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Prospective screening of novel antibacterial inhibitors of dihydrofolate reductase for mutational resistance

Prospective screening of novel antibacterial inhibitors of dihydrofolate reductase for mutational resistance

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Elucidating Features That Drive the Design of Selective Antifolates Using Crystal Structures of Human Dihydrofolate Reductase Propargyl-Linked Antifolates Are Potent Inhibitors of Drug-Sensitive and Drug-Resistant Mycobacterium tuberculosis Crystal structures of Klebsiella pneumoniae dihydrofolate reductase bound to propargyl-linked antifolates reveal features for potency and selectivity.Protein design algorithms predict viable resistance to an experimental antifolate Nonracemic Antifolates Stereoselectively Recruit Alternate Cofactors and Overcome Resistance in S. aureus.Crystal Structures of Trimethoprim-Resistant DfrA1 Rationalize Potent Inhibition by Propargyl-Linked Antifolates.Viable screening targets related to the bacterial cell wall.OSPREY Predicts Resistance Mutations Using Positive and Negative Computational Protein Design.Antibacterial Antifolates: From Development through Resistance to the Next Generation Emergence of trimethoprim resistance gene dfrG in Staphylococcus aureus causing human infection and colonization in sub-Saharan Africa and its import to Europe.MRSA Isolates from United States Hospitals Carry dfrG and dfrK Resistance Genes and Succumb to Propargyl-Linked Antifolates.Charged Nonclassical Antifolates with Activity Against Gram-Positive and Gram-Negative Pathogens.Charged Propargyl-Linked Antifolates Reveal Mechanisms of Antifolate Resistance and Inhibit Trimethoprim-Resistant MRSA Strains Possessing Clinically Relevant Mutations.

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Prospective screening of novel antibacterial inhibitors of dihydrofolate reductase for mutational resistance

http://www.wikidata.org/entity/Q36086509

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Prospective screening of novel ...... tase for mutational resistance

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Antimicrobial Agents and Chemotherapy

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Prospective screening of novel ...... tase for mutational resistance

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Amy C Anderson

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Kathleen M Frey

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Kishore Viswanathan

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P2860

Multidrug resistance in bacteria

Evolution of an antibiotic resistance enzyme constrained by stability and activity trade-offs

Crystal Structures of Wild-type and Mutant Methicillin-resistant Staphylococcus aureus Dihydrofolate Reductase Reveal an Alternate Conformation of NADPH That May Be Linked to Trimethoprim Resistance

Towards the understanding of resistance mechanisms in clinically isolated trimethoprim-resistant, methicillin-resistant Staphylococcus aureus dihydrofolate reductase

Toward New Therapeutics for Skin and Soft Tissue Infections: Propargyl-Linked Antifolates Are Potent Inhibitors of MRSA and Streptococcus pyogenes

Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction

Anticancer antifolates: current status and future directions

Preclinical evaluation of novel antibacterial agents by microbiological and molecular techniques

Effect of fluoroquinolone concentration on selection of resistant mutants of Mycobacterium bovis BCG and Staphylococcus aureus

Community-acquired methicillin-resistant Staphylococcus aureus: current perspectives.

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3556-3562

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scholarly article

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10.1128/AAC.06263-11

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7

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56

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Dennis L Wright

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2012-04-09T00:00:00Z

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22491688

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3393473

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