Wspólnotowy Serwis Informacyjny Badan i Rozwoju - 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.

Powiązane informacje

Reported by

Université de Poitiers
Avenue du Recteur Pineau, 40
86022 Poitiers
France
See on map
Śledź nas na: RSS Facebook Twitter YouTube Zarządzany przez Urząd Publikacji UE W górę