Drug action on ribonucleotide reductase
β Scribed by Joseph G. Cory; Gay L. Carter
- Book ID
- 118372034
- Publisher
- Elsevier Science
- Year
- 1985
- Tongue
- English
- Weight
- 891 KB
- Volume
- 24
- Category
- Article
- ISSN
- 0065-2571
No coin nor oath required. For personal study only.
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## Abstract Gemcitabine (2β²,2β²βdifluoroβ2β²βdeoxycytidine, dFdC) is a very promising anticancer drug, already approved for clinical use in three therapeutic indications. It is metabolized intracellularly to 5β²βdiphosphate (dFdCDP), which is known to be a potent inhibitor of ribonucleotide reductase
Mammalian ribonucleotide reductase (mRR) is a chemotherapeutic target. The enzyme is composed of 2 subunits (mR1 and mR2) and is inhibited by Ac-FTLDADF (denoted P7), corresponding to the C-terminus of mR2, which competes with mR2 for binding to mR1. mRR has 2 physiologically important active forms,