Enhancing the gastrointestinal stability of salmon calcitonin through peptide stapling.

Autor:	Ghareeb H; Institute of Chemistry, The Hebrew University of Jerusalem, Jerusalem 9190401, Israel. metanis@mail.huji.ac.il., Metanis N; Institute of Chemistry, The Hebrew University of Jerusalem, Jerusalem 9190401, Israel. metanis@mail.huji.ac.il.; Casali Center for Applied Chemistry, The Hebrew University of Jerusalem, Jerusalem 9190401, Israel.; The Center for Nanoscience and Nanotechnology, The Hebrew University of Jerusalem, Jerusalem 9190401, Israel.
Jazyk:	angličtina
Zdroj:	Chemical communications (Cambridge, England) [Chem Commun (Camb)] 2023 May 30; Vol. 59 (44), pp. 6682-6685. Date of Electronic Publication: 2023 May 30.
DOI:	10.1039/d3cc01140b
Abstrakt:	Salmon calcitonin (sCT) is a polypeptide hormone available in the clinic. sCT is degraded in the gastrointestinal tract in minutes. In this work, a stapled analogue of salmon calcitonin, KaY-1(R24Q), was developed using the cooperative stapling between Lys and Tyr, with R24Q substitution. The analogue exhibited an improved stability in simulated gastric and intestinal fluid and retained the ability to activate the calcitonin receptor. This work will serve as a starting point for the development of an oral sCT drug.
Databáze:	MEDLINE
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