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

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.

Authors:
 [1];  [1];  [1];  [1];  [2];  [2];  [1]
  1. Stony Brook Univ., NY (United States)
  2. Brookhaven National Lab. (BNL), Upton, NY (United States)
Publication Date:
Research Org.:
Brookhaven National Laboratory (BNL), Upton, NY (United States)
Sponsoring Org.:
National Institute of Health
OSTI Identifier:
1239783
Report Number(s):
BNL-111671-2015-JA
Journal ID: ISSN 0960-894X; R&D Project: MO-085; KP1503010
Grant/Contract Number:  
SC00112704
Resource Type:
Journal Article: Accepted Manuscript
Journal Name:
Bioorganic & Medicinal Chemistry Letters
Additional Journal Information:
Journal Volume: 25; Journal Issue: 21; Journal ID: ISSN 0960-894X
Country of Publication:
United States
Language:
English
Subject:
38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY; Positron emission tomography; InhA enoyl-ACP reductase; Residence time; Carbon-11; PK-PD

Citation Formats

Wang, Hui, Liu, Li, Lu, Yang, Pan, Pan, Hooker, Jacob M., Fowler, Joanna S., and Tonge, Peter J. Radiolabelling and positron emission tomography of PT70, a time-dependent inhibitor of InhA, the Mycobacterium tuberculosis enoyl-ACP reductase. United States: N. p., 2015. Web. doi:10.1016/j.bmcl.2015.07.019.
Wang, Hui, Liu, Li, Lu, Yang, Pan, Pan, Hooker, Jacob M., Fowler, Joanna S., & Tonge, Peter J. Radiolabelling and positron emission tomography of PT70, a time-dependent inhibitor of InhA, the Mycobacterium tuberculosis enoyl-ACP reductase. United States. doi:10.1016/j.bmcl.2015.07.019.
Wang, Hui, Liu, Li, Lu, Yang, Pan, Pan, Hooker, Jacob M., Fowler, Joanna S., and Tonge, Peter J. Tue . "Radiolabelling and positron emission tomography of PT70, a time-dependent inhibitor of InhA, the Mycobacterium tuberculosis enoyl-ACP reductase". United States. doi:10.1016/j.bmcl.2015.07.019. https://www.osti.gov/servlets/purl/1239783.
@article{osti_1239783,
title = {Radiolabelling and positron emission tomography of PT70, a time-dependent inhibitor of InhA, the Mycobacterium tuberculosis enoyl-ACP reductase},
author = {Wang, Hui and Liu, Li and Lu, Yang and Pan, Pan and Hooker, Jacob M. and Fowler, Joanna S. and Tonge, Peter J.},
abstractNote = {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.},
doi = {10.1016/j.bmcl.2015.07.019},
journal = {Bioorganic & Medicinal Chemistry Letters},
issn = {0960-894X},
number = 21,
volume = 25,
place = {United States},
year = {2015},
month = {7}
}

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Cited by: 1 work
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