|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
9
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|
pubmed:dateCreated |
1995-5-18
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|
pubmed:abstractText |
Replacement of the central amino methylene linkage of C[psi CH2NH]A[psi CH2NH]AX tetrapeptide inhibitors with carbon tethers led to compounds with potency in the nanomolar range. Some of the more potent olefinic compounds inhibit Ras processing in intact v-ras transformed NIH 3T3 cells with IC50 values in the 0.1 to 1 microM range, and inhibit selectively the anchorage-independent growth of H-ras transformed Rat1 cells at 10 microM.
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|
pubmed:language |
eng
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|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
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|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Sep
|
|
pubmed:issn |
0968-0896
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|
pubmed:author |
|
|
pubmed:issnType |
Print
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|
pubmed:volume |
2
|
|
pubmed:geneSymbol |
H-ras,
ras,
v-raf,
v-ras
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
N
|
|
pubmed:pagination |
939-47
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|
pubmed:dateRevised |
2006-11-15
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|
pubmed:meshHeading |
pubmed-meshheading:7712129-3T3 Cells,
pubmed-meshheading:7712129-Alkyl and Aryl Transferases,
pubmed-meshheading:7712129-Amino Acid Sequence,
pubmed-meshheading:7712129-Animals,
pubmed-meshheading:7712129-Cell Transformation, Viral,
pubmed-meshheading:7712129-Genes, ras,
pubmed-meshheading:7712129-Mice,
pubmed-meshheading:7712129-Molecular Sequence Data,
pubmed-meshheading:7712129-Molecular Structure,
pubmed-meshheading:7712129-Oligopeptides,
pubmed-meshheading:7712129-Stereoisomerism,
pubmed-meshheading:7712129-Structure-Activity Relationship,
pubmed-meshheading:7712129-Transferases
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|
pubmed:year |
1994
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|
pubmed:articleTitle |
Synthesis and biological activity of ras farnesyl protein transferase inhibitors. Tetrapeptide analogs with amino methyl and carbon linkages.
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|
pubmed:affiliation |
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486.
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pubmed:publicationType |
Journal Article
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