Antibiotics that target bacterial molecules not previously exploited are desperately needed. One such target is the protein FtsZ. The small molecule 3-methoxybenzamide (3-MBA) is known to inhibit FtsZ in Bacillus subtilis but is not bacteriocidal. Nonetheless, researchers reasoned that 3-MBA offered a good starting point for the synthesis of a molecule that might be a potential drug candidate. Over 500 3-MBA analogues were synthesized and screened; one called PA190723 was extremely potent in its capacity to bind FtsZ and inhibit bacterial growth. In fact, when used in a mouse model, PA190723 was bacteriocidal against methicillinand multidrug-resistant Staphylococcus aureus. What makes FtsZ a good drug target? What preliminary information about 3-MBA would be helpful if you were designing the 3-MBA analogues? As these researchers move forward with clinical (human) testing, what other parameters and outcomes must be assessed besides the bacteriocidal activity of PA190723?

Human Anatomy & Physiology (11th Edition)
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ISBN:9780134580999
Author:Elaine N. Marieb, Katja N. Hoehn
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Antibiotics that target bacterial molecules not previously exploited are desperately needed. One such target is the protein FtsZ. The small molecule 3-methoxybenzamide (3-MBA) is known to inhibit FtsZ in Bacillus subtilis but is not bacteriocidal. Nonetheless, researchers reasoned that 3-MBA offered a good starting point for the synthesis of a molecule that might be a potential drug candidate. Over 500 3-MBA analogues were synthesized and screened; one called PA190723 was extremely potent in its capacity to bind FtsZ and inhibit bacterial growth. In fact, when used in a mouse model, PA190723 was bacteriocidal against methicillinand multidrug-resistant Staphylococcus aureus.

  1. What makes FtsZ a good drug target?
  2. What preliminary information about 3-MBA would be helpful if you were designing the 3-MBA analogues?
  3. As these researchers move forward with clinical (human) testing, what other parameters and outcomes must be assessed besides the bacteriocidal activity of PA190723?
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