Radiolabelling and positron emission tomography of PT70, a time-dependent inhibitor of InhA, the Mycobacterium tuberculosis enoyl-ACP reductase

Hui Wang, Li Liu, Yang Lu, Pan Pan, Jacob M. Hooker, Joanna S. Fowler, Peter J. Tonge

Research output: Contribution to journalArticlepeer-review

8 Scopus citations

Abstract

PT70 is a diaryl ether inhibitor of InhA, the enoyl-ACP reductase in the Mycobacterium tuberculosis fatty acid biosynthesis pathway. It has a residence time of 24 min on the target, and also shows antibacterial activity in a mouse model of tuberculosis infection. Due to the interest in studying target tissue pharmacokinetics of PT70, we developed a method to radiolabel PT70 with carbon-11 and have studied its pharmacokinetics in mice and baboons using positron emission tomography.

Original languageEnglish
Pages (from-to)4782-4786
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume25
Issue number21
DOIs
StatePublished - 1 Nov 2015
Externally publishedYes

Keywords

  • Carbon-11
  • InhA enoyl-ACP reductase
  • PK-PD
  • Positron emission tomography
  • Residence time

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