Nucleotides that modulate the expression of protein-kinase C beta-1 isoforms and their use as skin depigmenting agents

摘要

Oligonucleotide (ON), containing 7-25, preferably 20, nucleotides, that can hybridize specifically with the gene, or gene product, encoding protein kinase C beta -1 (PKCb1) is new. ACTIVITY : Dermatological. No details of tests for dermatological activity are given. MECHANISM OF ACTION : Inhibiting melanin synthesis by preventing expression of PKCb1, an enzyme involved in the first step (phosphorylation of tyrosine) of melanin biosynthesis. M4Beu melanocytes were cultured for 3 days in presence of 1 mu M oligonucleotide (1) ACAC 4AGGCTCAACGATG (1) then the confluent cells washed; lysed; proteins separated by electrophoresis, and the membrane incubated with labeled antibody against human PCKb1, followed by chemiluminescent detection. Inhibition of PKCb1 was 100% at the protein level and 55% at the level of RNA expression.