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Synonyms: CVQ1IAY2G6 | FE 203799 | FE203799
Compound class:
Peptide or derivative
Comment: Apraglutide (FE 203799), a synthetic 33-amino-acid peptide and a long-acting GLP-2 analogue, with amino acid substitutions (Ala2>Gly, Met10>Ahx, Asn11>D-Phe, Asn16>Leu). The peptide's circulating half-life is elevated by the incorporation of Ahx (aminocaproic acid) in place of lysine which reduces degradation by lysine-targeting proteolytic enzymes. Apraglutide enhances adaptation and linear intestinal growth in a neonatal piglet model with total resection of the ileum that mimics human short bowel syndrome [2].
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
| References |
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1. Hargrove DM, Alagarsamy S, Croston G, Laporte R, Qi S, Srinivasan K, Sueiras-Diaz J, Wiśniewski K, Hartwig J, Lu M et al.. (2020)
Pharmacological Characterization of Apraglutide, a Novel Long-Acting Peptidic Glucagon-Like Peptide-2 Agonist, for the Treatment of Short Bowel Syndrome. J Pharmacol Exp Ther, 373 (2): 193-203. [PMID:32075870] |
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2. Slim GM, Lansing M, Wizzard P, Nation PN, Wheeler SE, Brubaker PL, Jeppesen PB, Wales PW, Turner JM. (2019)
Novel Long-Acting GLP-2 Analogue, FE 203799 (Apraglutide), Enhances Adaptation and Linear Intestinal Growth in a Neonatal Piglet Model of Short Bowel Syndrome with Total Resection of the Ileum. JPEN J Parenter Enteral Nutr, 43 (7): 891-898. [PMID:30614011] |
