Characterization and site-directed mutagenesis of the putative novel acyl carrier protein Rv0033 and Rv1344 from Mycobacterium tuberculosis

2006 ◽  
Vol 342 (2) ◽  
pp. 618-624 ◽  
Author(s):  
Yishu Huang ◽  
Jing Ge ◽  
Yongchao Yao ◽  
Qingzhong Wang ◽  
Hongbo Shen ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Acyl Carrier Protein ◽  
Site Directed Mutagenesis ◽  
Directed Mutagenesis ◽  
Carrier Protein

scholarly journals Active site labeling of fatty acid and polyketide acyl-carrier protein transacylases

2019 ◽  
Vol 17 (19) ◽  
pp. 4720-4724 ◽  
Author(s):  
Tony D. Davis ◽  
Jennifer M. Michaud ◽  
Michael D. Burkart
Keyword(s):  
Fatty Acid ◽  
Fluorescent Probe ◽  
Active Site ◽  
Polyketide Synthase ◽  
Acyl Carrier Protein ◽  
Site Directed Mutagenesis ◽  
Probe Design ◽  
Directed Mutagenesis ◽  
Carrier Protein

Fluorescent probe design and site-directed mutagenesis unveil new activity-based chemical reporters for fatty acid and polyketide synthase acyl-carrier protein transacylases.

scholarly journals Use of site-directed mutagenesis to probe the structure, function and isoniazid activation of the catalase/peroxidase, KatG, from Mycobacterium tuberculosis

1999 ◽  
Vol 338 (3) ◽  
pp. 753-760 ◽  
Author(s):  
Brigitte SAINT-JOANIS ◽  
Hélène SOUCHON ◽  
Martin WILMING ◽  
Kai JOHNSSON ◽  
Pedro M. ALZARI ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Acyl Carrier Protein ◽  
Site Directed Mutagenesis ◽  
Single Amino Acid ◽  
Directed Mutagenesis ◽  
Reduction Activity ◽  
Nitroblue Tetrazolium Reduction ◽  
Catalase Peroxidase ◽  
Tetrazolium Reduction

A series of mutants bearing single amino acid substitutions often encountered in the catalase/peroxidase, KatG, from isoniazid-resistant isolates of Mycobacterium tuberculosis has been produced by site-directed mutagenesis. The resultant enzymes were overexpressed, purified and characterized. Replacing Cys-20 by Ser abolished disulphide-bridge formation, but did not affect either dimerization of the enzyme or catalysis. The substitution of Thr-275, which is probably involved in electron transfer from the haem, by proline resulted in a highly unstable enzyme with insignificant enzyme activities. The most commonly occurring substitution in drug-resistant clinical isolates is the replacement of Ser-315 by Thr; this lowered catalase and peroxidase activities by 50% and caused a significant decrease in the KatG-mediated inhibition of the activity of the NADH-dependent enoyl-[acyl-carrier protein] reductase, InhA, in vitro. The ability of this enzyme to produce free radicals from isoniazid was severely impaired, as judged by its loss of NitroBlue Tetrazolium reduction activity. Replacement of Leu-587 by Pro resulted in marked instability of KatG, indicating that the C-terminal domain is also important for structural and functional integrity.

Piperazine derivatives: Synthesis, inhibition of the Mycobacterium tuberculosis enoyl-acyl carrier protein reductase and SAR studies

2015 ◽  
Vol 90 ◽  
pp. 436-447 ◽  
Author(s):  
Mariane Rotta ◽  
Kenia Pissinate ◽  
Anne Drumond Villela ◽  
Davi Fernando Back ◽  
Luis Fernando Saraiva Macedo Timmers ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Acyl Carrier Protein ◽  
Carrier Protein ◽  
Synthesis Inhibition ◽  
Piperazine Derivatives ◽  
Sar Studies

Structure–Function Analysis of the Acyl Carrier Protein Synthase (AcpS) from Mycobacterium tuberculosis

2009 ◽  
Vol 393 (4) ◽  
pp. 937-950 ◽  
Author(s):  
Orly Dym ◽  
Shira Albeck ◽  
Yoav Peleg ◽  
Alon Schwarz ◽  
Zippora Shakked ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Structure Function ◽  
Acyl Carrier Protein ◽  
Function Analysis ◽  
Carrier Protein

Design, synthesis and evaluation of diphenyl ether analogues as antitubercular agents

RSC Advances ◽  
2016 ◽  
Vol 6 (112) ◽  
pp. 110571-110582 ◽  
Author(s):  
Bharathkumar Inturi ◽  
Gurubasavaraj V. Pujar ◽  
Madhusudhan N. Purohit ◽  
Viswanathan B. Iyer ◽  
Sowmya G. S. ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Drug Design ◽  
Acyl Carrier Protein ◽  
Diphenyl Ether ◽  
Design Approach ◽  
Carrier Protein ◽  
Antitubercular Agents ◽  
Structure Based Drug Design ◽  
Design Synthesis ◽  
Diphenyl Ethers

We herein report the investigation of new diphenyl ethers asMycobacterium tuberculosisenoyl-acyl carrier protein reductase (InhA) inhibitors by structure-based drug design approach.

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