Chemical Versatility in Catalysis and Inhibition of the Class IIb Histone Deacetylases

DW Christianson - Accounts of Chemical Research, 2024 - ACS Publications
Conspectus The zinc-dependent histone deacetylases (HDACs 1–11) belong to the
arginase-deacetylase superfamily of proteins, members of which share a common α/β fold …

Structural and in vivo characterization of Tubastatin A, a widely used histone deacetylase 6 inhibitor

S Shen, M Svoboda, G Zhang… - ACS medicinal …, 2020 - ACS Publications
Tubastatin A, a tetrahydro-γ-carboline-capped selective HDAC6 inhibitor (HDAC6i), was
rationally designed 10 years ago, and has become the best investigated HDAC6i to date. It …

Histone deacetylases as targets for the treatment of neurodegenerative disorders: Challenges and future opportunities

DA Rodrigues, PSM Pinheiro… - Medicinal research …, 2020 - Wiley Online Library
Despite the applicability of histone deacetylase inhibitors (HDACis) for cancer treatment,
several works in the literature have shown that these inhibitors can be used in several other …

Difluoromethyl-1, 3, 4-oxadiazoles are slow-binding substrate analog inhibitors of histone deacetylase 6 with unprecedented isotype selectivity

E Cellupica, G Caprini, P Cordella, C Cukier… - Journal of Biological …, 2023 - ASBMB
Histone deacetylase 6 (HDAC6) is an attractive drug development target because of its role
in the immune response, neuropathy, and cancer. Knockout mice develop normally and …

Small molecules targeting HATs, HDACs, and BRDs in cancer therapy

D Wu, Y Qiu, Y Jiao, Z Qiu, D Liu - Frontiers in oncology, 2020 - frontiersin.org
Evidence for research over the past decade shows that epigenetic regulation mechanisms
run through the development and prognosis of tumors. Therefore, small molecular …

[HTML][HTML] Direct and indirect effects of tubulin post-translational modifications on microtubule stability: Insights and regulations

J Bär, Y Popp, M Bucher, M Mikhaylova - Biochimica et Biophysica Acta …, 2022 - Elsevier
Microtubules (MTs) mediate various cellular functions such as structural support,
chromosome segregation, and intracellular transport. To achieve this, the pivotal properties …

[HTML][HTML] Charcot-Marie-tooth disease type 2A: an update on pathogenesis and therapeutic perspectives

C Alberti, F Rizzo, A Anastasia, G Comi, S Corti… - Neurobiology of …, 2024 - Elsevier
Mutations in the gene encoding MFN2 have been identified as associated with Charcot–
Marie–Tooth disease type 2A (CMT2A), a neurological disorder characterized by a broad …

Inhibition of HDAC6 with CAY10603 ameliorates diabetic kidney disease by suppressing NLRP3 inflammasome

Q Hou, S Kan, Z Wang, J Shi, C Zeng, D Yang… - Frontiers in …, 2022 - frontiersin.org
Background: Diabetic nephropathy (DN) is one of the leading causes of chronic kidney
disease (CKD) worldwide, tubular injury is the driving force during the pathogenesis and …

Discovery of the first-in-class dual histone deacetylase–proteasome inhibitor

S Bhatia, V Krieger, M Groll, JD Osko… - Journal of medicinal …, 2018 - ACS Publications
Dual-or multitarget drugs have emerged as a promising alternative to combination therapies.
Proteasome inhibitors (PIs) possess synergistic activity with histone deacetylase (HDAC) …

Structure-based design and biological characterization of selective histone deacetylase 8 (HDAC8) inhibitors with anti-neuroblastoma activity

T Heimburg, FR Kolbinger, P Zeyen… - Journal of Medicinal …, 2017 - ACS Publications
Histone deacetylases (HDACs) are important modulators of epigenetic gene regulation and
additionally control the activity of non-histone protein substrates. While for HDACs 1–3 and 6 …