Target Information

Target General Infomation
Target ID
T36075
Former ID
TTDS00440
Target Name
Glucagon-like peptide 1 receptor
Gene Name
GLP1R
Synonyms
GLP-1 receptor; GLP-1-R; GLP-1R; GLP1R
Target Type
Successful
Disease Brain injury [ICD10: S09.90]
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1]
Irritable bowel syndrome; Dyspepsia [ICD9: 536.8, 564.1; ICD10: K30, K58]
Non-alcoholic steatohepatitis [ICD9: 571.8; ICD10: K76.0]
Non-insulin dependent diabetes [ICD10: E11.9]
Obesity [ICD9: 278; ICD10: E66]
Obesity; Diabetes [ICD9: 250, 278; ICD10: E08-E13, E66]
Type 2 diabetes [ICD9: 250; ICD10: E11]
Type 1/2 diabetes [ICD9: 250, 278; ICD10: E08-E13]
Type 1 diabetes [ICD9: 250; ICD10: E10]
Unspecified [ICD code not available]
Function
This is a receptor for glucagon-like peptide 1. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
BioChemical Class
GPCR secretin
Target Validation
T36075
UniProt ID
P43220
Sequence
MAGAPGPLRLALLLLGMVGRAGPRPQGATVSLWETVQKWREYRRQCQRSLTEDPPPATDL
FCNRTFDEYACWPDGEPGSFVNVSCPWYLPWASSVPQGHVYRFCTAEGLWLQKDNSSLPW
RDLSECEESKRGERSSPEEQLLFLYIIYTVGYALSFSALVIASAILLGFRHLHCTRNYIH
LNLFASFILRALSVFIKDAALKWMYSTAAQQHQWDGLLSYQDSLSCRLVFLLMQYCVAAN
YYWLLVEGVYLYTLLAFSVLSEQWIFRLYVSIGWGVPLLFVVPWGIVKYLYEDEGCWTRN
SNMNYWLIIRLPILFAIGVNFLIFVRVICIVVSKLKANLMCKTDIKCRLAKSTLTLIPLL
GTHEVIFAFVMDEHARGTLRFIKLFTELSFTSFQGLMVAILYCFVNNEVQLEFRKSWERW
RLEHLHIQRDSSMKPLKCPTSSLSSGATAGSSMYTATCQASCS
Drugs and Mode of Action
Drug(s) Albiglutide Drug Info Approved Type 2 diabetes [533123], [542408]
Bydureon Dual Chamber Pen Drug Info Approved Diabetes [550291]
Dulaglutide Drug Info Approved Type 2 diabetes [533123], [542621]
Exenatide Drug Info Approved Type 2 diabetes [530376], [532841], [536122], [551186]
Liraglutide Drug Info Approved Type 2 diabetes [531351], [538678]
Lixisenatide Drug Info Approved Type 2 diabetes [524621], [542409], [889440]
Pramlintide Drug Info Approved Type 1/2 diabetes [542505], [551186]
GLP-1 Drug Info Phase 3 Diabetes [549904]
LATIN T1D Drug Info Phase 3 Type 1 diabetes [551453]
Semaglutide Drug Info Phase 3 Type 2 diabetes [551972]
Taspoglutide Drug Info Phase 3 Type 1 diabetes [522861]
GTP-010 Drug Info Phase 2 Irritable bowel syndrome; Dyspepsia [536224]
Liraglutide Drug Info Phase 2 Obesity [531351], [538678]
Long-acting exenatide Drug Info Phase 2 Type 2 diabetes [530376], [532841], [551186]
LY-2428757 Drug Info Phase 2 Type 2 diabetes [522514]
LY2944876 Drug Info Phase 2 Diabetes [524727]
OI338GT Drug Info Phase 2 Type 1/2 diabetes [549240]
ORMD-0901 Drug Info Phase 2 Type 2 diabetes [548795]
PB-1023 Drug Info Phase 2 Type 2 diabetes [550056]
TT-401 Drug Info Phase 2 Type 2 diabetes [549337]
TTP-054 Drug Info Phase 2 Type 2 diabetes [524023]
UNI-rE-4 Drug Info Phase 2 Type 2 diabetes [530376], [532841], [551186]
CM3.1-AC100 Drug Info Phase 1 Diabetes [523118]
CNTO-3649 Drug Info Phase 1 Type 2 diabetes [522639]
CVX 096 Drug Info Phase 1 Type 2 diabetes [523368]
exenatide suspension Drug Info Phase 1 Unspecified [530376]
NN-9926 Drug Info Phase 1 Type 2 diabetes [523566]
OG987SC Drug Info Phase 1 Type 2 diabetes [549427]
PF-4603629 Drug Info Phase 1 Type 2 diabetes [530376], [532841], [551186]
SAR425899 Drug Info Phase 1 Diabetes [525144]
ZYOG1 Drug Info Phase 1 Diabetes [551790]
ZP2929 Drug Info Preclinical Obesity; Diabetes [551786]
CJC-1131 Drug Info Discontinued in Phase 2 Type 1 diabetes [547395]
LY-307161 SR Drug Info Discontinued in Phase 2 Type 2 diabetes [547340]
RG7685 Drug Info Discontinued in Phase 2 Type 2 diabetes [549037]
CM-GLP-1 Drug Info Discontinued in Phase 1/2 Brain injury [548232]
LY-315902 Drug Info Discontinued in Phase 1 Type 2 diabetes [546563]
AZM-134 Drug Info Terminated Type 2 diabetes [546517]
TH-0318 Drug Info Terminated Diabetes [547615]
Exenatide Drug Info Investigative Unspecified [537358]
Agonist AC-3174 Drug Info [530376], [532841], [551186]
CAM-2036 Drug Info [543638]
CM3.1-AC100 Drug Info [543638]
CNTO-3649 Drug Info [532107]
Dulaglutide Drug Info [533123]
GTP-010 Drug Info [536224]
LATIN T1D Drug Info [543638]
Liraglutide Drug Info [536122]
Long-acting exenatide Drug Info [530376], [532841]
NN-9926 Drug Info [551911]
ORMD-0901 Drug Info [531282]
Pramlintide Drug Info [536122]
Semaglutide Drug Info [543638]
SX-GLP1 Drug Info [543638]
Taspoglutide Drug Info [530530]
ZP-3022 Drug Info [543638]
ZYOG1 Drug Info [551790]
Modulator Albiglutide Drug Info [533123]
AMPE4L Drug Info [530376], [532841], [551186]
AZM-134 Drug Info [550154]
Bydureon Dual Chamber Pen Drug Info [532841]
CJC-1131 Drug Info [529693]
CM-GLP-1 Drug Info [529902]
CNTO-736 Drug Info [543638]
CVX 096 Drug Info [544390]
exenatide suspension Drug Info [530376]
F-18 exendin-4 derivative PET tracers Drug Info [530376], [532841], [551186]
GLP-1 Drug Info [543638]
Glucagon-like peptide-1 analog Drug Info [543638]
Lixisenatide Drug Info
LY-307161 SR Drug Info [526855]
LY-315902 Drug Info [526351]
LY2944876 Drug Info [1572591]
OG987SC Drug Info [551451]
OI338GT Drug Info [551450]
PB-1023 Drug Info [550091]
PF-4603629 Drug Info [530376], [532841]
PGC GLP-1 Drug Info [543638]
RG7685 Drug Info
SAR425899 Drug Info
SKL-18287 Drug Info [543638]
TH-0318 Drug Info [543638]
TT-401 Drug Info [532497]
TTP-054 Drug Info [544232]
UNI-rE-4 Drug Info [530376], [532841]
ZP2929 Drug Info
[123I] iodobenzoyl 12-Ex4 Drug Info [530376], [532841], [551186]
Modulator (allosteric modulator) BETP Drug Info [532871]
Inhibitor C[Asp22-Lys26][Gly8]GLP-1(7-37)-NH2 Drug Info [529424]
C[Cpa19-Lys26][Gly8]GLP-1(7-37)-NH2 Drug Info [529424]
C[Glu18-Lys22][Gly8]GLP-1(7-37)-NH2 Drug Info [529424]
C[Glu19-Lys23][Gly8]GLP-1(7-37)-NH2 Drug Info [529424]
C[Glu21-Lys25][Gly8]GLP-1(7-37)-NH2 Drug Info [529424]
C[Glu21-Lys26][Gly8]GLP-1(7-37)-NH2 Drug Info [529424]
C[Glu22-Lys26][Gly8]GLP-1(7-37)-NH2 Drug Info [529424]
C[Glu22-Orn26][Gly8]GLP-1(7-37)-NH2 Drug Info [529424]
C[Glu23-Lys27][Gly8]GLP-1(7-37)-NH2 Drug Info [529424]
C[Glu24-Lys28][Gly8]GLP-1(7-37)-NH2 Drug Info [529424]
C[Glu26-Lys30][Gly8]GLP-1(7-37)-NH2 Drug Info [529424]
C[hGlu22-Lys26][Gly8]GLP-1(7-37)-NH2 Drug Info [529424]
GLP-17-(7-36) derivative Drug Info [527207]
Glu20-Lys24][Gly8][GLP-1(7-37)-NH2 Drug Info [529424]
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG-NH2 Drug Info [529424]
HAEGTFTSDVSSYLEGQAAKEIFAWLVKGR Drug Info [529772]
NH2-HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR-CONH2 Drug Info [529763]
[Gly8, aib22]GLP-1(7-37)-NH2 Drug Info [529424]
[Gly8,Glu22]GLP-1(7,37)-NH2 Drug Info [529424]
[Gly8]GLP-1(7-37)-NH2 Drug Info [529424]
Binder Exenatide Drug Info [537358]
Stimulator LY-2428757 Drug Info [544122]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway cAMP signaling pathway
Neuroactive ligand-receptor interaction
Insulin secretion
Reactome Glucagon-like Peptide-1 (GLP1) regulates insulin secretion
G alpha (s) signalling events
Glucagon-type ligand receptors
WikiPathways GPCRs, Class B Secretin-like
Integration of energy metabolism
GPCR ligand binding
GPCR downstream signaling
References
Ref 522514ClinicalTrials.gov (NCT00804986) A Study for Patients With Type 2 Diabetes Mellitus. U.S. National Institutes of Health.
Ref 522639ClinicalTrials.gov (NCT00882726) A Study of the Safety, Pharmacokinetics, and Pharmacodynamics of CNTO 3649 in Healthy Adults and Patients With Type 2 Diabetes Mellitus. U.S. National Institutes of Health.
Ref 522861ClinicalTrials.gov (NCT01018173) A Study of Taspoglutide in Patients With Inadequately Controlled Diabetes Mellitus Type 2 and Cardiovascular Disease. U.S. National Institutes of Health.
Ref 523118ClinicalTrials.gov (NCT01165502) Clinical Study to Investigate Safety and Tolerability and Pharmacokinetics of Multiple Ascending Doses of CM3.1-AC100 in Healthy Male Volunteers. U.S. National Institutes of Health.
Ref 523368ClinicalTrials.gov (NCT01301456) Single-Dose And Multiple-Dose Safety And Tolerability Study Of PF-04856883 In Type 2 Diabetic Adult Females. U.S. National Institutes of Health.
Ref 523566ClinicalTrials.gov (NCT01405261) Trial Investigating the Safety of NNC 0113-0987 in Healthy Male Subjects. U.S. National Institutes of Health.
Ref 524023ClinicalTrials.gov (NCT01665352) A Study to Evaluate Safety and Efficacy of TTP054 for 12 Weeks in Subjects With Type 2 Diabetes. U.S. National Institutes of Health.
Ref 524621ClinicalTrials.gov (NCT02049034) Lixisenatide-The Effects on Glucose and Lipid Metabolism in Type 2 Diabetes. U.S. National Institutes of Health.
Ref 524727ClinicalTrials.gov (NCT02119819) A Study to Compare a New Drug for Type 2 Diabetes to Placebo and to a Treatment Already Available for Type 2 Diabetes. U.S. National Institutes of Health.
Ref 525144ClinicalTrials.gov (NCT02411825) Multiple Ascending Dose Study in Healthy Male Subjects. U.S. National Institutes of Health.
Ref 530376Exenatide and liraglutide: different approaches to develop GLP-1 receptor agonists (incretin mimetics)--preclinical and clinical results. Best Pract Res Clin Endocrinol Metab. 2009 Aug;23(4):463-77.
Ref 531351Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
Ref 532841Bydureon: first once weekly GLP-1 receptor agonist (exenatide LAR). Rev Med Liege. 2014 Apr;69(4):214-9.
Ref 5331232014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
Ref 536122Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
Ref 536224Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
Ref 537358Improved glycemic control and reduction of cardiometabolic risk factors in subjects with type 2 diabetes and metabolic syndrome treated with exenatide in a clinical practice setting. Diabetes TechnolTher. 2009 Jun;11(6):353-9.
Ref 538678(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: 1133).
Ref 542408(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: 7386).
Ref 542409(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: 7387).
Ref 542505(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: 7482).
Ref 542621(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: 7638).
Ref 546517Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008696)
Ref 546563Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008960)
Ref 547340Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015327)
Ref 547395Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015896)
Ref 547615Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017892)
Ref 548232Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023519)
Ref 548795Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028920)
Ref 549037Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031660)
Ref 549240Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800034087)
Ref 549337Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035378)
Ref 549427Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800036982)
Ref 549904Clinical pipeline report, company report or official report of Emisphere Technologies Inc.
Ref 550056Clinical pipeline report, company report or official report of PhaseBio Pharmaceuticals.
Ref 550291US FDA approves Bydureon? Pen (exenatide extended-release for injectable suspension) for once-weekly treatment of adults with type 2 diabetes
Ref 5511862005 approvals: Safety first. Nature Reviews Drug Discovery 5, 92-93 (February 2006).
Ref 551453Clinical pipeline report, company report or official report of Novo Nordisk A/S.
Ref 5517862011 Pipeline of Zealand Pharma.
Ref 5517902011 Pipeline of Zydus Cadila Group.
Ref 551972Clinical pipeline report, company report or official report of Novo Nordisk.
Ref 8894402016 FDA drug approvals. Nat Rev Drug Discov. 2017 Feb 2;16(2):73-76. doi: 10.1038/nrd.2017.14.
Ref
Ref 526351Glucagon-like peptide-1 analogue LY315902: effect on intestinal motility and release of insulin and somatostatin. Regul Pept. 2002 Jun 15;106(1-3):89-95.
Ref 526855Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Sep;25(7):565-97.
Ref 527207Bioorg Med Chem Lett. 2004 Sep 6;14(17):4395-8.Identification of CJC-1131-albumin bioconjugate as a stable and bioactive GLP-1(7-36) analog.
Ref 529424J Med Chem. 2008 May 8;51(9):2758-65. Epub 2008 Apr 15.Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo activity.
Ref 529693Pharmacokinetics and tolerability of a novel long-acting glucagon-like peptide-1 analog, CJC-1131, in healthy and diabetic subjects. Int J Clin Pharmacol Ther. 2008 Sep;46(9):443-52.
Ref 529763J Med Chem. 2008 Nov 27;51(22):7303-7.Influence of selective fluorination on the biological activity and proteolytic stability of glucagon-like peptide-1.
Ref 529772Bioorg Med Chem. 2008 Dec 1;16(23):10106-12. Epub 2008 Oct 5.Search for alpha-helical propensity in the receptor-bound conformation of glucagon-like peptide-1.
Ref 529902Reversal of diabetes in rats using GLP-1-expressing adult pancreatic duct-like precursor cells transformed from acinar to ductal cells. Stem Cells Dev. 2009 Sep;18(7):991-1002.
Ref 530376Exenatide and liraglutide: different approaches to develop GLP-1 receptor agonists (incretin mimetics)--preclinical and clinical results. Best Pract Res Clin Endocrinol Metab. 2009 Aug;23(4):463-77.
Ref 530530Pharmacokinetic and pharmacodynamic properties of taspoglutide, a once-weekly, human GLP-1 analogue, after single-dose administration in patients with Type 2 diabetes. Diabet Med. 2009 Nov;26(11):1156-64.
Ref 531282Novel glucagon-like peptide-1 analog delivered orally reduces postprandial glucose excursions in porcine and canine models. J Diabetes Sci Technol. 2010 Nov 1;4(6):1516-23.
Ref 532107GLP-1 receptor activation inhibits VLDL production and reverses hepatic steatosis by decreasing hepatic lipogenesis in high-fat-fed APOE*3-Leiden mice. PLoS One. 2012;7(11):e49152.
Ref 532497Relationship between systemic cytokines and complement factor H Y402H polymorphism in patients with dry age-related macular degeneration. Am J Ophthalmol. 2013 Dec;156(6):1176-83.
Ref 532841Bydureon: first once weekly GLP-1 receptor agonist (exenatide LAR). Rev Med Liege. 2014 Apr;69(4):214-9.
Ref 532871A potentiator of orthosteric ligand activity at GLP-1R acts via covalent modification. Nat Chem Biol. 2014 Aug;10(8):629-31.
Ref 5331232014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
Ref 536122Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
Ref 536224Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
Ref 537358Improved glycemic control and reduction of cardiometabolic risk factors in subjects with type 2 diabetes and metabolic syndrome treated with exenatide in a clinical practice setting. Diabetes TechnolTher. 2009 Jun;11(6):353-9.
Ref 543638(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: 249).
Ref 544122Role and development of GLP-1 receptor agonists in the management of diabetes. Diabetes Metab Syndr Obes. 2009; 2: 37-49.
Ref 544232Small Molecule Drug Discovery at the Glucagon-Like Peptide-1 Receptor. Exp Diabetes Res. 2012; 2012: 709893.
Ref 544390Chemically programmed antibodies. Trends Biotechnol. 2014 April; 32(4): 186-197.
Ref 550091On-target Effects of GLP-1 Receptor Agonists on Thyroid C-cells in Rats and Mice. Toxicol Pathol February 2013 vol. 41 no. 2 303-309.
Ref 550154US patent application no. 2011,0171,312, Modified therapeutic peptides, methods of their preparation and use.
Ref 5511862005 approvals: Safety first. Nature Reviews Drug Discovery 5, 92-93 (February 2006).
Ref 551450Clinical pipeline report, company report or official report of Novo Nordisk A/S.
Ref 551451Clinical pipeline report, company report or official report of Novo Nordisk A/S.
Ref 5517902011 Pipeline of Zydus Cadila Group.
Ref 551911Clinical pipeline report, company report or official report of Addex Pharmaceuticals.
Ref 1572591Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.

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