Matches in SemOpenAlex for { <https://semopenalex.org/work/W2020165342> ?p ?o ?g. }
Showing items 1 to 84 of
84
with 100 items per page.
- W2020165342 abstract "Arglabin [1(R),10(S)-epoxy-5(S),5(S),7(S)-guaia-3(4),11(13)-dien-6, 12-olide], a sesquiterpene gamma-lactone is isolated from Artemisia glabella, a species of wormwood endemic to the Karaganda region of Kazakstan. The compound has been modified to render it water-soluble through addition of a dimethylaminohydrochloride group to the C(13) carbohydride moiety to yield Arglabin-DMA. Arglabin-DMA is a registered antitumor substance in the Republic of Kazakstan. Previously, we have shown that this compound prevents protein farnesylation without altering geranylgeranylation. We now report that Arglabin-DMA inhibits the incorporation of [(3)H]farnesylpyrophosphate into human H-ras protein by FTase with an IC(50) of no greater than 25 microM. Kinetic studies show that the phosphorylated form of this compound competitively inhibits the binding of farnesyl diphosphate to FTase. This mechanism of action is different from other reported peptidomimetic FTIs which lower the affinity of ras protein to FTase. Our in vitro studies confirm that Arglabin-DMA inhibits post-translational modification of ras protein in cells. Arglabin-DMA inhibits anchorage-dependent proliferation of NB cells (IC50=10 microg/ml) and inhibits anchorage-independent growth of NB and KNRK cells with about the same IC(50). Soft-agar colony formation assay of H-ras and K-ras transformed cells show IC(50)s to be 2 and 5 microg/ml, respectively. In primary cultures of human tumor cells, Arglabin-DMA inhibits cell proliferation of a variety of tumor types with IC(90)s in the range of 0.85 to 5.0 microg/ml. Because of these pharmacologic properties, we propose that Arglabin-DMA is suitable for the treatment of ras related malignancies." @default.
- W2020165342 created "2016-06-24" @default.
- W2020165342 creator A5006256037 @default.
- W2020165342 creator A5017465926 @default.
- W2020165342 creator A5022667578 @default.
- W2020165342 creator A5059740421 @default.
- W2020165342 creator A5062883426 @default.
- W2020165342 creator A5086257215 @default.
- W2020165342 creator A5086839893 @default.
- W2020165342 date "2001-01-01" @default.
- W2020165342 modified "2023-10-16" @default.
- W2020165342 title "Arglabin-DMA, a plant derived sesquiterpene, inhibits farnesyltransferase." @default.
- W2020165342 doi "https://doi.org/10.3892/or.8.1.173" @default.
- W2020165342 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/11115593" @default.
- W2020165342 hasPublicationYear "2001" @default.
- W2020165342 type Work @default.
- W2020165342 sameAs 2020165342 @default.
- W2020165342 citedByCount "11" @default.
- W2020165342 countsByYear W20201653422012 @default.
- W2020165342 countsByYear W20201653422015 @default.
- W2020165342 countsByYear W20201653422016 @default.
- W2020165342 countsByYear W20201653422020 @default.
- W2020165342 countsByYear W20201653422021 @default.
- W2020165342 countsByYear W20201653422023 @default.
- W2020165342 crossrefType "journal-article" @default.
- W2020165342 hasAuthorship W2020165342A5006256037 @default.
- W2020165342 hasAuthorship W2020165342A5017465926 @default.
- W2020165342 hasAuthorship W2020165342A5022667578 @default.
- W2020165342 hasAuthorship W2020165342A5059740421 @default.
- W2020165342 hasAuthorship W2020165342A5062883426 @default.
- W2020165342 hasAuthorship W2020165342A5086257215 @default.
- W2020165342 hasAuthorship W2020165342A5086839893 @default.
- W2020165342 hasConcept C124790011 @default.
- W2020165342 hasConcept C1491633281 @default.
- W2020165342 hasConcept C181199279 @default.
- W2020165342 hasConcept C185592680 @default.
- W2020165342 hasConcept C2776211264 @default.
- W2020165342 hasConcept C2777827897 @default.
- W2020165342 hasConcept C2778396349 @default.
- W2020165342 hasConcept C2779243328 @default.
- W2020165342 hasConcept C2779281246 @default.
- W2020165342 hasConcept C2779716203 @default.
- W2020165342 hasConcept C2781018059 @default.
- W2020165342 hasConcept C29537977 @default.
- W2020165342 hasConcept C55493867 @default.
- W2020165342 hasConcept C57790582 @default.
- W2020165342 hasConcept C62112901 @default.
- W2020165342 hasConcept C71240020 @default.
- W2020165342 hasConcept C86803240 @default.
- W2020165342 hasConceptScore W2020165342C124790011 @default.
- W2020165342 hasConceptScore W2020165342C1491633281 @default.
- W2020165342 hasConceptScore W2020165342C181199279 @default.
- W2020165342 hasConceptScore W2020165342C185592680 @default.
- W2020165342 hasConceptScore W2020165342C2776211264 @default.
- W2020165342 hasConceptScore W2020165342C2777827897 @default.
- W2020165342 hasConceptScore W2020165342C2778396349 @default.
- W2020165342 hasConceptScore W2020165342C2779243328 @default.
- W2020165342 hasConceptScore W2020165342C2779281246 @default.
- W2020165342 hasConceptScore W2020165342C2779716203 @default.
- W2020165342 hasConceptScore W2020165342C2781018059 @default.
- W2020165342 hasConceptScore W2020165342C29537977 @default.
- W2020165342 hasConceptScore W2020165342C55493867 @default.
- W2020165342 hasConceptScore W2020165342C57790582 @default.
- W2020165342 hasConceptScore W2020165342C62112901 @default.
- W2020165342 hasConceptScore W2020165342C71240020 @default.
- W2020165342 hasConceptScore W2020165342C86803240 @default.
- W2020165342 hasLocation W20201653421 @default.
- W2020165342 hasLocation W20201653422 @default.
- W2020165342 hasOpenAccess W2020165342 @default.
- W2020165342 hasPrimaryLocation W20201653421 @default.
- W2020165342 hasRelatedWork W1964186173 @default.
- W2020165342 hasRelatedWork W1984485872 @default.
- W2020165342 hasRelatedWork W2038634407 @default.
- W2020165342 hasRelatedWork W2048406231 @default.
- W2020165342 hasRelatedWork W2073826564 @default.
- W2020165342 hasRelatedWork W2103221476 @default.
- W2020165342 hasRelatedWork W2126918368 @default.
- W2020165342 hasRelatedWork W2174826339 @default.
- W2020165342 hasRelatedWork W2339901706 @default.
- W2020165342 hasRelatedWork W2726590128 @default.
- W2020165342 isParatext "false" @default.
- W2020165342 isRetracted "false" @default.
- W2020165342 magId "2020165342" @default.
- W2020165342 workType "article" @default.