TY - JOUR
T1 - High-Quality In Vivo Chemical Probes for Protein Kinases Disclosed in 2024
AU - Serafim, Ricardo A.M.
AU - Gehringer, Matthias
N1 - Publisher Copyright:
© 2025 The Authors. Published by American Chemical Society. https://creativecommons.org/licenses/by/4.0/
PY - 2025/8/8
Y1 - 2025/8/8
N2 - 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.
AB - 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.
KW - chemical probes
KW - drug discovery
KW - protein kinase inhibitors
KW - target validation
KW - understudied kinome
UR - https://www.scopus.com/pages/publications/105013497675
UR - https://www.webofscience.com/api/gateway?GWVersion=2&SrcApp=pure_univeritat_ramon_llull&SrcAuth=WosAPI&KeyUT=WOS:001530842200001&DestLinkType=FullRecord&DestApp=WOS_CPL
UR - http://hdl.handle.net/20.500.14342/5518
U2 - 10.1021/acsptsci.5c00293
DO - 10.1021/acsptsci.5c00293
M3 - Review
C2 - 40810168
AN - SCOPUS:105013497675
SN - 2575-9108
VL - 8
SP - 2401
EP - 2414
JO - ACS Pharmacology and Translational Science
JF - ACS Pharmacology and Translational Science
IS - 8
ER -