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Tuyển tập các báo cáo nghiên cứu về y học được đăng trên tạp chí y học General Psychiatry cung cấp cho các bạn kiến thức về ngành y đề tài:A new weapon against an old target. | Fiehn Arthritis Research Therapy 2011 13 122 http arthritis-research.eom content 13 4 122 EDITORIAL L_ A new weapon against an old target Christoph Fiehn See related research by Lu etal. http arthritis-research.eom content 13 2 R56 Abstract High expression of folate receptors is characteristic for the effector cell population of synovial macrophages in synovial inflammation. A new drug conjugate EC0746 targets the folate inhibitor aminopterin to folate receptors. In vitro studies show that this conjugate acts antiproliferatively and inhibits cytokine production by macrophage cell lines. Moreover it shows strong anti-arthritic effects in the rat model of adjuvant-induced arthritis in vivo. Toxicity of aminopterin was reduced 40-fold by using equimolar doses of the drug conjugate. In conclusion this new treatment approach has the potential to further improve the most successful principle of folate inhibition in the treatment of arthritis. Methotrexate MTX has been established as the anchor drug in the treatment of rheumatoid arthritis RA for decades. Its major role as an effective and well-tolerated substance impressively demonstrates that the principle of folate inhibition has key anti-inflammatory effects in the pathomechanism of arthritis. MTX enters the cell primarily by two ways the reduced folate carrier RFC and the folate receptor FR -p. The latter is the target of a novel interesting approach for treating arthritis that was introduced in a previous issue of Arthritis Research Therapy 1 . RFC is a transmembrane folate transport mechanism that has a ubiquitous distribution throughout the body 2 3 . The high affinity of MTX for RFC may explain why MTX has effects on a large number of cell types. Some are therapeutic targets such as synovial lymphocytes but others such as organ cells of liver or kidney are sensitive to toxic effects of MTX thus constituting a dose-limiting factor. In contrast to RFC FR-P has a restricted distribution mainly on activated