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Literature DB >> 1659814

Potent and preferential inhibition of Ca2+/calmodulin-dependent protein kinase II by K252a and its derivative, KT5926.

Y Hashimoto¹, T Nakayama, T Teramoto, H Kato, T Watanabe, M Kinoshita, K Tsukamoto, K Tokunaga, K Kurokawa, S Nakanishi.

Abstract

Effects of protein kinase inhibitors, K252a and its derivative KT5926, on Ca2+/calmodulin-dependent protein kinase II were examined. Both compounds potently inhibited Ca2+/calmodulin-dependent protein kinase II. Kinetic analyses indicated that the inhibitory effect of K252a and KT5926 was competitive with respect to ATP (Ki: 1.8 and 4.4 nM, respectively) and noncompetitive with respect to the substrates. Taken together with a previous report (Nakanishi et al. Mol. Pharmacol. 37, 482, 1990) concerning the Ki values of these compounds for ATP with various protein kinases, the results suggest that K252a and KT5926 are potent and preferential inhibitors of Ca2+/calmodulin-dependent protein kinase II.

Entities: Chemical

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Year: 1991 PMID： 1659814 DOI： 10.1016/s0006-291x(05)81436-6

Source DB: PubMed Journal: Biochem Biophys Res Commun ISSN： 0006-291X Impact factor: 3.575

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Potent and preferential inhibition of Ca2+/calmodulin-dependent protein kinase II by K252a and its derivative, KT5926.

1. The trkA receptor mediates growth cone turning toward a localized source of nerve growth factor.

2. Localized sources of neurotrophins initiate axon collateral sprouting.

3. K252a: a new blocker of the cell-cycle at G1 phase in a human hepatoma cell line.

4. Ceramide alters endothelial cell permeability by a nonapoptotic mechanism.

5. Neurotrophins protect cultured cerebellar granule neurons against the early phase of cell death by a two-component mechanism.

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