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Conformation-activity relationship of the archazolids: Development of a novel class of highly potent V-ATPase inhibitors

Projektnummer

0051407

Zusammenfassung

Vacuolar type ATPases (V-ATPases) are heteromultimeric, proton translocating proteins which are localized in a multitude of eukaryotic membranes and energize many different transport processes. Their malfunction is correlated with various diseases such as renal acidosis or cancer. The polyketide natural products archazolid A and B constitute novel types of particularly efficient (IC50 in the low nanomolar range) and specific inhibitors of V-ATPases, both in vitro and in vivo. Their unique structures have not been synthetically attained, nor has the conformation of the archazolids been ...

Projektinformationen

Status:

Beendet

Startdatum:

01.12.2006

Enddatum:

31.01.2008

Fördersumme:

79.400 €

Profilbereich:

Beendete Förderinitiativen

Förderinitiative:

Konformationelle Kontrolle biomolekularer Funktionen