[HTML][HTML] HDAC inhibitors: innovative strategies for their design and applications

M Daśko, B de Pascual-Teresa, I Ortín, A Ramos - Molecules, 2022 - mdpi.com
Histone deacetylases (HDACs) are a large family of epigenetic metalloenzymes that are
involved in gene transcription and regulation, cell proliferation, differentiation, migration, and …

[HTML][HTML] Chemo-proteomics exploration of HDAC degradability by small molecule degraders

Y Xiong, KA Donovan, NA Eleuteri, N Kirmani… - Cell chemical …, 2021 - cell.com
Targeted protein degradation refers to the use of small molecules that recruit a ubiquitin
ligase to a target protein for ubiquitination and subsequent proteasome-dependent …

Histone deacetylase 6 inhibitors with blood-brain barrier penetration as a potential strategy for CNS-Disorders therapy

X Gu, H Zhang, M Jiao, B Han, Z Zhang, J Li… - European Journal of …, 2022 - Elsevier
Histone deacetylase 6 inhibitors (HDAC6is) have been applied to certain cancer diseases
and more recently to central nervous system (CNS) disorders including Rett syndrome …

[HTML][HTML] 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 …

[HTML][HTML] HDAC6 inhibition reverses long-term doxorubicin-induced cognitive dysfunction by restoring microglia homeostasis and synaptic integrity

BR McAlpin, R Mahalingam, AK Singh, S Dharmaraj… - Theranostics, 2022 - ncbi.nlm.nih.gov
Breast cancer is the most common female malignancy in both the developed and
developing world. Doxorubicin is one of the most commonly used chemotherapies for breast …

Role of fluorination in the histone deacetylase 6 (HDAC6) selectivity of benzohydroxamate-based inhibitors

G Sandrone, CD Cukier, K Zrubek… - ACS Medicinal …, 2021 - ACS Publications
Nonselective histone deacetylase (HDAC) inhibitors show dose-limiting side effects due to
the inhibition of multiple, essential HDAC subtypes that can be limited or prevented by …

Potent inhibition of human tyrosinase inhibitor by verproside from the whole plant of Pseudolysimachion rotundum var. subintegrum

S Jung, SY Woo, MH Park, DY Kim… - Journal of Enzyme …, 2023 - Taylor & Francis
Affinity-based ultrafiltration–mass spectrometry coupled with ultraperformance liquid
chromatography–quadrupole time-of-flight mass spectrometry was utilised for the structural …

Discovery of Benzylpiperazine Derivatives as CNS-Penetrant and Selective Histone Deacetylase 6 Inhibitors

K Hashimoto, S Ide, M Arata, A Nakata… - ACS Medicinal …, 2022 - ACS Publications
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 …

[HTML][HTML] The impact of fluorination on the design of histone deacetylase inhibitors

D Tien Anh, N Hai Nam, B Kircher, D Baecker - Molecules, 2023 - mdpi.com
In recent years, histone deacetylases (HDACs) have emerged as promising targets in the
treatment of cancer. The approach is to inhibit HDACs with drugs known as HDAC inhibitors …

Discovery of a Highly Potent and Selective HDAC8 Degrader: Advancing the Functional Understanding and Therapeutic Potential of HDAC8

Y Xiao, N Awasthee, Y Liu, C Meng… - Journal of Medicinal …, 2024 - ACS Publications
HDAC8 plays crucial roles in biological processes, from gene regulation to cell motility,
making it a highly desirable target for therapeutic intervention. HDAC8 also has deacetylase …