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.
: Despite significant research progress on the pathogenesis, molecular biology, diagnosis, treatment, and prevention of cancer its morbidity and mortality is still high around the world. The emerging resistance of cancer cells to anticancer drugs remains still a significant problem in oncology today. Furthermore, an important challenge is the inability of anticancer drugs to selectively target tumor cells thus sparing healthy cells. One of new potential options for efficient and safe therapy can be provided by opioid growth factor (OGF), chemically termed Met-enkephalin. It is an endogenous pentapeptide (Tyr-Gly-Gly-Phe-Met) with antitumor, analgesic and immune-boosting properties. Clinical trials have demonstrated that OGF therapy alone, as well as in combination with standard chemotherapies, is a safe, non-toxic anticancer agent that reduces tumor size. In this paper, we review the structure-activity relationship of OGF and its analogues. We highlight also OGF derivatives with analgesic, immunomodulatory activity and the ability to penetrate the blood-brain barrier and may be used as a safe agents enhancing chemotherapy efficacy and improving quality of life in cancer patients. The reviewed papers indicate that Met-enkephalin, as well as its analogues are interesting candidates for the development of novel, non-toxic and endowed with an analgesic activity anticancer drugs. More preclinical and clinical studies are needed to explore these opportunities.
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