Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
21
pubmed:dateCreated
1988-12-15
pubmed:abstractText
Challenge of human cells with auranofin, 2,3,4,6-tetra-O-acetyl-1-thio-beta-D-glucopyranosato-S-triethylpho sphine gold(I) (Ridaura), a gold-containing compound approved by the FDA for the treatment of rheumatoid arthritis, induces the specific synthesis of a 32-kD stress protein (p32) [Caltabiano et al., Biochem. biophys. Res. Commun. 138, 1074 (1986)]. To establish a structure-activity relationship for this effect, a series of auranofin ligands, gold analogs, and other anti-arthritic agents were examined for their abilities to stimulate p32 synthesis. The results indicate that the gold atom is necessary for enhanced expression of p32. However, the structure of co-ordinated ligands also affected potency, and gold complexes bearing several phosphine or thiosugar groups exhibited the greatest activity. These data indicate that the distinct potencies of auranofin analogs probably reflect their membrane permeability and subsequent delivery of pharmacologically active concentrations of gold to the cytoplasmic compartment.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Nov
pubmed:issn
0006-2952
pubmed:author
pubmed:issnType
Print
pubmed:day
1
pubmed:volume
37
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
4089-93
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1988
pubmed:articleTitle
Induction of the 32-kD human stress protein by auranofin and related triethylphosphine gold analogs.
pubmed:affiliation
Department of Cell Biology, Smith Kline & French Laboratories, Philadelphia, PA 19101.
pubmed:publicationType
Journal Article, In Vitro