Chemistries of bifunctional PROTAC degraders
C Cao, M He, L Wang, Y He, Y Rao - Chemical Society Reviews, 2022 - pubs.rsc.org
Proteolysis targeting chimeras (PROTACs) technology is a novel and promising therapeutic
strategy using small molecules to induce ubiquitin-dependent degradation of proteins. It has …
strategy using small molecules to induce ubiquitin-dependent degradation of proteins. It has …
Proximity-based modalities for biology and medicine
Molecular proximity orchestrates biological function, and blocking existing proximities is an
established therapeutic strategy. By contrast, strengthening or creating neoproximity with …
established therapeutic strategy. By contrast, strengthening or creating neoproximity with …
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 …
Current advances and development strategies of orally bioavailable PROTACs
S Zeng, Y Ye, H Xia, J Min, J Xu, Z Wang, Y Pan… - European Journal of …, 2023 - Elsevier
Proteolysis-targeting chimeras (PROTACs) have been an area of intensive research with the
potential to extend drug space not target to traditional molecules. In the last half decade, we …
potential to extend drug space not target to traditional molecules. In the last half decade, we …
Development of potent and selective coactivator-associated arginine methyltransferase 1 (CARM1) degraders
CARM1 is amplified or overexpressed in many cancer types, and its overexpression
correlates with poor prognosis. Potent small-molecule inhibitors for CARM1 have been …
correlates with poor prognosis. Potent small-molecule inhibitors for CARM1 have been …
[HTML][HTML] Direct-to-biology, automated, nano-scale synthesis, and phenotypic screening-enabled E3 ligase modulator discovery
Thalidomide and its analogs are molecular glues (MGs) that lead to targeted ubiquitination
and degradation of key cancer proteins via the cereblon (CRBN) E3 ligase. Here, we …
and degradation of key cancer proteins via the cereblon (CRBN) E3 ligase. Here, we …
A versatile and sustainable multicomponent platform for the synthesis of protein degraders: proof-of-concept application to BRD4-degrading PROTACs
IP Bhela, A Ranza, FC Balestrero… - Journal of Medicinal …, 2022 - ACS Publications
The use of small molecules to induce targeted protein degradation is increasingly growing in
the drug discovery landscape, and protein degraders have progressed rapidly through the …
the drug discovery landscape, and protein degraders have progressed rapidly through the …
Reversible assembly of proteolysis targeting chimeras
PROteolysis TArgeting Chimeras (PROTACs) are of significant current interest for the
development of probe molecules and drug leads. However, they suffer from certain …
development of probe molecules and drug leads. However, they suffer from certain …
Innovative, combinatorial and high-throughput approaches to degrader synthesis
R Stevens, JDF Thompson, JCL Fournier… - Chemical Society …, 2024 - pubs.rsc.org
Targeted protein degraders such as PROTACs and molecular glues are a rapidly emerging
therapeutic modality within industry and academia. Degraders possess unique mechanisms …
therapeutic modality within industry and academia. Degraders possess unique mechanisms …
Integrated direct-to-biology platform for the nanoscale synthesis and biological evaluation of PROTACs
R Stevens, E Bendito-Moll, DJ Battersby… - Journal of Medicinal …, 2023 - ACS Publications
Proteolysis targeting chimeras (PROTACs) are heterobifunctional molecules that co-opt the
cell's natural proteasomal degradation mechanisms to degrade undesired proteins. A …
cell's natural proteasomal degradation mechanisms to degrade undesired proteins. A …