Protein kinase C-a PKC

The primary application of LNA has been in antisense therapy due to the aforementioned properties. It has been used to knock down human protein kinase C-a (PKC-ot) with greater efficiency than the corresponding phosphor-othioate ODN, as an inhibitor of human telomerase, to block the synthesis of RNA polymerase II and to inhibit human vascular smooth muscle cell growth. LNA-modified oligonucleotides have also been used in RNA interference (RNAi). ... 

Protein kinase C-a (PKC-a) is a cytoplasmic serine/threonine kinase that belongs to the family of isoenzymes involved in signal transduction in response to growth factors, hormones, and neurotransmitters. It regulates cell proliferation and differentiation. Overexpression of this kinase causes uncOTitrolled proliferation of cancer cells in several tumors. The antitumor activity of antisense inhibitors of PKC-a has been illustrated in cell culture studies [26,93] and in animal models [94]. A number... 

AP-1 A major transcriptional activator PKC, PKCa, 3, y Protein kinase C,a, P, y subforms... 

This mechanism may also underlie the FA-induced apoptosis in rat and human pancreatic / -cells. Ghronic treatment with high physiological levels of saturated FA, but not with mono- or polyunsaturated FA, triggers apoptosis in about 20% of cultured /1-cells [94]. Apoptosis restricted to saturated FA was also observed in primary cultured human / -cells, suggesting that this mechanism is potentially relevant in vivo in humans. Apoptosis was accompanied by a rapid nuclear translocation of protein kinase C-b (PKC-d) and subsequent lamin BI disassembly. This translocation was impaired by inhibition of phospholipase C, which also considerably reduced apoptosis. Furthermore, lamin BI disassembly and apoptosis were decreased by cell transfection with a dominant-negative mutant form of PKC- ... 

ACPD receptors are linked by G-proteins to the phosphoinositide-protein kinase C (PI-PKC) and adenylate cyclase-cyclic AMP second messenger systems (Conn and Desai, 1991 Winder and Conn, 1992). Actions on the PI system promote the release of Ca from intracellular stores (Conn and Desai, 1991). The most selective agonist for ACPD receptors is lS,3R-trans-ACPD, although Glu, ibotenate and Quis also act at these receptors. A related class of metabotropic receptors is activated by APB. Seven different metabotropic Glu receptors (mGluRl-7) have been cloned to date (Hollmann and Heinemann, 1994 Saugstad et al.,... 

The spatial and steric requirements for high affinity binding to protein kinase C (PKC), a macromolecule that has not yet been crystallized, were determined. Protein kinase C plays a critical role in cellular signal transduction and is in part responsible for cell differentiation. PKC was identified as the macromolecular target for the potent tumor-promoting phorbol esters (25). The natural agonists for PKC are diacylglycerols (DAG) (26). The arrows denote possible sites of interaction. 

The tjipanazoles (18, 19a-d, 20a-b) a group of A-glycosides of indolo-[2,3-a]carbazole, have been isolated from the moderately antifungal extract of the blue-green alga Tolypothrix tjipanasensis. These alkaloids do not exhibit antitumor or protein kinase C (PKC) inhibitory activity, which is in contrast with the... 

Heterologous desensitization is a form of desensitization which does not require agonist binding of the receptor. Second messenger dependent kinases such as protein kinase A (PKA) and protein kinase C (PKC) are involved in this form of receptor desensitization. Heterologous desensitization simply depends on the overall kinase activity which is regulated by many different stimuli. 

Fat Increased glucose transport GLUT4-translocation PI 3-kinase/Akt mediated translocation of GLUT4 into the plasma membrane. Potential involvement of atypical forms of protein kinase C (PKC and A)... 

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