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Selective inhibition of protein kinase C isozymes by the indolocarbazole Gö 6976.
In vitro kinase assays indicated that interference with Ca2+ or its binding site is not responsible for the differential inhibition of PKC isozymes by Gö 6976, and Kinetic analysis revealed that PKC inhibition by Gö 7076 was competitive with respect to ATP, non-competitive withrespect to the protein substrate, and mixed type with respectto phosphatidylserine. Expand
Vanilloid (Capsaicin) receptors and mechanisms.
This paper focuses on hot pepper, which is eaten on a daily basis by an estimated one-quarter of the world’s population and has potential to be a biological target for regenerative medicine. Expand
Distribution of mRNA for vanilloid receptor subtype 1 (VR1), and VR1-like immunoreactivity, in the central nervous system of the rat and human.
The finding that VR1 is expressed not only in primary sensory neurons but also in several brain nuclei is of great importance in that it places VRs in a much broader perspective than pain perception. Expand
Regulation of cell apoptosis by protein kinase c δ
The isoforms of the PKC family are activated in response to mitogenic stimuli, to inflammatory stimuli, and to stress and play important roles in a variety of cellular functions including apoptosis.Expand
Crystal structure of the Cys2 activator-binding domain of protein kinase Cδ in complex with phorbol ester
The structure of the second activator-binding domain of PKC delta has been determined in complex with phorbol 13-acetate, which binds in a groove between two pulled-apart beta strands at the tip of the domain, explaining how the activator promotes insertion of PKCs into membranes. Expand
Molecular Determinants of Vanilloid Sensitivity in TRPV1*
Key residues (Met547 and Thr550) in transmembrane regions 3 and 4 of rat and human TRPV1 that confer vanilloid sensitivity, [3H]RTX binding and competitive antagonist binding to rabbit TRpV1 are identified and it is shown that these residues differentially affect ligand recognition as well as the assays of functional response versus ligand binding. Expand
Phosphorylation Specificities of Protein Kinase C Isozymes for Bovine Cardiac Troponin I and Troponin T and Sites within These Proteins and Regulation of Myofilament Properties*
Protein kinase C (PKC) isozymes α, δ, ε, and ζ, shown to be expressed in adult rat cardiomyocytes, displayed distinct substrate specificities in phosphorylating troponin I and troponin T subunits inExpand
Vanilloid (capsaicin) receptors in the rat: distribution in the brain, regional differences in the spinal cord, axonal transport to the periphery, and depletion by systemic vanilloid treatment
The present results suggest a discrete expression of vanilloid receptors in the brain stem (sensory nuclei); although intrinsic vanilloids receptor-expressing neurons are though to exist in the rat brain, they remain undetected by the present [3H]RTX autoradiography methodology. Expand
Expression and distribution of vanilloid receptor 1 (TRPV1) in the adult rat brain.
TRPV1 expression shows wide distribution in the brain of the rat, being found in astrocytes and pericytes as well as in neurons, which is consistent with multiple functions within the central nervous system, including the regulation of brain vasculature. Expand
Tyrosine Phosphorylation of Protein Kinase Cδ Is Essential for Its Apoptotic Effect in Response to Etoposide
A role of PKCδ in the apoptosis induced by etoposide is suggested and tyrosine phosphorylation of PK cδ as an important regulator of this effect is implicate. Expand