SILVIO ERNESTO PEREA RODRIGUEZ,OSVALDO REYES ACOSTA,NELSON FRANCISCO SANTIAGO VISPO,YAQUELÍN PUCHADES IZAGUIRRE,RICARDO SILVA RODRIGUEZ,ALEJANDRO MORO SORIA,ALICIA SANTOS SAVIO,LUIS JAVIER GONZALEZ LO
申请号:
IS7320
公开号:
IS2906B
申请日:
2004.06.16
申请国别(地区):
IS
年份:
2014
代理人:
摘要:
11 specific peptides (A), also their homologous variants and mimetics produced by synthetic or recombinant methods, that bind to the phosphorylation site of casein kinase II, are new. 11 specific peptides (A), of formulae (1)-(11) also their homologous variants and mimetics produced by synthetic or recombinant methods, that bind to the phosphorylation site of casein kinase II, are new. (1) Cys-Ser-Val-Arg-Gln-Gly-Pro-Val-Gln-Lys-Cys; (2) Cys-Ser-Ser-Cys-Gln-Asn-Ser-Pro-Ala-Leu-Cys; (3) Cys-Gln-Ile-Pro-Gln-Arg-Thr-Ala-Thr-Arg-Cys; (4) Cys-Ala-Lys-Gln-Arg-Thr-Asp-Pro-Gly-Tyr-Cys; (5) Cys-Trp-Met-Ser-Pro-Arg-His-Leu-Gly-Thr-Cys; (6) Cys-Arg-Asn-Cys-Thr-Val-Ile-Gln-Phe-Ser-Cys; (7) Cys-His-Tyr-Ile-Ala-Gly-Thr-Val-Gln-Gly-Cys; (8) Cys-Pro-Leu-Val-Ser-Leu-Arg-Asp-His-Ser-Cys; (9) Cys-Lys-Gln-Ser-Tyr-Leu-His-His-Leu-Leu-Cys; (10) Cys-Phe-Gln-Pro-Leu-Thr-Pro-Leu-Cys-Arg-Cys; and (11) Cys-Gln-Ser-Tyr-His-Glu-Leu-Leu-Leu-Gln-Cys. An independent claim is also included for an expression vector, functional in mammalian cells, that contains a DNA sequence encoding (A). ACTIVITY : Cytostatic. H-125 non-small cell lung carcinoma cells were implanted in mice together with 10 mg/kg of peptide (1) Cys-Ser-Val-Arg-Gln-Gly-Pro-Val-Gln-Lys-Cys and the same dose of peptide administered every other day. After 30 days, the tumor volume was about 0.6 mm 3>; compared with 1.5 mm 3>; for untreated controls. MECHANISM OF ACTION : (A) inhibit casein kinase II and also bind to the phosphorylation site at positions 28-38 in the E7 oncoprotein of HPV, so are toxic to cervical carcinoma cells and also increase the sensitivity of such cells to interferon; Gene therapy.