Methotrexate
Dihydrofolate reductase inhibitor / A synthetic folic acid analog with immunosuppressant and cancer chemotherapeutic activity.1 Inhibits thymidylate synthetase and de novo purine synthesis.2,3 Displays beneficial effects in rheumatoid arthritis by inhibiting the production of cytokines induced by T-cell activation4 and stimulation of adenosine release5. It is the classic disease-modifying antirheumatic drug (DMARD).6
Biochemicals & reagents
133073-73-1
Amethopterin; CL-14377; NSC740
1) Wessels et al. (2008), Recent insights in the pharmacological actions of methotrexate in the treatment of rheumatoid arthritis; Rheumatology (Oxford), 47 249 2) Allegra et al. (1987), Evidence for direct inhibition of de novo purine synthesis in human MCF-7 breast cells as a principal mode of metabolic inhibition by methotrexate; J. Biol. Chem., 262 13520 3) Chu et al. (1990), Mechanism of thymidylate synthase inhibition by methotrexate in human neoplastic cell lines and normal human myeloid progenitor cells; J. Biol. Chem., 265 8470 4) Gerards et al. (2003), Inhibition of cytokine production by methotrexate. Studies in healthy volunteers and patients with rheumatoid arthritis; Rheumatology (Oxford), 42 1189 5) Friedman and Cronstein (2019), Methotrexate mechanism in treatment of rheumatoid arthritis; Joint Bone Spine, 86 301 6) Smolen and Steiner (2003), Therapeutic strategies for rheumatoid arthritis; Nat. Rev. Drug Discov., 2 473
-20°C
TARGET: DHFR (Dihydrofolate reductase); DNA; RNA -- PATHWAY: Nucleoside/tide biosynthesis; DNA synthesis; Cytokine; Protein synthesis; Cell adhesion -- RESEARCH AREA: Immunology -- DISEASE AREA: Cancer; Inflammation