[HTML][HTML] Bifunctional HDAC therapeutics: one drug to rule them all?

JP Smalley, SM Cowley, JT Hodgkinson - Molecules, 2020 - mdpi.com
Histone deacetylase (HDAC) enzymes play crucial roles in epigenetic gene expression and
are an attractive therapeutic target. Five HDAC inhibitors have been approved for cancer …

[HTML][HTML] Identification of novel natural dual HDAC and Hsp90 inhibitors for metastatic TNBC using e-pharmacophore modeling, molecular docking, and molecular …

N AbdElmoniem, M H. Abdallah, R M. Mukhtar… - Molecules, 2023 - mdpi.com
Breast cancer (BC) is one of the main types of cancer that endangers women's lives. The
characteristics of triple-negative breast cancer (TNBC) include a high rate of recurrence and …

Glutamylation is a negative regulator of microtubule growth

J Chen, A Roll-Mecak - Molecular Biology of the Cell, 2023 - Am Soc Cell Biol
Microtubules are noncovalent polymers built from αβ-tubulin dimers. The disordered C-
terminal tubulin tails are functionalized with multiple glutamate chains of variable lengths …

[HTML][HTML] Human histone deacetylase 6 shows strong preference for tubulin dimers over assembled microtubules

L Skultetyova, K Ustinova, Z Kutil, Z Novakova… - Scientific reports, 2017 - nature.com
Abstract Human histone deacetylase 6 (HDAC6) is the major deacetylase responsible for
removing the acetyl group from Lys40 of α-tubulin (αK40), which is located lumenally in …

Exploring the inhibitory activity of valproic acid against the HDAC family using an MMGBSA approach

Y Sixto-López, M Bello, J Correa-Basurto - Journal of Computer-Aided …, 2020 - Springer
Valproic acid (VPA) is a compound currently used in clinical practice for the treatment of
epilepsy as well as bipolar and mood disorders. VPA targets histone deacetylases (HDACs) …

Posttranslational modifications of the cytoskeleton

B MacTaggart, A Kashina - Cytoskeleton, 2021 - Wiley Online Library
The cytoskeleton plays important roles in many essential processes at the cellular and
organismal levels, including cell migration and motility, cell division, and the establishment …

Structural basis of catalysis and inhibition of HDAC6 CD1, the enigmatic catalytic domain of histone deacetylase 6

JD Osko, DW Christianson - Biochemistry, 2019 - ACS Publications
Histone deacetylase 6 (HDAC6) is emerging as a target for inhibition in therapeutic
strategies aimed at treating cancer, neurodegenerative disease, and other disorders. Among …

Rational design of suprastat: a novel selective histone deacetylase 6 inhibitor with the ability to potentiate immunotherapy in melanoma models

S Noonepalle, S Shen, J Ptáček… - Journal of Medicinal …, 2020 - ACS Publications
Selective inhibition of histone deacetylase 6 (HDAC6) is being recognized as a therapeutic
approach for cancers. In this study, we designed a new HDAC6 inhibitor, named Suprastat …

[HTML][HTML] Pharmacological inhibition of HDAC6 attenuates NLRP3 inflammatory response and protects dopaminergic neurons in experimental models of Parkinson's …

S Yan, X Wei, W Jian, Y Qin, J Liu, S Zhu… - Frontiers in Aging …, 2020 - frontiersin.org
Aim To investigate the role of histone deacetylase 6 (HDAC6) deacetylation activity in
nucleotide-binding oligomerization domain and leucine-rich repeat pyrin 3 domain (NLRP3) …

[HTML][HTML] Discovery of 1-benzhydryl-piperazine-based HDAC inhibitors with anti-breast cancer activity: synthesis, molecular modeling, in vitro and in vivo biological …

D Ruzic, B Ellinger, N Djokovic, JF Santibanez, S Gul… - Pharmaceutics, 2022 - mdpi.com
Isoform-selective histone deacetylase (HDAC) inhibition is promoted as a rational strategy to
develop safer anti-cancer drugs compared to non-selective HDAC inhibitors. Despite this …