Chemistries of bifunctional PROTAC degraders DOI
Chao-Guo Cao,

Ming He,

Liguo Wang

et al.

Chemical Society Reviews, Journal Year: 2022, Volume and Issue: 51(16), P. 7066 - 7114

Published: Jan. 1, 2022

Proteolysis targeting chimeras (PROTACs) technology is a novel and promising therapeutic strategy using small molecules to induce ubiquitin-dependent degradation of proteins.

Language: Английский

Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity DOI
Satomi Imaide, Kristin M. Riching, Nikolai Makukhin

et al.

Nature Chemical Biology, Journal Year: 2021, Volume and Issue: 17(11), P. 1157 - 1167

Published: Oct. 21, 2021

Language: Английский

Citations

176
Heat Shock Protein 90 Inhibitors: An Update on Achievements, Challenges, and Future Directions DOI
Li Li, Lei Wang, Qidong You

et al.

Journal of Medicinal Chemistry, Journal Year: 2019, Volume and Issue: 63(5), P. 1798 - 1822

Published: Oct. 30, 2019

Hsp90 is one of the most important chaperones involved in regulating maturation more than 300 client proteins, many which are closely associated with refractory diseases, including cancer, neurodegenerative and viral infections. Clinical inhibitors bind to ATP pocket N-terminal domain subsequently suppress ATPase activity Hsp90. Recently, increased understanding discrepancies isoforms modes Hsp90-co-chaperone-client complex interactions, some new strategies for inhibition have emerged. Novel that offer selective suppression or specific disruption Hsp90-co-chaperone protein–protein interactions expected show satisfactory efficacy safety profiles. This review summarizes recent progress inhibitors. Additionally, inhibitory emphasized this review.

Language: Английский

Citations

171
EED-Targeted PROTACs Degrade EED, EZH2, and SUZ12 in the PRC2 Complex DOI Creative Commons

Jessie Hao-Ru Hsu,

Timothy Rasmusson,

James Robinson

et al.

Cell chemical biology, Journal Year: 2019, Volume and Issue: 27(1), P. 41 - 46.e17

Published: Nov. 27, 2019

Language: Английский

Citations

171
Harnessing the Power of Proteolysis for Targeted Protein Inactivation DOI Creative Commons
Rati Verma,

Dane Mohl,

Raymond J. Deshaies

et al.

Molecular Cell, Journal Year: 2020, Volume and Issue: 77(3), P. 446 - 460

Published: Jan. 30, 2020

Language: Английский

Citations

171
Chemistries of bifunctional PROTAC degraders DOI
Chao-Guo Cao,

Ming He,

Liguo Wang

et al.

Chemical Society Reviews, Journal Year: 2022, Volume and Issue: 51(16), P. 7066 - 7114

Published: Jan. 1, 2022

Proteolysis targeting chimeras (PROTACs) technology is a novel and promising therapeutic strategy using small molecules to induce ubiquitin-dependent degradation of proteins.

Language: Английский

Citations

170