【摘 要】
：
Pralatrexate was rationally designed to be a much more potent anti-folate than the widely used methotrexate.Pralatrexate was designed to have higher affinity to reduced folate carrier 1 (RFC1), to enh
【机 构】
：
Spectrum Pharmaceuticals Inc.USA
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Pralatrexate was rationally designed to be a much more potent anti-folate than the widely used methotrexate.Pralatrexate was designed to have higher affinity to reduced folate carrier 1 (RFC1), to enhance uptake into cells, as well as higher affinity to folylpoly-gamma-glutamate synthetase to enhance polyglutamylation and, therefore, intracellular retention.True to its design, pralatrexate was found to have much higher anti-tumor activity than methotrexate in tumor models.Considering the wide variety applications for methotrexate, it was expected that pralatrexate would also be a useful anti-folate and would help treat difficult to treat diseases.
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