Source:http://linkedlifedata.com/resource/pubmed/id/14987000
Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
|
pubmed:dateCreated |
2004-2-27
|
pubmed:abstractText |
Three analogues of RA-VII (1), an antitumor bicyclic hexapeptide from Rubia plants, were synthesized. Three analogues, [Gly-1]RA-VII (4), [Gly-2]RA-VII (5), and [Gly-4]RA-VII (6), in which one of the three alanine residues in 1 was replaced by a glycine residue, were prepared by linking of the cycloisodityrosine unit, obtained by degradation of 1, to three different glycine-containing tetrapeptides followed by macrocyclization. Of these three analogues, analogue 4 showed the highest cytotoxic activity. The NMR study revealed that in solution the conformer structures and their ratios of analogue 4 were very similar to those of natural peptide 1, suggesting that the methyl groups at Ala-2 and Ala-4 should be essential for producing the bioactive conformation, whereas that at D-Ala-1 is not essential.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Antineoplastic Agents, Phytogenic,
http://linkedlifedata.com/resource/pubmed/chemical/Bicyclo Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Glycine,
http://linkedlifedata.com/resource/pubmed/chemical/Peptides, Cyclic,
http://linkedlifedata.com/resource/pubmed/chemical/RA VII
|
pubmed:status |
MEDLINE
|
pubmed:month |
Mar
|
pubmed:issn |
0022-3263
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:day |
5
|
pubmed:volume |
69
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
1481-6
|
pubmed:meshHeading |
pubmed-meshheading:14987000-Animals,
pubmed-meshheading:14987000-Antineoplastic Agents, Phytogenic,
pubmed-meshheading:14987000-Bicyclo Compounds,
pubmed-meshheading:14987000-Cell Survival,
pubmed-meshheading:14987000-Cyclization,
pubmed-meshheading:14987000-Glycine,
pubmed-meshheading:14987000-Mice,
pubmed-meshheading:14987000-Molecular Structure,
pubmed-meshheading:14987000-Peptides, Cyclic,
pubmed-meshheading:14987000-Protein Conformation,
pubmed-meshheading:14987000-Rubia,
pubmed-meshheading:14987000-Structure-Activity Relationship,
pubmed-meshheading:14987000-Tumor Cells, Cultured
|
pubmed:year |
2004
|
pubmed:articleTitle |
Synthesis of [Gly-1]RA-VII, [Gly-2]RA-VII, and [Gly-4]RA-VII. Glycine-containing analogues of RA-VII, an antitumor bicyclic hexapeptide from Rubia plants.
|
pubmed:affiliation |
School of Pharmacy, Tokyo University of Pharmacy and Life Science, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan.
|
pubmed:publicationType |
Journal Article
|