Matches in SemOpenAlex for { <https://semopenalex.org/work/W3082888053> ?p ?o ?g. }
- W3082888053 endingPage "10414" @default.
- W3082888053 startingPage "10394" @default.
- W3082888053 abstract "The selective recognition and imaging of oncogene specific G-quadruplex (GQ) structures holds great promise in the development of diagnostic therapy (theranostics) for cancer and has been challenging due to their structural dynamics and diversity. We report selective recognition of GQ by a small molecule through unique hybrid loop stacking and groove binding mode with turn on far-red fluorescence response and anticancer activity demonstrating the potential implications for GQ-targeted cancer theranostics. Methods: Biophysical investigation reveal the turn on far-red emission property of TGP18 for selective recognition of GQ. In cellulo studies including DNA damage and oxidative stress evaluation guided us to perform in vitro (3D spheroid) and in vivo (xenograft mice model) anti-cancer activity, and tumor tissue imaging to assess the theranostic potential of TGP18. Results: Neocuproine-based far-red turn on fluorescence probe TGP18 shows GQ-to-duplex selectivity and specifically recognizes BCL-2 GQ with high affinity through a unique hybrid binding mode involving loop-stacking and groove interactions. Our study reveals that the selective recognition originating from the distinct loop structure of GQ that alters the overall probe interaction and binding affinity. TGP18 binding to anti-apoptotic BCL-2 GQ ablates the pro-survival function and elicit anti-cancer activity by inducing apoptosis in cancer cells. We deciphered that inhibition of BCL-2 transcription synergized with signaling cascade of nucleolar stress, DNA damage and oxidative stress in triggering apoptosis signaling pathway. Conclusion: Intervention of GQ mediated lethality by TGP18 has translated into anti-cancer activity in both in vitro 3D spheroid culture and in vivo xenograft models of lung and breast cancer with superior efficacy for the former. In vivo therapeutic efficacy supplemented with tumor 3D spheroid and tissue imaging potential define the role of TGP18 in GQ-targeted cancer theranostics." @default.
- W3082888053 created "2020-09-08" @default.
- W3082888053 creator A5001779926 @default.
- W3082888053 creator A5042701686 @default.
- W3082888053 creator A5045800036 @default.
- W3082888053 creator A5066876761 @default.
- W3082888053 date "2020-01-01" @default.
- W3082888053 modified "2023-10-07" @default.
- W3082888053 title "Recognition of G-quadruplex topology through hybrid binding with implications in cancer theranostics" @default.
- W3082888053 cites W1450574606 @default.
- W3082888053 cites W1571487648 @default.
- W3082888053 cites W1752089945 @default.
- W3082888053 cites W1788301610 @default.
- W3082888053 cites W1789563956 @default.
- W3082888053 cites W1878608668 @default.
- W3082888053 cites W1926837394 @default.
- W3082888053 cites W1967652154 @default.
- W3082888053 cites W1969524738 @default.
- W3082888053 cites W1972311492 @default.
- W3082888053 cites W1974175020 @default.
- W3082888053 cites W1977258127 @default.
- W3082888053 cites W1978981036 @default.
- W3082888053 cites W1982823397 @default.
- W3082888053 cites W1983470925 @default.
- W3082888053 cites W1985775217 @default.
- W3082888053 cites W1990635146 @default.
- W3082888053 cites W1990802782 @default.
- W3082888053 cites W1998700258 @default.
- W3082888053 cites W1998778866 @default.
- W3082888053 cites W2001866617 @default.
- W3082888053 cites W2005616551 @default.
- W3082888053 cites W2008182786 @default.
- W3082888053 cites W2009911964 @default.
- W3082888053 cites W2012006084 @default.
- W3082888053 cites W2021191052 @default.
- W3082888053 cites W2032054503 @default.
- W3082888053 cites W2035052265 @default.
- W3082888053 cites W2038138229 @default.
- W3082888053 cites W2038502978 @default.
- W3082888053 cites W2039233074 @default.
- W3082888053 cites W2042374693 @default.
- W3082888053 cites W2044279725 @default.
- W3082888053 cites W2046025625 @default.
- W3082888053 cites W2053919910 @default.
- W3082888053 cites W2059306569 @default.
- W3082888053 cites W2063733156 @default.
- W3082888053 cites W2073722866 @default.
- W3082888053 cites W2076411328 @default.
- W3082888053 cites W2080103757 @default.
- W3082888053 cites W2083158919 @default.
- W3082888053 cites W2084644507 @default.
- W3082888053 cites W2093320042 @default.
- W3082888053 cites W2094454542 @default.
- W3082888053 cites W2100877489 @default.
- W3082888053 cites W2105332242 @default.
- W3082888053 cites W2105668062 @default.
- W3082888053 cites W2106231921 @default.
- W3082888053 cites W2117692326 @default.
- W3082888053 cites W2124871299 @default.
- W3082888053 cites W2128525472 @default.
- W3082888053 cites W2151510603 @default.
- W3082888053 cites W2155616092 @default.
- W3082888053 cites W2155773930 @default.
- W3082888053 cites W2165451456 @default.
- W3082888053 cites W2169214364 @default.
- W3082888053 cites W2171830519 @default.
- W3082888053 cites W2225755444 @default.
- W3082888053 cites W2239639879 @default.
- W3082888053 cites W2313142763 @default.
- W3082888053 cites W2318569979 @default.
- W3082888053 cites W2423718667 @default.
- W3082888053 cites W2426177481 @default.
- W3082888053 cites W2468369037 @default.
- W3082888053 cites W2477718940 @default.
- W3082888053 cites W2510312826 @default.
- W3082888053 cites W2549811144 @default.
- W3082888053 cites W2553622516 @default.
- W3082888053 cites W2585186968 @default.
- W3082888053 cites W2588267243 @default.
- W3082888053 cites W2590327834 @default.
- W3082888053 cites W2612390718 @default.
- W3082888053 cites W2765648233 @default.
- W3082888053 cites W2768554905 @default.
- W3082888053 cites W2771607273 @default.
- W3082888053 cites W2780065863 @default.
- W3082888053 cites W2790138464 @default.
- W3082888053 cites W2891416544 @default.
- W3082888053 cites W2898240189 @default.
- W3082888053 cites W2909441045 @default.
- W3082888053 cites W2913753776 @default.
- W3082888053 cites W2922708208 @default.
- W3082888053 cites W2973721774 @default.
- W3082888053 cites W2975651250 @default.
- W3082888053 cites W2998739628 @default.
- W3082888053 cites W3010432254 @default.
- W3082888053 cites W3012568988 @default.
- W3082888053 doi "https://doi.org/10.7150/thno.48675" @default.
- W3082888053 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/7482797" @default.