title: Structure determination and synthesis of lysine isopeptides influencing on cell proliferation.
abstract: The clavicepamines are lysine-rich basic proteins isolated from saprophytic culture of ergot (Claviceps purpurea), having human pharmacological importance. Based on structure determinations, it was demonstrated that the epsilon-lysine (poly)peptides are the fundamental structural units of clavicepamines. To study the relationship between chemical structure and biological effect, solution and solid-phase synthesis of lysine isopeptides were performed. Poly-epsilon-lysines were synthesized with polycondensation via application of p-nitrophenylester temporarily protecting groups together with simultaneous activation. The biological investigations of poly-epsilon-lysines showed a cell-proliferation retarding effect, so they inhibit growth of some animal tumors, practically without toxic side effects.
authors.affiliation: Department of Organic Chemistry, Eötvös University, Budapest, Hungary.
authors.forename: G
authors.initials: G
authors.lastname: Szókán
authors.forename: M
authors.initials: M
authors.lastname: Almás
authors.forename: K
authors.initials: K
authors.lastname: Krizsán
authors.forename: A R
authors.initials: AR
authors.lastname: Khlafulla
authors.forename: E
authors.initials: E
authors.lastname: Tyihák
authors.forename: B
authors.initials: B
authors.lastname: Szende
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D002851:Chromatography, High Pressure Liquid; D002855:Chromatography, Thin Layer; D002967:Claviceps / Q000737:chemistry*; D003619:Dansyl Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000302:isolation & purification; D005656:Fungal Proteins / Q000737:chemistry; D006801:Humans; D008239:Lysine / Q000737:chemistry; D008970:Molecular Weight; D011107:Polylysine / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D003619:Dansyl Compounds; D005656:Fungal Proteins; D011107:Polylysine; D008239:Lysine