PROTACs: past, present and future

K Li, CM Crews - Chemical Society Reviews, 2022 - pubs.rsc.org
Proteolysis-targeting chimeras (PROTACs) are heterobifunctional molecules consisting of
one ligand that binds to a protein of interest (POI) and another that can recruit an E3 …

Targeted protein degradation: mechanisms, strategies and application

L Zhao, J Zhao, K Zhong, A Tong, D Jia - Signal transduction and …, 2022 - nature.com
Traditional drug discovery mainly focuses on direct regulation of protein activity. The
development and application of protein activity modulators, particularly inhibitors, has been …

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 …

Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders

CJ Diehl, A Ciulli - Chemical Society Reviews, 2022 - pubs.rsc.org
The von Hippel-Lindau (VHL) Cullin RING E3 ligase is an essential enzyme in the ubiquitin-
proteasome system that recruits substrates such as the hypoxia inducible factor for …

Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity

S Imaide, KM Riching, N Makukhin, V Vetma… - Nature chemical …, 2021 - nature.com
Bivalent proteolysis-targeting chimeras (PROTACs) drive protein degradation by
simultaneously binding a target protein and an E3 ligase and forming a productive ternary …

Emerging strategies to overcome resistance to third-generation EGFR inhibitors

K Shi, G Wang, J Pei, J Zhang, J Wang… - Journal of Hematology & …, 2022 - Springer
Epidermal growth factor receptor (EGFR), the receptor for members of the epidermal growth
factor family, regulates cell proliferation and signal transduction; moreover, EGFR is related …

PROTAC degraders as chemical probes for studying target biology and target validation

V Němec, MP Schwalm, S Müller… - Chemical Society Reviews, 2022 - pubs.rsc.org
Small molecule degraders such as PROTACs (PROteolysis TArgeting Chimeras) have
emerged as new promising pharmacological modalities and the first PROTAC drug …

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 …

Strategies targeting protein tyrosine phosphatase SHP2 for cancer therapy

Y Song, S Wang, M Zhao, X Yang… - Journal of Medicinal …, 2022 - ACS Publications
The protein tyrosine phosphatase SHP2 encoded by PTPN11 is a promising therapeutic
target for cancer therapy, while the multifaceted roles of SHP2 complicate the drug discovery …

Advancing strategies for proteolysis-targeting chimera design

M Li, Y Zhi, B Liu, Q Yao - Journal of medicinal chemistry, 2023 - ACS Publications
Proteolysis-targeting chimeras (PROTACs) have shown great therapeutic potential by
degrading various disease-causing proteins, particularly those related to tumors. Therefore …