Rationally designed peptide regulators of protein kinase C

EN Churchill, N Qvit, D Mochly-Rosen - Trends in Endocrinology & …, 2009 - cell.com
Protein–protein interactions sequester enzymes close to their substrates. Protein kinase C
(PKC) is one example of a ubiquitous signaling molecule with effects that are dependent …

[HTML][HTML] Modulating protein kinase C signal transduction

D Mochly-Rosen, LM Kauvar - Advances in pharmacology, 1998 - Elsevier
Protein Kinase C (PKC) is a family of serine–threonine kinases found in most cell types
whose activity has a strong influence on a wide variety of signal transduction events …

Competitive inhibitors and allosteric activators of protein kinase C isoenzymes: a personal account and progress report on transferring academic discoveries to the …

GR Budas, T Koyanagi, EN Churchill… - Biochemical Society …, 2007 - portlandpress.com
PKC (protein kinase C) isoenzymes are related protein kinases, involved in many signalling
events in normal state and in disease. Basic research into identifying the molecular basis of …

Isozyme-specific inhibitors and activators of protein kinase C

D Schechtman, D Mochly-Rosen - Methods in enzymology, 2002 - Elsevier
In cells, signal transduction often occurs within “signaling complexes” where physical
associations among several enzymes are coordinated by scaffold proteins. 1 The scaffold is …

Toward the identification of selective modulators of protein kinase C (PKC) isozymes: establishment of a binding assay for PKC isozymes using synthetic C1 peptide …

M Shindo, K Irie, A Nakahara, H Ohigashi… - Bioorganic & medicinal …, 2001 - Elsevier
Conventional and novel protein kinase C (PKC) isozymes contain two cysteine-rich C1
domains (C1A and C1B), both of which are candidate phorbol-12, 13-dibutyrate (PDBu) …

Irreversible Inactivation of Protein Kinase C by a Peptide-Substrate Analog (∗)

NE Ward, KR Gravitt, CA O'Brian - Journal of Biological Chemistry, 1995 - ASBMB
Protein kinase C (PKC) is a phospholipid-dependent isozyme family that plays a pivotal role
in mammalian signal-transduction pathways that mediate cell growth and differentiation and …

Peptide inhibitors targeting protein kinases

H Eldar-Finkelman, M Eisenstein - Current pharmaceutical …, 2009 - ingentaconnect.com
Phosphorylation by protein kinases is a central theme in biological systems. Aberrant protein
kinase activity has been implicated in a variety of human diseases, therefore, modulation 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 …

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 …

A highly potent and selective PKCα inhibitor generated via combinatorial modification of a peptide scaffold

JH Lee, SK Nandy, DS Lawrence - Journal of the American …, 2004 - ACS Publications
A potent and highly selective inhibitor of protein kinase C α has been generated via the
combinatorial modification of a consensus sequence peptide. The inhibitor displays a K i of …