Synthesis and chemical characterisation of target identification reagents based on an inhibitor of human cell invasion by the parasite Toxoplasma gondii

Kathryn M. Evans, Jeralyn D. Haraldsen, Russell J. Pearson, Alexandra M. Z. Slawin, Gary E. Ward, Nicholas J. Westwood

Research output: Contribution to journalArticlepeer-review

7 Citations (Scopus)

Abstract

The use of phenotype-based screens as an approach for identifying novel small molecule tools is reliant on successful protein target identification strategies. Here we report on the synthesis and chemical characterisation of a novel reagent for protein target identification based on a small molecule inhibitor of human cell invasion by the parasite Toxoplasma gondii. A detailed H-1 NMR study and biological testing confirmed that incorporation of an amino-containing functional group into the aryl ring of this inhibitor was possible without loss of biological activity. Interesting chemical reactivity differences were identified resulting from incorporation of the new substituent. The amine functionality was then used to prepare a biotinylated reagent that is central to our current protein target identification studies with this inhibitor.

Original languageEnglish
Pages (from-to)2063-2069
Number of pages7
JournalOrganic & Biomolecular Chemistry
Volume5
DOIs
Publication statusPublished - 2007

Keywords

  • ROUTE

Fingerprint

Dive into the research topics of 'Synthesis and chemical characterisation of target identification reagents based on an inhibitor of human cell invasion by the parasite Toxoplasma gondii'. Together they form a unique fingerprint.

Cite this