4.7 Article

Discovery of BRD4-HDAC Dual Inhibitors with Improved Fungal Selectivity and Potent Synergistic Antifungal Activity against Fluconazole-Resistant Candida albicans

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

BET-HDAC Dual Inhibitors for Combinational Treatment of Breast Cancer and Concurrent Candidiasis

Yahui Huang et al.

Summary: Breast cancer is susceptible to Candida infections, and candidiasis has an enhancing effect on the progression and metastasis of tumor. Dual inhibitors targeting both BET and HDAC were designed for combinational treatment of breast cancer and resistant Candida albicans infections, showing improved antitumor efficacy and synergistic effect with fluconazole.

JOURNAL OF MEDICINAL CHEMISTRY (2023)

Article Microbiology

Modulation of Virulence-Associated Traits in Aspergillus fumigatus by BET Inhibitor JQ1

Anastasia Orekhova et al.

Summary: In this study, the impact of the BET inhibitor JQ1 on the extracellular proteins and virulence of A. fumigatus was evaluated. The results showed that JQ1 could significantly modulate the expression of extracellular proteins and attenuate the virulence of A. fumigatus. Furthermore, JQ1 was found to inhibit the expression of intracellular laccase Abr2 in A. fumigatus.

MICROORGANISMS (2022)

Article Pharmacology & Pharmacy

The Antifungal Pipeline: Fosmanogepix, Ibrexafungerp, Olorofim, Opelconazole, and Rezafungin

Martin Hoenigl et al.

Summary: The epidemiology of invasive fungal infections is changing due to increased usage of antifungal agents leading to resistance. Limited therapeutic options are further challenged by drug-drug interactions, toxicity, and administration constraints. Despite the lack of new antifungal drug classes in the past two decades, there are promising new classes in late-stage clinical development, offering hope for improved treatment options.
Article Chemistry, Medicinal

4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads

Linda Schaeker-Huebner et al.

Summary: Novel multitarget drugs showed stronger anti-leukemia activity by inducing apoptosis more effectively than combination therapies, suggesting an advantage of dual HDAC/BET inhibitors over two single targeted compounds.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Chemistry, Multidisciplinary

Potent Dual BET/HDAC Inhibitors for Efficient Treatment of Pancreatic Cancer

Shipeng He et al.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2020)

Review Microbiology

Drug resistance and tolerance in fungi

Judith Berman et al.

NATURE REVIEWS MICROBIOLOGY (2020)

Article Multidisciplinary Sciences

Structural basis for species-selective targeting of Hsp90 in a pathogenic fungus

Luke Whitesell et al.

NATURE COMMUNICATIONS (2019)

Article Chemistry, Medicinal

Discovery of simplified sampangine derivatives as novel fungal biofilm inhibitors

Na Liu et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2018)

Review Biotechnology & Applied Microbiology

Epigenetic Control of Oxidative Stresses by Histone Acetyltransferases in Candida albicans

Jueun Kim et al.

JOURNAL OF MICROBIOLOGY AND BIOTECHNOLOGY (2018)

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)

Review Biochemistry & Molecular Biology

Portrait of Candida Species Biofilm Regulatory Network Genes

Daniela Araujo et al.

TRENDS IN MICROBIOLOGY (2017)

Article Chemistry, Medicinal

Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors

Mingfeng Shao et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2017)

Article Biochemistry & Molecular Biology

Synthesis and evaluation of novel dual BRD4/HDAC inhibitors

Seika Amemiya et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2017)

Article Pharmacology & Pharmacy

Inhibition of BET bromodomains alleviates inflammation in human RPE cells

M. Hytti et al.

BIOCHEMICAL PHARMACOLOGY (2016)

Article Multidisciplinary Sciences

Inhibiting fungal multidrug resistance by disrupting an activator-Mediator interaction

Joy L. Nishikawa et al.

NATURE (2016)

Article Microbiology

Histone Deacetylases and Their Inhibition in Candida Species

Cecile Garnaud et al.

FRONTIERS IN MICROBIOLOGY (2016)

Review Microbiology

Candida albicans Biofilms and Human Disease

Clarissa J. Nobile et al.

ANNUAL REVIEW OF MICROBIOLOGY, VOL 69 (2015)

Article Infectious Diseases

The Rpd3/Hda1 family of histone deacetylases regulates azole resistance in Candida albicans

Xiaofang Li et al.

JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY (2015)

Review Microbiology

Histone deacetylase-mediated morphological transition in Candida albicans

Jueun Kim et al.

JOURNAL OF MICROBIOLOGY (2015)

Review Biotechnology & Applied Microbiology

Targeting bromodomains: epigenetic readers of lysine acetylation

Panagis Filippakopoulos et al.

NATURE REVIEWS DRUG DISCOVERY (2014)

Review Pharmacology & Pharmacy

Invasive candidiasis: update on current pharmacotherapy options and future perspectives

Athanasios Tragiannidis et al.

EXPERT OPINION ON PHARMACOTHERAPY (2013)

Article Cardiac & Cardiovascular Systems

BET acetyl-lysine binding proteins control pathological cardiac hypertrophy

Jessica I. Spiltoir et al.

JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY (2013)

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)

Review Oncology

BET domain co-regulators in obesity, inflammation and cancer

Anna C. Belkina et al.

NATURE REVIEWS CANCER (2012)

Article Multidisciplinary Sciences

Selective inhibition of BET bromodomains

Panagis Filippakopoulos et al.

NATURE (2010)

Article Medicine, General & Internal

International Study of the Prevalence and Outcomes of Infection in Intensive Care Units

Jean-Louis Vincent et al.

JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION (2009)

Article Biotechnology & Applied Microbiology

Histone deacetylase inhibitors may reduce pathogenicity and virulence in Candida albicans

Giovanna Simonetti et al.

FEMS YEAST RESEARCH (2007)

Article Biochemistry & Molecular Biology

Histone deacetylases in fungi: novel members, new facts

P Trojer et al.

NUCLEIC ACIDS RESEARCH (2003)

Review Biochemistry & Molecular Biology

Bromodomain: an acetyl-lysine binding domain

L Zeng et al.

FEBS LETTERS (2002)