Asteropsins B-D, sponge-derived knottins with potential utility as a novel scaffold for oral peptide drugs.

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.

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.

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

SUBMITTER: Li H 

PROVIDER: S-EPMC4139099 | biostudies-literature | 2014 Mar

REPOSITORIES: biostudies-literature