Linked Life Data

7108896

Source:http://linkedlifedata.com/resource/pubmed/id/7108896

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
7
pubmed:dateCreated
1982-10-21
pubmed:abstractText
Syntheses are described of p1-(adenosine-5')-p3-(glucose-6) triphosphate (Ap3 glucose), Ap4 glucose, and p1-(adenosine-5')-P3-(thymidine-5') triphosphate (Ap3T). The compounds were not substrates of any of the enzymes used in the present studies. Ap3 glucose and Ap4 glucose were inhibitors of yeast hexokinase (HK) and the rat isozymes HK I-III; in general, they had less affinity for the enzymes than the substrates ATP and glucose. Inhibition constants (Ki values) of Ap3T with rat mitochondrial thymidine kinase (M-TK) and rat cytoplasmic TK (C-TK) were determined for variable thymidine (TdR) with a constant saturating level of ATP and for variable ATP with constant saturating TdR. Ap3T was a potent and selective inhibitor of M-TK [KM (TdR)/Ki = 1.6, KM (ATP)/Ki = 38 with variable ATP; KM (TdR) Ki = 0.06, KM (ATP)/Ki = 1.4 with variable TdR] relative to C-TK [KM (TdR)/Ki = 0.006, KM (ATP)/Ki = 0.7 with variable ATP; KM (TdR)/Ki = 0.001, KM (ATP)/Ki = 0.12 with variable TdR]. Inhibition of M-TK and C-TK by Ap3T differed qualitatively and quantitatively from inhibition under the same conditions by the metabolic feedback inhibitor TdR 5'-triphosphate.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jul
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:volume
25
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
801-5
pubmed:dateRevised
2008-11-21
pubmed:meshHeading
pubmed:year
1982
pubmed:articleTitle
Species- or isozyme-specific enzyme inhibitors. 6. Synthesis and evaluation of two-substrate condensation products as inhibitors of hexokinases and thymidine kinases.
pubmed:publicationType
Journal Article, In Vitro, Research Support, U.S. Gov't, P.H.S., Research Support, Non-U.S. Gov't