A bicyclic cispentacin derivative as a novel reverse turn inducer in a GnRH mimetic.
A cispentacin-derived bicyclic beta-amino acid (Bic) has been synthesized and incorporated into the 6-position of GnRH. The new GnRH analogue has been characterized with respect to its structure in solution and its activity and affinity toward the human GnRH receptor.
D000595:Amino Acid Sequence; D000596:Amino Acids / Q000138:chemical synthesis* / Q000737:chemistry; D001643:Bridged Bicyclo Compounds / Q000737:chemistry* / Q000494:pharmacology; D018360:Crystallography, X-Ray; D003515:Cycloleucine / Q000031:analogs & derivatives / Q000494:pharmacology; D007987:Gonadotropin-Releasing Hormone / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000737:chemistry; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D018716:Molecular Mimicry; D015394:Molecular Structure; D011487:Protein Conformation; D011966:Receptors, LHRH / Q000502:physiology; D013329:Structure-Activity Relationship
D000596:Amino Acids; D001643:Bridged Bicyclo Compounds; D011966:Receptors, LHRH; D003515:Cycloleucine; D007987:Gonadotropin-Releasing Hormone; C065594:cispentacin