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Identification of Mycobacterial Genes Involved in Antibiotic Sensitivity: Implications for the Treatment of Tuberculosis with β-Lactam-Containing Regimens.
Antimicrob Agents Chemother
July 2017
CSIR - Centre for Cellular and Molecular Biology, Hyderabad, India
In a mutant library screen, transposon mutants with insertions in , , , and displayed hypersusceptibility to antibiotics, including the β-lactams meropenem, ampicillin, amoxicillin, and cefotaxime. Sub-MIC levels of octoclothepin, a psychotic drug inhibiting ParA, phenocopied the insertion and enhanced the bactericidal activity of meropenem against in combination with clavulanate. Our study identifies novel factors associated with antibiotic resistance, with implications in repurposing β-lactams for tuberculosis treatment.
View Article and Find Full Text PDFA whole cell pathway screen reveals seven novel chemosensitizers to combat chloroquine resistant malaria.
Sci Rep
February 2014
Department of Microbiology, National University of Singapore, Singapore.
Due to the widespread prevalence of resistant parasites, chloroquine (CQ) was removed from front-line antimalarial chemotherapy in the 1990s despite its initial promise of disease eradication. Since then, resistance-conferring mutations have been identified in transporters such as the PfCRT, that allow for the efflux of CQ from its primary site of action, the parasite digestive vacuole. Chemosensitizing/chemoreversing compounds interfere with the function of these transporters thereby sensitizing parasites to CQ once again.
View Article and Find Full Text PDFTargeting the chromosome partitioning protein ParA in tuberculosis drug discovery.
J Antimicrob Chemother
November 2010
School of Biological Sciences, Victoria University of Wellington, Wellington, New Zealand.
Objective: To identify inhibitors of the essential chromosome partitioning protein ParA that are active against Mycobacterium tuberculosis.
Methods: Antisense expression of the parA orthologue MSMEG_6939 was induced on the Mycobacterium smegmatis background. Screening of synthetic chemical libraries was performed to identify compounds with higher anti-mycobacterial activity in the presence of parA antisense.
Molecular field analysis of clozapine analogs in the development of a pharmacophore model of antipsychotic drug action.
J Mol Graph Model
February 2002
Department of Medicinal Chemistry, Victorian College of Pharmacy, Monash University, 381 Royal Parade, Parkville, Australia.
In an attempt to elucidate some aspects of clozapine's favorable receptor binding profile, we modeled a series of 30 clozapine analogs using a pharmacophore based on the ligands octoclothepin and tefludazine. Molecular field analysis using CoMFA combined with HINT was carried out on published D2 receptor binding affinities. Several alternative alignments of the analogs gave r2 values in the range of 0.
View Article and Find Full Text PDFFurther investigations of the interactions of antipsychotics with the (-)2,5-dimethoxy-4-methylamphetamine (DOM) discriminative stimulus.
Neuropharmacology
October 1997
Department of Pharmacology and Toxicology, School of Medicine and Biomedical Sciences, State University of New York at Buffalo, USA.
Stimulus control induced by (-)-2,5-dimethoxy-4-methylamphetamine (DOM) is believed to be mediated by agonism at 5-HT2A receptors. We hypothesized that blockade of (-) DOM-induced stimulus control may thus prove useful in the pre-clinical characterization of novel antipsychotic agents by providing an in vivo index of antagonism at that receptor. A previous study (Fiorella et al.
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