☆ 4.7 Article

Medicinal chemistry updates of novel HDACs inhibitors (2020 to present)

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

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

Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis

Zhuang Li et al.

Summary: A series of novel carboline fungal HDAC inhibitors were designed and synthesized to combat antifungal drug resistance, with compound D12 showing potent synergistic effects with fluconazole against resistant Candida albicans infection. D12 reduced the virulence of C. albicans by blocking morphological mutual transformation and inhibiting biofilm formation, and reversed drug resistance by downregulating the expression of the azole target gene ERG11 and efflux gene CDR1.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Studying Histone Deacetylase Inhibition and Apoptosis Induction of Psammaplin A Monomers with Modified Thiol Group

Yu Bao et al.

Summary: Psammaplin A (PsA) is a compound with histone deacetylase (HDAC) inhibition capabilities that acts through the reduced monomer PsA-SH. PsA-SH and 10b induce apoptosis in human leukemia cells and inhibit the growth of several solid tumor cell lines.

ACS MEDICINAL CHEMISTRY LETTERS (2021)

添加到收藏夹

Article Biochemistry & Molecular Biology

Design, synthesis and antitumor activity evaluation of novel HDAC inhibitors with tetrahydrobenzothiazole as the skeleton

Simin Sun et al.

Summary: The study focused on the design and synthesis of a series of HDAC inhibitors, identifying compound 6h as a promising candidate with potent antitumor effects. Compound 6h exhibited high cytotoxicity against various cancer cell lines, arrested cell cycle, induced apoptosis, and demonstrated anti-migration and anti-angiogenesis activities. Additionally, compound 6h increased the expression of acetylated alpha-tubulin and acetylated histone H3, fitting well into the active sites of HDAC2 and 6, suggesting its potential for further preclinical studies.

BIOORGANIC CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Investigation of the in vitro and in vivo efficacy of peptoid-based HDAC inhibitors with dual-stage antiplasmodial activity

Marcel K. W. Mackwitz et al.

Summary: This study reports on a new peptoid-based HDAC inhibitor with dual-stage antiplasmodial activity, showing potential activity against malaria parasites and selectivity for human cells. These data provide a foundation for future improvements to these dual-stage inhibitors as potential drug leads for malaria.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors

Leandro A. Alves Avelar et al.

Summary: Targeting epigenetic dysregulation as a therapeutic strategy in cancer treatment, especially combining histone deacetylase inhibitors with established anti-cancer drugs, has shown promising results in preclinical and clinical studies. Structural optimization of alkoxyamide-based inhibitors has led to improved analogs that exhibit potent efficacy in cisplatin-resistant head and neck carcinoma cells and bortezomib-resistant leukemia cells. The most valuable alkoxyamide-based HDACi has demonstrated strong ex vivo anticancer efficacy against therapy-resistant leukemic entities.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Pragmatic recruitment of memantine as the capping group for the design of HDAC inhibitors: A preliminary attempt to unravel the enigma of glioblastoma

Kunal Nepali et al.

Summary: The team designed and synthesized a series of hydroxamic acid compounds with high blood-brain barrier permeability and preferential HDAC6 inhibitory activity, with hydroxamic acid 16 showing significant anti-proliferative effects against GBM cells and prolonging the survival of mice in in vivo experiments.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Novel quinolone-based potent and selective HDAC6 inhibitors: Synthesis, molecular modeling studies and biological investigation

Nicola Relitti et al.

Summary: This study describes the synthesis of potent and selective quinolone-based histone deacetylase 6 (HDAC6) inhibitors, which showed good to excellent anticancer activity in cellular studies by inducing tumor cell death through modulation of protein deacetylation.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Review Pharmacology & Pharmacy

An update on the emerging approaches for histone deacetylase (HDAC) inhibitor drug discovery and future perspectives

Ma Su et al.

Summary: HDACs catalyze the removal of acetyl groups from protein substrates, with different HDACs having distinct biological functions and genomic recruitment. HDAC inhibitors have shown promise in treating various diseases, but there is still room for improvement in terms of isoform identification, selectivity optimization, and discovering effective scaffolds and pharmacophores.

EXPERT OPINION ON DRUG DISCOVERY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Unique Molecular Interaction with the Histone Deacetylase 6 Catalytic Tunnel: Crystallographic and Biological Characterization of a Model Chemotype

Olasunkanmi O. Olaoye et al.

Summary: In this study, a structure-activity relationship study led to the discovery of TO-317, a potent and selective HDAC6 inhibitor that binds the catalytic domain with high affinity, exhibiting a novel binding mechanism involving a direct hydrogen bond with Zn2+ coordinating residue His614. This newly identified structural motif targeting the second-sphere His614 interaction provides potential pharmacophores for developing high-affinity, HDAC6-selective inhibitors.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of Novel Plasmodium falciparum HDAC1 Inhibitors with Dual-Stage Antimalarial Potency and Improved Safety Based on the Clinical Anticancer Drug Candidate Quisinostat

Ruoxi Li et al.

Summary: In this study, a total of 31 novel spirocyclic hydroxamic acid derivatives were synthesized based on the structure of the clinical anticancer drug candidate quisinostat, with compound 11 displaying broad potency against various multidrug-resistant malarial parasites both in vitro and in vivo. The compound showed specific efficacy against schizonts, acceptable metabolic stability, and pharmacokinetic properties, making it a promising PfHDAC1 inhibitor for malaria treatment and research.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

HDAC7 Inhibition by Phenacetyl and Phenylbenzoyl Hydroxamates

Jeffrey Y. W. Mak et al.

Summary: The study focuses on developing new inhibitors for the zinc-containing histone deacetylase enzyme HDAC7, which show increased selectivity and potency. The addition of phthalimide capping groups improves drug performance by decreasing rotational freedom and providing hydrogen bond acceptor carbonyl/sulfonamide oxygens.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Synthesis of HDAC Inhibitor Libraries via Microscale Workflow

Kevin D. Dykstra et al.

Summary: An integrated workflow has been established for the synthesis, purification, and biological testing of compound libraries on a microgram scale, utilizing mass directed preparative HPLC with CAD. This new approach delivered libraries of HDAC inhibitors with high fidelity biological testing, greatly reducing material requirements and allowing for high-throughput experimentation.

ACS MEDICINAL CHEMISTRY LETTERS (2021)

添加到收藏夹

Article Chemistry, Medicinal

Evaluation of 5-(Trifluoromethyl)-1,2,4-oxadiazole-Based Class Ila HDAC Inhibitors for Huntington's Disease

Andrew J. Stott et al.

Summary: Through an iterative structure-activity relationship approach, a CNS-penetrant compound TFMO suitable for probing HDAC inhibition was identified. The study demonstrated a good correlation between in vivo pharmacodynamic response and in vitro cellular activity of the compound. Additionally, the compound exhibited >100-fold selectivity over class I/IIb HDACs, enabling accurate measurement of its effects in vivo.

ACS MEDICINAL CHEMISTRY LETTERS (2021)

添加到收藏夹

Article Chemistry, Medicinal

Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction

Douglas C. Beshore et al.

Summary: A novel series of histone deacetylase (HDAC) inhibitors lacking a zinc-binding moiety has been developed, showing selectivity for certain HDAC isozymes and no interaction with the catalytic zinc. These compounds are promising for further optimization due to their nonmutagenic and off-target profiles, and exhibit efficacy comparable to marketed HDAC inhibitors belinostat and vorinostat. These results suggest a need to revise the long-standing pharmacophore model of HDAC inhibitors and present a distinct class of HDAC inhibitors.

ACS MEDICINAL CHEMISTRY LETTERS (2021)

添加到收藏夹

Article Biochemistry & Molecular Biology

Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors

Mauricio Temotheo Tavares et al.

Summary: This study presented a series of urea-based cinnamyl hydroxamate derivatives as potential anticancer histone deacetylase inhibitors, showing significant antiproliferative effects against both solid and hematological human tumor cell lines. Structure-activity relationship (SAR) studies were conducted to determine the influence of linker on biological profile of the compounds, and the results demonstrated potent HDAC6 inhibitory activity with selectivity against acute lymphoblastic leukemia cells.

BIOORGANIC & MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of Ethyl Ketone-Based Highly Selective HDACs 1, 2, 3 Inhibitors for HIV Latency Reactivation with Minimum Cellular Potency Serum Shift and Reduced hERG Activity

Wensheng Yu et al.

Summary: The discovery of histone deacetylase (HDACs) 1, 2, and 3 inhibitors with ethyl ketone as the zinc-binding group is described. These inhibitors exhibit good enzymatic and cellular activity, high selectivity against hERG, minimized serum shift in cellular potency, and improved selectivity over HDACs 6 and 8. They contain a variety of substituted heterocycles on the imidazole or oxazole scaffold, with compounds 31 and 48 standing out for their potency, selectivity, reduced hERG activity, optimized serum shift, and good PK profiles in rats and dogs.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model

Sida Shen et al.

Summary: The study introduces a new HDAC6 inhibitor, SW-101, which exhibits excellent potency, selectivity, metabolic stability, and druglike properties compared to SW-100. Treatment with SW-101 is shown to improve neuropathic symptoms in a CMT2A mouse model, suggesting its potential as a disease-modifying HDAC6 inhibitor.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of macrocyclic HDACs 1, 2, and 3 selective inhibitors for HIV latency reactivation

Wensheng Yu et al.

Summary: A series of unique macrocyclic HDACs 1, 2, and 3 selective inhibitors were identified, showing good enzymatic activity and high selectivity over HDACs 6 and 8. Compounds 25 and 26 stood out as leads with low double-digit nM EC(50)s in the 2C4 cell-based HIV latency reactivation assay, but the PK profiles of these macrocyclic HDAC inhibitors still needed improvement.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2021)

添加到收藏夹

Article Biochemistry & Molecular Biology

Synthesis, biological evaluation, and molecular docking analysis of novel linker-less benzamide based potent and selective HDAC3 inhibitors

Ganesh Routholla et al.

Summary: The newly designed and synthesized novel HDAC inhibitors show high selectivity for HDAC3 and promising anticancer activity, with potent antiproliferative effects on various cancer cell lines and low cytotoxicity to normal cells. These compounds may serve as potential anticancer therapeutics with HDAC3 inhibitory activity.

BIOORGANIC CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity

Xin-Hui Zhang et al.

Summary: In this study, a series of 1,3-diaryl-1,2,4-triazole-capped HDAC6 inhibitors were designed, synthesized and verified, with compound 9r showing the best inhibitory activity with potential for gastric cancer therapy. The high selectivity and affinity of 9r to HDAC6, along with its ability to upregulate acetylated alpha-tubulin levels and exhibit antiproliferative and anti-metastatic effects without significant toxicity, suggest that 9r could serve as a lead compound for the development of novel therapeutic agents for gastric cancer.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Synthesis and biological evaluation of phenothiazine derivative-containing hydroxamic acids as potent class II histone deacetylase inhibitors

Kai-Cheng Hsu et al.

Summary: The study showed that modifying the acridine ring with phenothiazine derivatives can effectively inhibit the activity of class II HDACs, with compound 4f exhibiting the strongest inhibitory effect and promoting neurite outgrowth.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Design, synthesis and biological evaluation of brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction

Zheng Guo et al.

Summary: HDAC6 has become a promising therapeutic target for central nervous system diseases due to its complex protein structure and biological functions, but its inhibitors face limitations in brain penetration. A series of selective HDAC6 inhibitors were designed with compound 5 showing strong selectivity and good blood-brain barrier penetration, providing therapeutic potential for ischemic stroke treatment.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Development of HDAC Inhibitors Exhibiting Therapeutic Potential in T-Cell Prolymphocytic Leukemia

Krimo Toutah et al.

Summary: Epigenetic targeting, especially with HDAC inhibitors like KT-531, has shown promising efficacy in treating hematological cancers. In the case of T-cell prolymphocytic leukemia (T-PLL), overexpression of HDAC6 has been identified as a target for therapy, with KT-531 demonstrating strong inhibitory potency and safety in preclinical studies. Combination studies with approved cancer drugs have shown synergistic effects, indicating the potential for durable remission in T-PLL patients.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

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)

添加到收藏夹

Article Biochemistry & Molecular Biology

Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells

Yodita Asfaha et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment

Navdeep Kaur et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Biochemistry & Molecular Biology

Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity

Bocheng Wu et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Biochemistry & Molecular Biology

Synthesis and biological evaluation of 6-phenylpurine linked hydroxamates as novel histone deacetylase inhibitors

Dizhong Chen et al.

BIOORGANIC CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Novel 2, 5-diketopiperazine derivatives as potent selective histone deacetylase 6 inhibitors: Rational design, synthesis and antiproliferative activity

Xin Chen et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Review Chemistry, Medicinal

Histone deacetylase (HDAC) inhibitors in cancer: a patent review (2017-present)

Chunlong Zhao et al.

EXPERT OPINION ON THERAPEUTIC PATENTS (2020)

添加到收藏夹

Article Chemistry, Medicinal

Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors

Shu-Wei Zhang et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Review Oncology

Novel Selective Histone Deacetylase 6 (HDAC6) Inhibitors: A Patent Review (2016-2019)

Xingrui He et al.

RECENT PATENTS ON ANTI-CANCER DRUG DISCOVERY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia

Andrew E. Shouksmith et al.

ACS MEDICINAL CHEMISTRY LETTERS (2020)

添加到收藏夹

Article Chemistry, Medicinal

Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease

Hui-Ju Tseng et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening

Jian Liu et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Achiral Derivatives of Hydroxamate AR-42 Potently Inhibit Class I HDAC Enzymes and Cancer Cell Proliferation

Jiahui Tng et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity

Xiaoyang Li et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Development of Selective Histone Deacetylase 6 (HDAC6) Degraders Recruiting Von Hippel-Lindau (VHL) E3 Ubiquitin Ligase

Ka Yang et al.

ACS MEDICINAL CHEMISTRY LETTERS (2020)

添加到收藏夹

Article Chemistry, Multidisciplinary

Hydroxamic Acids Immobilized on Resins (HAIRs): Synthesis of Dual-Targeting HDAC Inhibitors and HDAC Degraders (PROTACs)

Laura Sinatra et al.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2020)

添加到收藏夹

Article Biochemistry & Molecular Biology

Exploration of certain 1,3-oxazole-and 1,3-thiazole-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents

Duong Tien Anh et al.

BIOORGANIC CHEMISTRY (2020)

添加到收藏夹

Article Biochemistry & Molecular Biology

Design, synthesis and biological evaluation of coumarin-based N-hydroxycinnamamide derivatives as novel histone deacetylase inhibitors with anticancer activities

Jiaoli Ding et al.

BIOORGANIC CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Purine/purine isoster based scaffolds as new derivatives of benzamide class of HDAC inhibitors

Kunal Nepali et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer

Mingming Wei et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight

Terence C. S. Ho et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Characterization of Conformationally Constrained Benzanilide Scaffolds for Potent and Selective HDAC8 Targeting

Muhammad Murtaza Hassan et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Development of a selective HDAC inhibitor aimed at reactivating the HIV latent reservoir

Dane J. Clausen et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2020)

添加到收藏夹

Article Chemistry, Medicinal

PTG-0861: A novel HDAC6-selective inhibitor as a therapeutic strategy in acute myeloid leukaemia

Justyna M. Gawel et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Selective Class I HDAC Inhibitors Based on Aryl Ketone Zinc Binding Induce HIV-1 Protein for Clearance

Jian Liu et al.

ACS MEDICINAL CHEMISTRY LETTERS (2020)

添加到收藏夹

Article Chemistry, Medicinal

Multicomponent Synthesis, Binding Mode, and Structure-Activity Relationship of Selective Histone Deacetylase 6 (HDAC6) Inhibitors with Bifurcated Capping Groups

Nina Ressing et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Rational Design of Suprastat: A Novel Selective Histone Deacetylase 6 Inhibitor with the Ability to Potentiate Immunotherapy in Melanoma Models

Satish Noonepalle et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Spiroindoline-Capped Selective HDAC6 Inhibitors: Design, Synthesis, Structural Analysis, and Biological Evaluation

A. Prasanth Saraswati et al.

ACS MEDICINAL CHEMISTRY LETTERS (2020)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of Highly Selective and Potent HDAC3 Inhibitors Based on a 2-Substituted Benzamide Zinc Binding Group

Jian Liu et al.

ACS MEDICINAL CHEMISTRY LETTERS (2020)

添加到收藏夹

Article Pharmacology & Pharmacy

Y Dual inhibitors of histone deacetylases and other cancer-related targets: A pharmacological perspective

Yuan Gao et al.

BIOCHEMICAL PHARMACOLOGY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Design, synthesis and evaluation of novel indirubin-based N- hydroxybenzamides, N-hydroxypropenamides and N-hydroxyheptanamides as histone deacetylase inhibitors and antitumor agents

Duong Tien Anh et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2020)

添加到收藏夹

Article Chemistry, Medicinal

Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer

Dahong Yao et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Multidisciplinary

Discovery of histone deacetylase 3 (HDAC3)-specific PROTACs

Yufeng Xiao et al.

CHEMICAL COMMUNICATIONS (2020)

添加到收藏夹

Article Chemistry, Multidisciplinary

PROTAC-mediated degradation of class I histone deacetylase enzymes in corepressor complexes

Joshua P. Smalley et al.

CHEMICAL COMMUNICATIONS (2020)

添加到收藏夹

Review Biochemistry & Molecular Biology

Targeting epigenetic modifications in cancer therapy: erasing the roadmap to cancer

Helai P. Mohammad et al.

NATURE MEDICINE (2019)

添加到收藏夹

Article Chemistry, Medicinal

Development of Multifunctional Histone Deacetylase 6 Degraders with Potent Antimyeloma Activity

Hao Wu et al.

JOURNAL OF MEDICINAL CHEMISTRY (2019)

添加到收藏夹

Review Biotechnology & Applied Microbiology

Bromodomains: a new target class for drug development

Andrea G. Cochran et al.

NATURE REVIEWS DRUG DISCOVERY (2019)

添加到收藏夹

Article Chemistry, Medicinal

Synthesis and structure activity relationship of 1, 3-benzo-thiazine-2-thiones as selective HDAC8 inhibitors

Benjamin Wolff et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)

添加到收藏夹

Review Oncology

Histone deacetylase 6 in cancer

Ting Li et al.

JOURNAL OF HEMATOLOGY & ONCOLOGY (2018)

添加到收藏夹

Article Biochemistry & Molecular Biology

Beyond histone acetylation-writing and erasing histone acylations

Shuai Zhao et al.

CURRENT OPINION IN STRUCTURAL BIOLOGY (2018)

添加到收藏夹

Article Biotechnology & Applied Microbiology

Dynamics and functional interplay of histone lysine butyrylation, crotonylation, and acetylation in rice under starvation and submergence

Yue Lu et al.

GENOME BIOLOGY (2018)

添加到收藏夹

Review Chemistry, Medicinal

The Search for Potent, Small-Molecule HDACIs in Cancer Treatment: A Decade After Vorinostat

Chiara Zagni et al.

MEDICINAL RESEARCH REVIEWS (2017)

添加到收藏夹

Review Biotechnology & Applied Microbiology

Chidamide in the treatment of peripheral T-cell lymphoma

Thomas S. Chan et al.

ONCOTARGETS AND THERAPY (2017)

添加到收藏夹

Article Multidisciplinary Sciences

Histone deacetylase 10 structure and molecular function as a polyamine deacetylase

Yang Hai et al.

NATURE COMMUNICATIONS (2017)

添加到收藏夹

Editorial Material Chemistry, Medicinal

Why Hydroxamates May Not Be the Best Histone Deacetylase InhibitorsWhat Some May Have Forgotten or Would Rather Forget?

Sida Shen et al.

CHEMMEDCHEM (2016)

添加到收藏夹

Article Pharmacology & Pharmacy

HDAC 3-selective inhibitor RGFP966 demonstrates anti-inflammatory properties in RAW 264.7 macrophages and mouse precision-cut lung slices by attenuating NF-κB p65 transcriptional activity

Niek G. J. Leus et al.

BIOCHEMICAL PHARMACOLOGY (2016)

添加到收藏夹

Article Biochemistry & Molecular Biology

Identification of Histone Deacetylase Inhibitors with Benzoylhydrazide Scaffold that Selectively Inhibit Class I Histone Deacetylases

Yunfei Wang et al.

CHEMISTRY & BIOLOGY (2015)

添加到收藏夹

Review Genetics & Heredity

The role dietary of bioactive compounds on the regulation of histone acetylases and deacetylases: A review

F. Vahid et al.

GENE (2015)

添加到收藏夹

Article Chemistry, Organic

Investigations of possible prodrug structures for 2-(2-mercaptophenyl) tetrahydropyrimidines: reductive conversion from anti-HIV agents with pyrimidobenzothiazine and isothiazolopyrimidine scaffolds

Shiho Okazaki et al.

ORGANIC & BIOMOLECULAR CHEMISTRY (2015)

添加到收藏夹

Review Cell Biology

HDAC Family Members Intertwined in the Regulation of Autophagy: A Druggable Vulnerability in Aggressive Tumor Entities

Emily Koeneke et al.

CELLS (2015)

添加到收藏夹

Article Biochemical Research Methods

Systematic identification of Class I HDAC substrates

Tingting Li et al.

BRIEFINGS IN BIOINFORMATICS (2014)

添加到收藏夹

Article Chemistry, Medicinal

Structure and Ligand-Based Design of mTOR and PI3-Kinase Inhibitors Leading to the Clinical Candidates VS-5584 (SB2343) and SB2602

Anders Poulsen et al.

JOURNAL OF CHEMICAL INFORMATION AND MODELING (2014)

添加到收藏夹

Article Multidisciplinary Sciences

Structure of the DDBI-CRBN E3 ubiquitin ligase in complex with thalidomide

Eric S. Fischer et al.

NATURE (2014)

添加到收藏夹

Article Chemistry, Medicinal

Potent and Orally Efficacious Bisthiazole-Based Histone Deacetylase Inhibitors

Fei Chen et al.

ACS MEDICINAL CHEMISTRY LETTERS (2014)

添加到收藏夹

Article Biochemistry & Molecular Biology

The physiological roles of histone deacetylase (HDAC) 1 and 2: complex co-stars with multiple leading parts

Richard D. W. Kelly et al.

BIOCHEMICAL SOCIETY TRANSACTIONS (2013)

添加到收藏夹

Article Cell Biology

Hopx and Hdac2 Interact to Modulate Gata4 Acetylation and Embryonic Cardiac Myocyte Proliferation

Chinmay M. Trivedi et al.

DEVELOPMENTAL CELL (2010)

添加到收藏夹

Article Biochemistry & Molecular Biology

Enhanced deacetylation of p53 by the anti-apoptotic protein HSCO in association with histone deacetylase 1

Hisako Higashitsuji et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2007)

添加到收藏夹

Article Neurosciences

Intracellular trafficking of histone deacetylase 4 regulates neuronal cell death

TA Bolger et al.

JOURNAL OF NEUROSCIENCE (2005)

添加到收藏夹

Article Biochemistry & Molecular Biology

HDAC6 regulates Hsp90 acetylation and chaperone-dependent activation of glucocorticoid receptor

JJ Kovacs et al.

MOLECULAR CELL (2005)

添加到收藏夹

Article Biochemistry & Molecular Biology

Histone deacetylase HDAC8 associates with smooth muscle α-actin and is essential for smooth muscle cell contractility

D Waltregny et al.

FASEB JOURNAL (2005)

添加到收藏夹

Article Biochemistry & Molecular Biology

Histone deacetylases 5 and 9 govern responsiveness of the heart to a subset of stress signals and play redundant roles in heart development

SR Chang et al.

MOLECULAR AND CELLULAR BIOLOGY (2004)

添加到收藏夹

Article Pathology

Expression of histone deacetylase 8, a class I histone deacetylase, is restricted to cells showing smooth muscle differentiation in normal human tissues

D Waltregny et al.

AMERICAN JOURNAL OF PATHOLOGY (2004)

添加到收藏夹

Article Immunology

HDAC7, a thymus-specific class II histone deacetylase, regulates Nur77 transcription and TCR-mediated apoptosis

F Dequiedt et al.

IMMUNITY (2003)

添加到收藏夹

Review Biochemistry & Molecular Biology

Histone deacetylases (HDACs): characterization of the classical HDAC family

AJM De Ruijter et al.

BIOCHEMICAL JOURNAL (2003)

添加到收藏夹

Article Biochemistry & Molecular Biology

HDAC-6 interacts with and deacetylates tubulin and microtubules in vivo

Y Zhang et al.

EMBO JOURNAL (2003)

添加到收藏夹

Article Biochemistry & Molecular Biology

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

DD Fischer et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2002)

添加到收藏夹

Article Biochemistry & Molecular Biology

Molecular cloning and characterization of a novel histone deacetylase HDAC10

AR Guardiola et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2002)

添加到收藏夹

Article Biochemistry & Molecular Biology

Isolation and characterization of mammalian HDAC10, a novel histone deacetylase

HY Kao et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2002)

添加到收藏夹

Article Multidisciplinary Sciences

Genomewide studies of histone deacetylase function in yeast

BE Bernstein et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2000)

添加到收藏夹

Article Biochemistry & Molecular Biology

Regulation of E2F1 activity by acetylation

MA Martínez-Balbás et al.

EMBO JOURNAL (2000)

添加到收藏夹

© Peeref 2019-2024. All rights reserved.