Matches in SemOpenAlex for { <https://semopenalex.org/work/W3042358676> ?p ?o ?g. }
Showing items 1 to 88 of
88
with 100 items per page.
- W3042358676 endingPage "4861" @default.
- W3042358676 startingPage "4861" @default.
- W3042358676 abstract "4861 Protein tyrosine kinases (PTK) have been recognized as promising therapeutic targets involved in a variety of human diseases and in particular several types of cancer. An effort towards the development of new and more effective PTK inhibitors represents an attractive therapeutic strategy for cancer therapy. Here we report the identification of some potent c-Src tyrosine kinase inhibitors by an automated high-throughput screening (HTS) strategy based on the orthogonal-compound-mixing ELISA method. Hematoxylin (26), the main component of the plant Heamatoxylon campechianum (Leguminosae), stood out as one of the most remarkable c-Src inhibitors of 32,200 compounds. Further studies revealed that hematoxylin is an ATP competitive broad-spectrum PTK inhibitor in vitro, with IC50 values ranging from nanomolar to micromolar level. In addition, hematoxylin is also noted to inhibit the phosphorylation of PTK and arrest the downstream signaling pathways in cellular level. Moreover, other ten new homoisoflavonoids (1-10), together with sixteen known homoisoflavonoids and chalcones (11-26), were isolated from the stems of H. campechianum upon bioassay-guided fractionation. The structure-activity relationship of these compounds was further performed by assessing the PTK inhibitory potency with concurrent molecular docking simulation. Interestingly, the catechol moiety in ring A and the hematoxylin-like three-dimensional structure are essential for c-Src-targeted activities. Together, with the availability of the established ELISA-based HTS screening approach, hematoxylin and its natural analogues were substantially validated to function as a new class of PTK inhibitors." @default.
- W3042358676 created "2020-07-23" @default.
- W3042358676 creator A5001392142 @default.
- W3042358676 creator A5001543291 @default.
- W3042358676 creator A5016087217 @default.
- W3042358676 creator A5017496773 @default.
- W3042358676 creator A5034965904 @default.
- W3042358676 creator A5043148241 @default.
- W3042358676 creator A5058334717 @default.
- W3042358676 creator A5061074781 @default.
- W3042358676 creator A5062979525 @default.
- W3042358676 creator A5076615377 @default.
- W3042358676 creator A5080277040 @default.
- W3042358676 creator A5089348951 @default.
- W3042358676 date "2008-05-01" @default.
- W3042358676 modified "2023-09-29" @default.
- W3042358676 title "Naturally occurring homoisoflavonoids function as potent protein tyrosine kinases inhibitors by c-Src-based high-throughput screening" @default.
- W3042358676 hasPublicationYear "2008" @default.
- W3042358676 type Work @default.
- W3042358676 sameAs 3042358676 @default.
- W3042358676 citedByCount "0" @default.
- W3042358676 crossrefType "journal-article" @default.
- W3042358676 hasAuthorship W3042358676A5001392142 @default.
- W3042358676 hasAuthorship W3042358676A5001543291 @default.
- W3042358676 hasAuthorship W3042358676A5016087217 @default.
- W3042358676 hasAuthorship W3042358676A5017496773 @default.
- W3042358676 hasAuthorship W3042358676A5034965904 @default.
- W3042358676 hasAuthorship W3042358676A5043148241 @default.
- W3042358676 hasAuthorship W3042358676A5058334717 @default.
- W3042358676 hasAuthorship W3042358676A5061074781 @default.
- W3042358676 hasAuthorship W3042358676A5062979525 @default.
- W3042358676 hasAuthorship W3042358676A5076615377 @default.
- W3042358676 hasAuthorship W3042358676A5080277040 @default.
- W3042358676 hasAuthorship W3042358676A5089348951 @default.
- W3042358676 hasConcept C11960822 @default.
- W3042358676 hasConcept C159110408 @default.
- W3042358676 hasConcept C184235292 @default.
- W3042358676 hasConcept C185592680 @default.
- W3042358676 hasConcept C41685203 @default.
- W3042358676 hasConcept C42362537 @default.
- W3042358676 hasConcept C55493867 @default.
- W3042358676 hasConcept C62478195 @default.
- W3042358676 hasConcept C71924100 @default.
- W3042358676 hasConcept C74187038 @default.
- W3042358676 hasConcept C86803240 @default.
- W3042358676 hasConcept C98274493 @default.
- W3042358676 hasConceptScore W3042358676C11960822 @default.
- W3042358676 hasConceptScore W3042358676C159110408 @default.
- W3042358676 hasConceptScore W3042358676C184235292 @default.
- W3042358676 hasConceptScore W3042358676C185592680 @default.
- W3042358676 hasConceptScore W3042358676C41685203 @default.
- W3042358676 hasConceptScore W3042358676C42362537 @default.
- W3042358676 hasConceptScore W3042358676C55493867 @default.
- W3042358676 hasConceptScore W3042358676C62478195 @default.
- W3042358676 hasConceptScore W3042358676C71924100 @default.
- W3042358676 hasConceptScore W3042358676C74187038 @default.
- W3042358676 hasConceptScore W3042358676C86803240 @default.
- W3042358676 hasConceptScore W3042358676C98274493 @default.
- W3042358676 hasLocation W30423586761 @default.
- W3042358676 hasOpenAccess W3042358676 @default.
- W3042358676 hasPrimaryLocation W30423586761 @default.
- W3042358676 hasRelatedWork W1840208272 @default.
- W3042358676 hasRelatedWork W2023293447 @default.
- W3042358676 hasRelatedWork W2048030161 @default.
- W3042358676 hasRelatedWork W2061576044 @default.
- W3042358676 hasRelatedWork W2079677704 @default.
- W3042358676 hasRelatedWork W2081895140 @default.
- W3042358676 hasRelatedWork W2160953463 @default.
- W3042358676 hasRelatedWork W2170050478 @default.
- W3042358676 hasRelatedWork W2179715433 @default.
- W3042358676 hasRelatedWork W2185406231 @default.
- W3042358676 hasRelatedWork W2329789195 @default.
- W3042358676 hasRelatedWork W2563224463 @default.
- W3042358676 hasRelatedWork W2791676400 @default.
- W3042358676 hasRelatedWork W2793991650 @default.
- W3042358676 hasRelatedWork W2891059578 @default.
- W3042358676 hasRelatedWork W2891783064 @default.
- W3042358676 hasRelatedWork W2904187456 @default.
- W3042358676 hasRelatedWork W2952691035 @default.
- W3042358676 hasRelatedWork W2980552617 @default.
- W3042358676 hasRelatedWork W599275125 @default.
- W3042358676 hasVolume "68" @default.
- W3042358676 isParatext "false" @default.
- W3042358676 isRetracted "false" @default.
- W3042358676 magId "3042358676" @default.
- W3042358676 workType "article" @default.