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 …

Proteolysis-targeting chimeras (PROTACs) in cancer therapy

X Li, W Pu, Q Zheng, M Ai, S Chen, Y Peng - Molecular cancer, 2022 - Springer
Proteolysis-targeting chimeras (PROTACs) are engineered techniques for targeted protein
degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits …

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 bibliometric analysis of PROTAC from 2001 to 2021

D Li, D Yu, Y Li, R Yang - European journal of medicinal chemistry, 2022 - Elsevier
Proteolysis targeting chimera (PROTAC) technology, one of the targeted protein degradation
technologies, has drawn marked attention from researchers of both academia and industry …

Targeted protein degradation: advances in drug discovery and clinical practice

G Zhong, X Chang, W **e, X Zhou - Signal Transduction and Targeted …, 2024 - nature.com
Targeted protein degradation (TPD) represents a revolutionary therapeutic strategy in
disease management, providing a stark contrast to traditional therapeutic approaches like …

Medicinal chemistry updates of novel HDACs inhibitors (2020 to present)

X He, Z Hui, L Xu, R Bai, Y Gao, Z Wang, T **e… - European Journal of …, 2022 - Elsevier
Epigentic enzymes histone deacetylases (HDACs) catalyze the removal of acetyl groups
from the ε-N-acetylated lysine residues of various protein substrates including both histone …

Chemo-proteomics exploration of HDAC degradability by small molecule degraders

Y **ong, 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 …

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 …

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 …

Cu-Catalyzed α-Alkylation of Glycine Derivatives for C(sp3)–H/C(sp3)–H Bond Selective Functionalization

H **ang, Y Ye - ACS Catalysis, 2023 - ACS Publications
Herein, we present the example of Cu-catalyzed oxidation coupling of amino acids/peptides
for producing α-alkylated unnatural glycine derivatives by the activation of double C (sp3) …