By a News Reporter-Staff News Editor at Biotech Week -- A new study on Drugs and Therapies is now available. According to news reporting from Fukuoka, Japan, by NewsRx journalists, research stated, "The emergence of multidrug-resistant Staphylococcus aureus (S. aureus) makes the treatment of infectious diseases in hospitals more difficult and increases the mortality of the patients. In this study, we attempted to identify novel potent antibiotic candidate compounds against S. aureus dihydrofolate reductase (saDHFR)."
The news correspondents obtained a quote from the research from the Kyushu Institute of Technology, "We performed three-step in silico structure-based drug screening (SBDS) based on the crystal structure of saDHFR using a 154,118 chemical compound library. We subsequently evaluated whether candidate chemical compounds exhibited inhibitory effects on the growth of the model bacterium: Staphylococcus epidermidis (S. epidermidis). The compound KB1 showed a strong inhibitory effect on the growth of S. epidermidis. Moreover, we rescreened chemical structures similar to KB1 from a 461,397 chemical compound library. Three of the four KB1 analogs (KBS1, KBS3, and KBS4) showed inhibitory effects on the growth of S. epidermidis and enzyme inhibitory effects on saDHFR We performed structure-activity relationship (SAR) analysis of active chemical compounds and observed a correlative relationship among the IC50 values, interaction residues, and structure scaffolds. In addition, the active chemical compounds (KB1, KBS3, and KBS4) had no inhibitory effects on the growth of model enterobacteria (E. coli BL21 and JM109 strains) and no toxic effects on cultured mammalian cells (MDCK cells). Results obtained from Protein Ligand Interaction Fingerprint (PLIF) and Ligand Interaction (LI) analyses suggested that all of the active compounds exhibited potential inhibitory effects on mutated saDHFR of the drug-resistant strains."
According to the news reporters, the research concluded: "The structural and experimental information concerning these novel chemical compounds will likely contribute to the development of new antibiotics for both wild-type and drug-resistant S. aureus."
For more information on this research see: Identification of Novel Potential Antibiotics against Staphylococcus Using Structure-Based Drug Screening Targeting Dihydrofolate Reductase. Journal of Chemical Information and Modeling, 2014;54(4):1242-1253. Journal of Chemical Information and Modeling can be contacted at: Amer Chemical Soc, 1155 16TH St, NW, Washington, DC 20036, USA. (American Chemical Society - www.acs.org; Journal of Chemical Information and Modeling - www.pubs.acs.org/journal/jcisd8)
Our news journalists report that additional information may be obtained by contacting M. Kobayashi, Kyushu Inst Technol, Biomed Informat Res & Dev Center BMIRC, Iizuka, Fukuoka 8208502, Japan. Additional authors for this research include T. Kinjo, Y. Koseki, C.R. Bourne, W.W. Barrow and S. Aoki (see also Drugs and Therapies).
Keywords for this news article include: Asia, Antibacterial, Antibiotics, Antimicrobials, Japan, Fukuoka, Reductase, Bacillales, Staphylococcus, Staphylococcaceae, Drugs and Therapies, Gram-Positive Cocci, Enzymes and Coenzymes, Gram-Positive Bacteria, Gram-Positive Endospore-Forming Rods
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