scholarly journals Structure-Based Virtual Screening of Benzaldehyde Thiosemicarbazone Derivatives against DNA Gyrase B of Mycobacterium tuberculosis

2021 ◽  
Vol 2021 ◽  
pp. 1-11
Author(s):  
Andiyappan Kistan ◽  
Balakrishnan Anna Benedict ◽  
Sundaramoorthy Vasanthan ◽  
Alphonse PremKumar ◽  
Malathi Kullappan ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Resistance Mechanism ◽  
Dna Gyrase ◽  
The Novel ◽  
Extrinsic Factors ◽  
Replication Process ◽  
Antibiotic Resistant ◽  
Compound 21 ◽  
Benzaldehyde Thiosemicarbazone ◽  
Intrinsic And Extrinsic Factors

Emergence of antibiotic-resistant Mycobacterium tuberculosis (M. tuberculosis) restricts the availability of drugs for the treatment of tuberculosis, which leads to the increased morbidity and mortality of the disease worldwide. There are many intrinsic and extrinsic factors that have been reported for the resistance mechanism. To overcome such mechanisms, chemically synthesized benzaldehyde thiosemicarbazone derivatives were screened against M. tuberculosis to find potential inhibitor for tuberculosis. Such filtering process resulted in compound 13, compound 21, and compound 20 as the best binding energy compounds against DNA gyrase B, an important protein in the replication process. The ADMET prediction has shown the oral bioavailability of the novel compounds.

scholarly journals Structural Insights into the Quinolone Resistance Mechanism of Mycobacterium tuberculosis DNA Gyrase

PLoS ONE ◽  
2010 ◽  
Vol 5 (8) ◽  
pp. e12245 ◽  
Author(s):  
Jérémie Piton ◽  
Stéphanie Petrella ◽  
Marc Delarue ◽  
Gwénaëlle André-Leroux ◽  
Vincent Jarlier ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Resistance Mechanism ◽  
Dna Gyrase ◽  
Quinolone Resistance ◽  
Structural Insights

scholarly journals Functional Analysis of DNA Gyrase Mutant Enzymes Carrying Mutations at Position 88 in the A Subunit Found in Clinical Strains of Mycobacterium tuberculosis Resistant to Fluoroquinolones

2006 ◽  
Vol 50 (12) ◽  
pp. 4170-4173 ◽  
Author(s):  
Stéphanie Matrat ◽  
Nicolas Veziris ◽  
Claudine Mayer ◽  
Vincent Jarlier ◽  
Chantal Truffot-Pernot ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Dna Gyrase ◽  
Multidrug Resistant ◽  
Site Directed Mutagenesis ◽  
Fluoroquinolone Resistance ◽  
Directed Mutagenesis ◽  
The Novel ◽  
Wild Type ◽  
Clinical Strains ◽  
A Subunit

ABSTRACT We investigated the enzymatic efficiency and inhibition by quinolones of Mycobacterium tuberculosis DNA gyrases carrying the previously described GyrA G88C mutation and the novel GyrA G88A mutation harbored by two multidrug-resistant clinical strains and reproduced by site-directed mutagenesis. Fluoroquinolone MICs and 50% inhibitory concentrations for both mutants were 2- to 43-fold higher than for the wild type, demonstrating that these mutations confer fluoroquinolone resistance in M. tuberculosis.

scholarly journals Modulation of the multistate folding of designed TPR proteins through intrinsic and extrinsic factors

2012 ◽  
Vol 21 (3) ◽  
pp. 327-338 ◽  
Author(s):  
J. J. Phillips ◽  
Y. Javadi ◽  
C. Millership ◽  
E. R. G. Main
Keyword(s):  
Extrinsic Factors ◽  
Intrinsic And Extrinsic Factors

Intrinsic and extrinsic factors that may influence DNA preservation in skeletal remains: A review

2021 ◽  
Vol 325 ◽  
pp. 110859
Author(s):  
Caterina Raffone ◽  
Miriam Baeta ◽  
Nicole Lambacher ◽  
Eva Granizo-Rodríguez ◽  
Francisco Etxeberria ◽  
...  
Keyword(s):  
Skeletal Remains ◽  
Extrinsic Factors ◽  
Dna Preservation ◽  
Intrinsic And Extrinsic Factors

scholarly journals Presence of Chromosomal crpP-like Genes Is Not Always Associated with Ciprofloxacin Resistance in Pseudomonas aeruginosa Clinical Isolates Recovered in ICU Patients from Portugal and Spain

2021 ◽  
Vol 9 (2) ◽  
pp. 388
Author(s):  
Marta Hernández-García ◽  
María García-Castillo ◽  
Sergio García-Fernández ◽  
Diego López-Mendoza ◽  
Jazmín Díaz-Regañón ◽  
...  
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Protein Function ◽  
Resistance Mechanism ◽  
Amino Acid Position ◽  
Genomic Islands ◽  
Missense Mutations ◽  
The Novel ◽  
Surveillance Studies ◽  
Ciprofloxacin Resistance ◽  
Chromosomal Mutations

CrpP enzymes have been recently described as a novel ciprofloxacin-resistance mechanism. We investigated by whole genome sequencing the presence of crpP-genes and other mechanisms involved in quinolone resistance in MDR/XDR-Pseudomonas aeruginosa isolates (n = 55) with both ceftolozane-tazobactam susceptible or resistant profiles recovered from intensive care unit patients during the STEP (Portugal) and SUPERIOR (Spain) surveillance studies. Ciprofloxacin resistance was associated with mutations in the gyrA and parC genes. Additionally, plasmid-mediated genes (qnrS2 and aac(6′)-Ib-cr) were eventually detected. Ten chromosomal crpP-like genes contained in related pathogenicity genomic islands and 6 different CrpP (CrpP1-CrpP6) proteins were found in 65% (36/55) of the isolates. Dissemination of CrpP variants was observed among non-related clones of both countries, including the CC175 (Spain) high-risk clone and CC348 (Portugal) clone. Interestingly, 5 of 6 variants (CrpP1-CrpP5) carried missense mutations in an amino acid position (Gly7) previously defined as essential conferring ciprofloxacin resistance, and decreased ciprofloxacin susceptibility was only associated with the novel CrpP6 protein. In our collection, ciprofloxacin resistance was mainly due to chromosomal mutations in the gyrA and parC genes. However, crpP genes carrying mutations essential for protein function (G7, I26) and associated with a restored ciprofloxacin susceptibility were predominant. Despite the presence of crpP genes is not always associated with ciprofloxacin resistance, the risk of emergence of novel CrpP variants with a higher ability to affect quinolones is increasing. Furthermore, the spread of crpP genes in highly mobilizable genomic islands among related and non-related P. aeruginosa clones alert the dispersion of MDR pathogens in hospital settings.

scholarly journals Conceptualizing Mobility Inequality: Mobility and Accessibility for the Marginalized

2021 ◽  
pp. 088541222110128
Author(s):  
Isti Hidayati ◽  
Wendy Tan ◽  
Claudia Yamu
Keyword(s):  
Conceptual Understanding ◽  
Thought Experiments ◽  
Future Research ◽  
Planning Practice ◽  
Extrinsic Factors ◽  
Research Directions ◽  
Future Research Directions ◽  
Intrinsic And Extrinsic Factors

The burgeoning landscape of literature on mobility inequalities has led to discrepancies between a conceptual understanding of mobility inequalities and its implementation in planning practice. Reviewing 270 publications across five decades, this article identifies intrinsic and extrinsic factors and approaches for understanding and analyzing mobility inequality. Using two thought experiments to critically locate variations in factors and approaches, dilemmas and challenges in addressing mobility inequality for the marginalized are exposed. The article concludes with future research directions for investigating mobility inequality.

scholarly journals In Vitro Activities of the Novel Oxazolidinones DA-7867 and DA-7157 against Rapidly and Slowly Growing Mycobacteria

2006 ◽  
Vol 50 (12) ◽  
pp. 4027-4029 ◽  
Author(s):  
Lucio Vera-Cabrera ◽  
Barbara A. Brown-Elliott ◽  
Richard J. Wallace ◽  
Jorge Ocampo-Candiani ◽  
Oliverio Welsh ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Clinical Isolates ◽  
Nontuberculous Mycobacterium ◽  
The Novel ◽  
Broth Microdilution ◽  
Reference Species ◽  
Microdilution Method ◽  
Broth Microdilution Method ◽  
Aerobic Actinomycetes

ABSTRACT DA-7867 and DA-7157 are oxazolidinones active against pathogenic aerobic actinomycetes including Nocardia spp. and Mycobacterium tuberculosis. However, the activity of these drugs against nontuberculous mycobacterium (NTM) species is not known. In this work, we compared the susceptibilities of 122 clinical isolates and 29 reference species of both rapidly growing and slowly growing mycobacteria to linezolid, DA-7867, and DA-7157 by the broth microdilution method. The MICs for 50 and 90% of the strains tested (MIC50s and MIC90s, respectively) of DA-7867 and DA-7157 were lower than those of linezolid. In all of the cases, a MIC90 of <8 μg/ml was observed for all of the species tested in both groups of NTM. For M. kansasii and M. marinum isolates, the MIC90s of both DA-7867 and DA-7157 were less than 0.5 μg/ml. These results demonstrate the potential of these compounds to treat NTM infections.

scholarly journals Effect of Intrinsic and Extrinsic Factors on Global and Regional Cortical Thickness

PLoS ONE ◽  
2014 ◽  
Vol 9 (5) ◽  
pp. e96429 ◽  
Author(s):  
Koushik A. Govindarajan ◽  
Leorah Freeman ◽  
Chunyan Cai ◽  
Mohammad H. Rahbar ◽  
Ponnada A. Narayana
Keyword(s):  
Cortical Thickness ◽  
Extrinsic Factors ◽  
Intrinsic And Extrinsic Factors
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