4.5 Article

Dihydropyridine Lactam Analogs Targeting BET Bromodomains

相关参考文献

注意:仅列出部分参考文献,下载原文获取全部文献信息。
Article Chemistry, Medicinal

Targeting Bromodomain and Extraterminal Proteins for Drug Discovery: From Current Progress to Technological Development

Pan Tang et al.

Summary: BET proteins regulate chromatin dynamics, cellular processes, and disease progression by binding acetylated lysine residues in histones and nonhistone proteins, making them a promising strategy for treating malignant tumors and chronic inflammation. However, the clinical efficacy of current BET inhibitors is limited, leading to the development of new technologies to improve outcomes and minimize side effects.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Multidisciplinary Sciences

Discovery and characterization of bromodomain 2-specific inhibitors of BRDT

Zhifeng Yu et al.

Summary: BRDT, a member of the BET subfamily, is a validated contraceptive target with potential nonhormonal contraceptive properties. The discovery of selective and potent BRDT-BD2 inhibitors provides new insights into disrupting spermatogenesis and offers further evaluation of nonhormonal contraceptive potential in vitro and in vivo. The unique binding characteristics of BD2-specific compounds to BRDT-BD2 enable potential applications in contraceptive research.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2021)

Article Multidisciplinary Sciences

Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer

Emily J. Faivre et al.

NATURE (2020)

Review Pharmacology & Pharmacy

Make your best BET: The emerging role of BET inhibitor treatment in malignant tumors

Oliver Bechter et al.

PHARMACOLOGY & THERAPEUTICS (2020)

Review Genetics & Heredity

Essential Role of Histone Replacement and Modifications in Male Fertility

Tong Wang et al.

FRONTIERS IN GENETICS (2019)

Article Multidisciplinary Sciences

BET bromodomain proteins regulate enhancer function during adipogenesis

Jonathan D. Brown et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2018)

Article Chemistry, Medicinal

BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen

Alex M. Ayoub et al.

JOURNAL OF MEDICINAL CHEMISTRY (2017)

Article Multidisciplinary Sciences

Ectopic protein interactions within BRD4-chromatin complexes drive oncogenic megadomain formation in NUT midline carcinoma

Artyom A. Alekseyenko et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2017)

Article Biochemistry & Molecular Biology

Design and characterization of bivalent BET inhibitors

Minoru Tanaka et al.

NATURE CHEMICAL BIOLOGY (2016)

Article Biochemistry & Molecular Biology

BRD4 is a histone acetyltransferase that evicts nucleosomes from chromatin

Ballachanda N. Devaiah et al.

NATURE STRUCTURAL & MOLECULAR BIOLOGY (2016)

Article Biochemistry & Molecular Biology

BRD4 is a histone acetyltransferase that evicts nucleosomes from chromatin

Ballachanda N. Devaiah et al.

NATURE STRUCTURAL & MOLECULAR BIOLOGY (2016)

Correction Chemistry, Medicinal

Importance of Purity Evaluation and the Potential of Quantitative 1H NMR as a Purity Assay (vol 57, pg 9220, 2014)

Guido F. Pauli et al.

JOURNAL OF MEDICINAL CHEMISTRY (2015)

Review Cell Biology

50 years of protein acetylation: from gene regulation to epigenetics, metabolism and beyond

Eric Verdin et al.

NATURE REVIEWS MOLECULAR CELL BIOLOGY (2015)

Article Biochemistry & Molecular Biology

Acetyl-lysine Binding Site of Bromodomain-Containing Protein 4 (BRD4) Interacts with Diverse Kinase Inhibitors

Stuart W. J. Ember et al.

ACS CHEMICAL BIOLOGY (2014)

Review Biochemistry & Molecular Biology

Chromatin dynamics during spermiogenesis

Christina Rathke et al.

BIOCHIMICA ET BIOPHYSICA ACTA-GENE REGULATORY MECHANISMS (2014)

Article Chemistry, Medicinal

Naphthyridines as Novel BET Family Bromodomain Inhibitors

Olivier Mirguet et al.

CHEMMEDCHEM (2014)

Article Chemistry, Medicinal

Importance of Purity Evaluation and the Potential of Quantitative 1H NMR as a Purity Assay

Guido F. Pauli et al.

JOURNAL OF MEDICINAL CHEMISTRY (2014)

Article Multidisciplinary Sciences

RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain

Sarah Picaud et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2013)

Article Biochemistry & Molecular Biology

Small-Molecule Inhibition of BRDT for Male Contraception

Martin M. Matzuk et al.

Article Biochemistry & Molecular Biology

Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family

Panagis Filippakopoulos et al.

Article Biochemistry & Molecular Biology

Bromodomain-dependent stage-specific male genome programming by Brdt

Jonathan Gaucher et al.

EMBO JOURNAL (2012)

Article Obstetrics & Gynecology

Expression of BET genes in testis of men with different spermatogenic impairments

Shimi Barda et al.

FERTILITY AND STERILITY (2012)

Article Biochemical Research Methods

MolProbity: all-atom structure validation for macromolecular crystallography

Vincent B. Chen et al.

ACTA CRYSTALLOGRAPHICA SECTION D-STRUCTURAL BIOLOGY (2010)

Article Biochemical Research Methods

XDS

Wolfgang Kabsch

ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY (2010)

Article Biochemical Research Methods

Features and development of Coot

P. Emsley et al.

ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY (2010)

Article Biochemical Research Methods

PHENIX: a comprehensive Python-based system for macromolecular structure solution

Paul D. Adams et al.

ACTA CRYSTALLOGRAPHICA SECTION D-STRUCTURAL BIOLOGY (2010)

Article Chemistry, Multidisciplinary

phenix.model_vs_data: a high-level tool for the calculation of crystallographic model and data statistics

Pavel V. Afonine et al.

JOURNAL OF APPLIED CRYSTALLOGRAPHY (2010)

Article Multidisciplinary Sciences

Selective inhibition of BET bromodomains

Panagis Filippakopoulos et al.

NATURE (2010)

Article Multidisciplinary Sciences

Regulation of Cellular Metabolism by Protein Lysine Acetylation

Shimin Zhao et al.

SCIENCE (2010)

Article Multidisciplinary Sciences

Lysine Acetylation Targets Protein Complexes and Co-Regulates Major Cellular Functions

Chunaram Choudhary et al.

SCIENCE (2009)

Article Biochemical Research Methods

Amazing stability of phosphate-quaternary amine interactions

Amina S. Woods et al.

JOURNAL OF PROTEOME RESEARCH (2008)

Article Nutrition & Dietetics

Cation-π interactions involving aromatic amino acids

Dennis A. Dougherty

JOURNAL OF NUTRITION (2007)

Article Biochemical Research Methods

Molecular complexes at a glance: automated generation of two-dimensional complex diagrams

Katrin Stierand et al.

BIOINFORMATICS (2006)

Article Biochemical Research Methods

Amazing stability of the arginine-phosphate electrostatic interaction

AS Woods et al.

JOURNAL OF PROTEOME RESEARCH (2005)

Review Biochemistry & Molecular Biology

Acetylation: a regulatory modification to rival phosphorylation?

T Kouzarides

EMBO JOURNAL (2000)