☆ 4.7 Article

Rational design, synthesis and biological evaluation of benzo[d]isoxazole derivatives as potent BET bivalent inhibitors for potential treatment of prostate cancer

BIOORGANIC CHEMISTRY (2023)

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。

Review Biochemistry & Molecular Biology

BRD4 and MYC: power couple in transcription and disease

Aparna Kotekar et al.

Summary: The MYC proto-oncogene and BRD4 protein play essential roles in cell biology and disease, with their functions and regulation closely interlinked. They regulate gene expression, maintain chromatin structure, and ensure genome stability, and dysregulation can lead to diseases, particularly cancer.

FEBS JOURNAL (2023)

添加到收藏夹

Article Chemistry, Medicinal

Design, Synthesis, and Biological Evaluation of 1-(Indolizin-3-yl)ethan-1-ones as CBP Bromodomain Inhibitors for the Treatment of Prostate Cancer

Qiuping Xiang et al.

Summary: The study optimized a series of CBP inhibitor compounds, resulting in the synthesis of a compound with good pharmacokinetic properties that exhibited anti-proliferative, anti-colony formation, and anti-migratory effects on prostate cancer cells. The new inhibitor showed promising anti-tumor efficacy in an animal model.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Article Chemistry, Medicinal

A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes

Huarui Cui et al.

Summary: Chemical probes for epigenetic proteins are crucial for understanding gene regulation and therapeutic development. In this study, a structure-activity relationship analysis led to the discovery of selective small molecule inhibitors for the BRD4 N-terminal bromodomain, providing new design rules for selective inhibitors of individual BET bromodomain.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Article Chemistry, Medicinal

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

Zhiqing Liu et al.

Summary: A potent BRD4 BD1-selective inhibitor ZL0590 has been discovered, targeting a unique binding site and exhibiting significant anti-inflammatory activities. This finding provides new insights into the complex biology of bromodomain specificity among BRD4 and its protein-protein interaction partners.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Review Cell Biology

Modulation of cellular processes by histone and non-histone protein acetylation

Maria Shvedunova et al.

Summary: Lysine acetylation is a crucial protein post-translational modification that plays important roles in cellular and physiological processes. Lysine acetyltransferases and lysine deacetylases regulate gene expression and protein function by controlling acetylation and deacetylation.

NATURE REVIEWS MOLECULAR CELL BIOLOGY (2022)

添加到收藏夹

Article Chemistry, Medicinal

Structure-Based Discovery and Optimization of Furo[3,2-c]pyridin-4(5H)-one Derivatives as Potent and Second Bromodomain (BD2)-Selective Bromo and Extra Terminal Domain (BET) Inhibitors

Junhua Li et al.

Summary: A series of novel BD2-selective BET inhibitors were reported, with the representative compound 8l showing potent inhibitory activity and selectivity. It exhibited significant antiproliferative activity against multiple tumor cell lines and low cytotoxicity against normal cells. Additionally, 8l demonstrated good metabolic stability.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Review Endocrinology & Metabolism

Novel forms of prostate cancer chemoresistance to successful androgen deprivation therapy demand new approaches: Rationale for targeting BET proteins

Joakin O. Mori et al.

Summary: The duration of remission after ADT treatment varies in prostate cancer patients. Difficulties in predicting individual risk for progression and emergence of new forms of ADT resistance demand better understanding of resistance mechanisms and search for alternative treatments. Targeting the BET protein family and chromatin modifiers may be options worth exploring. However, more comprehensive analysis of a broader range of patients is needed before drawing definitive conclusions.

PROSTATE (2022)

添加到收藏夹

Article Chemistry, Medicinal

Bivalent BET Bromodomain Inhibitors Confer Increased Potency and Selectivity for BRDT via Protein Conformational Plasticity

Xianghong Guan et al.

Summary: Bromodomain and extraterminal domain (BET) proteins, including BRD4 and BRDT, play crucial roles in gene transcription and chromatin remodeling. Novel bivalent inhibitors show increased activity and selectivity for BRDT, due to differential plasticity of BET bromodomains upon inhibitor-induced dimerization. X-ray crystallographic and solution studies reveal unique structural states of BET proteins upon interaction with bivalent inhibitors.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Article Chemistry, Medicinal

Design and development of a novel series of oral bivalent BET inhibitors with potent anticancer activities

Menglan Luo et al.

Summary: Bromodomain and extraterminal domain (BET) subfamily members are potential targets for cancer treatment. This study presents a series of novel bivalent inhibitors with short and hydrophilic linkers, which exhibit improved activities and pharmacokinetic properties.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Review Pharmacology & Pharmacy

Mechanisms of enzalutamide resistance in castration-resistant prostate cancer and therapeutic strategies to overcome it

Yuanyuan Wang et al.

Summary: This review examines the emerging information on resistance mechanisms to enzalutamide in castration-resistant prostate cancer, including various signaling pathways and metabolic effects, and suggests potential therapeutic strategies for overcoming enzalutamide resistance.

BRITISH JOURNAL OF PHARMACOLOGY (2021)

添加到收藏夹

Article Oncology

Global cancer statistics 2020: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries

Hyuna Sung et al.

Summary: The global cancer burden in 2020 saw an estimated 19.3 million new cancer cases and almost 10.0 million cancer deaths. Female breast cancer surpassed lung cancer as the most commonly diagnosed cancer, while lung cancer remained the leading cause of cancer death. These trends are expected to rise in 2040, with transitioning countries experiencing a larger increase compared to transitioned countries due to demographic changes and risk factors associated with globalization and a growing economy. Efforts to improve cancer prevention measures and provision of cancer care in transitioning countries will be crucial for global cancer control.

CA-A CANCER JOURNAL FOR CLINICIANS (2021)

添加到收藏夹

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)

添加到收藏夹

Review Urology & Nephrology

Resistance to second-generation androgen receptor antagonists in prostate cancer

Keith T. Schmidt et al.

Summary: The introduction of second-generation androgen receptor antagonists has revolutionized the treatment of metastatic prostate cancer, offering tolerable and effective alternatives to chemotherapy. However, the issue of treatment resistance remains a significant challenge, and researchers are exploring various approaches to address this issue.

NATURE REVIEWS UROLOGY (2021)

添加到收藏夹

Article Biochemistry & Molecular Biology

Discovery of 3,5-dimethylisoxazole derivatives as novel, potent inhibitors for bromodomain and extraterminal domain (BET) family

Lincheng Fang et al.

Summary: The research found that compound 39, developed based on the BRD4 inhibitor compound 13, exhibited strong inhibitory activity against the BD1 protein and showed high anti-proliferation activity and apoptosis-inducing ability against U266 cancer cells. These results suggest that the BRD4 protein may be a therapeutic target, and compound 39 is an excellent lead compound for further development.

BIOORGANIC & MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of a Highly Selective BET BD2 Inhibitor from a DNA-Encoded Library Technology Screening Hit

Francesco Rianjongdee et al.

Summary: This study presents the discovery of a novel BET BD2-selective compound with unique structural features, exceptional selectivity, and good physicochemical properties, which can potentially advance the field of epigenetics research.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

4-Methyl-1,2,3-Triazoles as N-Acetyl-Lysine Mimics Afford Potent BET Bromodomain Inhibitors with Improved Selectivity

Huarui Cui et al.

Summary: The BET protein family recognizes acetylated lysines using two N-terminal bromodomains, and these interactions are therapeutic targets for BET-related diseases. A structure-activity relationship study of triazole-based inhibitors improved affinity, D1 selectivity, and microsomal stability by targeting specific residues on BRD4 D1. Lead inhibitors DW34 and 26 showed promising activity in suppressing c-Myc expression and downregulating IL-8, suggesting their potential as new leads for investigating anticancer and anti-inflammatory activity of BET proteins.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Review Biochemistry & Molecular Biology

The BET family in immunity and disease

Nian Wang et al.

Summary: The BET family plays a crucial role in regulating the transcription of genes associated with inflammation and immunity by recognizing acetylated histones and recruiting transcription factors and elongation complexes. Manipulating the BET family holds promise as a new treatment approach for disease.

SIGNAL TRANSDUCTION AND TARGETED THERAPY (2021)

添加到收藏夹

Article Multidisciplinary Sciences

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

Emily J. Faivre et al.

NATURE (2020)

添加到收藏夹

Article Multidisciplinary Sciences

Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation

Omer Gilan et al.

SCIENCE (2020)

添加到收藏夹

Article Chemistry, Medicinal

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

Zhiqing Liu et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Oncology

Combined Targeting of the BRD4-NUT-p300 Axis in NUT Midline Carcinoma by Dual Selective Bromodomain Inhibitor, NEO2734

Chevaun D. Morrison-Smiths et al.

MOLECULAR CANCER THERAPEUTICS (2020)

添加到收藏夹

Article Oncology

Bromodomain-Selective BET Inhibitors Are Potent Antitumor Agents against MYC-Driven Pediatric Cancer

P. Jake Slavish et al.

CANCER RESEARCH (2020)

添加到收藏夹

Article Chemistry, Medicinal

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

Alex Preston et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor

Jonathan T. Seal et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins

Robert J. Watson et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Identification of 3,5-Dimethylisoxazole Derivatives as BRD4 Inhibitors for the Treatment of Colorectal Cancer

Yifei Yang et al.

ACS MEDICINAL CHEMISTRY LETTERS (2020)

添加到收藏夹

Article Chemistry, Medicinal

Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer

Yan Zhang et al.

JOURNAL OF MEDICINAL CHEMISTRY (2019)

添加到收藏夹

Article Genetics & Heredity

BRD4 bimodal binding at promoters and drug-induced displacement at Pol II pause sites associates with I-BET sensitivity

P. Khoueiry et al.

EPIGENETICS & CHROMATIN (2019)

添加到收藏夹

Article Oncology

Clinical significance of serum PSA in breast cancer patients

Toru Hanamura et al.

BMC CANCER (2019)

添加到收藏夹

Review Oncology

NUT midline carcinoma: Current concepts and future perspectives of a novel tumour entity

Massimiliano Salati et al.

CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY (2019)

添加到收藏夹

Article Chemistry, Medicinal

Structure-Based Discovery and Optimization of Benzo[&ITd&IT]isoxazole Derivatives as Potent and Selective BET Inhibitors for Potential Treatment of Castration-Resistant Prostate Cancer (CRPC)

Maofeng Zhang et al.

JOURNAL OF MEDICINAL CHEMISTRY (2018)

添加到收藏夹

Review Cell Biology

Bromodomain-containing proteins in prostate cancer

Alfonso Urbanucci et al.

MOLECULAR AND CELLULAR ENDOCRINOLOGY (2018)

添加到收藏夹

Article Multidisciplinary Sciences

Spatially constrained tandem bromodomain inhibition bolsters sustained repression of BRD4 transcriptional activity for TNBC cell growth

Chunyan Ren et al.

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

添加到收藏夹

Article Multidisciplinary Sciences

SLAM-seq defines direct gene-regulatory functions of the BRD4-MYC axis

Matthias Muhar et al.

SCIENCE (2018)

添加到收藏夹

Article Cell Biology

AZD5153 Inhibits Prostate Cancer Cell Growth in Vitro and in Vivo

Gang Shen et al.

CELLULAR PHYSIOLOGY AND BIOCHEMISTRY (2018)

添加到收藏夹

Review Pharmacology & Pharmacy

BET inhibitors in metastatic prostate cancer: therapeutic implications and rational drug combinations

Mark C. Markowski et al.

EXPERT OPINION ON INVESTIGATIONAL DRUGS (2017)

添加到收藏夹

Article Biochemistry & Molecular Biology

Structural basis of PROTAC cooperative recognition for selective protein degradation

Morgan S. Gadd et al.

NATURE CHEMICAL BIOLOGY (2017)

添加到收藏夹

Review Cell Biology

Functions of bromodomain-containing proteins and their roles in homeostasis and cancer

Takao Fujisawa et al.

NATURE REVIEWS MOLECULAR CELL BIOLOGY (2017)

添加到收藏夹

Review Oncology

BET inhibitors: a novel epigenetic approach

D. B. Doroshow et al.

ANNALS OF ONCOLOGY (2017)

添加到收藏夹

Review Hematology

Update on rational targeted therapy in AML

Danielle Shafer et al.

BLOOD REVIEWS (2016)

添加到收藏夹

Review Biochemistry & Molecular Biology

The Bromodomain and Extra-Terminal Domain (BET) Family: Functional Anatomy of BET Paralogous Proteins

Yasushi Taniguchi

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2016)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation

Xiaoqian Xue et al.

JOURNAL OF MEDICINAL CHEMISTRY (2016)

添加到收藏夹

Article Chemistry, Medicinal

4-Acyl Pyrrole Derivatives Yield Novel Vectors for Designing Inhibitors of the Acetyl-Lysine Recognition Site of BRD4(1)

Martin Huegle et al.

JOURNAL OF MEDICINAL CHEMISTRY (2016)

添加到收藏夹

Article Chemistry, Medicinal

Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials

Brian K. Albrecht et al.

JOURNAL OF MEDICINAL CHEMISTRY (2016)

添加到收藏夹

Article Biochemistry & Molecular Biology

Potent and selective bivalent inhibitors of BET bromodomains

Michael J. Waring et al.

NATURE CHEMICAL BIOLOGY (2016)

添加到收藏夹

Article Biochemistry & Molecular Biology

Design and characterization of bivalent BET inhibitors

Minoru Tanaka et al.

NATURE CHEMICAL BIOLOGY (2016)

添加到收藏夹

Article Multidisciplinary Sciences

The BET inhibitor OTX015 reactivates latent HIV-1 through P-TEFb

Panpan Lu et al.

SCIENTIFIC REPORTS (2016)

添加到收藏夹

Article Biochemistry & Molecular Biology

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

Michael Zengerle et al.

ACS CHEMICAL BIOLOGY (2015)

添加到收藏夹

Article Biochemistry & Molecular Biology

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

Jing Lu et al.

CHEMISTRY & BIOLOGY (2015)

添加到收藏夹

Review Medicine, Research & Experimental

Targeting the adaptive molecular landscape of castration-resistant prostate cancer

Alexander W. Wyatt et al.

EMBO MOLECULAR MEDICINE (2015)

添加到收藏夹

Article Multidisciplinary Sciences

Phthalimide conjugation as a strategy for in vivo target protein degradation

Georg E. Winter et al.

SCIENCE (2015)

添加到收藏夹

Review Biotechnology & Applied Microbiology

Targeting bromodomains: epigenetic readers of lysine acetylation

Panagis Filippakopoulos et al.

NATURE REVIEWS DRUG DISCOVERY (2014)

添加到收藏夹

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)

添加到收藏夹

Article Biochemistry & Molecular Biology

BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc

Jake E. Delmore et al.

CELL (2011)

添加到收藏夹

Article Multidisciplinary Sciences

RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia

Johannes Zuber et al.

NATURE (2011)

添加到收藏夹

Article Multidisciplinary Sciences

Suppression of inflammation by a synthetic histone mimic

Edwige Nicodeme et al.

NATURE (2010)

添加到收藏夹

Article Multidisciplinary Sciences

Selective inhibition of BET bromodomains

Panagis Filippakopoulos et al.

NATURE (2010)

添加到收藏夹

© Peeref 2019-2024. All rights reserved.