Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
12
pubmed:dateCreated
1987-1-15
pubmed:abstractText
Diterpene esters containing 12-0-tetradecanoylphorbol-13-acetate (TPA) and the alkaloid teleocidins are structurally unrelated natural products that exhibit similar potent skin tumor-promoting activity. These promoters are classified as TPA-type promoters because they bind equally to the phorbol ester receptor. TPA can be considered as an amphiphilic compound, with a hydrophilic domain spanning the C-3 to C-20 region of the molecule and a lipophilic domain consisting of the acyl substituents on C-12 and C-13. Teleocidins can also be considered as amphiphilic compounds, with the hydrophilic domain spanning the C-11 to C-14 region of the molecule and the lipophilic domain consisting of the alkyl substituents on C-6, C-7 and C-12. Teleocidins exist in two conformational states, the TWIST form and the SOFA form, in solution. From the ratio of the two conformations in solution, the free-energy difference between them was calculated to be 0-1.5 kcal/mol. Therefore a possible role of one of the two conformations should be considered in the modeling of receptor mapping. Computer modeling of the SOFA form of teleocidins and TPA showed a marked similarity with regards to the hydrogen bonding sites of the hydrophilic substituents. In this case, good superposition of the lipophilic regions of both types of compounds was obtained.
pubmed:language
jpn
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Dec
pubmed:issn
0385-0684
pubmed:author
pubmed:issnType
Print
pubmed:volume
13
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
3365-75
pubmed:dateRevised
2007-11-15
pubmed:meshHeading
pubmed:year
1986
pubmed:articleTitle
[The active structure of tumor promoters].
pubmed:publicationType
Journal Article, English Abstract