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Artigo Revisado por pares
BIBTEX RIS

Calmodulin antagonists of improved potency and specificity for use in the study of calmodulin biochemistry

1988; Elsevier BV; Volume: 37; Issue: 9 Linguagem: Inglês

10.1016/0006-2952(88)90434-0

ISSN

1873-2968

Autores

Sheila MacNeil, Martin Griffin, Andy Cooke, Nancy J. Pettett, Rebecca Dawson, Robin Owen, G. Michael Blackburn,

Tópico(s)

Diet, Metabolism, and Disease

Resumo

Syntheses are described for a range of N-(ω-aminoalkyl)-5-iodo- and -5-cyanonaphthalene1-sulphonamides. The selective activity of these compounds as inhibitors for calmodulin-dependent phosphodiesterase (EC 3.1.4.17) is compared with their activity for the calmodulin-independent but calcium-dependent enzymes protein kinase C and transglutaminase (EC 2.3.2.13). The results show a drastic improvement in the selectivity of effect for the 5-iodo-compounds compared with the widely-used drug, W7, N-(6-aminohexyl)-5-chloronaphthalene-1-sulphonamide.

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