The evolution of protein kinase inhibitors from antagonists to agonists of cellular signaling
AC Dar, KM Shokat - Annual review of biochemistry, 2011 - annualreviews.org
Kinases are highly regulated enzymes with diverse mechanisms controlling their catalytic
output. Over time, chemical discovery efforts for kinases have produced ATP-competitive …
output. Over time, chemical discovery efforts for kinases have produced ATP-competitive …
[HTML][HTML] Structural features of the protein kinase domain and targeted binding by small-molecule inhibitors
C Arter, L Trask, S Ward, S Yeoh, R Bayliss - Journal of Biological …, 2022 - ASBMB
Protein kinases are key components in cellular signaling pathways as they carry out the
phosphorylation of proteins, primarily on Ser, Thr, and Tyr residues. The catalytic activity of …
phosphorylation of proteins, primarily on Ser, Thr, and Tyr residues. The catalytic activity of …
Protein kinase biochemistry and drug discovery
PA Schwartz, BW Murray - Bioorganic chemistry, 2011 - Elsevier
Protein kinases are fascinating biological catalysts with a rapidly expanding knowledge
base, a growing appreciation in cell regulatory control, and an ascendant role in successful …
base, a growing appreciation in cell regulatory control, and an ascendant role in successful …
Protein kinases as therapeutic targets
R Sridhar, O Hanson-Painton, DR Cooper - Pharmaceutical research, 2000 - Springer
Protein kinases and phosphatases are likely targets for the development of therapeutic
drugs since they are involved in specific signaling pathways which regulate cell functions …
drugs since they are involved in specific signaling pathways which regulate cell functions …
Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity
T Anastassiadis, SW Deacon, K Devarajan, H Ma… - Nature …, 2011 - nature.com
Small-molecule protein kinase inhibitors are widely used to elucidate cellular signaling
pathways and are promising therapeutic agents. Owing to evolutionary conservation of the …
pathways and are promising therapeutic agents. Owing to evolutionary conservation of the …
The selectivity of protein kinase inhibitors: a further update
J Bain, L Plater, M Elliott, N Shpiro, CJ Hastie… - Biochemical …, 2007 - portlandpress.com
The specificities of 65 compounds reported to be relatively specific inhibitors of protein
kinases have been profiled against a panel of 70–80 protein kinases. On the basis of this …
kinases have been profiled against a panel of 70–80 protein kinases. On the basis of this …
Chemical inhibitors of protein kinases
AJ Bridges - Chemical reviews, 2001 - ACS Publications
Many excellent and up to date reviews on kinase inhibitors exist, and this area certainly
does not meet the normal criteria for a Chemical Reviews article. However, most of these …
does not meet the normal criteria for a Chemical Reviews article. However, most of these …
Tinkering outside the kinase ATP box: allosteric (type IV) and bivalent (type V) inhibitors of protein kinases
KJ Cox, CD Shomin, I Ghosh - Future medicinal chemistry, 2011 - Taylor & Francis
Many members of the protein kinase family have emerged as key targets for
pharmacological intervention, most notably in cancer. However, the high sequence and …
pharmacological intervention, most notably in cancer. However, the high sequence and …
Small-molecule inhibitors binding to protein kinase. Part II: the novel pharmacophore approach of type II and type III inhibition
AC Backes, B Zech, B Felber, B Klebl… - Expert opinion on drug …, 2008 - Taylor & Francis
Background: Protein kinases are essential enzymes propagating cellular signal transduction
processes and consequently emerged as central targets for drug discovery against a wide …
processes and consequently emerged as central targets for drug discovery against a wide …
New directions in targeting protein kinases: focusing upon true allosteric and bivalent inhibitors
V Lamba, I Ghosh - Current pharmaceutical design, 2012 - ingentaconnect.com
Over the past decade, therapeutics that target subsets of the 518 human protein kinases
have played a vital role in the fight against cancer. Protein kinases are typically targeted at …
have played a vital role in the fight against cancer. Protein kinases are typically targeted at …