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Dynamic combinatorial chemistry to identify binders of ThiT, an S-component of the energy-coupling factor transporter for thiamine

Monjas, L., Swier, L. J. Y. M., Setyawati, I., Slotboom, D. J. & Hirsch, A. K. H. 6-Oct-2017 In : ChemMedChem. 12, 5 p.

Research output: Scientific - peer-reviewArticle

We applied dynamic combinatorial chemistry (DCC) to identify ligands of ThiT, the S-component of the energy-coupling factor (ECF) transporter for thiamine in Lactococcus lactis. We used a pre-equilibrated dynamic combinatorial library (DCL) and saturation-transfer difference (STD)-NMR to identify ligands of ThiT. This is the first report in which DCC is used for fragment growing to an ill-defined pocket, and one of the first reports for its application with an integral membrane protein as target.

Original languageEnglish
Number of pages5
JournalChemMedChem
Volume12
StateE-pub ahead of print - 6-Oct-2017

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