Abstract
An Australian marine sediment-derived isolate, Nocardiopsis sp. (CMB-M0232), yielded a new class of prenylated diketopiperazine, indicative of the action of a uniquely regioselective diketopiperazine indole prenyltransferase. The bridged scaffold of nocardioazine A proved to be a noncytotoxic inhibitor of the membrane protein efflux pump P-glycoprotein, reversing doxorubicin resistance in a multidrug resistant colon cancer cell.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
ATP Binding Cassette Transporter, Subfamily B, Member 1 / antagonists & inhibitors*
-
Actinomycetales / chemistry*
-
Australia
-
Diketopiperazines / chemistry
-
Diketopiperazines / isolation & purification*
-
Diketopiperazines / pharmacology*
-
Dimethylallyltranstransferase / metabolism*
-
Doxorubicin / pharmacology
-
Drug Resistance, Multiple / drug effects
-
Marine Biology
-
Models, Molecular
Substances
-
ATP Binding Cassette Transporter, Subfamily B, Member 1
-
Diketopiperazines
-
nocardioazine A
-
nocardioazine B
-
Doxorubicin
-
Dimethylallyltranstransferase