PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

M He, C Cao, Z Ni, Y Liu, P Song, S Hao, Y He… - … and Targeted Therapy, 2022 - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …

Epigenetic tools (The Writers, The Readers and The Erasers) and their implications in cancer therapy

S Biswas, CM Rao - European journal of pharmacology, 2018 - Elsevier
Addition of chemical tags on the DNA and modification of histone proteins impart a distinct
feature on chromatin architecture. With the advancement in scientific research, the key …

[HTML][HTML] The world of protein acetylation

A Drazic, LM Myklebust, R Ree, T Arnesen - Biochimica et Biophysica Acta …, 2016 - Elsevier
Acetylation is one of the major post-translational protein modifications in the cell, with
manifold effects on the protein level as well as on the metabolome level. The acetyl group …

HDAC6 as privileged target in drug discovery: A perspective

S Pulya, SA Amin, N Adhikari, S Biswas, T Jha… - Pharmacological …, 2021 - Elsevier
Abstract HDAC6, a class IIB HDAC isoenzyme, stands unique in its structural and
physiological functions. Besides histone modification, largely due to its cytoplasmic …

Histone deacetylase 6 in cancer

T Li, C Zhang, S Hassan, X Liu, F Song, K Chen… - Journal of hematology & …, 2018 - Springer
Histone acetylation and deacetylation are important epigenetic mechanisms that regulate
gene expression and transcription. Histone deacetylase 6 (HDAC6) is a unique member of …

Strategies for designing proteolysis targeting chimaeras (PROTACs)

S He, G Dong, J Cheng, Y Wu… - Medicinal Research …, 2022 - Wiley Online Library
Proteolysis targeting chimaeras (PROTACs) is a cutting edge and rapidly growing technique
for new drug discovery and development. Currently, the largest challenge in the molecular …

Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma

L Santo, T Hideshima, AL Kung… - Blood, The Journal …, 2012 - ashpublications.org
Histone deacetylase (HDAC) enzymatic activity has been linked to the transcription of DNA
in cancers including multiple myeloma (MM). Therefore, HDAC inhibitors used alone and in …

Rational design and simple chemistry yield a superior, neuroprotective HDAC6 inhibitor, tubastatin A

KV Butler, J Kalin, C Brochier, G Vistoli… - Journal of the …, 2010 - ACS Publications
Structure-based drug design combined with homology modeling techniques were used to
develop potent inhibitors of HDAC6 that display superior selectivity for the HDAC6 isozyme …

Post-translational modifications of tubulin: pathways to functional diversity of microtubules

Y Song, ST Brady - Trends in cell biology, 2015 - cell.com
Tubulin and microtubules are subject to a remarkable number of post-translational
modifications. Understanding the roles these modifications play in determining the functions …

Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes

M Bantscheff, C Hopf, MM Savitski, A Dittmann… - Nature …, 2011 - nature.com
The development of selective histone deacetylase (HDAC) inhibitors with anti-cancer and
anti-inflammatory properties remains challenging in large part owing to the difficulty of …