Synthesis of somatostatin analogs resistant to the action of trypsin.
The synthesis of a series of octapeptides based on the somatostatin analog cyclo(-Asn-Phe-Phe-D-Trp-Lys-Thr-Phe-Gaba-) containing the substitutions [Aap9], [D-Lys9], [L-Trp8, D-Lys9], [L-Orn9] and [D-aThr10] is reported. The analogs were designed and have been shown to inhibit proteolysis at the proposed (1) primary cleavage site between Lys9-Thr10 and thereby increase their stability to enzymic attack.
Allen
M C
MC
Ciba-Geigy Pharmaceuticals, Research Centre, Horsham, West Sussex, England.
Wade
R
R
D000595:Amino Acid Sequence; D007202:Indicators and Reagents; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000378:metabolism; D009904:Optical Rotation; D013004:Somatostatin / Q000031:analogs & derivatives* / Q000138:chemical synthesis*; D013379:Substrate Specificity; D014357:Trypsin
D007202:Indicators and Reagents; D009842:Oligopeptides; D013004:Somatostatin; D014357:Trypsin