Prostate cancer: diagnosis and treatment
Russian scientists have named promising substances for the treatment of prostate cancer
A group of researchers from four research centers - the Moscow Institute of Physics and Technology, Moscow State University, the National University of Science and Technology MISIS and the Skolkovo Institute of Science and Technology "Skoltech" has compiled a list of the most promising compounds for the treatment and diagnosis of prostate cancer. This is reported by the MIPT press service.
"The researchers identified 11 compounds as promising molecules. All these substances are now at the stage of clinical trials and have previously successfully passed preclinical studies on cell models and animals," the press release says.
Diagnostics
Prostate cancer is one of the most common types of cancer in men. Today, most methods of its therapy are insufficiently selective and have a detrimental effect not only on cancer cells, but also on healthy cells of the body. Therefore, scientists are looking for new drugs that would attack exclusively tumor cells, which will increase the effectiveness of treatment methods and reduce the negative impact of chemotherapy on the body as a whole.
To ensure the selectivity of such a drug, you need to find some object that is missing from all cells of the body, except cancer cells - a cancer marker. For example, the prostate-specific membrane antigen PSMA. Prostate cancer-affected tissues contain almost 10 times more of this substance than healthy tissues. Also, diagnosis with the help of PSMA allows you to detect the smallest metastases, repeated tumor foci that occur in other organs.
Treatment
"PSMA is one of the most promising biological targets for the development of new hybrids of molecules binding to PSMA and antitumor medicinal substances," the press service quotes the head of the Laboratory of Medical Chemistry and Bioinformatics of MIPT, Yan Ivanenkov.
All molecules capable of binding to PSMA can be divided into three groups. These are antibodies, aptamers and ligands. Antibodies are proteins synthesized by the immune system. Aptamers are protein molecules or DNA/RNA fragments capable of selectively binding to a given substance. And ligands are substances of a rather arbitrary nature that interact with enzymes.
Comparing all three groups, the researchers realized that the most promising for the treatment of cancer are named ligands – they are easier to synthesize, and they also have good pharmacokinetic indicators.
The most promising compounds for treatment
The search for ligands suitable for PSMA has been carried out in the world since the 1990s, and phosphorus compounds have long been considered the most promising of them. However, they demonstrated weak pharmacokinetic parameters for conducting clinical trials. Then, compounds with -SH groups became an alternative to phosphorus-containing chemicals. They showed high bioavailability when taking the drug by mouth, and also penetrated better through the cell membrane. However, these drugs adversely affected not only cancer cells and were modified during biochemical reactions in the body.
For a new class of ligands, the absence of the shortcomings of the precursors was required, and urea-based compounds became the next candidates for the role of a prostate cancer drug.
Now it is the most widely studied type of PSMA ligands and 11 compounds of this class have been identified by researchers as the most promising prostate cancer drugs.
The scientists' article was published in the Journal of Drug Targeting (Machulkin et al., Small-molecule PSMA ligands. Current state, SAR and perspectives).
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22.03.2016