Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T62306
|
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| Former ID |
TTDC00155
|
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| Target Name |
Motilin receptor
|
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| Gene Name |
MLNR
|
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| Synonyms |
Gprotein coupled receptor 38; MLNR
|
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| Target Type |
Clinical Trial
|
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| Disease | Constipation [ICD9: 564; ICD10: K59.0] | ||||
| Dyspepsia [ICD9: 536.8; ICD10: K30] | |||||
| Diarrhea [ICD9: 787.91; ICD10: A09, K59.1] | |||||
| Delayed gastric emptying; Gastroparesis [ICD9:536.3; ICD10: K31.8] | |||||
| Gastrointestinal disease [ICD10: K00-K93] | |||||
| Gastric motility disorder [ICD10: K22.4] | |||||
| Gastrointestinal disorders; Gastroesophageal reflux disease [ICD9: 530, 530-558; ICD10: K20-K64, K21] | |||||
| Gastroparesis [ICD9: 536.3; ICD10: K31.8] | |||||
| Gastroesophageal reflux disease [ICD9: 140-229, 530; ICD10: K21] | |||||
| Irritable bowel syndrome [ICD9: 564.1, 787.91; ICD10: A09, K58, K59.1] | |||||
| Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89] | |||||
| Function |
Receptor for motilin.
|
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| BioChemical Class |
GPCR rhodopsin
|
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| Target Validation |
T62306
|
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| UniProt ID | |||||
| Sequence |
MGSPWNGSDGPEGAREPPWPALPPCDERRCSPFPLGALVPVTAVCLCLFVVGVSGNVVTV
MLIGRYRDMRTTTNLYLGSMAVSDLLILLGLPFDLYRLWRSRPWVFGPLLCRLSLYVGEG CTYATLLHMTALSVERYLAICRPLRARVLVTRRRVRALIAVLWAVALLSAGPFLFLVGVE QDPGISVVPGLNGTARIASSPLASSPPLWLSRAPPPSPPSGPETAEAAALFSRECRPSPA QLGALRVMLWVTTAYFFLPFLCLSILYGLIGRELWSSRRPLRGPAASGRERGHRQTVRVL LVVVLAFIICWLPFHVGRIIYINTEDSRMMYFSQYFNIVALQLFYLSASINPILYNLISK KYRAAAFKLLLARKSRPRGFHRSRDTAGEVAGDTGGDTVGYTETSANVKTMG |
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| Drugs and Mode of Action | |||||
| Drug(s) | Camicinal | Drug Info | Phase 2 | Delayed gastric emptying; Gastroparesis | [1], [2] |
| Mitemcinal fumarate | Drug Info | Phase 2 | Pain | [3] | |
| DS-3801 | Drug Info | Phase 1 | Constipation | [4] | |
| GSK-1322888 | Drug Info | Phase 1 | Gastroparesis | [5] | |
| KOS-2187 | Drug Info | Phase 1 | Gastrointestinal disorders; Gastroesophageal reflux disease | [6] | |
| RWJ-68023 | Drug Info | Phase 1 | Irritable bowel syndrome | [7] | |
| GSK-326416 | Drug Info | Preclinical | Gastroparesis | [6] | |
| TZP-202 | Drug Info | Preclinical | Dyspepsia | [8] | |
| MOTILIN | Drug Info | Discontinued in Phase 4 | Discovery agent | [9], [10] | |
| KC-11458 | Drug Info | Discontinued in Phase 2 | Gastric motility disorder | [11] | |
| KW-5139 | Drug Info | Discontinued in Phase 2 | Pain | [12] | |
| SLV-305 | Drug Info | Discontinued in Phase 2 | Gastric motility disorder | [13] | |
| SLV-311 | Drug Info | Discontinued in Phase 1 | Gastrointestinal disease | [14] | |
| Modulator | Camicinal | Drug Info | [15] | ||
| KC-11458 | Drug Info | [16] | |||
| KW-5139 | Drug Info | [17] | |||
| SLV-305 | Drug Info | [15] | |||
| SLV-311 | Drug Info | [18] | |||
| Agonist | CEM-301 | Drug Info | [15] | ||
| DS-3801 | Drug Info | [19] | |||
| EM-523 | Drug Info | [20] | |||
| GSK-1322888 | Drug Info | [5] | |||
| GSK-326416 | Drug Info | [6] | |||
| KOS-2187 | Drug Info | [21] | |||
| KOS1326 | Drug Info | [20] | |||
| ME36 | Drug Info | [20] | |||
| ME4 | Drug Info | [20] | |||
| ME67 | Drug Info | [20] | |||
| Mitemcinal fumarate | Drug Info | [22] | |||
| RQ-00201894 | Drug Info | [15] | |||
| [Leu13]motilin (human) | Drug Info | [23] | |||
| Antagonist | GM-109 | Drug Info | [24] | ||
| MA-2029 | Drug Info | [25] | |||
| RWJ-68023 | Drug Info | [26] | |||
| TZP-201 | Drug Info | [15] | |||
| TZP-202 | Drug Info | [27] | |||
| Inhibitor | MOTILIN | Drug Info | [28] | ||
| Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
| TEP | EXP Info | ||||
| Pathways | |||||
| KEGG Pathway | Neuroactive ligand-receptor interaction | ||||
| Reactome | Peptide ligand-binding receptors | ||||
| G alpha (q) signalling events | |||||
| WikiPathways | GPCRs, Class A Rhodopsin-like | ||||
| Gastrin-CREB signalling pathway via PKC and MAPK | |||||
| GPCR ligand binding | |||||
| GPCR downstream signaling | |||||
| References | |||||
| REF 1 | ClinicalTrials.gov (NCT02210000) A Study to Evaluate the Effect of Camicinal on Gastroparesis Symptoms in Type 1 and 2 Diabetic Subjects With Gastroparesis. U.S. National Institutes of Health. | ||||
| REF 2 | (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: 4035). | ||||
| REF 3 | ClinicalTrials.gov (NCT00050882) Safety and Effectiveness of an Investigational Agent (GM-611) in Patients With Diabetic Gastroparesis. U.S. National Institutes of Health. | ||||
| REF 4 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800040749) | ||||
| REF 5 | ClinicalTrials.gov (NCT01294566) FTIH to Evaluate Safety, Tolerability, and Pharmacokinetics of Single Oral Doses of GSK1322888 in Healthy Caucasian and Japanese Volunteers. U.S. National Institutes of Health. | ||||
| REF 6 | Emerging drugs for postoperative ileus. Expert Opin Emerg Drugs. 2007 Nov;12(4):619-26. | ||||
| REF 7 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021456) | ||||
| 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 800023009) | ||||
| REF 9 | ClinicalTrials.gov (NCT02212821) Brain Mechanisms Underlying the Effect of the Motilin Receptor Agonist Erythromycin on Hunger in Normal Weight Subjects. U.S. National Institutes of Health. | ||||
| REF 10 | (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: 1459). | ||||
| REF 11 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008138) | ||||
| REF 12 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002731) | ||||
| REF 13 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014470) | ||||
| REF 14 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017412) | ||||
| REF 15 | (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: 297). | ||||
| REF 16 | Effect of the motilin agonist KC 11458 on gastric emptying in diabetic gastroparesis. Aliment Pharmacol Ther. 2004 Aug 1;20(3):333-8. | ||||
| REF 17 | Stimulating action of KW-5139 (Leu13-motilin) on gastrointestinal motility in the rabbit. Br J Pharmacol. 1994 Jan;111(1):288-94. | ||||
| REF 18 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017412) | ||||
| REF 19 | Clinical pipeline report, company report or official report of Daiichi Sankyo. | ||||
| REF 20 | Desensitization of the human motilin receptor by motilides. J Pharmacol Exp Ther. 2005 Jun;313(3):1397-405. Epub 2005 Mar 11. | ||||
| REF 21 | Kosan Announces Selection of KOS-2187 As Motilide Clinical Candidate at World Congress of Gastroenterology Meeting. Kosan. 2006. | ||||
| REF 22 | Clinical pipeline report, company report or official report of Roche (2009). | ||||
| REF 23 | Receptor for motilin identified in the human gastrointestinal system. Science. 1999 Jun 25;284(5423):2184-8. | ||||
| REF 24 | Design and synthesis of motilin antagonists derived from the [1-4] fragment of porcine motilin. J Med Chem. 2002 Jan 31;45(3):670-5. | ||||
| REF 25 | Oral administration of MA-2029, a novel selective and competitive motilin receptor antagonist, inhibits motilin-induced intestinal contractions and visceral pain in rabbits. Eur J Pharmacol. 2008 Mar10;581(3):296-305. | ||||
| REF 26 | Effects of a nonpeptide motilin receptor antagonist on proximal gastric motor function. Br J Clin Pharmacol. 2004 Apr;57(4):393-401. | ||||
| REF 27 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023009) | ||||
| REF 28 | J Med Chem. 2006 Nov 30;49(24):7190-7.Discovery of a new class of macrocyclic antagonists to the human motilin receptor. | ||||
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