Interaction of methotrexate metabolites with beef liver dihydrofolate reductase-I. Binary complex study. 1983

M Chauvet, and M Bourdeaux, and C Briand, and M Dell'Amico, and R Gilli, and M Diarra

In order to explain the difference of inhibition of dihydrofolate reductase (DHFR) by methotrexate (MTX) and its metabolites 7-hydroxymethotrexate [7OH (MTX)] and polyglutamate derivatives [MTX (G1) and MTX (G2)], direct determinations of binding parameters to beef liver DHFR were performed. Association constants are calculated by fluorescence titrations and thermodynamic parameters by microcalorimetric measurements. The parameters of interaction are nearly identical for MTX and polyglutamate derivatives but are different for MTX and 7OH (MTX). For this last derivative electrostatic forces are less predominant and a larger modification of its conformation appears in the enzyme during the complex formation.

UI MeSH Term Description Entries
D008099 Liver A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances. Livers
D008727 Methotrexate An antineoplastic antimetabolite with immunosuppressant properties. It is an inhibitor of TETRAHYDROFOLATE DEHYDROGENASE and prevents the formation of tetrahydrofolate, necessary for synthesis of thymidylate, an essential component of DNA. Amethopterin,Methotrexate Hydrate,Methotrexate Sodium,Methotrexate, (D)-Isomer,Methotrexate, (DL)-Isomer,Methotrexate, Dicesium Salt,Methotrexate, Disodium Salt,Methotrexate, Sodium Salt,Mexate,Dicesium Salt Methotrexate,Hydrate, Methotrexate,Sodium, Methotrexate
D002151 Calorimetry The measurement of the quantity of heat involved in various processes, such as chemical reactions, changes of state, and formations of solutions, or in the determination of the heat capacities of substances. The fundamental unit of measurement is the joule or the calorie (4.184 joules). (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
D002417 Cattle Domesticated bovine animals of the genus Bos, usually kept on a farm or ranch and used for the production of meat or dairy products or for heavy labor. Beef Cow,Bos grunniens,Bos indicus,Bos indicus Cattle,Bos taurus,Cow,Cow, Domestic,Dairy Cow,Holstein Cow,Indicine Cattle,Taurine Cattle,Taurus Cattle,Yak,Zebu,Beef Cows,Bos indicus Cattles,Cattle, Bos indicus,Cattle, Indicine,Cattle, Taurine,Cattle, Taurus,Cattles, Bos indicus,Cattles, Indicine,Cattles, Taurine,Cattles, Taurus,Cow, Beef,Cow, Dairy,Cow, Holstein,Cows,Dairy Cows,Domestic Cow,Domestic Cows,Indicine Cattles,Taurine Cattles,Taurus Cattles,Yaks,Zebus
D005493 Folic Acid Antagonists Inhibitors of the enzyme, dihydrofolate reductase (TETRAHYDROFOLATE DEHYDROGENASE), which converts dihydrofolate (FH2) to tetrahydrofolate (FH4). They are frequently used in cancer chemotherapy. (From AMA, Drug Evaluations Annual, 1994, p2033) Antifolate,Antifolates,Dihydrofolate Reductase Inhibitor,Folic Acid Antagonist,Dihydrofolate Reductase Inhibitors,Folic Acid Metabolism Inhibitors,Acid Antagonist, Folic,Acid Antagonists, Folic,Antagonist, Folic Acid,Antagonists, Folic Acid,Inhibitor, Dihydrofolate Reductase,Inhibitors, Dihydrofolate Reductase,Reductase Inhibitor, Dihydrofolate,Reductase Inhibitors, Dihydrofolate
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013050 Spectrometry, Fluorescence Measurement of the intensity and quality of fluorescence. Fluorescence Spectrophotometry,Fluorescence Spectroscopy,Spectrofluorometry,Fluorescence Spectrometry,Spectrophotometry, Fluorescence,Spectroscopy, Fluorescence

Related Publications

M Chauvet, and M Bourdeaux, and C Briand, and M Dell'Amico, and R Gilli, and M Diarra
July 1977, Science (New York, N.Y.),
M Chauvet, and M Bourdeaux, and C Briand, and M Dell'Amico, and R Gilli, and M Diarra
October 1986, Cancer research,
M Chauvet, and M Bourdeaux, and C Briand, and M Dell'Amico, and R Gilli, and M Diarra
January 1983, Biochemistry,
M Chauvet, and M Bourdeaux, and C Briand, and M Dell'Amico, and R Gilli, and M Diarra
January 1976, Archives of biochemistry and biophysics,
M Chauvet, and M Bourdeaux, and C Briand, and M Dell'Amico, and R Gilli, and M Diarra
October 2002, Proceedings of the National Academy of Sciences of the United States of America,
M Chauvet, and M Bourdeaux, and C Briand, and M Dell'Amico, and R Gilli, and M Diarra
July 1980, Nature,
M Chauvet, and M Bourdeaux, and C Briand, and M Dell'Amico, and R Gilli, and M Diarra
March 1998, Journal of molecular biology,
M Chauvet, and M Bourdeaux, and C Briand, and M Dell'Amico, and R Gilli, and M Diarra
November 1985, Annals of clinical biochemistry,
M Chauvet, and M Bourdeaux, and C Briand, and M Dell'Amico, and R Gilli, and M Diarra
July 1978, Proceedings of the National Academy of Sciences of the United States of America,
M Chauvet, and M Bourdeaux, and C Briand, and M Dell'Amico, and R Gilli, and M Diarra
June 1978, Biochemistry,
Copied contents to your clipboard!