Targeting mutant p53 for cancer therapy: direct and indirect strategies

J Hu, J Cao, W Topatana, S Juengpanich, S Li… - Journal of hematology & …, 2021 - Springer
TP53 is a critical tumor-suppressor gene that is mutated in more than half of all human
cancers. Mutations in TP53 not only impair its antitumor activity, but also confer mutant p53 …

Recent developments of HDAC inhibitors: Emerging indications and novel molecules

AD Bondarev, MM Attwood, J Jonsson… - British journal of …, 2021 - Wiley Online Library
The histone deacetylase (HDAC) enzymes, a class of epigenetic regulators, are historically
well established as attractive therapeutic targets. During investigation of trends within …

Sulfonamide derivatives as potential anti-cancer agents and their SARs elucidation

Y Wan, G Fang, H Chen, X Deng, Z Tang - European Journal of Medicinal …, 2021 - Elsevier
Currently, the arise of drug resistance and undesirable off-target effects of anti-cancer
agents are major challenges for cancer treatment, which energizes medicinal chemists to …

Anticancer therapy with HDAC inhibitors: mechanism-based combination strategies and future perspectives

R Jenke, N Reßing, FK Hansen, A Aigner, T Büch - Cancers, 2021 - mdpi.com
Simple Summary Beyond mutations, epigenetic changes have been described as drivers for
cancer as well. While leaving the overall DNA structure intact, they can be responsible for …

A review of progress in histone deacetylase 6 inhibitors research: structural specificity and functional diversity

XH Zhang, Qin-Ma, HP Wu, MY Khamis… - Journal of medicinal …, 2021 - ACS Publications
Histone deacetylases (HDACs) are essential for maintaining homeostasis by catalyzing
histone deacetylation. Aberrant expression of HDACs is associated with various human …

Strategies to design selective histone deacetylase inhibitors

J Melesina, CV Simoben, L Praetorius… - …, 2021 - Wiley Online Library
This review classifies drug‐design strategies successfully implemented in the development
of histone deacetylase (HDAC) inhibitors, which have many applications including cancer …

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 …

Combining histone deacetylase inhibitors (HDACis) with other therapies for cancer therapy

M Zhou, M Yuan, M Zhang, C Lei, O Aras… - European journal of …, 2021 - Elsevier
Histone deacetylases (HDACs) play an important role in regulating the expression of genes
involved in tumorigenesis and tumor maintenance, and hence they have been considered …

Hydroxamic acid derivatives: From synthetic strategies to medicinal chemistry applications

A Citarella, D Moi, L Pinzi, D Bonanni, G Rastelli - ACS omega, 2021 - ACS Publications
Since the approval of three hydroxamic acid-based HDAC inhibitors as anticancer drugs,
such functional groups acquired even more notoriety in synthetic medicinal chemistry. The …

Dissecting histone deacetylase 3 in multiple disease conditions: selective inhibition as a promising therapeutic strategy

N Adhikari, T Jha, B Ghosh - Journal of Medicinal Chemistry, 2021 - ACS Publications
The acetylation of histone and non-histone proteins has been implicated in several disease
states. Modulation of such epigenetic modifications has therefore made histone …