Carnosine-related dipeptides as potential therapeutics against cancer:
in silico estimation of activity, synthesis and in vitro analysis
Background and purpose: Peptides constitute an interesting starting
point for drugs, although research on them is quite slowed by the fact
that most of them are non-patentable. Given that carnosine, β-Ala-His
dipeptide, was found useful in cancer treatment, we aimed to inspect
whether its similar structures could also possess such activity.
Experimental Approach: The interdisciplinary approach allows for the
much more detailed analysis, hence our study presents computational
analysis of potential targets and therapeutic activities of dipeptides
with β-Ala or His at the N-end, synthesis and in vitro cytotoxicity and
apoptosis tests against a chosen cancerous and non-cancerous cell line.
Key Results: We preliminarily propose β-Ala-Ala, His-Val and His-Arg as
most potent entities, in regard to carnosine, a known anticancer
peptide. Conclusion and Implications: An interdisciplinary approach
allows for a much more complex analysis and in silico tests should be a
standard element of every toxicological report and we hope to popularize
that concept worldwide. Peptides indeed possess activity against cancer,
with little to no harm to non-cancerous cells, which is highly valuable.