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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
1984-8-22
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pubmed:abstractText |
Eight position-1 analogs of the 40-amino acid fragment and two position-1 analogs of human growth hormone-releasing factor were synthesized by solid phase methodology and their capacity to release growth hormone was determined using rat anterior pituitary cells in monolayer culture. Relative to hGRF(1-40)OH, which was arbitrarily assigned a potency value of 1, [D-Tyr1]hGRF(1-40)OH, [Phe1]hGRF(1-40)OH, [Trp1]hGRF(1-40)OH, [His1]hGRF(1-40)OH, [Ala1]hGRF(1-40)OH, [(-Ac)Tyr1]hGRF(1-40)OH, Arg0-hGRF(1-40)OH and Ala0-hGRF(1-40)OH have potencies of 0.022, 0.038, 0.003, 0.351, 0.010, 0.032, 0.002 and 0.007 respectively. Relative to hGRF(1-44)NH2 = 1, [(3-Me)His1]hGRF(1-44)NH2 and [(O-Me)Tyr1]hGRF(1-44)NH2 have potencies of 0.132 and 0.001 respectively. These results demonstrate the prerequisite for an aromatic residue at position-1 for potent biological activity and also suggest that the capacity for hydrogen bond formation with the first residue is required for full receptor-ligand interaction.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
0006-291X
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
18
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pubmed:volume |
122
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
304-10
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:6430292-Amino Acids,
pubmed-meshheading:6430292-Animals,
pubmed-meshheading:6430292-Cells, Cultured,
pubmed-meshheading:6430292-Chemical Phenomena,
pubmed-meshheading:6430292-Chemistry,
pubmed-meshheading:6430292-Growth Hormone-Releasing Hormone,
pubmed-meshheading:6430292-Humans,
pubmed-meshheading:6430292-Pituitary Gland, Anterior,
pubmed-meshheading:6430292-Rats,
pubmed-meshheading:6430292-Structure-Activity Relationship,
pubmed-meshheading:6430292-Tyrosine
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pubmed:year |
1984
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pubmed:articleTitle |
Synthesis and in vitro bioactivity of human growth hormone-releasing factor analogs substituted at position-1.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
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