Front Cover: Development and Characterization of Selective FAK Inhibitors and PROTACs with In Vivo Activity (ChemBioChem 19/2023)

PROteolysis‐TArgeting Chimeras (PROTACs) are a class of molecules that eliminate proteins through the cell's degradation machinery. Here, to degrade an attractive cancer drug target known as focal adhesion kinase (FAK), the Nabet and Jiang labs developed a novel FAK PROTAC (BSJ‐04‐146). They sh...

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Bibliographic Details
Published in:Chembiochem : a European journal of chemical biology 2023-10, Vol.24 (19)
Main Authors: Koide, Eriko, Mohardt, Mikaela L., Doctor, Zainab M., Yang, Annan, Hao, Mingfeng, Donovan, Katherine A., Kuismi, Christina C., Nelson, Alissa J., Abell, Kathryn, Aguiar, Mike, Che, Jianwei, Stokes, Matthew P., Zhang, Tinghu, Aguirre, Andrew J., Fischer, Eric S., Gray, Nathanael S., Jiang, Baishan, Nabet, Behnam
Format: Article
Language:English
Subjects:
Animal models
Cancer
Cell culture
Chimeras
Degradation
Focal adhesion kinase
Inhibitors
Kinases
Proteasomes
Proteolysis
Therapeutic targets
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Summary:PROteolysis‐TArgeting Chimeras (PROTACs) are a class of molecules that eliminate proteins through the cell's degradation machinery. Here, to degrade an attractive cancer drug target known as focal adhesion kinase (FAK), the Nabet and Jiang labs developed a novel FAK PROTAC (BSJ‐04‐146). They show that BSJ‐04‐146 triggers rapid and specific FAK degradation in cancer cells and in mouse models, and induces improved biological responses compared to small molecule inhibitors. The cover picture depicts a firefly (BSJ‐04‐146) luring a moth (FAK) to the carnivorous plant (proteasome) and was designed by DrawImpacts. More information can be found in the Research Article by B. Jiang, B. Nabet et al.
ISSN:1439-4227
1439-7633
DOI:10.1002/cbic.202300535