Beilstein J. Org. Chem.2018,14, 2881–2896, doi:10.3762/bjoc.14.267
increasingly become an attractive target over the past two decades [12][13][14].
PPIs are challenging targets because of their flat, large and hydrophobic bindingsurface, in comparison with the well-defined binding sites of more classical targets such as GPCRs, enzymes or ion channels (Figure 1). Moreover
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Graphical Abstract
Figure 1:
Illustration of a PPI modulator (stabilizer or inhibitor) vs a traditional drug target.
Beilstein J. Org. Chem.2018,14, 1769–1777, doi:10.3762/bjoc.14.151
. Optimization of these binding interactions could lead to the development of highly potent CSP-based QS modulators while the inclusion of non-natural amino acids within the CSP sequence would confer resistance to protease degradation, a requirement for drug candidates.
Keywords: bindingsurface; competence
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Graphical Abstract
Figure 1:
The competence regulon QS circuitry in S. pneumoniae. ComC is processed and secreted by ComAB as th...