title: [A synthetic fragment of insulin with insulin-like biological activity].
abstract: We have used computer modeling of insulin 3-D structure and experimental data about action of site point mutation on insulin activity to design functionally important domain with signaling activity and synthesized peptide than might be sufficient for the binding to insulin receptor. The designed and synthesized peptide consist of ten residues and may be obtained in two forms: oxidized and reduced (with or without disulfide bond). The synthesized decapeptide peptide represents functionally important site for binding to the insulin receptor. Amino acid residues at position 1-8 correlate with B-chain of insulin at position (B19-B26). Residues at position 9.10 correlate with A-chain at position A-10-A21. This peptide was tested with cell culture L-929 (glucose uptake) in comparison with bioactive commercial peptide (R-G-FF) and insulin. It was shown that synthesized peptide exhibit biological activity at molar concentration 0.01-1 mkM. Our results successfully demonstrate the synthetic insulin fragment have insulin-like biological activity.
authors.forename: V N
authors.initials: VN
authors.lastname: Prozorovskiĭ
authors.forename: E M
authors.initials: EM
authors.lastname: Maksimova
authors.forename: A E
authors.initials: AE
authors.lastname: Alekseeva
authors.forename: O G
authors.initials: OG
authors.lastname: Grebenshchikova
authors.forename: O Iu
authors.initials: OIu
authors.lastname: Abakumova
authors.forename: N G
authors.initials: NG
authors.lastname: Kutsenko
authors.forename: T A
authors.initials: TA
authors.lastname: Tsvetkova
authors.forename: A I
authors.initials: AI
authors.lastname: Archakov
mesh_terms: D000818:Animals; D002478:Cells, Cultured; D002851:Chromatography, High Pressure Liquid; D005947:Glucose / Q000378:metabolism; D007328:Insulin / Q000737:chemistry* / Q000494:pharmacology; D007739:L Cells; D051379:Mice; D009842:Oligopeptides / Q000138:chemical synthesis / Q000235:genetics / Q000302:isolation & purification / Q000494:pharmacology*; D010446:Peptide Fragments / Q000138:chemical synthesis / Q000235:genetics / Q000302:isolation & purification / Q000494:pharmacology*; D017354:Point Mutation; D051381:Rats; D015398:Signal Transduction / Q000235:genetics
chemical_list: D007328:Insulin; D009842:Oligopeptides; D010446:Peptide Fragments; C106675:glycyl-glutamyl-arginyl-glycyl-phenylalanyl-phenylalanyl-tyrosine; D005947:Glucose
vernacular_title: Sinteticheskiĭ fragment insulina s insulinopodobnoĭ biologicheskoĭ aktivnost'iu.