4.8 Article

Aza-SAHA Derivatives Are Selective Histone Deacetylase 10 Chemical Probes That Inhibit Polyamine Deacetylation and Phenocopy HDAC10 Knockout br

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 Biochemistry & Molecular Biology

First Fluorescent Acetylspermidine Deacetylation Assay for HDAC10 Identifies Selective Inhibitors with Cellular Target Engagement

Daniel Herp et al.

Summary: Histone deacetylases (HDACs) are important epigenetic regulators involved in many diseases, especially cancer. Five HDAC inhibitors have been approved for anticancer therapy and many are in clinical trials. HDAC10, one of the 11 zinc-dependent HDACs, has received little attention in drug discovery campaigns despite its involvement in the pathogenesis of neuroblastoma. This is partly due to a lack of robust enzymatic conversion assays. Recent research has shown that HDAC10 has strong preferences for deacetylation of oligoamine substrates, making it a polyamine deacetylase (PDAC).

CHEMBIOCHEM (2022)

Article Chemistry, Medicinal

Identification of histone deacetylase 10 (HDAC10) inhibitors that modulate autophagy in transformed cells

Patrik Zeyen et al.

Summary: In this study, piperidine-4-acrylhydroxamates were synthesized as potent and highly selective inhibitors of HDAC10. By mimicking the interaction of HDAC10's substrate, the acidic gatekeeper residue Glu274 was successfully targeted. The binding modes of the inhibitors were confirmed through experiments and analysis, and it was demonstrated that 10c and 13b are highly specific HDAC10 inhibitors.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

Article Biochemistry & Molecular Biology

Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target

Severin Lechner et al.

Summary: This study used a quantitative chemical proteomics assay to investigate the target landscape of 53 drugs that target HDAC. The results questioned the selectivity of some widely-used molecules and revealed the influence of HDAC complex composition on drug potency. Additionally, the study identified MBLAC2 as a frequent off-target of hydroxamate drugs and suggested it as a potential target for drug discovery due to its involvement in extracellular vesicle accumulation.

NATURE CHEMICAL BIOLOGY (2022)

Article Biochemistry & Molecular Biology

X-ray Crystallographic Snapshots of Substrate Binding in the Active Site of Histone Deacetylase 10

Corey J. Herbst-Gervasoni et al.

Summary: Histone deacetylase 10 (HDAC10) is a zinc-dependent polyamine deacetylase with potential as a target for cancer chemotherapy. Detailed structural information on the enzyme's active site is crucial for the design of selective inhibitors.

BIOCHEMISTRY (2021)

Review Chemistry, Medicinal

Strategies To Design Selective Histone Deacetylase Inhibitors

Jelena Melesina et al.

Summary: This review classifies successful drug-design strategies used in the development of histone deacetylase (HDAC) inhibitors, particularly focusing on selective HDAC inhibitors and their structure-activity relationships. The paper discusses how optimization of various structural features, such as the zinc binding group, linker, and cap group, can influence inhibitor selectivity. Additionally, it highlights the importance of targeting class-specific sub-pockets for improved inhibitor design.

CHEMMEDCHEM (2021)

Article Biochemistry & Molecular Biology

Chemo-proteomics exploration of HDAC degradability by small molecule degraders

Yuan Xiong et al.

Summary: The study synthesized a pan-HDAC degrader library for exploring acute degradation of chromatin-modifying enzymes, identifying leads for targeting HDACs 1-8 and 10. Cell line-driven target specificity and collateral loss of HDAC-containing repressive complexes were discovered upon HDAC degradation, potentially offering a new mechanism for controlling chromatin structure.

CELL CHEMICAL BIOLOGY (2021)

Article Biochemistry & Molecular Biology

Histone deacetylase 10 knockout activates chaperone-mediated autophagy and accelerates the decomposition of its substrate

Hitomi Obayashi et al.

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS (2020)

Article Multidisciplinary Sciences

HDAC10 deletion promotes Foxp3+ T-regulatory cell function

Satinder Dahiya et al.

SCIENTIFIC REPORTS (2020)

Article Chemistry, Medicinal

Design and Synthesis of Dihydroxamic Acids as HDAC6/8/10 Inhibitors

Michael Morgen et al.

CHEMMEDCHEM (2020)

Article Biochemistry & Molecular Biology

Structural Basis for the Selective Inhibition of HDAC10, the Cytosolic Polyamine Deacetylase

Corey J. Herbst-Gervasoni et al.

ACS CHEMICAL BIOLOGY (2020)

Article Chemistry, Medicinal

Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight

Terence C. S. Ho et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

Article Chemistry, Medicinal

Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated

Magalie Geraldy et al.

JOURNAL OF MEDICINAL CHEMISTRY (2019)

Article Multidisciplinary Sciences

Dual role of HDAC10 in lysosomal exocytosis and DNA repair promotes neuroblastoma chemoresistance

Johannes Ridinger et al.

SCIENTIFIC REPORTS (2018)

Review Oncology

Polyamine metabolism and cancer: treatments, challenges and opportunities

Robert A. Casero et al.

NATURE REVIEWS CANCER (2018)

Article Oncology

HDAC10 as a potential therapeutic target in ovarian cancer

Muhtadi M. Islam et al.

GYNECOLOGIC ONCOLOGY (2017)

Article Multidisciplinary Sciences

Histone deacetylase 10 structure and molecular function as a polyamine deacetylase

Yang Hai et al.

NATURE COMMUNICATIONS (2017)

Article Biochemistry & Molecular Biology

Histone Deacetylase 10 Regulates DNA Mismatch Repair and May Involve the Deacetylation of MutS Homolog 2

Rangasudhagar Radhakrishnan et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2015)

Review Biochemistry & Molecular Biology

Remaining Mysteries of Molecular Biology: The Role of Polyamines in the Cell

Leonor Miller-Fleming et al.

JOURNAL OF MOLECULAR BIOLOGY (2015)

Article Multidisciplinary Sciences

Target engagement and drug residence time can be observed in living cells with BRET

Matthew B. Robers et al.

NATURE COMMUNICATIONS (2015)

Article Biotechnology & Applied Microbiology

The role of ligand efficiency metrics in drug discovery

Andrew L. Hopkins et al.

NATURE REVIEWS DRUG DISCOVERY (2014)

Review Biotechnology & Applied Microbiology

Histone deacetylases and their inhibitors in cancer, neurological diseases and immune disorders

Katrina J. Falkenberg et al.

NATURE REVIEWS DRUG DISCOVERY (2014)

Article Biochemistry & Molecular Biology

Synthesis and evaluation of N8-acetylspermidine analogues as inhibitors of bacterial acetylpolyamine amidohydrolase

Christophe Decroos et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2013)

Article Biochemistry & Molecular Biology

Target validation using chemical probes

Mark E. Bunnage et al.

NATURE CHEMICAL BIOLOGY (2013)

Article Multidisciplinary Sciences

Histone deacetylase 10 promotes autophagy-mediated cell survival

Ina Oehme et al.

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

Article Biochemistry & Molecular Biology

Histone Deacetylases 9 and 10 Are Required for Homologous Recombination

Shweta Kotian et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2011)

Article Biochemical Research Methods

A Substrate-Independent TR-FRET Histone Deacetylase Inhibitor Assay

Bryan D. Marks et al.

JOURNAL OF BIOMOLECULAR SCREENING (2011)

Article Chemistry, Multidisciplinary

Rational Design and Simple Chemistry Yield a Superior, Neuroprotective HDAC6 Inhibitor, Tubastatin A

Kyle V. Butler et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2010)

Article Biochemistry & Molecular Biology

Chemical phylogenetics of histone deacetylases

James E. Bradner et al.

NATURE CHEMICAL BIOLOGY (2010)

Article Multidisciplinary Sciences

HDAC6 is a microtubule-associated deacetylase

C Hubbert et al.

NATURE (2002)

Article Biochemistry & Molecular Biology

Isolation and characterization of a novel class II histone deacetylase, HDAC10

DD Fischer et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2002)

Article Biochemistry & Molecular Biology

Molecular cloning and characterization of a novel histone deacetylase HDAC10

AR Guardiola et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2002)

Article Biochemistry & Molecular Biology

Isolation and characterization of mammalian HDAC10, a novel histone deacetylase

HY Kao et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2002)

Article Biochemistry & Molecular Biology

Identification of HDAC10, a novel class II human histone deacetylase containing a leucine-rich domain

JJ Tong et al.

NUCLEIC ACIDS RESEARCH (2002)