Linked Life Data

7097717

Source:http://linkedlifedata.com/resource/pubmed/id/7097717

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
6
pubmed:dateCreated
1982-9-24
pubmed:abstractText
Derivatives obtained by single replacements or substitutions of groups at eight positions of thymidine (TdR) have been examined as inhibitors of rat mitochondrial (M-TK) and cytoplasmic (C-TK) isozymes of thymidine kinase. A C-TK (pI = 7.5) and an M-TK (pI = 5.1) from rat spleen were purified to apparent isozymic homogeneity by isoelectric focusing. Affinities relative to that of TdR for the TdR sites of the isozymes were derived by dividing the Michaelis constants of TdR by the inhibition constants. Of the eight types of TdR derivatives, five had higher affinity for the M-TK site and two had higher affinity for the C-TK site. The most potent and/or selective inhibitors were 3'-O-benzyl-TdR (affinity for M-TK relative to TdR, 100%; differential affinity for M-TK vs. C-TK, 7.5), 5-amino-2'-deoxyuridine (relative affinity for M-TK, 11%; differential affinity affinity for M-TK, 26), 5'-amino-5'-deoxy-TdR (relative affinity for C-TK, 67%; differential affinity for C-TK, greater than 25). Effects of modifying certain of the substituents indicate that at least some of these TdR derivatives are potential progenitors of TK inhibitors of higher potency and selectivity.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jun
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:volume
25
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
644-9
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:year
1982
pubmed:articleTitle
Species- or isozyme-specific enzyme inhibitors. 5. Differential effects of thymidine substituents on affinity for rat thymidine kinase isozymes.
pubmed:publicationType
Journal Article, In Vitro, Research Support, U.S. Gov't, P.H.S., Research Support, Non-U.S. Gov't