Forschungs- & Entwicklungsinformationsdienst der Gemeinschaft - CORDIS

A series of active compounds that would affect the function of CFTR

A new set of molecules from various chemical families were tested in the screening process. This included novel MPB derivatives as part of a Structure Activity Relationship (SAR) study. Our criteria to exclude drugs for further analysis is 20% or less of stimulation at 250 microM concentration. Among the different derivatives tested, some have promising activity on CFTR. The best candidates as activator of wild-type CFTR and G551D-CFTR are MPB-91, MPB-97, MPB-77, MPB-104, MPB-107, MPB-96, and MPB-95.

A similar analysis is concerning the effect of these derivatives on F508del-expressing cells, still needs to be performed and is under way. A structure-activity study demonstrated the importance and the nature of chemical groups within the MPB skeleton. For example MPB-80, and MPB-70 are not active on CFTR.

More recently, we found that by adding an alkyl group in C5 we obtained MPB-91 a derivative that is more potent than MPB-07. Now we discovered MPB-104 and MPB-107 that are 100-fold more potent than MPB-07. These two agents are subject of extensive study to determine the mechanism of action to rescue F508del.

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Eric ESPERET, (Rector)
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