Chapter title |
Discovering Selective Diguanylate Cyclase Inhibitors: From PleD to Discrimination of the Active Site of Cyclic-di-GMP Phosphodiesterases.
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Chapter number | 32 |
Book title |
c-di-GMP Signaling
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Published in |
Methods in molecular biology, January 2017
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DOI | 10.1007/978-1-4939-7240-1_32 |
Pubmed ID | |
Book ISBNs |
978-1-4939-7239-5, 978-1-4939-7240-1
|
Authors |
Rinaldo, S, Giardina, G, Mantoni, F, Paiardini, A, Paone, Alessio, Cutruzzolà, Francesca, S. Rinaldo, G. Giardina, F. Mantoni, A. Paiardini, Alessio Paone, Francesca Cutruzzolà |
Abstract |
One of the most important signals involved in controlling biofilm formation is represented by the intracellular second messenger 3',5'-cyclic diguanylic acid (c-di-GMP). Since the pathways involved in c-di-GMP biosynthesis and breakdown are found only in bacteria, targeting c-di-GMP metabolism represents an attractive strategy for the development of biofilm-disrupting drugs. Here, we present the workflow required to perform a structure-based design of inhibitors of diguanylate cyclases, the enzymes responsible for c-di-GMP biosynthesis. Downstream of the virtual screening process, detailed in the first part of the chapter, we report the step-by-step protocols required to test the positive hits in vitro and to validate their selectivity, thus minimizing possible off-target effects. |
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Other | 0 | 0% |
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