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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
3
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pubmed:dateCreated |
2002-1-24
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pubmed:abstractText |
A series of cyclic peptides having the general structure H-Phe-c[-N(epsilon)-Lys-X-NH-(CH(2))(n)-CO-] were designed on the basis of structure-activity relationship studies of motilin. All were motilin antagonists. The cyclic peptides, in which X is a 3-tert-butyl-substituted tyrosine residue (H-Phe-c[-N(epsilon)-Lys-Tyr(3-tBu)-beta Ala-] (3), H-Phe-c[-N(epsilon)-Lys-Tyr(3-tBu)-Gly-] (6), H-Phe-c[-N(epsilon)-Lys-Tyr(3-tBu)-Abu-] (7), and H-Phe-c[-N(epsilon)-Lys-Tyr(3-tBu)-Ahx-] (8)) showed potent motilin receptor antagonistic activity in the rabbit smooth muscle (pA(2) > 7). The 3-tert-butyl Tyr was found to be the moiety responsible for enhanced binding to the motilin receptor, while the size of the ring had little importance.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
31
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pubmed:volume |
45
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
670-5
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:11806718-Animals,
pubmed-meshheading:11806718-Motilin,
pubmed-meshheading:11806718-Muscle, Smooth,
pubmed-meshheading:11806718-Muscle Contraction,
pubmed-meshheading:11806718-Peptide Fragments,
pubmed-meshheading:11806718-Peptides, Cyclic,
pubmed-meshheading:11806718-Rabbits,
pubmed-meshheading:11806718-Receptors, Gastrointestinal Hormone,
pubmed-meshheading:11806718-Receptors, Neuropeptide,
pubmed-meshheading:11806718-Structure-Activity Relationship
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pubmed:year |
2002
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pubmed:articleTitle |
Design and synthesis of motilin antagonists derived from the [1-4] fragment of porcine motilin.
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pubmed:affiliation |
Fuji-Gotemba Research Laboratories, Chugai Pharmaceutical Co. Ltd., 1-135 Komakado, Gotemba-shi, Shizuoka 412-8513, Japan. mharamura@chugaibio.com
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pubmed:publicationType |
Journal Article,
In Vitro
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