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 …
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 …
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 …
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 …
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 …
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 …
of histone deacetylase (HDAC) inhibitors, which have many applications including cancer …
Chemo-proteomics exploration of HDAC degradability by small molecule degraders
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 …
ligase to a target protein for ubiquitination and subsequent proteasome-dependent …
Combining histone deacetylase inhibitors (HDACis) with other therapies for cancer therapy
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 …
involved in tumorigenesis and tumor maintenance, and hence they have been considered …
Hydroxamic acid derivatives: From synthetic strategies to medicinal chemistry applications
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 …
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
The acetylation of histone and non-histone proteins has been implicated in several disease
states. Modulation of such epigenetic modifications has therefore made histone …
states. Modulation of such epigenetic modifications has therefore made histone …