Target Information
Target General Infomation | |||||
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Target ID |
T59604
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Former ID |
TTDC00127
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Target Name |
Growth hormone secretagogue receptor type 1
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Gene Name |
GHSR
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Synonyms |
GH-releasing peptide receptor; GHRP; GHS-R; Ghrelin receptor; Growth hormone secretagogue receptor; GHSR
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Target Type |
Successful
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Disease | Anorexia nervosa cachexia [ICD9: 307.1, 799.4; ICD10: F50.0-F50.1] | ||||
Alcohol use disorders [ICD9: 303; ICD10: F10.2] | |||||
Cachexia [ICD9: 799.4; ICD10: R64] | |||||
Carbohydrate metabolism disorder [ICD10: E73-E74] | |||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Functional bowel disorder [ICD10: K00-K93] | |||||
Frailty [ICD10: R54] | |||||
Fibromyalgia [ICD9: 729.1; ICD10: M79.7] | |||||
Growth hormone deficiency [ICD9: 253.0, 253.3; ICD10: E22.0, E23.0] | |||||
Gastric motility disorder [ICD10: K22.4] | |||||
Ileus; Gastroparesis; Miscellaneous gastrointestinal disorders [ICD9: 530-558, 536.3, 537.2, 560.1, 560.31, 777.1, 777.4; ICD10: K20-K64, K31.5, K31.8, K56.0, K56.3, K56.7, P76.1] | |||||
Metabolic disorders [ICD9: 270-279; ICD10: E70-E89] | |||||
Obesity [ICD9: 278; ICD10: E66] | |||||
Postoperative ileus [ICD9: 537.2, 560.1, 560.31, 777.1, 777.4; ICD10: K31.5, K56.0, K56.3, K56.7, P76.1] | |||||
Type 2 diabetes [ICD9: 250; ICD10: E11] | |||||
Function |
Receptor for ghrelin, coupled to G-alpha-11 proteins. Stimulates growth hormone secretion. Binds also other growth hormone releasing peptides (GHRP) (e.g. Met-enkephalin and GHRP-6) as well as non-peptide, low molecular weight secretagogues (e.g. L-692,429, MK-0677, adenosine).
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T59604
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UniProt ID | |||||
Sequence |
MWNATPSEEPGFNLTLADLDWDASPGNDSLGDELLQLFPAPLLAGVTATCVALFVVGIAG
NLLTMLVVSRFRELRTTTNLYLSSMAFSDLLIFLCMPLDLVRLWQYRPWNFGDLLCKLFQ FVSESCTYATVLTITALSVERYFAICFPLRAKVVVTKGRVKLVIFVIWAVAFCSAGPIFV LVGVEHENGTDPWDTNECRPTEFAVRSGLLTVMVWVSSIFFFLPVFCLTVLYSLIGRKLW RRRRGDAVVGASLRDQNHKQTVKMLAVVVFAFILCWLPFHVGRYLFSKSFEPGSLEIAQI SQYCNLVSFVLFYLSAAINPILYNIMSKKYRVAVFRLLGFEPFSQRKLSTLKDESSRAWT ESSINT |
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Drugs and Mode of Action | |||||
Drug(s) | GHRP-2 | Drug Info | Approved | Growth hormone deficiency | [551871] |
Ibutamoren | Drug Info | Approved | Fibromyalgia | [536647], [541176] | |
Anamorelin | Drug Info | Phase 3 | Carbohydrate metabolism disorder | [523546] | |
Macimorelin | Drug Info | Phase 3 | Growth hormone deficiency | [521987] | |
TZP-101 | Drug Info | Phase 2b | Ileus; Gastroparesis; Miscellaneous gastrointestinal disorders | [536527], [540467] | |
GTP-200 | Drug Info | Phase 2 | Cancer | [548242] | |
RQ-00000005 | Drug Info | Phase 2 | Frailty | [522109] | |
Tabimorelin | Drug Info | Phase 2 | Growth hormone deficiency | [525551] | |
Ipamorelin | Drug Info | Phase 1/2 | Postoperative ileus | [536527] | |
PF-05190457 | Drug Info | Phase 1 | Type 2 diabetes | [523786] | |
ST-1141 | Drug Info | Phase 1 | Functional bowel disorder | [548492] | |
AEZS-123 | Drug Info | Preclinical | Alcohol use disorders | [550214] | |
EP-01492 | Drug Info | Preclinical | Obesity | [536122] | |
TZP-301 | Drug Info | Preclinical | Metabolic disorders | [551744] | |
CYT-009-GhrQb | Drug Info | Discontinued in Phase 1/2 | Obesity | [536122] | |
LY-444711 | Drug Info | Discontinued in Phase 1 | Growth hormone deficiency | [547057] | |
SUN-11031 | Drug Info | Terminated | Anorexia nervosa cachexia | [536225] | |
Inhibitor | 4-(3-hexylureido)-N-phenylbenzenesulfonamide | Drug Info | [530395] | ||
AwFwLL-NH2 | Drug Info | [528740] | |||
DprwFwLL-NH2 | Drug Info | [528740] | |||
DwFwLL-NH2 | Drug Info | [528740] | |||
HwFwLL-NH2 | Drug Info | [528740] | |||
KwFwLL-NH2 | Drug Info | [528740] | |||
QwFwLL-NH2 | Drug Info | [528740] | |||
RPKPfQwFwLL-NH2 | Drug Info | [528740] | |||
RwFwLL-NH2 | Drug Info | [528740] | |||
WFwGG-NH2 | Drug Info | [528740] | |||
WFwLL-NH2 | Drug Info | [528740] | |||
Antagonist | Abbott 14c | Drug Info | [528319] | ||
AEZS-123 | Drug Info | [550214] | |||
CYT-009-GhrQb | Drug Info | [536122] | |||
EP-01492 | Drug Info | [536122] | |||
EX-1311 | Drug Info | [543633] | |||
GSK1614343 | Drug Info | [531003] | |||
JMV3008 | Drug Info | [529089] | |||
NOX-B11 | Drug Info | [543633] | |||
TZP-301 | Drug Info | [551744] | |||
YIL781 | Drug Info | [528960] | |||
Stimulator | Anamorelin | Drug Info | [537066] | ||
Agonist | EX-1314 | Drug Info | [543633] | ||
GHRP-2 | Drug Info | [535349] | |||
GSK-894281 | Drug Info | [543633] | |||
GTP-200 | Drug Info | [544045] | |||
LY-444711 | Drug Info | [527265] | |||
Macimorelin | Drug Info | [550490] | |||
RQ-00000005 | Drug Info | [532719] | |||
SM-130,686 | Drug Info | [526224] | |||
ST-1141 | Drug Info | [550985] | |||
SUN-11031 | Drug Info | [536225] | |||
TZP-101 | Drug Info | [537004], [537157], [537305] | |||
[35S]ibutamoren | Drug Info | [534355] | |||
Modulator | Ibutamoren | Drug Info | [553238] | ||
Ipamorelin | Drug Info | ||||
PF-05190457 | Drug Info | [551215] | |||
Tabimorelin | Drug Info | [525551] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | cAMP signaling pathway | ||||
Neuroactive ligand-receptor interaction | |||||
NetPath Pathway | Leptin Signaling Pathway | ||||
Reactome | Peptide ligand-binding receptors | ||||
G alpha (q) signalling events | |||||
WikiPathways | GPCRs, Class A Rhodopsin-like | ||||
Gastrin-CREB signalling pathway via PKC and MAPK | |||||
Peptide GPCRs | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
References | |||||
Ref 521987 | ClinicalTrials.gov (NCT00448747) Investigation of a New, Oral Growth Hormone Secretagogue, Macimorelin (AEZS-130) as a Growth Hormone Stimulation Test.. U.S. National Institutes of Health. | ||||
Ref 522109 | ClinicalTrials.gov (NCT00527046) Effects Of An Oral Growth Hormone Secretagogue In Older Functionally Limited Adults. U.S. National Institutes of Health. | ||||
Ref 523546 | ClinicalTrials.gov (NCT01395914) Anamorelin HCl in the Treatment of Non-Small Cell Lung Cancer-Cachexia (NSCLC-C): An Extension Study (ROMANA 3). U.S. National Institutes of Health. | ||||
Ref 523786 | ClinicalTrials.gov (NCT01522807) A Study Of Three PF-05190457 Formulations In Healthy Volunteers. U.S. National Institutes of Health. | ||||
Ref 525551 | Pharmacological characterisation of a new oral GH secretagogue, NN703. Eur J Endocrinol. 1999 Aug;141(2):180-9. | ||||
Ref 536122 | Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. | ||||
Ref 536225 | Emerging drugs for eating disorder treatment. Expert Opin Emerg Drugs. 2006 May;11(2):315-36. | ||||
Ref 540467 | (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: 3535). | ||||
Ref 541176 | (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: 5867). | ||||
Ref 547057 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012573) | ||||
Ref 548242 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023682) | ||||
Ref 525551 | Pharmacological characterisation of a new oral GH secretagogue, NN703. Eur J Endocrinol. 1999 Aug;141(2):180-9. | ||||
Ref 526224 | Oxindole derivatives as orally active potent growth hormone secretagogues. J Med Chem. 2001 Dec 20;44(26):4641-9. | ||||
Ref 527265 | Synthesis and biological evaluation of an orally active ghrelin agonist that stimulates food consumption and adiposity in rats. Bioorg Med Chem Lett. 2004 Dec 6;14(23):5873-6. | ||||
Ref 528319 | Discovery and pharmacological evaluation of growth hormone secretagogue receptor antagonists. J Med Chem. 2006 Jul 27;49(15):4459-69. | ||||
Ref 528740 | J Biol Chem. 2007 May 25;282(21):15799-811. Epub 2007 Mar 19.Identification of an efficacy switch region in the ghrelin receptor responsible for interchange between agonism and inverse agonism. | ||||
Ref 528960 | Small-molecule ghrelin receptor antagonists improve glucose tolerance, suppress appetite, and promote weight loss. Endocrinology. 2007 Nov;148(11):5175-85. Epub 2007 Jul 26. | ||||
Ref 529089 | Toward potent ghrelin receptor ligands based on trisubstituted 1,2,4-triazole structure. 2. Synthesis and pharmacological in vitro and in vivo evaluations. J Med Chem. 2007 Nov 15;50(23):5790-806. Epub 2007 Oct 10. | ||||
Ref 530395 | Bioorg Med Chem Lett. 2009 Nov 1;19(21):6237-40. Epub 2009 Aug 26.Discovery and optimization of novel 4-[(aminocarbonyl)amino]-N-[4-(2-aminoethyl)phenyl]benzenesulfonamide ghrelin receptor antagonists. | ||||
Ref 531003 | Discovery process and characterization of novel carbohydrazide derivatives as potent and selective GHSR1a antagonists. ChemMedChem. 2010 Sep 3;5(9):1450-5. | ||||
Ref 532719 | Hypotensive effects of ghrelin receptor agonists mediated through a novel receptor. Br J Pharmacol. 2014 Mar;171(5):1275-86. | ||||
Ref 534355 | Molecular analysis of rat pituitary and hypothalamic growth hormone secretagogue receptors. Mol Endocrinol. 1997 Apr;11(4):415-23. | ||||
Ref 535349 | GH-releasing peptide-2 increases fat mass in mice lacking NPY: indication for a crucial mediating role of hypothalamic agouti-related protein. Endocrinology. 2002 Feb;143(2):558-68. | ||||
Ref 536122 | Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. | ||||
Ref 536225 | Emerging drugs for eating disorder treatment. Expert Opin Emerg Drugs. 2006 May;11(2):315-36. | ||||
Ref 537004 | Effect of the ghrelin receptor agonist TZP-101 on colonic transit in a rat model of postoperative ileus. Eur J Pharmacol. 2009 Feb 14;604(1-3):132-7. Epub 2008 Dec 14. | ||||
Ref 537066 | Pharmacodynamic hormonal effects of anamorelin, a novel oral ghrelin mimetic and growth hormone secretagogue in healthy volunteers. Growth Horm IGF Res. 2009 Jun;19(3):267-73. Epub 2009 Feb 3. | ||||
Ref 537157 | Ghrelin receptor agonist (TZP-101) accelerates gastric emptying in adults with diabetes and symptomatic gastroparesis. Aliment Pharmacol Ther. 2009 Jun 1;29(11):1179-87. Epub 2009 Feb 27. | ||||
Ref 537305 | Contribution of protein binding to the pharmacokinetics of the ghrelin receptor agonist TZP-101 in healthy volunteers and adults with symptomatic gastroparesis: two randomized, double-blind studies and a binding profile study. Clin Drug Investig. 2009;29(6):409-18. doi: 10.2165/00044011-200929060-00004. | ||||
Ref 543633 | (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: 246). |
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