Small Natural Molecules Targeting DNA G-Quadruplexes

2014 ◽  
Vol 955-959 ◽  
pp. 423-426
Author(s):  
Zi Jian Li ◽  
Yan Ping Ding ◽  
Su Lin Zhang ◽  
Yan Ling Wu ◽  
Wen Zhang
Keyword(s):  
Natural Products ◽  
Drug Target ◽  
Binding Mode ◽  
Current Understanding ◽  
Tumor Treatment ◽  
Potential Significance ◽  
New Drug ◽  
G4 Dna ◽  
G Quadruplex

DNA G-quadruplex (G4-DNA) has emerged as a new drug target for anti-tumor. The small compounds can induce the formation of G4-DNA and stabilize its structures, which is of potential significance for the tumor treatment. This paper focuses on our current understanding about the structure of G4-DNA, the binding mode between G4-DNA and small molecular ligands, and natural products targeting G4-DNA.

Synthetic Small Molecules Targeting G-Quadruplexes and their Application

2015 ◽  
Vol 1088 ◽  
pp. 507-513
Author(s):  
Hui Yu ◽  
Yan Li Wang ◽  
Xiao Yin Zhao ◽  
Wen Zhang
Keyword(s):  
Drug Design ◽  
Small Molecules ◽  
Small Molecule ◽  
Binding Mode ◽  
Current Understanding ◽  
Promising Target ◽  
G Quadruplex ◽  
Small Molecule Ligands

G-quadruplex is expected to be a promising target for drug design. The manually synthesized small-molecule compounds are able to induce the formation of and stabilize G-quadruplexes. In this paper, we summarize the current understanding of the structure of G-quadruplexes, the binding mode of G-quadruplexes and small-molecule ligands, and important synthesized small molecules targeting G-quadruplexes as potential drugs.

scholarly journals Binding Study of the Fluorescent Carbazole Derivative with Human Telomeric G-Quadruplexes

Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3154 ◽  
Author(s):  
Agata Głuszyńska ◽  
Bernard Juskowiak ◽  
Błażej Rubiś
Keyword(s):  
Binding Constants ◽  
Binding Mode ◽  
Cd Spectroscopy ◽  
Telomeric Sequence ◽  
Potassium Ions ◽  
Carbazole Derivative ◽  
Quadruplex Dna ◽  
G4 Dna ◽  
G Quadruplex ◽  
Sodium And Potassium

The carbazole ligand 3 was synthesized, characterized and its binding interactions with human telomeric (22HT) G-quadruplex DNA in Na+ and K+-containing buffer were investigated by ultraviolet-visible (UV-Vis) spectrophotometry, fluorescence, circular dichroism (CD) spectroscopy, and DNA melting. The results showed that the studied carbazole ligand interacted and stabilized the intramolecular G-quadruplexes formed by the telomeric sequence in the presence of sodium and potassium ions. In the UV-Vis titration experiments a two-step complex formation between ligand and G-quadruplex was observed. Very low fluorescence intensity of the carbazole derivative in Tris HCl buffer in the presence of the NaCl or KCl increased significantly after addition of the 22HT G4 DNA. Binding stoichiometry of the ligand/G-quadruplex was investigated with absorbance-based Job plots. Carbazole ligand binds 22HT with about 2:1 stoichiometry in the presence of sodium and potassium ions. The binding mode appeared to be end-stacking with comparable binding constants of ~105 M−1 as determined from UV-Vis and fluorescence titrations data. The carbazole ligand is able to induce formation of G4 structure of 22HT in the absence of salt, which was proved by CD spectroscopy and melting studies. The derivative of carbazole 3 shows significantly higher cytotoxicity against breast cancer cells then for non-tumorigenic breast epithelial cells. The cytotoxic activity of ligand seems to be not associated with telomerase inhibition.

CGMP as a New Drug Target in Atrial Fibrillation

2020 ◽  
Author(s):  
N. I. Bork ◽  
N. Grammatika-Pavlidou ◽  
B. Reiter ◽  
E. Girdauskas ◽  
H. Reichenspurner ◽  
...  
Keyword(s):  
Atrial Fibrillation ◽  
Drug Target ◽  
New Drug

Antitubercular Marine Natural Products

2018 ◽  
Vol 25 (20) ◽  
pp. 2304-2328 ◽  
Author(s):  
Lishu Wang ◽  
Jungfeng Wang ◽  
Juan Liu ◽  
Yonghong Liu
Keyword(s):  
Natural Products ◽  
Marine Natural Products ◽  
Antitubercular Activity ◽  
Marine Resources ◽  
Drug Candidates ◽  
New Drug ◽  
Chemical Constitution

Due to the importance of nature as a source of new drug candidates, the purpose of this article is to emphasize the marine natural products, which exhibit antitubercular activity, published between January 2000 and May 2016, with 138 quotations to 250 compounds obtained from marine resources. These metabolites are organized by chemical constitution and named as simple alkyl lipids derivatives, aromatics derivatives, peptides, alkaloids, terpenoids, steroids, macrolides, and polycyclic polyketides.

Lanthionine Synthetase Component C-Like Protein 2: A New Drug Target for Inflammatory Diseases and Diabetes

2014 ◽  
Vol 15 (6) ◽  
pp. 565-572 ◽  
Author(s):  
Pinyi Lu ◽  
Raquel Hontecillas ◽  
Casandra Philipson ◽  
Josep Bassaganya-Riera
Keyword(s):  
Drug Target ◽  
Inflammatory Diseases ◽  
New Drug ◽  
Component C
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