Peroxidase activity–structure relationship of the intermolecular four-stranded G-quadruplex–hemin complexes and their application in Hg2+ ion detection

Talanta ◽  
2009 ◽  
Vol 80 (2) ◽  
pp. 459-465 ◽  
Author(s):  
De-Ming Kong ◽  
Jing Wu ◽  
Na Wang ◽  
Wei Yang ◽  
Han-Xi Shen
Author(s):  
Hüseyin K. Beker ◽  
Işıl Yıldırım

Background: Heterocyclic compounds play an important role in the pharmaceutical and biological processes. Among all heterocycles, quinolinone/quinoline has one of the most unique structures in the discovery of these compounds. These derivatives have been prepared by various on the structures, positions, and they have attracted a great deal of attention in the field of medicinal chemistry. The great interest to medicinal chemists is the basic scaffold of the fused quinolines derivative. The large road maps of gene and protein expression produced by these methods often can be used to classify cancers or predict responses to certain types of treatments targeting regulated at both the level of transcription and translation and at the level of enzyme activity. These specific regulations may open the door for the discovery of novel drug candidates including an anti-cancer target. Objective: This review will attempt to provide a comprehensive description of different quinolinone derivatives especially by concentrating on compounds containing benzimidazole ring. Quinolones moieties are experimentally proven anticancer pharmacophores. We think these pharmacophore and additional substitutions on these scaffolds would further enhance their activity as anticancer agents. This activity associate with the positioning of these different functional groups, such as fluoro, methoxy, methyl, amino, hydroxy, nitro, bromo, chloro, methylamino, ethoxy, carbonyl, iodo, and trifluoromethyl groups. Among the functional groups, most of the electronwithdrawing groups such as fluoro, chloro, nitro, amino, and carbonyl groups showed stronger activity than those with electron-donating groups such as methyl and methoxy groups. Presence of electron-withdrawing or electron-donating group by varying the quinolinone redox properties affect its capacity of DNA synthesis. Conclusion: The structural motifs attributed to noteworthy inhibitory results have been identified and highlighted in order to encourage further research and develop more efficient. This work to aim to present knowledge and it hoped that this review can be help researchers to explore an interesting quinoline class, and researchers will be able to develop a new vision in the search for rational designs of more powerful, active and less toxic quinoline-based anticancer drugs.


Processes ◽  
2021 ◽  
Vol 9 (2) ◽  
pp. 329
Author(s):  
Yuko Tsuda ◽  
Koushi Hidaka ◽  
Keiko Hojo ◽  
Yoshio Okada

Plasmin (Plm), a trypsin-like serine protease, is responsible for fibrinolysis pathway and pathologic events, such as angiogenesis, tumor invasion, and metastasis, and alters the expression of cytokines. A growing body of data indicates that a Plm inhibitor is a potential candidate as an anti-inflammatory and anti-cancer agent. A class of active site-directed plasmin inhibitors containing tranexamic acid residue has been designed. As evidenced by docking studies, the inhibitor binds to the active site not to the lysine binding site (LBS) in plasmin, thus preventing plasmin from digesting the substrate. Further optimization of the series, concerning both activity and selectivity, led to the second generation of inhibitors. This review focuses on the Plm inhibitory activity-structure relationship of Plm inhibitors with the goal of realizing their design and clinical application.


2013 ◽  
Vol 20 (38) ◽  
pp. 4836-4843 ◽  
Author(s):  
E. Zavyalova ◽  
A. Golovin ◽  
G. Pavlova ◽  
A. Kopylov

CrystEngComm ◽  
2014 ◽  
Vol 16 (30) ◽  
pp. 6963 ◽  
Author(s):  
Gui-lin Zhuang ◽  
Li Tan ◽  
Wu-lin Chen ◽  
Jia-qi Bai ◽  
Xing Zhong ◽  
...  

Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3073 ◽  
Author(s):  
Lucie Dupin ◽  
Mathieu Noël ◽  
Silvère Bonnet ◽  
Albert Meyer ◽  
Thomas Géhin ◽  
...  

The Gram negative bacterium Pseudomonas aeruginosa (PA) is an opportunistic bacterium that causes severe and chronic infection of immune-depressed patients. It has the ability to form a biofilm that gives a selective advantage to the bacteria with respect to antibiotherapy and host defenses. Herein, we have focused on the tetrameric soluble lectin which is involved in bacterium adherence to host cells, biofilm formation, and cytotoxicity. It binds to l-fucose, d-mannose and glycan exposing terminal fucose or mannose. Using a competitive assay on microarray, 156 oligosaccharides and polysaccharides issued from fermentation or from the biomass were screened toward their affinity to LecB. Next, the five best ligands (Lewisa, Lewisb, Lewisx, siayl-Lewisx and 3-fucosyllactose) were derivatized with a propargyl aglycon allowing the synthesis of 25 trivalent, 25 tetravalent and 5 monovalent constructions thanks to copper catalyzed azide alkyne cycloaddition. The 55 clusters were immobilized by DNA Directed immobilization leading to the fabrication of a glycocluster microarray. Their binding to LecB was studied. Multivalency improved the binding to LecB. The binding structure relationship of the clusters is mainly influenced by the carbohydrate residues. Molecular simulations indicated that the simultaneous contact of both binding sites of monomer A and D seems to be energetically possible.


2021 ◽  
Vol 61 (11) ◽  
pp. 2765-2772
Author(s):  
Chengjun Liu ◽  
Rui Zhang ◽  
Yifan Meng ◽  
Zhen Wang ◽  
Shiyan Jiao ◽  
...  

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