Methotrexate (MTX) an FDA-approved folic acid antagonist is highly effective in treating rheumatoid arthritis psoriasis inflammatory bowel disease and various cancers including acute leukemia head and neck cancer and osteosarcoma. However systemic administration of anticancer agents often suffers from off-target effects impacting efficacy and tolerability. Photopharmacology which employs photoswitchable drugs is well-suited for enhancing drug activity. Precise spatiotemporal control reduces off-target effects allowing higher doses for improved efficacy.This book delves into MTX's historical development and current applications exploring its potential as a photoswitchable inhibitor for human and E. coli DHFR through a comprehensive structure-based drug discovery approach. It guides readers through methotrexate's evolution highlighting its role as a pioneer in precision medicine. The book emphasizes the integration of conventional pharmacological principles with innovative photopharmacological strategies shaping a promising frontier in targeted therapeutic interventions.
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