Target Information

Target General Infomation
Target ID
T62306
Former ID
TTDC00155
Target Name
Motilin receptor
Gene Name
MLNR
Synonyms
Gprotein coupled receptor 38; MLNR
Target Type
Clinical Trial
Disease Constipation [ICD9: 564; ICD10: K59.0]
Delayed gastric emptying; Gastroparesis [ICD9:536.3; ICD10: K31.8]
Dyspepsia [ICD9: 536.8; ICD10: K30]
Diarrhea [ICD9: 787.91; ICD10: A09, K59.1]
Gastroesophageal reflux disease [ICD9: 140-229, 530; ICD10: K21]
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]
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.
BioChemical Class
GPCR rhodopsin
Target Validation
T62306
UniProt ID
O43193
Sequence
MGSPWNGSDGPEGAREPPWPALPPCDERRCSPFPLGALVPVTAVCLCLFVVGVSGNVVTV
MLIGRYRDMRTTTNLYLGSMAVSDLLILLGLPFDLYRLWRSRPWVFGPLLCRLSLYVGEG
CTYATLLHMTALSVERYLAICRPLRARVLVTRRRVRALIAVLWAVALLSAGPFLFLVGVE
QDPGISVVPGLNGTARIASSPLASSPPLWLSRAPPPSPPSGPETAEAAALFSRECRPSPA
QLGALRVMLWVTTAYFFLPFLCLSILYGLIGRELWSSRRPLRGPAASGRERGHRQTVRVL
LVVVLAFIICWLPFHVGRIIYINTEDSRMMYFSQYFNIVALQLFYLSASINPILYNLISK
KYRAAAFKLLLARKSRPRGFHRSRDTAGEVAGDTGGDTVGYTETSANVKTMG
Drugs and Mode of Action
Drug(s) Camicinal Drug Info Phase 2 Delayed gastric emptying; Gastroparesis [524864], [540638]
Mitemcinal fumarate Drug Info Phase 2 Pain [521541]
DS-3801 Drug Info Phase 1 Constipation [549561]
GSK-1322888 Drug Info Phase 1 Gastroparesis [523354]
KOS-2187 Drug Info Phase 1 Gastrointestinal disorders; Gastroesophageal reflux disease [536527]
RWJ-68023 Drug Info Phase 1 Irritable bowel syndrome [548041]
GSK-326416 Drug Info Preclinical Gastroparesis [536527]
TZP-202 Drug Info Preclinical Dyspepsia [548199]
MOTILIN Drug Info Discontinued in Phase 4 Discovery agent [524869], [538929]
KC-11458 Drug Info Discontinued in Phase 2 Gastric motility disorder [546439]
KW-5139 Drug Info Discontinued in Phase 2 Pain [545295]
SLV-305 Drug Info Discontinued in Phase 2 Gastric motility disorder [547249]
SLV-311 Drug Info Discontinued in Phase 1 Gastrointestinal disease [547571]
Modulator Camicinal Drug Info [543753]
KC-11458 Drug Info [527150]
KW-5139 Drug Info [533848]
SLV-305 Drug Info [543753]
SLV-311 Drug Info [547570]
Agonist CEM-301 Drug Info [543753]
DS-3801 Drug Info [550587]
EM-523 Drug Info [527468]
GSK-1322888 Drug Info [523354]
GSK-326416 Drug Info [536527]
KOS-2187 Drug Info [551564]
KOS1326 Drug Info [527468]
ME36 Drug Info [527468]
ME4 Drug Info [527468]
ME67 Drug Info [527468]
Mitemcinal fumarate Drug Info [551607]
RQ-00201894 Drug Info [543753]
[Leu13]motilin (human) Drug Info [525522]
Antagonist GM-109 Drug Info [526253]
MA-2029 Drug Info [529236]
RWJ-68023 Drug Info [527000]
TZP-201 Drug Info [543753]
TZP-202 Drug Info [548200]
Inhibitor MOTILIN Drug Info [528545]
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 521541ClinicalTrials.gov (NCT00050882) Safety and Effectiveness of an Investigational Agent (GM-611) in Patients With Diabetic Gastroparesis. U.S. National Institutes of Health.
Ref 523354ClinicalTrials.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 524864ClinicalTrials.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 524869ClinicalTrials.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 536527Emerging drugs for postoperative ileus. Expert Opin Emerg Drugs. 2007 Nov;12(4):619-26.
Ref 538929(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 540638(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 545295Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002731)
Ref 546439Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008138)
Ref 547249Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014470)
Ref 547571Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017412)
Ref 548041Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021456)
Ref 548199Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023009)
Ref 549561Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800040749)
Ref 523354ClinicalTrials.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 525522Receptor for motilin identified in the human gastrointestinal system. Science. 1999 Jun 25;284(5423):2184-8.
Ref 526253Design 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 527000Effects of a nonpeptide motilin receptor antagonist on proximal gastric motor function. Br J Clin Pharmacol. 2004 Apr;57(4):393-401.
Ref 527150Effect of the motilin agonist KC 11458 on gastric emptying in diabetic gastroparesis. Aliment Pharmacol Ther. 2004 Aug 1;20(3):333-8.
Ref 527468Desensitization of the human motilin receptor by motilides. J Pharmacol Exp Ther. 2005 Jun;313(3):1397-405. Epub 2005 Mar 11.
Ref 528545J Med Chem. 2006 Nov 30;49(24):7190-7.Discovery of a new class of macrocyclic antagonists to the human motilin receptor.
Ref 529236Oral 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 533848Stimulating action of KW-5139 (Leu13-motilin) on gastrointestinal motility in the rabbit. Br J Pharmacol. 1994 Jan;111(1):288-94.
Ref 536527Emerging drugs for postoperative ileus. Expert Opin Emerg Drugs. 2007 Nov;12(4):619-26.
Ref 543753(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 547570Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017412)
Ref 548200Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023009)
Ref 550587Clinical pipeline report, company report or official report of Daiichi Sankyo.
Ref 551564Kosan Announces Selection of KOS-2187 As Motilide Clinical Candidate at World Congress of Gastroenterology Meeting. Kosan. 2006.
Ref 551607Clinical pipeline report, company report or official report of Roche (2009).

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