High-Quality In Vivo Chemical Probes for Protein Kinases Disclosed in 2024
Protein kinases are highly relevant drug targets, yet a significant fraction of the human kinome remains underexplored. Highly potent and selective small-molecule inhibitors used as chemical probes are invaluable tools for enabling the validation and translation of new kinase targets. This review pr...
| Authors: | , |
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| Format: | article |
| Publication Date: | 2025 |
| Country: | España |
| Institution: | Universitat Ramon Llull (URL) |
| Repository: | DAU Arxiu Digital de la Universitat Ramon Llull |
| OAI Identifier: | oai:dau.url.edu:20.500.14342/5518 |
| Online Access: | http://hdl.handle.net/20.500.14342/5518 https://doi.org/10.1021/acsptsci.5c00293 |
| Access Level: | Open access |
| Keyword: | Chemical probes Protein kinase inhibitors Target validation Drug discovery Understudied kinome Proteïnes quinases--Inhibidors Descobriment de fàrmacs 577 |
| Summary: | Protein kinases are highly relevant drug targets, yet a significant fraction of the human kinome remains underexplored. Highly potent and selective small-molecule inhibitors used as chemical probes are invaluable tools for enabling the validation and translation of new kinase targets. This review provides an overview and analysis of the high-quality in vivo chemical probes for protein kinases published and deposited at the Chemical Probes Portal in the year 2024. We discuss the design strategies, molecular mechanism of action, details of their use in vitro and in vivo, as well as their application in target (in)validation. We also highlight the importance of wisely selecting chemical probes and encourage best practices in using such tool compounds. |
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