An FDA-Drug Library Screen for Compounds with Bioactivities against Meticillin-Resistant Staphylococcus aureus (MRSA)

Antibiotics

Qiu Ying Lau¹  Yoke Yan Fion Tan¹  Vanessa Chai Yin Goh¹  David Jing Qin Lee¹  Fui Mee Ng¹  Esther H. Q. Ong²  Jeffrey Hill²  Cheng San Brian Chia¹ 

[1] Experimental Therapeutics Centre, Agency for Science, Technology and Research (ASTAR), 31 Biopolis Way, 2 Nanos #03-01, Singapore 138669, Singapore;

关键词: drug library screen;    drug repurposing;    drug repositioning;    MRSA;   

DOI  :  10.3390/antibiotics4040424

来源: mdpi

【 摘 要 】

The lack of new antibacterial drugs entering the market and their misuse have resulted in the emergence of drug-resistant bacteria, posing a major health crisis worldwide. In particular, meticillin-resistant Staphylococcus aureus (MRSA), a pathogen responsible for numerous human infections, has become endemic in hospitals worldwide. Drug repurposing, the finding of new therapeutic indications for approved drugs, is deemed a plausible solution to accelerate drug discovery and development in this area. Towards this end, we screened 1163 drugs approved by the Food and Drug Administration (FDA) for bioactivities against MRSA in a 10 μM single-point assay. After excluding known antibiotics and antiseptics, six compounds were identified and their MICs were determined against a panel of clinical MRSA strains. A toxicity assay using human keratinocytes was also conducted to gauge their potential for repurposing as topical agents for treating MRSA skin infections.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.