Zur Synthese von Human-Little-Gastrin-I und dessen Leucin-15-, Norleucin-15- und Methoxinin-15-Analoga

Abstract
Human little gastrin exhibits a high tendency to air oxidation of its methionine-15 residue to the corresponding S-oxide derivative, with concomitant loss of biological activity. Since its leucine-15 analog, even if fully biologically active, differs significantly from the parent hormone in the immunological properties, the norleucine-15 and methoxinine-15 analogs were synthesized. For the required comparative analyses new syntheses of human little gastrin I and of its leucine-15 analog were additionally elaborated. Upon an optimized condensation of the fragments, followed by the deprotection step, partition chromatography and preparative high performance liquid chromatography led to the desired gastrins in satisfactory yields and high degree of purity as judged by the expected and known side products.

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