PMID:10801470

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Citation

Kopytek, SJ, Standaert, RF, Dyer, JC and Hu, JC (2000) Chemically induced dimerization of dihydrofolate reductase by a homobifunctional dimer of methotrexate. Chem. Biol. 7:313-21

Abstract

Chemically induced dimerization (CID) can be used to manipulate cellular regulatory pathways from signal transduction to transcription, and to create model systems for study of the specific interactions between proteins and small-molecule chemical ligands. However, few CID systems are currently available. The properties of, and interactions between, Escherichia coli dihydrofolate reductase (DHFR) and the ligand methotrexate (MTX) meet many of the desired criteria for the development of a new CID system.

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Keywords

Binding Sites; Biological Availability; Chromatography, Gel; Dimerization; Escherichia coli/enzymology; Ligands; Macromolecular Substances; Methotrexate/analogs & derivatives; Methotrexate/chemistry; Methotrexate/metabolism; Organophosphorus Compounds/chemistry; Tetrahydrofolate Dehydrogenase/chemistry; Tetrahydrofolate Dehydrogenase/metabolism

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