Target Information
Target General Information | Top | |||||
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Target ID |
T87875
(Former ID: TTDC00286)
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Target Name |
Glucagon receptor messenger RNA (GCGR mRNA)
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Synonyms |
Glucagon receptor (mRNA); GLR (mRNA); GL-R (mRNA)
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Gene Name |
GCGR
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Target Type |
Clinical trial target
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[1] | ||||
Disease | [+] 2 Target-related Diseases | + | ||||
1 | Acute diabete complication [ICD-11: 5A2Y] | |||||
2 | Type 2 diabetes mellitus [ICD-11: 5A11] | |||||
Function |
Regulates the rate of hepatic glucose production by promoting glycogen hydrolysis and gluconeogenesis. Plays an important role in mediating the responses to fasting. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Promotes activation of adenylate cyclase. Besides, plays a role in signaling via a phosphatidylinositol-calcium second messenger system. G-protein coupled receptor for glucagon that plays a central role in the regulation of blood glucose levels and glucose homeostasis.
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BioChemical Class |
mRNA target
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UniProt ID | ||||||
Sequence |
MPPCQPQRPLLLLLLLLACQPQVPSAQVMDFLFEKWKLYGDQCHHNLSLLPPPTELVCNR
TFDKYSCWPDTPANTTANISCPWYLPWHHKVQHRFVFKRCGPDGQWVRGPRGQPWRDASQ CQMDGEEIEVQKEVAKMYSSFQVMYTVGYSLSLGALLLALAILGGLSKLHCTRNAIHANL FASFVLKASSVLVIDGLLRTRYSQKIGDDLSVSTWLSDGAVAGCRVAAVFMQYGIVANYC WLLVEGLYLHNLLGLATLPERSFFSLYLGIGWGAPMLFVVPWAVVKCLFENVQCWTSNDN MGFWWILRFPVFLAILINFFIFVRIVQLLVAKLRARQMHHTDYKFRLAKSTLTLIPLLGV HEVVFAFVTDEHAQGTLRSAKLFFDLFLSSFQGLLVAVLYCFLNKEVQSELRRRWHRWRL GKVLWEERNTSNHRASSSPGHGPPSKELQFGRGGGSQDSSAETPLAGGLPRLAESPF Click to Show/Hide
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Drugs and Modes of Action | Top | |||||
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Clinical Trial Drug(s) | [+] 3 Clinical Trial Drugs | + | ||||
1 | IONIS-GCGR-Rx | Drug Info | Phase 2 | Type-2 diabetes | [2] | |
2 | ISIS-GCGR | Drug Info | Phase 2 | Diabetic complication | [3] | |
3 | ISIS 325568 | Drug Info | Phase 1 | Type-2 diabetes | [4] | |
Mode of Action | [+] 1 Modes of Action | + | ||||
Inhibitor | [+] 1 Inhibitor drugs | + | ||||
1 | IONIS-GCGR-Rx | Drug Info | [5] |
Cell-based Target Expression Variations | Top | |||||
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Cell-based Target Expression Variations |
Target Profiles in Patients | Top | |||||
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Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
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Reactome | [+] 4 Reactome Pathways | + | ||||
1 | Glucagon signaling in metabolic regulation | |||||
2 | G alpha (q) signalling events | |||||
3 | G alpha (s) signalling events | |||||
4 | Glucagon-type ligand receptors |
Target-Related Models and Studies | Top | |||||
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Target Validation |
References | Top | |||||
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REF 1 | Design and development of antisense drugs. Expert Opin. Drug Discov. 2008 3(10):1189-1207. | |||||
REF 2 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 3 | ClinicalTrials.gov (NCT01885260) Safety, Tolerability and Efficacy of ISIS-GCGRRx in Type 2 Diabetes. U.S. National Institutes of Health. | |||||
REF 4 | ClinicalTrials.gov (NCT00519727) Safety Study of ISIS 325568 in Healthy Volunteers. U.S. National Institutes of Health. | |||||
REF 5 | Clinical pipeline report, company report or official report of Ionis Pharmaceuticals. | |||||
REF 6 | Clinical pipeline report, company report or official report of ISIS Pharmaceuticals (2011). |
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