DKPs have been shown to inhibit the activities of bacteria, fungi, viruses, and potentially protozoa, as well as exhibit antitumor and antiprion properties. The molecule glionitrin, for instance, proved to be very effective against methicillin-resistant Staphylococcus aureus (MRSA), in addition to four different human cancer cell lines in vitro. As antivirals, however, DPKs appear to have a poor outlook when compared to those already on the market.
Despite the great potential for diversity in this class of molecules, natural DPKs containing proline are significantly overrepresented among those known to be biologically active. There also appears to be some bias with regards to stereochemistry, as DD-stereoisomers tend to display stronger antibiotic capabilities.