POLYPEPTIDE DERIVATIVES, METHOD OF CALCIUM CHANNEL INHIBITION Russian patent published in 1998 - IPC

Abstract RU 2120945 C1

FIELD: organic chemistry, chemistry of peptides. SUBSTANCE: invention relates to derivatives of polypeptides of the general formula (I): where A: A1-A4 is Leu-Phe-Glu-Cys-Cys-Leu-Gly- -Glu-; Cys-Ala-Glu-Phe-; Ser-Cys-Gly-His-; Leu-Ile-Glu-Cys-; A5 is Ala, Val, Gln, Asn; B: B6-B9 is Leu-Ser-Cys-Asp-; Ser-Lys-Cys-Lys-; Gly-Thr-Pro-Cys-; Val-Pro-Cys-Asp-; Phe-Ser- -Cys-Asp-; B10 is Ile, Lys, Glu; C: C11-C14 is Lys-Lys-Asn-Gly-; Asp-Ser-Gly-Cys-; Lys-Asn-Trp-Asp-; Thr-Lys-Asn-Gly-; Asp-Arg-Pro-Asn; C15 is Lys, Cys; D: D16-D19 is Pro-Cys-Lys-Pro-; Gly-Thr-Leu-Glu-; Cys-Lys-Gly-Lys-; Cys-Ser-Lys-Thr-; D20 is Cys, Val, Gly, Lys; E: E21-E24 is Gly-Glu-Lys-Lys-; Ser-Pro-Thr- -Trp-; Cys-Leu-Glu-Pro-; E25 is Cys, Lys, Trp, Thr; F: F26-F30 is Ser-Gly-Gly-Trp-; Trp-Cys-Val-Tyr-; Lys-Leu-Cys-Ala-; Gly-Tyr- -Gly-Arg; F30 is Arg, Cys, Pro, Tyr; G: G31-G34 is Cys-Lys-Ile- -Asn-; Ser-Pro-Phe-; Glu-Ser-Pro-Phe-; Tyr-Ala-Ser-Tyr-; Cys-Leu-Lys-Val-; G35 is Phe, Tyr, simple bond; Z is OH, Cys- -Leu-Lys-Val-OH, Cys-Leu-Ile-OH; Ser-Tyr-Lys-Thr-Leu-OH being six cysteine residues in compound (I) are bound by disulfide bonds. Method of inhibition of calcium channel involves administration of polypeptide in cell at effective amount. Invention can be used in medicine for treatment of mammals with sicknesses mediated by calcium channels. EFFECT: simplified method, enhanced effectiveness of method. 3 cl, 9 ex, 9 tbl

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RU 2 120 945 C1

Authors

Din M.Nejson Ii

Duglas Fillips

Nikolas Sakkomano

Robert A.Volkmann

Dates

1998-10-27Published

1993-09-28Filed