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Asteropsins B-D, sponge-derived knottins with potential utility as a novel scaffold for oral peptide drugs.
- Source :
-
Biochimica et biophysica acta [Biochim Biophys Acta] 2014 Mar; Vol. 1840 (3), pp. 977-84. Date of Electronic Publication: 2013 Nov 10. - Publication Year :
- 2014
-
Abstract
- Background: Known linear knottins are unsuitable as scaffolds for oral peptide drug due to their gastrointestinal instability. Herein, a new subclass of knottin peptides from Porifera is structurally described and characterized regarding their potential for oral peptide drug development.<br />Methods: Asteropsins B-D (ASPB, ASPC, and ASPD) were isolated from the marine sponge Asteropus sp. The tertiary structures of ASPB and ASPC were determined by solution NMR spectroscopy and that of ASPD by homology modeling.<br />Results: The isolated asteropsins B-D, together with the previously reported asteropsin A (ASPA), compose a new subclass of knottins that share a highly conserved structural framework and remarkable stability against the enzymes in gastrointestinal tract (chymotrypsin, elastase, pepsin, and trypsin) and human plasma.<br />Conclusion: Asteropsins can be considered as promising peptide scaffolds for oral bioavailability.<br />General Significance: The structural details of asteropsins provide essential information for the engineering of orally bioavailable peptides.<br /> (Copyright © 2013 Elsevier B.V. All rights reserved.)
Details
- Language :
- English
- ISSN :
- 0006-3002
- Volume :
- 1840
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Biochimica et biophysica acta
- Publication Type :
- Academic Journal
- Accession number :
- 24225326
- Full Text :
- https://doi.org/10.1016/j.bbagen.2013.11.001