A Bifunctional Molecule That Displays Context-Dependent Cellular Activity

The cell-permeable dihydrofolate reductase inhibitor methotrexate was covalently linked to a ligand for the protein FKBP to create a bifunctional molecule called MTXSLF. The covalent tether between the two ligands was designed to be prohibitively short, so that unfavorable protein−protein interactio...

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Veröffentlicht in:	Journal of the American Chemical Society 2003-06, Vol.125 (25), p.7575-7580
Hauptverfasser:	Braun, Patrick D, Barglow, Katherine T, Lin, Yun-Ming, Akompong, Thomas, Briesewitz, Roger, Ray, Gregory T, Haldar, Kasturi, Wandless, Thomas J
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acid Sequence Animals Antimalarials - chemistry Antimalarials - metabolism Antimalarials - pharmacology Biological and medical sciences Cell Line Female Folic Acid Antagonists - chemistry Folic Acid Antagonists - metabolism Folic Acid Antagonists - pharmacology Fundamental and applied biological sciences. Psychology Humans Kinetics Ligands Methotrexate - analogs & derivatives Methotrexate - chemistry Methotrexate - metabolism Methotrexate - pharmacology Molecular and cellular biology Molecular Sequence Data Peptidylprolyl Isomerase Plasmodium falciparum - drug effects Plasmodium falciparum - enzymology Tacrolimus Binding Proteins - chemistry Tacrolimus Binding Proteins - metabolism Tetrahydrofolate Dehydrogenase - metabolism Uterus - cytology Uterus - drug effects
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