title: Conformationally constrained mimetics of laminin peptide YIGSR as precursors for antimetastatic disintegrins.
abstract: Conformationally constrained mimetics of the laminin cell-adhesion site, YIGSR, are described. The site is the natural antagonist of the integrin-associated laminin receptor 1 (LAMR1) known to mediate metastatic tumor adhesion. The attachment of selected metastatic cell lines toward the constrained antagonists has been assessed. Observed differential responses prompted by folding preferences of the mimetics revealed stronger attachment activities for turnlike structures. The results permit the conformational design of antimetastatic disintegrins.
authors: Department of Chemistry, University of Leicester, Leicester LE1 7RH, UK.
authors: Angelo
authors: A
authors: Bella
authors: Helen
authors: H
authors: Lewis
authors: Jennifer
authors: J
authors: Phu
authors: Andrew R
authors: AR
authors: Bottrill
authors: Sharad C
authors: SC
authors: Mistry
authors: Christine E
authors: CE
authors: Pullar
authors: Maxim G
authors: MG
authors: Ryadnov
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D040761:Biomimetic Materials / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D019483:Disintegrins / Q000737:chemistry*; D005354:Fibrosarcoma / Q000188:drug therapy / Q000473:pathology; D006367:HeLa Cells; D006801:Humans; D007797:Laminin / Q000737:chemistry*; D008546:Melanoma, Experimental / Q000188:drug therapy / Q000473:pathology; D051379:Mice; D009842:Oligopeptides / Q000737:chemistry* / Q000494:pharmacology; D010456:Peptides, Cyclic / Q000737:chemistry* / Q000494:pharmacology; D011487:Protein Conformation; D017474:Receptors, Laminin / Q000037:antagonists & inhibitors; D012269:Ribosomal Proteins
chemical_list: D000970:Antineoplastic Agents; D019483:Disintegrins; D007797:Laminin; D009842:Oligopeptides; D010456:Peptides, Cyclic; C510624:RPSA protein, human; D017474:Receptors, Laminin; D012269:Ribosomal Proteins; C081571:tyrosyl-isoleucyl-glycyl-seryl-arginine