| Prototypic G protein-coupled receptor for the intestinotrophic factor glucagon-like peptide 2. | |
| | |
MedLine Citation:
|
PMID: 9990065 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
|
Glucagon-like peptide 2 (GLP-2) is a 33-aa proglucagon-derived peptide produced by intestinal enteroendocrine cells. GLP-2 stimulates intestinal growth and up-regulates villus height in the small intestine, concomitant with increased crypt cell proliferation and decreased enterocyte apoptosis. Moreover, GLP-2 prevents intestinal hypoplasia resulting from total parenteral nutrition. However, the mechanism underlying these actions has remained unclear. Here we report the cloning and characterization of cDNAs encoding rat and human GLP-2 receptors (GLP-2R), a G protein-coupled receptor superfamily member expressed in the gut and closely related to the glucagon and GLP-1 receptors. The human GLP-2R gene maps to chromosome 17p13.3. Cells expressing the GLP-2R responded to GLP-2, but not GLP-1 or related peptides, with increased cAMP production (EC50 = 0.58 nM) and displayed saturable high-affinity radioligand binding (Kd = 0.57 nM), which could be displaced by synthetic rat GLP-2 (Ki = 0.06 nM). GLP-2 analogs that activated GLP-2R signal transduction in vitro displayed intestinotrophic activity in vivo. These results strongly suggest that GLP-2, like glucagon and GLP-1, exerts its actions through a distinct and specific novel receptor expressed in its principal target tissue, the gastrointestinal tract. |
| | |
Authors:
|
D G Munroe; A K Gupta; F Kooshesh; T B Vyas; G Rizkalla; H Wang; L Demchyshyn; Z J Yang; R K Kamboj; H Chen; K McCallum; M Sumner-Smith; D J Drucker; A Crivici |
Related Documents
:
|
2981675 - Involvement of plasma membrane enzymes in the proteolytic cleavage of luteinizing hormo... 4039605 - One-step immunoaffinity purification of active progesterone receptor. further evidence ... 2856405 - Solubilization of receptors for thyrotropin-releasing hormone from gh4c1 rat pituitary ... 9010775 - Purification and functional reconstitution with gtp-binding regulatory proteins of hexa... 11465095 - Activation-induced apoptosis and cell surface expression of fas (cd95) ligand are recip... 15240635 - Increased expression of the relaxin receptor (lgr7) in human endometrium during the sec... |
Publication Detail:
|
Type: Journal Article |
Journal Detail:
|
Title: Proceedings of the National Academy of Sciences of the United States of America Volume: 96 ISSN: 0027-8424 ISO Abbreviation: Proc. Natl. Acad. Sci. U.S.A. Publication Date: 1999 Feb |
Date Detail:
|
Created Date: 1999-03-25 Completed Date: 1999-03-25 Revised Date: 2009-11-18 |
Medline Journal Info:
|
Nlm Unique ID: 7505876 Medline TA: Proc Natl Acad Sci U S A Country: UNITED STATES |
Other Details:
|
Languages: eng Pagination: 1569-73 Citation Subset: IM |
Affiliation:
|
Allelix Biopharmaceuticals Inc., 6850 Goreway Drive, Mississauga, Ontario L4V 1V7, Canada. dmunroe@allelix.com |
| Data Bank Information | |
Bank Name/Acc. No.:
|
GENBANK/AF105367; AF105368 |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
Amino Acid Sequence Animals Brain / metabolism COS Cells Cloning, Molecular Cyclic AMP / metabolism GTP-Binding Proteins / metabolism* Gene Library Glucagon-Like Peptide 1 Glucagon-Like Peptide 2 Humans Intestines / metabolism Kinetics Molecular Sequence Data Organ Specificity Peptide Fragments / pharmacology Peptides / pharmacology, physiology* Rats Receptors, Glucagon / chemistry, genetics, physiology* Sequence Alignment Sequence Homology, Amino Acid Signal Transduction Structure-Activity Relationship Transfection |
| Chemical | |
Reg. No./Substance:
|
0/Glucagon-Like Peptide 2; 0/Peptide Fragments; 0/Peptides; 0/Receptors, Glucagon; 0/glucagon-like peptide receptor; 60-92-4/Cyclic AMP; 89750-14-1/Glucagon-Like Peptide 1; EC 3.6.1.-/GTP-Binding Proteins |
| Comments/Corrections | |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Mutation of Pten/Mmac1 in mice causes neoplasia in multiple organ systems.
Next Document: Multinuclear solid-state three-dimensional MRI of bone and synthetic calcium phosphates.