Design and Synthesis of Dihydroxamic Acids as HDAC6/8/10 Inhibitors
Sign Up to like & getrecommendations! Published in 2020 at "Chemmedchem"
DOI: 10.1002/cmdc.202000149
Abstract: We report the synthesis and evaluation of a class of selective multitarget agents for the inhibition of HDAC6, HDAC8, and HDAC10. The concept for this study grew out of a structural analysis of the two… read more here.
Keywords: design synthesis; hdac6 inhibitors; dihydroxamic acids; synthesis dihydroxamic ... See more keywords
Discovery of specific HDAC6 inhibitor with anti-metastatic effects in pancreatic cancer cells through virtual screening and biological evaluation.
Sign Up to like & getrecommendations! Published in 2020 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2020.103679
Abstract: Histone deacetylase 6 (HDAC6) has been demonstrated to play a major role in cell motility and aggresome formation, and HDAC6 inhibition is therefore considered as a promising epigenetic strategy for cancer treatment. At present, only… read more here.
Keywords: virtual screening; hdac6 inhibitors; cefoperazone sodium; cancer ... See more keywords
Novel pyrrolo[2,1-c][1,4]benzodiazepine-3,11-dione (PBD) derivatives as selective HDAC6 inhibitors to suppress tumor metastasis and invasion in vitro and in vivo.
Sign Up to like & getrecommendations! Published in 2021 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2021.105081
Abstract: Selective inhibition of histone deacetylase 6 (HDAC6) has been emerged as a promising approach to cancer treatment. As a pivotal strategy for drug discovery,molecular hybridization was introduced in this study and a series of pyrrolo[2,1-c][1,4]… read more here.
Keywords: hdac6 inhibitors; vitro vivo; metastasis; selective hdac6 ... See more keywords
Structure-Based Drug Designing Recommends HDAC6 Inhibitors To Attenuate Microtubule-Associated Tau-Pathogenesis.
Sign Up to like & getrecommendations! Published in 2019 at "ACS chemical neuroscience"
DOI: 10.1021/acschemneuro.8b00405
Abstract: Protein acetylation and deacetylation play vital roles in the structural and physiological behavior of target proteins. Histone deacetylase 6 (HDAC6) remains a key therapeutic target in several chronic diseases such as cancer, neurodegenerative, and hematological… read more here.
Keywords: hdac6 inhibitors; microtubule associated; associated tau; tau pathogenesis ... See more keywords
Novel HDAC6 inhibitors increase tubulin acetylation and rescue axonal transport of mitochondria in a model of Charcot-Marie-Tooth Type 2F.
Sign Up to like & getrecommendations! Published in 2019 at "ACS chemical neuroscience"
DOI: 10.1021/acschemneuro.9b00338
Abstract: Disruption of axonal transport causes a number of rare, inherited axonopathies and is heavily implicated in a wide range of more common neurodegenerative disorders, many of them age-related. Acetylation of α-tubulin is one important regulatory… read more here.
Keywords: acetylation; hdac6 inhibitors; rescue axonal; transport ... See more keywords
Discovery of Benzylpiperazine Derivatives as CNS-Penetrant and Selective Histone Deacetylase 6 Inhibitors.
Sign Up to like & getrecommendations! Published in 2022 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.2c00081
Abstract: Inhibition of histone deacetylase 6 (HDAC6) in the brain is a highly attractive therapeutic target for the treatment of neurodegenerative diseases. The low blood-brain barrier permeability of most known HDAC6 inhibitors, however, prevents their application… read more here.
Keywords: cns penetrant; hdac6 inhibitors; histone deacetylase; benzylpiperazine derivatives ... See more keywords
Synthesis of potent and selective HDAC6 inhibitors led to unexpected opening of a quinazoline ring
Sign Up to like & getrecommendations! Published in 2022 at "RSC Advances"
DOI: 10.1039/d2ra01753a
Abstract: Histone deacetylase (HDAC) inhibitors are highly involved in the regulation of many pharmacological responses, which results in anti-inflammatory and anti-cancer effects. In the present work, chemoinformatic analyses were performed to obtain two potent and selective… read more here.
Keywords: hdac6 inhibitors; inhibitors led; selective hdac6; synthesis potent ... See more keywords
A patent review of histone deacetylase 6 inhibitors in neurodegenerative diseases (2014-2019)
Sign Up to like & getrecommendations! Published in 2019 at "Expert Opinion on Therapeutic Patents"
DOI: 10.1080/13543776.2019.1708901
Abstract: ABSTRACT Introduction: Histone deacetylase 6 (HDAC6) is unique in comparison with other zinc-dependent HDAC family members. An increasing amount of evidence from clinical and preclinical research demonstrates the potential of HDAC6 inhibition as an effective… read more here.
Keywords: hdac6 inhibitors; inhibitors neurodegenerative; 2014 2019; neurodegenerative diseases ... See more keywords
Discovery of novel benzohydroxamate-based histone deacetylase 6 (HDAC6) inhibitors with the ability to potentiate anti-PD-L1 immunotherapy in melanoma
Sign Up to like & getrecommendations! Published in 2023 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2023.2201408
Abstract: Abstract In this study, a novel series of histone deacetylases 6 (HDAC6) inhibitors containing polycyclic aromatic rings were discovered and evaluated for their pharmacological activities. The most potent compound 10c exhibited high HDAC6 inhibitory activity… read more here.
Keywords: discovery novel; histone; novel benzohydroxamate; hdac6 ... See more keywords
Abstract 6235: Discovery of novel HDAC6 inhibitors that enhance proteasomal activity to boost antigen presentation and trigger anti-myeloma T-cell immunity
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-6235
Abstract: Transformative success of cancer immunotherapy has revolutionized cancer treatment and can induce long lasting responses in patients with cancers from a wide range of histologies. However, only a fraction of patients respond to immunotherapy and… read more here.
Keywords: cell; hdac6 inhibitors; antigen presentation; activity ... See more keywords
Short-Chain Fatty Acid Butyrate Induces Cilia Formation and Potentiates the Effects of HDAC6 Inhibitors in Cholangiocarcinoma Cells
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Cell and Developmental Biology"
DOI: 10.3389/fcell.2021.809382
Abstract: Cholangiocarcinoma (CCA) is a deadly form of liver cancer with limited therapeutic approaches. The pathogenesis of CCA involves the loss of primary cilia in cholangiocytes, an important organelle that regulates several key cellular functions including… read more here.
Keywords: cell; cilia formation; hdac6 inhibitors; butyrate ... See more keywords