scholarly journals G-quadruplex ligands exhibit differential G-tetrad selectivity

2015 ◽  
Vol 51 (38) ◽  
pp. 8048-8050 ◽  
Author(s):  
D. D. Le ◽  
M. Di Antonio ◽  
L. K. M. Chan ◽  
S. Balasubramanian
Keyword(s):  
Site Specific ◽  
Specific Fluorescence ◽  
Equilibrium Binding ◽  
Fluorescence Quench ◽  
G Quadruplex ◽  
Selective Ligands

Site-specific fluorescence quench assay allows for targeted G-quadruplex equilibrium binding measurements to investigate G-tetrad selective ligands.

scholarly journals Monohydrazone Based G-Quadruplex Selective Ligands Induce DNA Damage and Genome Instability in Human Cancer Cells

2020 ◽  
Vol 63 (6) ◽  
pp. 3090-3103 ◽  
Author(s):  
Jussara Amato ◽  
Giulia Miglietta ◽  
Rita Morigi ◽  
Nunzia Iaccarino ◽  
Alessandra Locatelli ◽  
...  
Keyword(s):  
Dna Damage ◽  
Cancer Cells ◽  
Genome Instability ◽  
Human Cancer ◽  
Human Cancer Cells ◽  
G Quadruplex ◽  
Selective Ligands

scholarly journals Site-Specific and Trigger-Activated Modification of Proteins by Means of Catalytic Hemin/G-quadruplex (hGQ) DNAzyme Nanostructures

2020 ◽  
Author(s):  
Jordi Keijzer ◽  
Bauke Albada
Keyword(s):  
Heavy Chain ◽  
Protein Modification ◽  
Site Specificity ◽  
Site Specific ◽  
Antibody Drug Conjugates ◽  
Synthetic Dna ◽  
Drug Conjugates ◽  
Sds Page ◽  
G Quadruplex ◽  
Antibody Drug

<div>Synthetic DNA that forms various G-quadruplex nanostructures, in combination with hemin, <i>N</i>-methyl luminol derivatives, and H2O2 can site-specifically modify proteins (i.e. evidence is provided for lysozyme and human alpha-thrombin). The catalytic modification is completed in 15-30 mins, and the site-specificity is influenced by the G-quadruplex topology (a total of 22 G-quadruplex forming sequences was tested). We also show that the heavy chain of the therapeutic antibody trastuzumab is modified, which facilitates the preparation of antibody-drug conjugates. Furthermore, a trigger can be programmed into this synthetic DNA so that the protein modification chemistry is made dependent on an external trigger.</div><div><br></div>Techniques used: HPLC, SDS-PAGE, LC-MS/MS, NMR.

scholarly journals G4-Selective Ligand Induced Autophagy

2021 ◽  
Author(s):  
Piyali Majumder ◽  
Chinmayee Shukla ◽  
Bhaskar Datta
Keyword(s):  
Gene Regulation ◽  
Negative Regulator ◽  
Homeostatic Mechanism ◽  
Selective Ligand ◽  
Carbocyanine Dye ◽  
G Quadruplex ◽  
Selective Ligands ◽  
Functional Context ◽  
Stabilizing Ligands ◽  
Mtor Activity

G-quadruplex (G4) structures have emerged as singular therapeutic targets for cancer and neurodegeneration. Autophagy is a housekeeping cellular homeostatic mechanism and deregulation of autophagy is common in cancer and in neurodegenerative diseases. In this study, we identified the presence of 46 putative G4 sequences in the MTOR gene by use of QGRS mapper tool. We sought to connect these putative G4 sequences to a functional context by leveraging G4-targeting ligands. A G4-selective dimeric carbocyanine dye Bis-4,3 and the porphyrin TMPyP4 were used to affect the replication, transcription and translation of the MTOR gene. The ligand-induced induction of autophagic pathway via MTOR gene regulation was monitored upon treatment of HeLa and SHSY-5Y cells with G4-targeting ligands. The use of Bis-4,3 was compared with the known G4-stabilizing activity of TMPyP4. Our results show that treatment with G4-selective ligands downregulates mTOR activity and leads to the induction of excessive autophagy. This is first report on effect of G4-selective ligands on MTOR regulation and mTOR expression. mTOR being the key negative regulator of autophagy, the current work suggests potential of G4 stabilizing ligands towards induction of autophagy through the downregulation of mTOR.

Site specific self-cleavage of certain assemblies of G-quadruplex

2008 ◽  
pp. 380-382 ◽  
Author(s):  
Xiaoqian Liu ◽  
Xinming Li ◽  
Tianyan Zhou ◽  
Yifan Wang ◽  
Magdeline Tao Tao Ng ◽  
...  
Keyword(s):  
Site Specific ◽  
G Quadruplex

scholarly journals A site-specific self-assembled light-up rotor probe for selective recognition and stabilization of c-MYC G-quadruplex DNA

Nanoscale ◽  
2020 ◽  
Vol 12 (24) ◽  
pp. 12950-12957
Author(s):  
Marco Deiana ◽  
Karam Chand ◽  
Jan Jamroskovic ◽  
Rabindra Nath Das ◽  
Ikenna Obi ◽  
...  
Keyword(s):  
Selective Recognition ◽  
Site Specific ◽  
Quadruplex Dna ◽  
G Quadruplex ◽  
Sensitivity And Selectivity ◽  
Self Assembled ◽  
A Site

A self-assembled light-up rotor probe with outstanding sensitivity and selectivity for the c-MYC promoter G-quadruplex DNA is reported.

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