FROM BENCH TO BEDSIDE: A THOROUGH EXPLORATION OF FOLATE ANTAGONISTS IN MEDICINE

Abstract

Folate antagonists have considerable potentials in medical therapeutics especially occasions in oncology and antimicrobial therapy. Herein, this exhaustive review looks into their actions at molecular levels, into clinical applications as well as assesses the currently emerging state of use. It starts with describing the activity of folate in DNA synthesis and cell division which forms the basis to comprehend the mechanism of disruption of these processes by folate antagonists. The talk is related to the main antifolate drugs, such as methotrexate, aminopterin, and trimethoprim, whose mechanism of action reflects an impact on an enzyme
facilitating folate metabolism, namely dihydrofolate reductase (DHFR). The review in oncology outlines their use as chemotherapeutic agents, including mechanisms of action, dose selection, and related toxicities, and focuses in particular on the trade-offs between therapeutic effect and hematologic and gastrointestinal toxicities. With regards to antimicrobial therapy, the review deals with the application of trimethoprim on bacterial DHFR used as a treatment of infection. Future views are concluded in the paper on the development of new agents, innovative ones and development of a drug delivery, as well as the strategy of overcoming resistance. The given review has two different purposes: it can be helpful to the researchers and to the clinicians in order to gain deeper insight into the use of the folate antagonists and their modernization in contemporary medicine.