| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T66040 | ||||
| Target Name | Bacterial Penicillin binding protein 2 (Bact mrdA) | ||||
| Type of Target |
Successful |
||||
| Drug Potency against Target | Amdinocillin | Drug Info | IC90 = 100 ng/mL | [3] | |
| Imipenem | Drug Info | IC50 = 50 ng/mL | [1] | ||
| Action against Disease Model | Imipenem | Drug Info | Ceftobiprole exhibited tight binding to PBP2a in methicillin-resistant Staphylococcus aureus, PBP2x in penicillin-resistant Streptococcus pne uMoniae, and PBP3 and other essential penicillin-binding proteins in methicillin-susceptible S. aureus, Escherichia coli, and Pseudomonas aeruginosa. Ceftobiprole also bound well to PBP2 in the latter organisms, contributing to the broad-spectr uM antibacterial activity against gram-negative and gram-positive bacteria. | [2] | |
| References | |||||
| REF 1 | Neutrophil-anti-microbial interaction in the established infection: effect on Staphylococcus aureus. J Infect. 2006 May;52(5):320-8. | ||||
| REF 2 | Binding of ceftobiprole and comparators to the penicillin-binding proteins of Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and ... Antimicrob Agents Chemother. 2007 Jul;51(7):2621-4. | ||||
| REF 3 | Interaction of (2,3)-methylenepenams with penicillin-binding proteins. Antimicrob Agents Chemother. 1987 Jul;31(7):1069-74. | ||||
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