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Kemptide is an inhibitor drug that inhibits protein kinase C (PKC). Kemptide binds to the phosphorylated form of PKC and prevents it from translocating into the cell membrane. When PKC is bound by Kemptide, it cannot be phosphorylated, which prevents its activation. This results in a decrease in protein synthesis and cell proliferation. Kemptide has been shown to inhibit the growth of t84 cells and 3t3-l1 preadipocytes. In vitro assays have shown that basic fibroblasts are more sensitive to Kemptide than basic protein, which may be due to steric interactions with the enzyme.
Kemptide was structurally analyzed using X-ray crystallography, which confirmed its binding mode with PKC. The kinetic analysis showed that Kemptide has a slow rate of inhibition on PKC activity and competitively inhibits PKC with respect to ATP as a substrate molecule.
