FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2549147908> ?p ?o ?g. }

• W2549147908 endingPage "1938" @default.
• W2549147908 startingPage "1926" @default.
• W2549147908 abstract "Cancer cells resort to activating hypoxia-inducible factor-1 (HIF-1) as one of several responses to hypoxic conditions. Overexpression of HIF-1, the transcriptional regulator for a group of malignant-pathway related genes including vascular endothelial growth factor (VEGF), is associated with increased tumor growth, vascularization, and metastasis. HIF-1 is composed of an inducible subunit, HIF-1α and a constitutively expressed subunit, HIF-1ß. HIF-1 activity is mainly dependent on the level of HIF-1α protein, the inducible and regulatory subunit of the HIF-1 heterodimer complex; thus, identification of novel anti-HIF-1α agents will lead to effective blockage of the HIF-1 (HIF-1α)-mediated switch-on function for those malignant-pathway related genes and suppression of the HIF-1α/VEGF-mediated signaling pathway that promotes cancer progression and metastasis. While there is an extremely large number of small molecule compounds in the database (compound libraries), the currently existing screening system is inefficient and time-consuming; or, at best, the application of the existing screening system is very limited as it is usually not coupled with biological validation processes. The further development of potential drugs is partly hindered due to the cumbersome steps in between the primary screen and consequent validation: the slow, exhausted and sometimes lack of a linked biological validation process contributes to the dismal fate of scant compounds uncovered in the primary screen. To improve upon the status quo, we developed a prototype screening system that is coupled anti-HIF-1α primary screen with secondary anti-VEGF/anti-angiogenesis validation screens. We used breast cancer cells as the model to select potent anti-HIF-1α small-molecule compounds by their abilities to inhibit transactivation of a VEGF promoter fused to a luciferase reporter gene under hypoxia. Positive compounds were then validated by a series of assays that confirm compounds' anti-HIF-1α activities including measurement of their effects on HIF-1α downstream VEGF gene expression and angiogenic ability of breast cancer cells. Moreover, we demonstrated that we could further improve the compound's potency of anti-HIF-1α and anti-angiogenesis by modifying the identified lead to synthesize a superior (novel) drug." @default.
• W2549147908 created "2016-11-30" @default.
• W2549147908 creator A5018639891 @default.
• W2549147908 creator A5019408853 @default.
• W2549147908 creator A5026231888 @default.
• W2549147908 date "2016-01-01" @default.
• W2549147908 modified "2023-10-12" @default.
• W2549147908 title "Selection, Analysis and Improvement of Anti-Angiogenesis Compounds Identified by an Anti-HIF-1α Screening and Validation System" @default.
• W2549147908 cites W1493048246 @default.
• W2549147908 cites W1534920898 @default.
• W2549147908 cites W1624342207 @default.
• W2549147908 cites W1682474579 @default.
• W2549147908 cites W1935819037 @default.
• W2549147908 cites W1978139448 @default.
• W2549147908 cites W2000019513 @default.
• W2549147908 cites W2009084109 @default.
• W2549147908 cites W2011810742 @default.
• W2549147908 cites W2012520088 @default.
• W2549147908 cites W2020105314 @default.
• W2549147908 cites W2023042442 @default.
• W2549147908 cites W2024206845 @default.
• W2549147908 cites W2035550438 @default.
• W2549147908 cites W2047253593 @default.
• W2549147908 cites W2050848188 @default.
• W2549147908 cites W2054605167 @default.
• W2549147908 cites W2062549580 @default.
• W2549147908 cites W206348675 @default.
• W2549147908 cites W2072227408 @default.
• W2549147908 cites W2081561797 @default.
• W2549147908 cites W2104114689 @default.
• W2549147908 cites W2104134459 @default.
• W2549147908 cites W2104143436 @default.
• W2549147908 cites W2105294528 @default.
• W2549147908 cites W2107806932 @default.
• W2549147908 cites W2108652737 @default.
• W2549147908 cites W2130219349 @default.
• W2549147908 cites W2137038184 @default.
• W2549147908 cites W2137090229 @default.
• W2549147908 cites W2141046053 @default.
• W2549147908 cites W2146270900 @default.
• W2549147908 cites W2148270074 @default.
• W2549147908 cites W2160592082 @default.
• W2549147908 cites W2163069245 @default.
• W2549147908 cites W2168014041 @default.
• W2549147908 cites W2169063134 @default.
• W2549147908 cites W2467657054 @default.
• W2549147908 cites W25524544 @default.
• W2549147908 cites W4285719527 @default.
• W2549147908 cites W620385815 @default.
• W2549147908 doi "https://doi.org/10.7150/jca.15603" @default.
• W2549147908 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/5118656" @default.
• W2549147908 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/27877208" @default.
• W2549147908 hasPublicationYear "2016" @default.
• W2549147908 type Work @default.
• W2549147908 sameAs 2549147908 @default.
• W2549147908 citedByCount "6" @default.
• W2549147908 countsByYear W25491479082017 @default.
• W2549147908 countsByYear W25491479082018 @default.
• W2549147908 countsByYear W25491479082019 @default.
• W2549147908 countsByYear W25491479082020 @default.
• W2549147908 countsByYear W25491479082021 @default.
• W2549147908 countsByYear W25491479082023 @default.
• W2549147908 crossrefType "journal-article" @default.
• W2549147908 hasAuthorship W2549147908A5018639891 @default.
• W2549147908 hasAuthorship W2549147908A5019408853 @default.
• W2549147908 hasAuthorship W2549147908A5026231888 @default.
• W2549147908 hasBestOaLocation W25491479081 @default.
• W2549147908 hasConcept C104292427 @default.
• W2549147908 hasConcept C104317684 @default.
• W2549147908 hasConcept C121608353 @default.
• W2549147908 hasConcept C127716648 @default.
• W2549147908 hasConcept C160450060 @default.
• W2549147908 hasConcept C167734588 @default.
• W2549147908 hasConcept C2777025900 @default.
• W2549147908 hasConcept C2779013556 @default.
• W2549147908 hasConcept C2780394083 @default.
• W2549147908 hasConcept C502942594 @default.
• W2549147908 hasConcept C54355233 @default.
• W2549147908 hasConcept C60644358 @default.
• W2549147908 hasConcept C6929976 @default.
• W2549147908 hasConcept C70721500 @default.
• W2549147908 hasConcept C86803240 @default.
• W2549147908 hasConceptScore W2549147908C104292427 @default.
• W2549147908 hasConceptScore W2549147908C104317684 @default.
• W2549147908 hasConceptScore W2549147908C121608353 @default.
• W2549147908 hasConceptScore W2549147908C127716648 @default.
• W2549147908 hasConceptScore W2549147908C160450060 @default.
• W2549147908 hasConceptScore W2549147908C167734588 @default.
• W2549147908 hasConceptScore W2549147908C2777025900 @default.
• W2549147908 hasConceptScore W2549147908C2779013556 @default.
• W2549147908 hasConceptScore W2549147908C2780394083 @default.
• W2549147908 hasConceptScore W2549147908C502942594 @default.
• W2549147908 hasConceptScore W2549147908C54355233 @default.
• W2549147908 hasConceptScore W2549147908C60644358 @default.
• W2549147908 hasConceptScore W2549147908C6929976 @default.
• W2549147908 hasConceptScore W2549147908C70721500 @default.
• W2549147908 hasConceptScore W2549147908C86803240 @default.
• W2549147908 hasIssue "14" @default.

• next