Trimethoprim(an anti-bacterial
drug) and methotrexate(MTX, an anti-cancer drug)
binds to DHFR much easier than folate.
Therefore, analogues of trimethoprim and methotrexate becomes
good candidates for binding tests.
科普導讀：天下文化所出版《
基因聖戰》（Jerry Bishop 著，楊玉齡 譯），1994, 10
Where to obtain the molecules?
from Brookheaven Protein Databank(US. $70, one CD)
available from ftp.csie.ntu.edu.tw(台大資訊系), including Xray, CT, MRI,
Ultrasound data.
Selective Inhibitors of Dihydrofolate Reductase (Nobel Lecture)
Prof. George H. Hitchings Jr.
Wellcome Research Laboratories, Burroughs Wellcome Co., 3030 Cornwallis Road, Research Triangle Park, NC 27709(USA)
Purine and pyrimidine derivatives acting as nucleic base antagonists and inhibitors of dihydrofolate-reductase(DHFR), which is an essential enzyme for nuclei acid synthesis in vivo, have opened up access to the chemotherapy of cancer, particularly leukemia, to immunosuppression, and to the treatment of gout and virus diseases. Examples from the Nobel lectures of Gertrude Elion and George Hitchings are the clinically extremely important antiviral agent acyclovir 1 (purine derivative) and the DHFR inhibitor trimetrexate 2 (pyrimidine derivative).
