Plasticity in binding confers selectivity in ligand-induced protein degradation

Nature Chemical Biology, Год журнала: 2018, Номер 14(7), С. 706 - 714

Опубликована: Июнь 8, 2018

Язык: Английский

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Ubiquitylation at the crossroads of development and disease

Nature Reviews Molecular Cell Biology, Год журнала: 2017, Номер 19(1), С. 59 - 70

Опубликована: Сен. 20, 2017

Язык: Английский

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PROTACs: great opportunities for academia and industry

Signal Transduction and Targeted Therapy, Год журнала: 2019, Номер 4(1)

Опубликована: Дек. 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.

Язык: Английский

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A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity

Nature Medicine, Год журнала: 2019, Номер 25(12), С. 1938 - 1947

Опубликована: Дек. 1, 2019

Язык: Английский

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Structural basis of lenalidomide-induced CK1α degradation by the CRL4CRBN ubiquitin ligase

Nature, Год журнала: 2016, Номер 532(7597), С. 127 - 130

Опубликована: Фев. 23, 2016

Язык: Английский

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