* Novel acyclic nucleotide analogues GS-343074 and GS-424044 demonstrate antiproliferative and pro-apoptotic activity in canine neoplastic cell lines.
- GS-9219, a novel prodrug of the nucleotide analogue 9-(2-phosphonylmethoxyethyl) guanine (PMEG) has significant activity as monotherapy in dogs with non-Hodgkin's lymphoma. Phase I trials have been initiated in humans based on the encouraging activity observed in canine lymphoma. Two new analogues of GS-9219 (GS-343074 and GS-424044) were recently produced for evaluation as potential novel antineoplastic agents against solid tumours. As a preclinical step, effect of GS-343074 and GS-424044 were evaluated against ten canine cancer cell lines for antiproliferative effect. Both analogues displayed antiproliferative activity against multiple canine cancer cell lines, although GS-343074 was more potent and of broader spectrum compared to GS-424044. Flow cytometric analysis of cells that experienced growth inhibition support apoptotic death as a mechanism of action for both analogues. On the basis of in vitro results described here, GS-343074 and GS-424044 show promise as novel anticancer agents in canine cancer.
=>意義深い, 重大な, 意味のある, 意味ありげな, 重要な
Overview of adj significant
The adj significant has 4 senses (first 4 from tagged texts)
1. (18) significant, important -- (important in effect or meaning; "a significant change in tax
laws"; "a significant change in the Constitution"; "a significant contribution"; "significant
details"; "statistically significant")
2. (9) significant, substantial -- (fairly large; "won by a substantial margin")
3. (3) significant -- (too closely correlated to be attributed to chance and therefore indicating a
systematic relation; "the interaction effect is significant at the .01 level"; "no significant
difference was found")
4. (2) meaning, pregnant, significant -- (rich in significance or implication; "a meaning look")
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PubMed database: last updated on 2020-11-30 (c)sirasawa 2019