FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2078741614> ?p ?o ?g. }

• W2078741614 endingPage "1047" @default.
• W2078741614 startingPage "1042" @default.
• W2078741614 abstract "The rhodacyanine, MKT-077, has anti-proliferative activity against cancer cell lines through its ability to inhibit members of the heat shock protein 70 (Hsp70) family of molecular chaperones. However, MKT-077 is rapidly metabolized, which limits its use as either a chemical probe or potential therapeutic. We report the synthesis and characterization of MKT-077 analogs designed for greater stability. The most potent molecules, such as 30 (JG-98), were at least 3-fold more active than MKT-077 against the breast cancer cell lines MDA-MB-231 and MCF-7 (EC50 values of 0.4 ± 0.03 μM and 0.7 ± 0.2 μM, respectively). The analogs modestly destabilized the chaperone clients, Akt1 and Raf1, and induced apoptosis in these cells. Further, the microsomal half-life of JG-98 was improved at least 7-fold (t1/2 = 37 min) compared to MKT-077 (t1/2 < 5 min). Finally, NMR titration experiments suggested that these analogs bind an allosteric site that is known to accommodate MKT-077. These studies advance MKT-077 analogs as chemical probes for studying Hsp70's roles in cancer." @default.
• W2078741614 created "2016-06-24" @default.
• W2078741614 creator A5009411980 @default.
• W2078741614 creator A5014931443 @default.
• W2078741614 creator A5032859600 @default.
• W2078741614 creator A5043300541 @default.
• W2078741614 creator A5055171905 @default.
• W2078741614 creator A5067529915 @default.
• W2078741614 creator A5069778809 @default.
• W2078741614 creator A5083818614 @default.
• W2078741614 creator A5085456274 @default.
• W2078741614 date "2013-09-17" @default.
• W2078741614 modified "2023-09-25" @default.
• W2078741614 title "Analogues of the Allosteric Heat Shock Protein 70 (Hsp70) Inhibitor, MKT-077, As Anti-Cancer Agents" @default.
• W2078741614 cites W1972121275 @default.
• W2078741614 cites W1983388930 @default.
• W2078741614 cites W2009782661 @default.
• W2078741614 cites W2018343730 @default.
• W2078741614 cites W2033580819 @default.
• W2078741614 cites W2039367486 @default.
• W2078741614 cites W2042838776 @default.
• W2078741614 cites W2056693633 @default.
• W2078741614 cites W2056911532 @default.
• W2078741614 cites W2071906362 @default.
• W2078741614 cites W2079227113 @default.
• W2078741614 cites W2088225005 @default.
• W2078741614 cites W2095231417 @default.
• W2078741614 cites W2096038757 @default.
• W2078741614 cites W2112374700 @default.
• W2078741614 cites W2114918609 @default.
• W2078741614 cites W2122361685 @default.
• W2078741614 cites W2125007784 @default.
• W2078741614 cites W2147163420 @default.
• W2078741614 cites W2163541635 @default.
• W2078741614 cites W2170573493 @default.
• W2078741614 cites W2171977059 @default.
• W2078741614 doi "https://doi.org/10.1021/ml400204n" @default.
• W2078741614 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3845967" @default.
• W2078741614 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/24312699" @default.
• W2078741614 hasPublicationYear "2013" @default.
• W2078741614 type Work @default.
• W2078741614 sameAs 2078741614 @default.
• W2078741614 citedByCount "119" @default.
• W2078741614 countsByYear W20787416142014 @default.
• W2078741614 countsByYear W20787416142015 @default.
• W2078741614 countsByYear W20787416142016 @default.
• W2078741614 countsByYear W20787416142017 @default.
• W2078741614 countsByYear W20787416142018 @default.
• W2078741614 countsByYear W20787416142019 @default.
• W2078741614 countsByYear W20787416142020 @default.
• W2078741614 countsByYear W20787416142021 @default.
• W2078741614 countsByYear W20787416142022 @default.
• W2078741614 countsByYear W20787416142023 @default.
• W2078741614 crossrefType "journal-article" @default.
• W2078741614 hasAuthorship W2078741614A5009411980 @default.
• W2078741614 hasAuthorship W2078741614A5014931443 @default.
• W2078741614 hasAuthorship W2078741614A5032859600 @default.
• W2078741614 hasAuthorship W2078741614A5043300541 @default.
• W2078741614 hasAuthorship W2078741614A5055171905 @default.
• W2078741614 hasAuthorship W2078741614A5067529915 @default.
• W2078741614 hasAuthorship W2078741614A5069778809 @default.
• W2078741614 hasAuthorship W2078741614A5083818614 @default.
• W2078741614 hasAuthorship W2078741614A5085456274 @default.
• W2078741614 hasBestOaLocation W20787416142 @default.
• W2078741614 hasConcept C104317684 @default.
• W2078741614 hasConcept C121608353 @default.
• W2078741614 hasConcept C142724271 @default.
• W2078741614 hasConcept C153911025 @default.
• W2078741614 hasConcept C166342909 @default.
• W2078741614 hasConcept C181199279 @default.
• W2078741614 hasConcept C185592680 @default.
• W2078741614 hasConcept C205260736 @default.
• W2078741614 hasConcept C2775962898 @default.
• W2078741614 hasConcept C502942594 @default.
• W2078741614 hasConcept C54355233 @default.
• W2078741614 hasConcept C55493867 @default.
• W2078741614 hasConcept C68991219 @default.
• W2078741614 hasConcept C71924100 @default.
• W2078741614 hasConcept C86803240 @default.
• W2078741614 hasConcept C96232424 @default.
• W2078741614 hasConceptScore W2078741614C104317684 @default.
• W2078741614 hasConceptScore W2078741614C121608353 @default.
• W2078741614 hasConceptScore W2078741614C142724271 @default.
• W2078741614 hasConceptScore W2078741614C153911025 @default.
• W2078741614 hasConceptScore W2078741614C166342909 @default.
• W2078741614 hasConceptScore W2078741614C181199279 @default.
• W2078741614 hasConceptScore W2078741614C185592680 @default.
• W2078741614 hasConceptScore W2078741614C205260736 @default.
• W2078741614 hasConceptScore W2078741614C2775962898 @default.
• W2078741614 hasConceptScore W2078741614C502942594 @default.
• W2078741614 hasConceptScore W2078741614C54355233 @default.
• W2078741614 hasConceptScore W2078741614C55493867 @default.
• W2078741614 hasConceptScore W2078741614C68991219 @default.
• W2078741614 hasConceptScore W2078741614C71924100 @default.
• W2078741614 hasConceptScore W2078741614C86803240 @default.
• W2078741614 hasConceptScore W2078741614C96232424 @default.
• W2078741614 hasIssue "11" @default.
• W2078741614 hasLocation W20787416141 @default.

• next