[HTML][HTML] Substrate affinity differentially influences protein kinase C regulation and inhibitor potency
RF Sommese, S Sivaramakrishnan - Journal of Biological Chemistry, 2016 - ASBMB
The overlapping network of kinase-substrate interactions provides exquisite specificity in cell
signaling pathways, but also presents challenges to our ability to understand the …
signaling pathways, but also presents challenges to our ability to understand the …
[HTML][HTML] Distinct structural mechanisms determine substrate affinity and kinase activity of protein kinase Cα
Protein kinase Cα (PKCα) belongs to the family of AGC kinases that phosphorylate multiple
peptide substrates. Although the consensus sequence motif has been identified and used to …
peptide substrates. Although the consensus sequence motif has been identified and used to …
[HTML][HTML] ATP competitive protein kinase C inhibitors demonstrate distinct state-dependent inhibition
IM Smith, N Hoshi - PLoS One, 2011 - journals.plos.org
We previously reported that some ATP competitive protein kinase C (PKC) inhibitors are
either competitive or uncompetitive inhibitors with respect to substrate peptides. In this …
either competitive or uncompetitive inhibitors with respect to substrate peptides. In this …
[HTML][HTML] Active site inhibitors protect protein kinase C from dephosphorylation and stabilize its mature form
Conformational changes acutely control protein kinase C (PKC). We have previously shown
that the autoinhibitory pseudosubstrate must be removed from the active site in order for 1) …
that the autoinhibitory pseudosubstrate must be removed from the active site in order for 1) …
[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 C intervention—the state of play
J Roffey, C Rosse, M Linch, A Hibbert… - Current opinion in cell …, 2009 - Elsevier
Intervention in protein kinase C (PKC) has a chequered history, partly because of the poor
selectivity of many inhibitors and partly a reflection of the sometimes antagonistic action of …
selectivity of many inhibitors and partly a reflection of the sometimes antagonistic action of …
Insight into intra-and inter-molecular interactions of PKC: design of specific modulators of kinase function
V Kheifets, D Mochly-Rosen - Pharmacological research, 2007 - Elsevier
Protein kinase C (PKC) is a family of kinases that are critical in many cellular events. These
enzymes are activated by lipid-derived second messengers, are dependent on binding to …
enzymes are activated by lipid-derived second messengers, are dependent on binding to …
Divergent modulation of Src-family kinase regulatory interactions with ATP-competitive inhibitors
SE Leonard, AC Register, R Krishnamurty… - ACS Chemical …, 2014 - ACS Publications
Multidomain protein kinases, central controllers of signal transduction, use regulatory
domains to modulate catalytic activity in a complex cellular environment. Additionally, these …
domains to modulate catalytic activity in a complex cellular environment. Additionally, these …
[HTML][HTML] Molecular mechanism of regulation of the atypical protein kinase C by N-terminal domains and an allosteric small compound
H Zhang, S Neimanis, LA Lopez-Garcia, JM Arencibia… - Chemistry & biology, 2014 - cell.com
Protein kinases play important regulatory roles in cells and organisms. Therefore, they are
subject to specific and tight mechanisms of regulation that ultimately converge on the …
subject to specific and tight mechanisms of regulation that ultimately converge on the …
Protein kinase C pharmacology: refining the toolbox
AX Wu-Zhang, AC Newton - Biochemical Journal, 2013 - portlandpress.com
PKC (protein kinase C) has been in the limelight since the discovery three decades ago that
it acts as a major receptor for the tumour-promoting phorbol esters. Phorbol esters, with their …
it acts as a major receptor for the tumour-promoting phorbol esters. Phorbol esters, with their …