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Engineering Small Molecule Specificity in Nearly Identical Cellular Environments

Methotrexate (MTX), an inhibitor of dihydrofolate reductase, was tethered to an FKBP12 ligand (SLF), and the resulting bifunctional molecule (MTXSLF) potently inhibits either enzyme but not both simultaneously. MTXSLF is cytotoxic to fibroblasts derived from FKBP12-null mice but is detoxified 40-fol...

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Hlavní autoři: Sellmyer, Mark A., Stankunas, Kryn, Briesewitz, Roger, Crabtree, Gerald R., Wandless, Thomas J.
Médium: Artigo
Jazyk:Inglês
Vydáno: 2007
Témata:
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC1949043/
https://ncbi.nlm.nih.gov/pubmed/17383876
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2007.03.012
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