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 …
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 …
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
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 …
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 …
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 …
factor family, regulates cell proliferation and signal transduction; moreover, EGFR is related …
PROTAC degraders as chemical probes for studying target biology and target validation
Small molecule degraders such as PROTACs (PROteolysis TArgeting Chimeras) have
emerged as new promising pharmacological modalities and the first PROTAC drug …
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 …
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 …
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 …
degrading various disease-causing proteins, particularly those related to tumors. Therefore …