Conformationally restricted biologically active peptides, method

Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Chemical aftertreatment – e.g. – acylation – methylation – etc.

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204 72, 204 78, 20415782, 530303, 530311, 530312, 530315, C07K 100, C25B 300

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active

053648510

ABSTRACT:
Electrochemical methods, preferably the Kolbe coupling reaction, are utilized to create intramolecularly bridged peptides, segments or peptide isosteres which are conformationally restricted and preferably, biologically active. Preferably, the peptide analogues contain methylene groups bridging particular amino acid side chains. Analogues of a variety of peptide hormones, including insulin, insulin-like growth factors, somatostatin, melanocyte stimulating hormone, and the like are prepared by the above methods. Such peptides are useful as agonists or antagonists for treatment of diseases associated with deficiency of the hormone or dysregulation of hormone activity, as well as for mechanistic studies to understand the interactions between peptide hormones and cells.

REFERENCES:
patent: 3446789 (1969-05-01), Rudinger et al.
patent: 3816385 (1974-06-01), Gillessen et al.
patent: 4191754 (1980-03-01), Veber et al.
patent: 4485039 (1984-11-01), Hruby et al.
Morikawa, et al., "Synthesis of EelCalcitonin and [Asu.sup.1,7 ]-Eel Calcitonin: Contribution of the Disulfide Bond to the Hormonal Activty", Experientia, pp. 1104-1106, 1976.
Hase et al., "Synthesis of a Biologically Active Analog of Deamino-8-Arginine-Vasopress in which Does not Contain a Disulphide Bond", Experientia, 25, 1239-1240, 1969.
Nutt et al. "Useful Intermediates for Synthesis of Dicarba Analogues of Cystine Peptides: Selectively Protected .alpha.-Aminosuberic Acid and .alpha.,.alpha..sup.1 -Diaminosuberic Acid of Defined Stereochemistry", J. Org. Chem., vol. 45, No. 15, pp. 3078-3080, 1980.
Charpentier et al., "Cyclic cholecystokinin analogues with high selectivity for central receptors", Proc. Natl. Acad. Sci. USA, vol. 85, pp. 1968-1972, Mar. 1988.
Ho et al., "Synthesis of cyclic (Asu.sup.1,7)-eel calcitonin by segment synthesis condensation on solid support", Proc. Eleventh Amer. Peptide Symp., ed. by J. Rivier & G. Marshall (1990). ESCOM.
Veber et al., "Highly active cyclic and bicyclic somatostatin analogues of reduced ring size", Nature, vol. 280, pp. 512-514, Aug. 1979.

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