Target Information
Target General Information | Top | |||||
---|---|---|---|---|---|---|
Target ID |
T34843
(Former ID: TTDNS00544)
|
|||||
Target Name |
Glucagon-like peptide 2 receptor (GLP2R)
|
|||||
Synonyms |
GLP2R; GLP2 receptor
Click to Show/Hide
|
|||||
Gene Name |
GLP2R
|
|||||
Target Type |
Successful target
|
[1] | ||||
Disease | [+] 1 Target-related Diseases | + | ||||
1 | Neonatal malabsorption syndrome [ICD-11: KB89] | |||||
Function |
This is a receptor for glucagon-like peptide 2. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
Click to Show/Hide
|
|||||
BioChemical Class |
GPCR secretin
|
|||||
UniProt ID | ||||||
Sequence |
MKLGSSRAGPGRGSAGLLPGVHELPMGIPAPWGTSPLSFHRKCSLWAPGRPFLTLVLLVS
IKQVTGSLLEETTRKWAQYKQACLRDLLKEPSGIFCNGTFDQYVCWPHSSPGNVSVPCPS YLPWWSEESSGRAYRHCLAQGTWQTIENATDIWQDDSECSENHSFKQNVDRYALLSTLQL MYTVGYSFSLISLFLALTLLLFLRKLHCTRNYIHMNLFASFILRTLAVLVKDVVFYNSYS KRPDNENGWMSYLSEMSTSCRSVQVLLHYFVGANYLWLLVEGLYLHTLLEPTVLPERRLW PRYLLLGWAFPVLFVVPWGFARAHLENTGCWTTNGNKKIWWIIRGPMMLCVTVNFFIFLK ILKLLISKLKAHQMCFRDYKYRLAKSTLVLIPLLGVHEILFSFITDDQVEGFAKLIRLFI QLTLSSFHGFLVALQYGFANGEVKAELRKYWVRFLLARHSGCRACVLGKDFRFLGKCPKK LSEGDGAEKLRKLQPSLNSGRLLHLAMRGLGELGAQPQQDHARWPRGSSLSECSEGDVTM ANTMEEILEESEI Click to Show/Hide
|
|||||
3D Structure | Click to Show 3D Structure of This Target | AlphaFold |
Drugs and Modes of Action | Top | |||||
---|---|---|---|---|---|---|
Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
1 | Teduglutide | Drug Info | Approved | Short bowel syndrome | [1], [2], [3] | |
Clinical Trial Drug(s) | [+] 3 Clinical Trial Drugs | + | ||||
1 | Elsiglutide | Drug Info | Phase 2 | Diarrhea | [4] | |
2 | SAN-134 | Drug Info | Phase 1 | Osteoporosis | [5] | |
3 | ZP-1848 | Drug Info | Phase 1 | Inflammatory bowel disease | [6] | |
Mode of Action | [+] 2 Modes of Action | + | ||||
Modulator | [+] 5 Modulator drugs | + | ||||
1 | Teduglutide | Drug Info | [1] | |||
2 | Elsiglutide | Drug Info | [7] | |||
3 | ZP-1848 | Drug Info | [9] | |||
4 | AMX-256 | Drug Info | [10] | |||
5 | FE-203799 | Drug Info | [10] | |||
Inhibitor | [+] 1 Inhibitor drugs | + | ||||
1 | SAN-134 | Drug Info | [8] |
Cell-based Target Expression Variations | Top | |||||
---|---|---|---|---|---|---|
Cell-based Target Expression Variations |
Different Human System Profiles of Target | Top |
---|---|
Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Pathway Affiliation
Biological Network Descriptors
|
There is no similarity protein (E value < 0.005) for this target
|
KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
---|---|---|---|
Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
|
Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy |
Degree | 1 | Degree centrality | 1.07E-04 | Betweenness centrality | 0.00E+00 |
---|---|---|---|---|---|
Closeness centrality | 1.77E-01 | Radiality | 1.29E+01 | Clustering coefficient | 0.00E+00 |
Neighborhood connectivity | 1.50E+01 | Topological coefficient | 1.00E+00 | Eccentricity | 13 |
Download | Click to Download the Full PPI Network of This Target | ||||
Chemical Structure based Activity Landscape of Target | Top |
---|---|
Target Profiles in Patients | Top | |||||
---|---|---|---|---|---|---|
Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
---|---|---|---|---|---|---|
KEGG Pathway | [+] 1 KEGG Pathways | + | ||||
1 | Neuroactive ligand-receptor interaction | |||||
Reactome | [+] 2 Reactome Pathways | + | ||||
1 | G alpha (s) signalling events | |||||
2 | Glucagon-type ligand receptors | |||||
WikiPathways | [+] 3 WikiPathways | + | ||||
1 | GPCRs, Class B Secretin-like | |||||
2 | GPCR ligand binding | |||||
3 | GPCR downstream signaling |
References | Top | |||||
---|---|---|---|---|---|---|
REF 1 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7049). | |||||
REF 3 | ClinicalTrials.gov (NCT02099084) Short Bowel Syndrome and Teduglutide VS Placebo. U.S. National Institutes of Health. | |||||
REF 4 | ClinicalTrials.gov (NCT01543451) Proof-of-Concept Study in Cancer Patients to Assess Efficacy of Elsiglutide in Preventing Chemotherapy-Induced Diarrhea. U.S. National Institutes of Health. | |||||
REF 5 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020865) | |||||
REF 6 | ClinicalTrials.gov (NCT00868660) Healthy Normal Single Ascending Dose and Crohn's Patient Multiple Ascending Dose. | |||||
REF 7 | Poster Abstracts. Volume 10, Issue Supplement S8, pages 126-209, December 2014. | |||||
REF 8 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020865) | |||||
REF 9 | US patent application no. 8,580,918, Peptidic glp-2 agonists. | |||||
REF 10 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 250). |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.