[HTML][HTML] Applications of protein ubiquitylation and deubiquitylation in drug discovery

Y Chen, H Xue, J Jin - Journal of Biological Chemistry, 2024 - Elsevier
The ubiquitin-proteasome system (UPS) is the major machinery mediating specific protein
turnover in eukaryotic cells. By ubiquitylating unwanted, damaged, or harmful proteins and …

[HTML][HTML] Protein–protein interactions: developing small-molecule inhibitors/stabilizers through covalent strategies

B Lucero, KR Francisco, LJ Liu, CR Caffrey… - Trends in …, 2023 - cell.com
The development of small-molecule inhibitors or stabilizers of selected protein–protein
interactions (PPIs) of interest holds considerable promise for the development of research …

[HTML][HTML] Expanding PROTACtable genome universe of E3 ligases

Y Liu, J Yang, T Wang, M Luo, Y Chen, C Chen… - Nature …, 2023 - nature.com
Proteolysis-targeting chimera (PROTAC) and other targeted protein degradation (TPD)
molecules that induce degradation by the ubiquitin-proteasome system (UPS) offer new …

Emerging targeted protein degradation tools for innovative drug discovery: From classical PROTACs to the novel and beyond

Y Zhong, F Chi, H Wu, Y Liu, Z Xie, W Huang… - European journal of …, 2022 - Elsevier
Targeted protein degradation technology has evolved a brand-new therapeutic modality
from an innovative drug discovery perspective. Though the classical PROTACs has …

Extracellular targeted protein degradation: an emerging modality for drug discovery

JA Wells, K Kumru - Nature Reviews Drug Discovery, 2024 - nature.com
Targeted protein degradation (TPD) has emerged in the past decade as a major new drug
modality to remove intracellular proteins with bispecific small molecules that recruit the …

Clinical translation of targeted protein degraders

NR Kong, LH Jones - Clinical Pharmacology & Therapeutics, 2023 - Wiley Online Library
Targeted protein degradation (TPD) has emerged as a potentially transformational
therapeutic modality with considerable promise. Molecular glue degraders remodel the …

[HTML][HTML] From discovery to bedside: targeting the ubiquitin system

IE Wertz, X Wang - Cell chemical biology, 2019 - cell.com
The ubiquitin/proteasome system is a primary conduit for selective intracellular protein
degradation. Since its discovery over 30 years ago, this highly regulated system continues to …

Target and tissue selectivity of PROTAC degraders

RG Guenette, SW Yang, J Min, B Pei… - Chemical Society …, 2022 - pubs.rsc.org
Targeted protein degradation (TPD) strategies have revolutionized how scientists tackle
challenging protein targets deemed undruggable with traditional small molecule inhibitors …

Heterobifunctional molecules induce dephosphorylation of kinases–a proof of concept study

S Yamazoe, J Tom, Y Fu, W Wu, L Zeng… - Journal of medicinal …, 2019 - ACS Publications
Heterobifunctional molecules have proven powerful tools to induce ligase-dependent
ubiquitination of target proteins. We describe here a chemical strategy for controlling a …

[HTML][HTML] Identification and selectivity profiling of small-molecule degraders via multi-omics approaches

NS Scholes, C Mayor-Ruiz, GE Winter - Cell Chemical Biology, 2021 - cell.com
The therapeutic modality of targeted protein degradation promises to overcome limitations of
traditional pharmacology. Small-molecule degraders recruit disease-causing proteins to E3 …