FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W1847375317> ?p ?o ?g. }

• W1847375317 endingPage "2460" @default.
• W1847375317 startingPage "2447" @default.
• W1847375317 abstract "SMYD3 is a histone lysine methyltransferase that plays an important role in transcriptional activation as a member of an RNA polymerase complex, and its oncogenic role has been described in different cancer types. We studied the expression and activity of SMYD3 in a preclinical model of colorectal cancer (CRC) and found that it is strongly upregulated throughout tumorigenesis both at the mRNA and protein level. Our results also showed that RNAi-mediated SMYD3 ablation impairs CRC cell proliferation indicating that SMYD3 is required for proper cancer cell growth. These data, together with the importance of lysine methyltransferases as a target for drug discovery, prompted us to carry out a virtual screening to identify new SMYD3 inhibitors by testing several candidate small molecules. Here we report that one of these compounds (BCI-121) induces a significant reduction in SMYD3 activity both in vitro and in CRC cells, as suggested by the analysis of global H3K4me2/3 and H4K5me levels. Of note, the extent of cell growth inhibition by BCI-121 was similar to that observed upon SMYD3 genetic ablation. Most of the results described above were obtained in CRC; however, when we extended our observations to tumor cell lines of different origin, we found that SMYD3 inhibitors are also effective in other cancer types, such as lung, pancreatic, prostate, and ovarian. These results represent the proof of principle that SMYD3 is a druggable target and suggest that new compounds capable of inhibiting its activity may prove useful as novel therapeutic agents in cancer treatment." @default.
• W1847375317 created "2016-06-24" @default.
• W1847375317 creator A5003044125 @default.
• W1847375317 creator A5008704314 @default.
• W1847375317 creator A5022863809 @default.
• W1847375317 creator A5027468637 @default.
• W1847375317 creator A5029952418 @default.
• W1847375317 creator A5038210500 @default.
• W1847375317 creator A5048973625 @default.
• W1847375317 creator A5067734935 @default.
• W1847375317 creator A5073078017 @default.
• W1847375317 creator A5081139093 @default.
• W1847375317 creator A5083555539 @default.
• W1847375317 creator A5087975070 @default.
• W1847375317 creator A5091304067 @default.
• W1847375317 date "2015-06-23" @default.
• W1847375317 modified "2023-10-11" @default.
• W1847375317 title "A SMYD3 Small-Molecule Inhibitor Impairing Cancer Cell Growth" @default.
• W1847375317 cites W1973059973 @default.
• W1847375317 cites W1980192737 @default.
• W1847375317 cites W1987126775 @default.
• W1847375317 cites W1988323955 @default.
• W1847375317 cites W2005784985 @default.
• W1847375317 cites W2009858080 @default.
• W1847375317 cites W2015735594 @default.
• W1847375317 cites W2026044471 @default.
• W1847375317 cites W2037215281 @default.
• W1847375317 cites W2040426919 @default.
• W1847375317 cites W2041368867 @default.
• W1847375317 cites W2049828484 @default.
• W1847375317 cites W2051406272 @default.
• W1847375317 cites W2052346464 @default.
• W1847375317 cites W2070772602 @default.
• W1847375317 cites W2078616374 @default.
• W1847375317 cites W2089288158 @default.
• W1847375317 cites W2101892858 @default.
• W1847375317 cites W2144127584 @default.
• W1847375317 cites W2146634563 @default.
• W1847375317 cites W2159132468 @default.
• W1847375317 cites W2163412990 @default.
• W1847375317 cites W2167779364 @default.
• W1847375317 doi "https://doi.org/10.1002/jcp.24975" @default.
• W1847375317 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/4988495" @default.
• W1847375317 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/25728514" @default.
• W1847375317 hasPublicationYear "2015" @default.
• W1847375317 type Work @default.
• W1847375317 sameAs 1847375317 @default.
• W1847375317 citedByCount "91" @default.
• W1847375317 countsByYear W18473753172015 @default.
• W1847375317 countsByYear W18473753172016 @default.
• W1847375317 countsByYear W18473753172017 @default.
• W1847375317 countsByYear W18473753172018 @default.
• W1847375317 countsByYear W18473753172019 @default.
• W1847375317 countsByYear W18473753172020 @default.
• W1847375317 countsByYear W18473753172021 @default.
• W1847375317 countsByYear W18473753172022 @default.
• W1847375317 countsByYear W18473753172023 @default.
• W1847375317 crossrefType "journal-article" @default.
• W1847375317 hasAuthorship W1847375317A5003044125 @default.
• W1847375317 hasAuthorship W1847375317A5008704314 @default.
• W1847375317 hasAuthorship W1847375317A5022863809 @default.
• W1847375317 hasAuthorship W1847375317A5027468637 @default.
• W1847375317 hasAuthorship W1847375317A5029952418 @default.
• W1847375317 hasAuthorship W1847375317A5038210500 @default.
• W1847375317 hasAuthorship W1847375317A5048973625 @default.
• W1847375317 hasAuthorship W1847375317A5067734935 @default.
• W1847375317 hasAuthorship W1847375317A5073078017 @default.
• W1847375317 hasAuthorship W1847375317A5081139093 @default.
• W1847375317 hasAuthorship W1847375317A5083555539 @default.
• W1847375317 hasAuthorship W1847375317A5087975070 @default.
• W1847375317 hasAuthorship W1847375317A5091304067 @default.
• W1847375317 hasBestOaLocation W18473753172 @default.
• W1847375317 hasConcept C104317684 @default.
• W1847375317 hasConcept C10679952 @default.
• W1847375317 hasConcept C121608353 @default.
• W1847375317 hasConcept C127561419 @default.
• W1847375317 hasConcept C166703698 @default.
• W1847375317 hasConcept C173396325 @default.
• W1847375317 hasConcept C190232843 @default.
• W1847375317 hasConcept C33288867 @default.
• W1847375317 hasConcept C41091548 @default.
• W1847375317 hasConcept C502942594 @default.
• W1847375317 hasConcept C54355233 @default.
• W1847375317 hasConcept C555283112 @default.
• W1847375317 hasConcept C62112901 @default.
• W1847375317 hasConcept C67705224 @default.
• W1847375317 hasConcept C81885089 @default.
• W1847375317 hasConcept C86803240 @default.
• W1847375317 hasConcept C91965660 @default.
• W1847375317 hasConcept C96232424 @default.
• W1847375317 hasConceptScore W1847375317C104317684 @default.
• W1847375317 hasConceptScore W1847375317C10679952 @default.
• W1847375317 hasConceptScore W1847375317C121608353 @default.
• W1847375317 hasConceptScore W1847375317C127561419 @default.
• W1847375317 hasConceptScore W1847375317C166703698 @default.
• W1847375317 hasConceptScore W1847375317C173396325 @default.
• W1847375317 hasConceptScore W1847375317C190232843 @default.
• W1847375317 hasConceptScore W1847375317C33288867 @default.

• next