FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W3087110721> ?p ?o ?g. }

• W3087110721 endingPage "127557" @default.
• W3087110721 startingPage "127557" @default.
• W3087110721 abstract "Epidermal growth factor receptor tyrosine kinase (EGFR-TK) has been proved as a target for the treatment of non-small cell lung cancer (NSCLC) with specific gene mutations. However, EGFR-TK inhibitors (EGFR-TKIs) need to enter cancer cells and then competitively interact with the active site of tyrosine kinase receptors to suppress the downstream signaling pathway to inhibit tumor proliferation. In this study, in order to improve the tumor cell targeting ability of EGFR-TKI, EGFR-TKI erlotinib was conjugated with the cancer cell-targeting heptamethine cyanine dyes to form seventeen novel erlotinib-dye conjugates. The efficiency of tumor targeting properties of conjugates against cancer cell growth and EGFR-TK inhibition was evaluated in vitro. The result revealed that most erlotinib-dye conjugates exhibited stronger inhibitory effect on A549, H460, H1299 and MDA-MB-231 cell lines than the parent drug erlotinib. Meanwhile, representative compounds exhibited weak cytotoxicity on human normal mammary epithelial MCF-10A cells. Moreover, the conjugate CE17 also showed ~14-fold higher EGFR-TK inhibition activity (IC50 = 0.124 μM) than erlotinib (IC50 = 5.182 μM) in A549 cell line. Finally, molecular docking analysis verified that the erlotinib moiety of compound CE17 could form hydrogen bond with Met-769 and occupy active cavity of EGFR-TK. Therefore, we believed the integration strategy between heptamethine cyanine dyes and EGFR-TKI will contribute to enhancing the therapeutic effect of EGFR-TKI for NSCLC treatment." @default.
• W3087110721 created "2020-09-25" @default.
• W3087110721 creator A5005564764 @default.
• W3087110721 creator A5019549501 @default.
• W3087110721 creator A5024914206 @default.
• W3087110721 creator A5025865949 @default.
• W3087110721 creator A5050727001 @default.
• W3087110721 date "2020-12-01" @default.
• W3087110721 modified "2023-10-17" @default.
• W3087110721 title "Design, synthesis and biological evaluation of novel heptamethine cyanine dye-erlotinib conjugates as antitumor agents" @default.
• W3087110721 cites W1836179493 @default.
• W3087110721 cites W1994643935 @default.
• W3087110721 cites W2019921658 @default.
• W3087110721 cites W2036456322 @default.
• W3087110721 cites W2046993936 @default.
• W3087110721 cites W2133051701 @default.
• W3087110721 cites W2147952742 @default.
• W3087110721 cites W2156384683 @default.
• W3087110721 cites W2160982674 @default.
• W3087110721 cites W2161541244 @default.
• W3087110721 cites W2385742822 @default.
• W3087110721 cites W2535355244 @default.
• W3087110721 cites W2784371446 @default.
• W3087110721 cites W2829448710 @default.
• W3087110721 cites W2912061231 @default.
• W3087110721 cites W2921852243 @default.
• W3087110721 cites W2938314941 @default.
• W3087110721 cites W2950569747 @default.
• W3087110721 cites W2964471257 @default.
• W3087110721 cites W2970041409 @default.
• W3087110721 cites W4249152066 @default.
• W3087110721 cites W916516836 @default.
• W3087110721 doi "https://doi.org/10.1016/j.bmcl.2020.127557" @default.
• W3087110721 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/32949719" @default.
• W3087110721 hasPublicationYear "2020" @default.
• W3087110721 type Work @default.
• W3087110721 sameAs 3087110721 @default.
• W3087110721 citedByCount "6" @default.
• W3087110721 countsByYear W30871107212021 @default.
• W3087110721 countsByYear W30871107212022 @default.
• W3087110721 countsByYear W30871107212023 @default.
• W3087110721 crossrefType "journal-article" @default.
• W3087110721 hasAuthorship W3087110721A5005564764 @default.
• W3087110721 hasAuthorship W3087110721A5019549501 @default.
• W3087110721 hasAuthorship W3087110721A5024914206 @default.
• W3087110721 hasAuthorship W3087110721A5025865949 @default.
• W3087110721 hasAuthorship W3087110721A5050727001 @default.
• W3087110721 hasConcept C109316439 @default.
• W3087110721 hasConcept C1491633281 @default.
• W3087110721 hasConcept C170493617 @default.
• W3087110721 hasConcept C185592680 @default.
• W3087110721 hasConcept C202751555 @default.
• W3087110721 hasConcept C2777506169 @default.
• W3087110721 hasConcept C2778087573 @default.
• W3087110721 hasConcept C2779438470 @default.
• W3087110721 hasConcept C2909325608 @default.
• W3087110721 hasConcept C42362537 @default.
• W3087110721 hasConcept C502942594 @default.
• W3087110721 hasConcept C55493867 @default.
• W3087110721 hasConcept C62112901 @default.
• W3087110721 hasConcept C62478195 @default.
• W3087110721 hasConcept C81729549 @default.
• W3087110721 hasConcept C86803240 @default.
• W3087110721 hasConcept C98274493 @default.
• W3087110721 hasConceptScore W3087110721C109316439 @default.
• W3087110721 hasConceptScore W3087110721C1491633281 @default.
• W3087110721 hasConceptScore W3087110721C170493617 @default.
• W3087110721 hasConceptScore W3087110721C185592680 @default.
• W3087110721 hasConceptScore W3087110721C202751555 @default.
• W3087110721 hasConceptScore W3087110721C2777506169 @default.
• W3087110721 hasConceptScore W3087110721C2778087573 @default.
• W3087110721 hasConceptScore W3087110721C2779438470 @default.
• W3087110721 hasConceptScore W3087110721C2909325608 @default.
• W3087110721 hasConceptScore W3087110721C42362537 @default.
• W3087110721 hasConceptScore W3087110721C502942594 @default.
• W3087110721 hasConceptScore W3087110721C55493867 @default.
• W3087110721 hasConceptScore W3087110721C62112901 @default.
• W3087110721 hasConceptScore W3087110721C62478195 @default.
• W3087110721 hasConceptScore W3087110721C81729549 @default.
• W3087110721 hasConceptScore W3087110721C86803240 @default.
• W3087110721 hasConceptScore W3087110721C98274493 @default.
• W3087110721 hasIssue "23" @default.
• W3087110721 hasLocation W30871107211 @default.
• W3087110721 hasOpenAccess W3087110721 @default.
• W3087110721 hasPrimaryLocation W30871107211 @default.
• W3087110721 hasRelatedWork W1994763147 @default.
• W3087110721 hasRelatedWork W2023597833 @default.
• W3087110721 hasRelatedWork W2035762060 @default.
• W3087110721 hasRelatedWork W2091301838 @default.
• W3087110721 hasRelatedWork W2103997800 @default.
• W3087110721 hasRelatedWork W2120992361 @default.
• W3087110721 hasRelatedWork W2168841302 @default.
• W3087110721 hasRelatedWork W2360123363 @default.
• W3087110721 hasRelatedWork W2541392164 @default.
• W3087110721 hasRelatedWork W3003805320 @default.
• W3087110721 hasVolume "30" @default.
• W3087110721 isParatext "false" @default.
• W3087110721 isRetracted "false" @default.

• next