Receptor for motilin identified in the human gastrointestinal system.
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.
Feighner
S D
SD
Department of Metabolic Disorders, Department of Medicinal Chemistry, Merck Research Laboratories, Building RY-80Y-265, 126 East Lincoln Avenue, Rahway, NJ 07065, USA.
Tan
C P
CP
McKee
K K
KK
Palyha
O C
OC
Hreniuk
D L
DL
Pong
S S
SS
Austin
C P
CP
Figueroa
D
D
MacNeil
D
D
Cascieri
M A
MA
Nargund
R
R
Bakshi
R
R
Abramovitz
M
M
Stocco
R
R
Kargman
S
S
O'Neill
G
G
Van Der Ploeg
L H
LH
Evans
J
J
Patchett
A A
AA
Smith
R G
RG
Howard
A D
AD
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
D008024:Ligands; D011964:Receptors, Gastrointestinal Hormone; D018013:Receptors, Neuropeptide; C050802:motilin receptor; D009037:Motilin; D004917:Erythromycin; D019204:GTP-Binding Proteins; D002118:Calcium