Selected article for: "active compound and high activity"
Author: Chan, Wai Ting; Balsa, Dolors; Espinosa, Manuel
Title: One cannot rule them all: Are bacterial toxins-antitoxins druggable?
  • Document date: 2015_3_21
    • ID: 68an60qu_9
    Snippet: Strategies that have been pointed out as potential for drug discovery like exploiting the bacterial TAs, although constitute a dispute on its druggability, yet still comprise compelling rationales that worth to be explored (Alonso et al., 2007; Mutschler and Meinhart 2011; Gerdes 2013) . In this review, we will discuss the possible druggability of TAs, which is not as simple as previously envisaged, but also in terms of choosing the proper toxin .....
    Document: Strategies that have been pointed out as potential for drug discovery like exploiting the bacterial TAs, although constitute a dispute on its druggability, yet still comprise compelling rationales that worth to be explored (Alonso et al., 2007; Mutschler and Meinhart 2011; Gerdes 2013) . In this review, we will discuss the possible druggability of TAs, which is not as simple as previously envisaged, but also in terms of choosing the proper toxin (or combination of two), their delivery and their targets, because many biologically active molecules can show a high activity in vitro, but would not reach the clinical phases due to lack of intestinal absorption and/or poor in vivo metabolic stability and tissue distribution, the so-called 'ADME' (absorption, distribution, metabolism and excretion) properties. In summary, development of novel antimicrobial drugs is a combination of chemical, biological and industrial approaches in order to design the active compound, validate its usefulness and developing it for clinical use (De Clercq 2010).

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