DHFRgátlása

DHFR gátlása refers to the inhibition of dihydrofolate reductase (DHFR). DHFR is a crucial enzyme in the folate metabolism pathway, responsible for converting dihydrofolate into tetrahydrofolate. Tetrahydrofolate is an essential cofactor for the synthesis of purines and pyrimidines, which are the building blocks of DNA and RNA. Therefore, inhibiting DHFR effectively halts DNA replication and cell division.

This mechanism of action makes DHFR inhibitors valuable therapeutic agents, particularly in cancer chemotherapy and antimicrobial treatments. By blocking DHFR, these drugs prevent rapidly dividing cancer cells and microbial pathogens from synthesizing the necessary components for growth and reproduction.

Examples of DHFR inhibitors include methotrexate, a widely used chemotherapy drug for various cancers like leukemia and lymphoma, as well as autoimmune diseases. Trimethoprim is another significant DHFR inhibitor, commonly employed as an antibiotic, often in combination with sulfamethoxazole, to treat bacterial infections, especially urinary tract infections. The differential sensitivity of DHFR in various organisms allows for selective targeting. Cancer cells and bacteria often have a higher dependency on this pathway compared to normal human cells, enabling therapeutic efficacy with manageable side effects. Research continues to explore new DHFR inhibitors with improved specificity and reduced resistance profiles.