an Improved Selectivity Profile over SMARCA2.

ACS Omega. 2021 Aug 9;6(33):21327-21338. doi: 10.1021/acsomega.1c01555. eCollection 2021 Aug 24.

Drug discovery in the era of cryo-electron microscopy.

Trends Biochem Sci. 2022 Feb;47(2):124-135. doi: 10.1016/j.tibs.2021.06.008. Epub 2021 Jul 16.

Gene Signature Associated With Bromodomain Genes Predicts the Prognosis of Kidney Renal Clear Cell Carcinoma.

Front Genet. 2021 Jun 2;12:643935. doi: 10.3389/fgene.2021.643935. eCollection 2021.

Discovery of Chemical Inhibitors of Human Bromodomains.

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Discovery of Chemical Inhibitors of Human Bromodomains.

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