发明名称 POLYPEPTIDE DERIVATIVES, METHOD OF CALCIUM CHANNEL INHIBITION
摘要 FIELD: organic chemistry, chemistry of peptides. SUBSTANCE: invention relates to derivatives of polypeptides of the general formula (I): $$$ where A: $$$ is Leu-Phe-Glu-Cys-Cys-Leu-Gly- -Glu-; Cys-Ala-Glu-Phe-; Ser-Cys-Gly-His-; Leu-Ile-Glu-Cys-; $$$ is Ala, Val, Gln, Asn; B: $$$ is Leu-Ser-Cys-Asp-; Ser-Lys-Cys-Lys-; Gly-Thr-Pro-Cys-; Val-Pro-Cys-Asp-; Phe-Ser- -Cys-Asp-; $$$ is Ile, Lys, Glu; C: $$$ is Lys-Lys-Asn-Gly-; Asp-Ser-Gly-Cys-; Lys-Asn-Trp-Asp-; Thr-Lys-Asn-Gly-; Asp-Arg-Pro-Asn; $$$ is Lys, Cys; D: $$$ is Pro-Cys-Lys-Pro-; Gly-Thr-Leu-Glu-; Cys-Lys-Gly-Lys-; Cys-Ser-Lys-Thr-; $$$ is Cys, Val, Gly, Lys; E: $$$ is Gly-Glu-Lys-Lys-; Ser-Pro-Thr- -Trp-; Cys-Leu-Glu-Pro-; $$$ is Cys, Lys, Trp, Thr; F: $$$ is Ser-Gly-Gly-Trp-; Trp-Cys-Val-Tyr-; Lys-Leu-Cys-Ala-; Gly-Tyr- -Gly-Arg; $$$ is Arg, Cys, Pro, Tyr; G: $$$ is Cys-Lys-Ile- -Asn-; Ser-Pro-Phe-; Glu-Ser-Pro-Phe-; Tyr-Ala-Ser-Tyr-; Cys-Leu-Lys-Val-; $$$ 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
申请公布号 RU2120945(C1) 申请公布日期 1998.10.27
申请号 RU19950109941 申请日期 1993.09.28
申请人 PFAJZER INK.;EHN-PI-EHS FARMAS'JUTIKALZ, INK. 发明人 DIN M.NEJSON II;DUGLAS FILLIPS;NIKOLAS SAKKOMANO;ROBERT A.VOLKMANN
分类号 A61K38/00;A61K38/16;A61P1/00;A61P9/00;A61P9/06;A61P9/08;A61P9/12;A61P13/02;A61P15/00;A61P25/00;A61P43/00;C07K1/20;C07K14/00;C07K14/35;C07K14/435;(IPC1-7):C07K14/00 主分类号 A61K38/00
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