scholarly journals Recognition of (2S)-Aminomalonyl-Acyl Carrier Protein (ACP) and (2R)-Hydroxymalonyl-ACP by Acyltransferases in Zwittermicin A Biosynthesis

Biochemistry ◽  
2010 ◽  
Vol 49 (17) ◽  
pp. 3667-3677 ◽  
Author(s):  
Yolande A. Chan ◽  
Michael G. Thomas
Keyword(s):  
Acyl Carrier Protein ◽  
Carrier Protein ◽  
Zwittermicin A

4-Aryl-1,4-Dihydropyridines as Potential Enoyl-Acyl Carrier Protein Reductase Inhibitors: Antitubercular Activity and Molecular Docking Study

2020 ◽  
Vol 20 ◽  
Author(s):  
Katharigatta N. Venugopala ◽  
Christophe Tratrat ◽  
Melendhran Pillay ◽  
Pran Kishore Deb ◽  
Deepak Chopra ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Acyl Carrier Protein ◽  
Phenyl Group ◽  
Antitubercular Activity ◽  
Docking Study ◽  
Benzyl Ester ◽  
Multi Drug Resistance ◽  
Carrier Protein ◽  
Molecular Docking Study ◽  
Lipinski’S Rule

Background: Tuberculosis remains one of the most deadly infectious diseases worldwide due to the emergence of multi-drug resistance (MDR) and extensively drug resistance (XDR) strains of Mycobacterium tuberculosis (MTB). Materials and Methods: Herein, the screening of a total of eight symmetrical 1,4-dihydropyridine (1,4-DHP) derivatives (4a-4h) was carried out for whole-cell anti-TB activity against the susceptible H37Rv and MDR strains of MTB. Results and Discussion: Most of the compounds exhibited moderate to excellent activity against the susceptible H37Rv. Moreover, the most promising compound 4f (against H37Rv) having para-trifluoromethyl phenyl group at 4-position and bis para-methoxy benzyl ester group at 3- and 5-positions of 1,4-dihydropyridine pharmacophore, exhibited no toxicity, but demonstrated weak activity against MTB strains resistant to isoniazid and rifampicin. In light of the inhibitory profile of the title compounds, enoyl-acyl carrier protein reductase (InhA) appeared to be the appropriate molecular target. Docking study of these derivatives against InhA receptor revealed favorable binding interactions. Further, in silico predicted ADME properties of these compounds 4a-4h were found to be in the acceptable ranges including satisfactory Lipinski’s rule of five, thereby indicating their potential as drug-like molecules. Conclusion: In particular, the 1,4-DHP derivative 4f can be considered as an attractive lead molecule for further exploration and development of more potent anti-TB agents as InhA inhibitors.

scholarly journals Acyl Carrier Protein

1972 ◽  
Vol 247 (19) ◽  
pp. 6234-6242
Author(s):  
Daniel A.K. Roncari ◽  
Ralph A. Bradshaw ◽  
P. Roy Vagelos
Keyword(s):  
Acyl Carrier Protein ◽  
Carrier Protein

scholarly journals Acyl Carrier Protein

1965 ◽  
Vol 240 (2) ◽  
pp. 618-621 ◽  
Author(s):  
Philip W. Majerus ◽  
A.W. Alberts ◽  
P. Roy Vagelos
Keyword(s):  
Acyl Carrier Protein ◽  
Carrier Protein
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