title: Receptor for motilin identified in the human gastrointestinal system.
abstract: Motilin is a 22-amino acid peptide hormone expressed throughout the gastrointestinal (GI) tract of humans and other species. It affects gastric motility by stimulating interdigestive antrum and duodenal contractions. A heterotrimeric guanosine triphosphate-binding protein (G protein)-coupled receptor for motilin was isolated from human stomach, and its amino acid sequence was found to be 52 percent identical to the human receptor for growth hormone secretagogues. The macrolide antibiotic erythromycin also interacted with the cloned motilin receptor, providing a molecular basis for its effects on the human GI tract. The motilin receptor is expressed in enteric neurons of the human duodenum and colon. Development of motilin receptor agonists and antagonists may be useful in the treatment of multiple disorders of GI motility.
authors.affiliation: Department of Metabolic Disorders, Department of Medicinal Chemistry, Merck Research Laboratories, Building RY-80Y-265, 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
authors.forename: S D
authors.initials: SD
authors.lastname: Feighner
authors.forename: C P
authors.initials: CP
authors.lastname: Tan
authors.forename: K K
authors.initials: KK
authors.lastname: McKee
authors.forename: O C
authors.initials: OC
authors.lastname: Palyha
authors.forename: D L
authors.initials: DL
authors.lastname: Hreniuk
authors.forename: S S
authors.initials: SS
authors.lastname: Pong
authors.forename: C P
authors.initials: CP
authors.lastname: Austin
authors.forename: D
authors.initials: D
authors.lastname: Figueroa
authors.forename: D
authors.initials: D
authors.lastname: MacNeil
authors.forename: M A
authors.initials: MA
authors.lastname: Cascieri
authors.forename: R
authors.initials: R
authors.lastname: Nargund
authors.forename: R
authors.initials: R
authors.lastname: Bakshi
authors.forename: M
authors.initials: M
authors.lastname: Abramovitz
authors.forename: R
authors.initials: R
authors.lastname: Stocco
authors.forename: S
authors.initials: S
authors.lastname: Kargman
authors.forename: G
authors.initials: G
authors.lastname: O'Neill
authors.forename: L H
authors.initials: LH
authors.lastname: Van Der Ploeg
authors.forename: J
authors.initials: J
authors.lastname: Evans
authors.forename: A A
authors.initials: AA
authors.lastname: Patchett
authors.forename: R G
authors.initials: RG
authors.lastname: Smith
authors.forename: A D
authors.initials: AD
authors.lastname: Howard
mesh_terms: D017398:Alternative Splicing; D000595:Amino Acid Sequence; D001483:Base Sequence; D001665:Binding Sites; D002118:Calcium / Q000378:metabolism; D002460:Cell Line; D002874:Chromosome Mapping; D002882:Chromosomes, Human, Pair 13; D003001:Cloning, Molecular; D003106:Colon / Q000378:metabolism*; D004917:Erythromycin / Q000378:metabolism; D019204:GTP-Binding Proteins / Q000378:metabolism; D005753:Gastric Mucosa / Q000378:metabolism*; D006801:Humans; D017403:In Situ Hybridization; D007421:Intestine, Small / Q000378:metabolism*; D008024:Ligands; D008969:Molecular Sequence Data; D009037:Motilin / Q000031:analogs & derivatives / Q000378:metabolism*; D011964:Receptors, Gastrointestinal Hormone / Q000737:chemistry* / Q000235:genetics* / Q000378:metabolism; D018013:Receptors, Neuropeptide / Q000737:chemistry* / Q000235:genetics* / Q000378:metabolism; D013961:Thyroid Gland / Q000378:metabolism; D014162:Transfection
chemical_list: D008024:Ligands; D011964:Receptors, Gastrointestinal Hormone; D018013:Receptors, Neuropeptide; C050802:motilin receptor; D009037:Motilin; D004917:Erythromycin; D019204:GTP-Binding Proteins; D002118:Calcium