scholarly journals Recent developments in compounds acting in the DNA minor groove

MedChemComm ◽  
2019 ◽  
Vol 10 (1) ◽  
pp. 26-40 ◽  
Author(s):  
Adeyemi Rahman ◽  
Patrick O'Sullivan ◽  
Isabel Rozas
Keyword(s):  
Small Molecules ◽  
Minor Groove ◽  
Dna Minor Groove ◽  
Recent Developments

DNA minor groove is the target: the small molecules' attack.

scholarly journals DNA-Minor Groove Binding Agents as Anti-Tubercular Probes. Old Tools for a New Challenge?

2018 ◽  
Vol 16 (2) ◽  
pp. 71-79 ◽  
Author(s):  
Federico Brucoli
Keyword(s):  
Small Molecules ◽  
Antibacterial Properties ◽  
Minor Groove ◽  
Structural Features ◽  
Minor Groove Binding ◽  
Molecular Scaffolds ◽  
Groove Binding ◽  
Dna Minor Groove ◽  
Bacterial Cell Death ◽  
Binding Agents

Tuberculosis, an ancient infectious disease caused by Mycobacterium tuberculosis, ranks as one of the top ten killers worldwide. The limited number of validated targets and scarce therapeutic options demand that renewed efforts should be made to identify tuberculosis drugs with novel mechanisms of action. To this end, mycobacterial DNA might represent a potential target for the development of effective anti-tubercular compounds. In particular, the minor groove of DNA offers an important recognition site for small-molecules that can be programmed to bind to this region in a sequence-selective manner to disrupt mycobacterial transcription factors activity and ultimately cause bacterial cell death. This review describes the structural features of the DNA-minor groove, the requirements for small molecules to bind to this site and the remarkable biophysical and antibacterial properties of DNA-minor groove binding agents, including netropsin, distamycin and their poly-heterocyclic analogues, diamidines, benzimidazole-containing molecules, duocarmycins and pyrrolo[2,1-c][1,4]benzodiazepines (PBDs). Furthermore, the ability of selected heterocyclic-polyamides and PBDs to significantly inhibit the growth of pathogenic, slow-growing M. tuberculosis and other non-pathogenic mycobacterial strains is highlighted. In summary, DNA-minor groove binding agents may serve as molecular scaffolds for the design of highly efficient probes to treat M. tuberculosis infections.

scholarly journals DNA minor groove binding of small molecules: Experimental and computational evidence

2010 ◽  
Vol 122 (2) ◽  
pp. 247-257 ◽  
Author(s):  
Prateek Pandya ◽  
Md Maidul Islam ◽  
G. Suresh Kumar ◽  
B. Jayaram ◽  
Surat Kumar
Keyword(s):  
Small Molecules ◽  
Minor Groove ◽  
Minor Groove Binding ◽  
Groove Binding ◽  
Dna Minor Groove
Sign in / Sign up

Export Citation Format

Share Document