Covalently engineered nanobody chimeras for targeted membrane protein degradation
H Zhang, Y Han, Y Yang, F Lin, K Li… - Journal of the …, 2021 - ACS Publications
The targeted degradation of membrane proteins would afford an attractive and general
strategy for treating various diseases that remain difficult with the current proteolysis …
strategy for treating various diseases that remain difficult with the current proteolysis …
Hijacking the E3 ubiquitin ligase cereblon to efficiently target BRD4
J Lu, Y Qian, M Altieri, H Dong, J Wang, K Raina… - Chemistry & biology, 2015 - cell.com
BRD4, a bromodomain and extraterminal domain (BET) family member, is an attractive
target in multiple pathological settings, particularly cancer. While BRD4 inhibitors have …
target in multiple pathological settings, particularly cancer. While BRD4 inhibitors have …
The rise of covalent proteolysis targeting chimeras
R Gabizon, N London - Current opinion in chemical biology, 2021 - Elsevier
Targeted protein degradation offers several advantages over direct inhibition of protein
activity and is gaining increasing interest in chemical biology and drug discovery …
activity and is gaining increasing interest in chemical biology and drug discovery …
Impact of target warhead and linkage vector on inducing protein degradation: comparison of bromodomain and extra-terminal (BET) degraders derived from …
The design of proteolysis-targeting chimeras (PROTACs) is a powerful small-molecule
approach for inducing protein degradation. PROTACs conjugate a target warhead to an E3 …
approach for inducing protein degradation. PROTACs conjugate a target warhead to an E3 …
Development of a BCL-xL and BCL-2 dual degrader with improved anti-leukemic activity
Abstract PROteolysis-TArgeting Chimeras (PROTACs) have emerged as an innovative drug
development platform. However, most PROTACs have been generated empirically because …
development platform. However, most PROTACs have been generated empirically because …
Targeted protein degradation: elements of PROTAC design
SL Paiva, CM Crews - Current opinion in chemical biology, 2019 - Elsevier
Targeted protein degradation using Proteolysis Targeting Chimeras (PROTACs) has
emerged as a novel therapeutic modality in drug discovery. PROTACs mediate the …
emerged as a novel therapeutic modality in drug discovery. PROTACs mediate the …
Discovery of E3 ligase ligands for target protein degradation
Target protein degradation has emerged as a promising strategy for the discovery of novel
therapeutics during the last decade. Proteolysis-targeting chimera (PROTAC) harnesses a …
therapeutics during the last decade. Proteolysis-targeting chimera (PROTAC) harnesses a …
Stimuli‐Responsive PROTACs for Controlled Protein Degradation
K An, X Deng, H Chi, Y Zhang, Y Li… - Angewandte Chemie …, 2023 - Wiley Online Library
Abstract Proteolysis Targeting Chimeras (PROTACs) represent a promising therapeutic
modality to address undruggable and resistant issues in drug discovery. However, potential …
modality to address undruggable and resistant issues in drug discovery. However, potential …
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 …