Structural basis of lenalidomide-induced CK1α degradation by the CRL4CRBN ubiquitin ligase DOI
Georg Petzold, Eric S. Fischer, Nicolas H. Thomä

et al.

Nature, Journal Year: 2016, Volume and Issue: 532(7597), P. 127 - 130

Published: Feb. 23, 2016

Language: Английский

Plasticity in binding confers selectivity in ligand-induced protein degradation DOI
Radosław P. Nowak, Stephen L. DeAngelo, Dennis L. Buckley

et al.

Nature Chemical Biology, Journal Year: 2018, Volume and Issue: 14(7), P. 706 - 714

Published: June 8, 2018

Language: Английский

Citations

527
Ubiquitylation at the crossroads of development and disease DOI
Michael Rapé

Nature Reviews Molecular Cell Biology, Journal Year: 2017, Volume and Issue: 19(1), P. 59 - 70

Published: Sept. 20, 2017

Language: Английский

Citations

517
PROTACs: great opportunities for academia and industry DOI Creative Commons
Xiuyun Sun, Hongying Gao, Yiqing Yang

et al.

Signal Transduction and Targeted Therapy, Journal Year: 2019, Volume and Issue: 4(1)

Published: Dec. 24, 2019

Although many kinds of therapies are applied in the clinic, drug-resistance is a major and unavoidable problem. Another disturbing statistic limited number drug targets, which presently only 20-25% all protein targets that currently being studied. Moreover, focus current explorations their enzymatic functions, ignores functions from scaffold moiety. As promising appealing technology, PROteolysis TArgeting Chimeras (PROTACs) have attracted great attention both academia industry for finding available approaches to solve above problems. PROTACs regulate function by degrading target proteins instead inhibiting them, providing more sensitivity drug-resistant greater chance affect nonenzymatic functions. been proven show better selectivity compared classic inhibitors. can be described as chemical knockdown approach with rapidity reversibility, presents new different biology other gene editing tools avoiding misinterpretations arise potential genetic compensation and/or spontaneous mutations. PRTOACs widely explored throughout world outperformed not cancer diseases, but also immune disorders, viral infections neurodegenerative diseases. present very powerful crossing hurdles discovery tool development biology, efforts needed gain get deeper insight into efficacy safety clinic. More binders E3 ligases applicable developing waiting exploration.

Language: Английский

Citations

516
A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity DOI
Sajid Khan, Xuan Zhang, Dongwen Lv

et al.

Nature Medicine, Journal Year: 2019, Volume and Issue: 25(12), P. 1938 - 1947

Published: Dec. 1, 2019

Language: Английский

Citations

508
Structural basis of lenalidomide-induced CK1α degradation by the CRL4CRBN ubiquitin ligase DOI
Georg Petzold, Eric S. Fischer, Nicolas H. Thomä

et al.

Nature, Journal Year: 2016, Volume and Issue: 532(7597), P. 127 - 130

Published: Feb. 23, 2016

Language: Английский

Citations

496