Literature DB >> 26227776

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

Hui Wang1, Li Liu1, Yang Lu1, Pan Pan1, Jacob M Hooker2, Joanna S Fowler2, Peter J Tonge3.   

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.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Carbon-11; InhA enoyl-ACP reductase; PK–PD; Positron emission tomography; Residence time

Mesh：

Substances：

Year:  2015        PMID： 26227776      PMCID： PMC4607644          DOI： 10.1016/j.bmcl.2015.07.019

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  41 in total

Review 1.  Issues in pharmacokinetics and pharmacodynamics of anti-infective agents: distribution in tissue.

Authors:  Markus Müller; Amparo dela Peña; Hartmut Derendorf
Journal:  Antimicrob Agents Chemother       Date:  2004-05       Impact factor: 5.191

2.  Structural basis and mechanism of enoyl reductase inhibition by triclosan.

Authors:  M J Stewart; S Parikh; G Xiao; P J Tonge; C Kisker
Journal:  J Mol Biol       Date:  1999-07-23       Impact factor: 5.469

Review 3.  The role of positron emission tomography in pharmacokinetic analysis.

Authors:  A J Fischman; N M Alpert; J W Babich; R H Rubin
Journal:  Drug Metab Rev       Date:  1997-11       Impact factor: 4.518

4.  Mycobacterium tuberculosis growth at the cavity surface: a microenvironment with failed immunity.

Authors:  Gilla Kaplan; Frank A Post; Andre L Moreira; Helen Wainwright; Barry N Kreiswirth; Melike Tanverdi; Barun Mathema; Srinivas V Ramaswamy; Gabi Walther; Lafras M Steyn; Clifton E Barry; Linda-Gail Bekker
Journal:  Infect Immun       Date:  2003-12       Impact factor: 3.441

5.  inhA, a gene encoding a target for isoniazid and ethionamide in Mycobacterium tuberculosis.

Authors:  A Banerjee; E Dubnau; A Quemard; V Balasubramanian; K S Um; T Wilson; D Collins; G de Lisle; W R Jacobs
Journal:  Science       Date:  1994-01-14       Impact factor: 47.728

6.  Implications of multidrug resistance for the future of short-course chemotherapy of tuberculosis: a molecular study.

Authors:  B Heym; N Honoré; C Truffot-Pernot; A Banerjee; C Schurra; W R Jacobs; J D van Embden; J H Grosset; S T Cole
Journal:  Lancet       Date:  1994-07-30       Impact factor: 79.321

7.  Characterization of the catalase-peroxidase gene (katG) and inhA locus in isoniazid-resistant and -susceptible strains of Mycobacterium tuberculosis by automated DNA sequencing: restricted array of mutations associated with drug resistance.

Authors:  J M Musser; V Kapur; D L Williams; B N Kreiswirth; D van Soolingen; J D van Embden
Journal:  J Infect Dis       Date:  1996-01       Impact factor: 5.226

8.  Catalase-peroxidase gene sequences in isoniazid-sensitive and -resistant strains of Mycobacterium tuberculosis from New York City.

Authors:  M Y Stoeckle; L Guan; N Riegler; I Weitzman; B Kreiswirth; J Kornblum; F Laraque; L W Riley
Journal:  J Infect Dis       Date:  1993-10       Impact factor: 5.226

9.  The catalase-peroxidase gene and isoniazid resistance of Mycobacterium tuberculosis.

Authors:  Y Zhang; B Heym; B Allen; D Young; S Cole
Journal:  Nature       Date:  1992-08-13       Impact factor: 49.962

10.  The isoniazid-NAD adduct is a slow, tight-binding inhibitor of InhA, the Mycobacterium tuberculosis enoyl reductase: adduct affinity and drug resistance.

Authors:  Richa Rawat; Adrian Whitty; Peter J Tonge
Journal:  Proc Natl Acad Sci U S A       Date:  2003-11-17       Impact factor: 11.205
View more
  1 in total

1.  Improved synthesis of SV2A targeting radiotracer [11C]UCB-J.

Authors:  Johanna Rokka; Eva Schlein; Jonas Eriksson
Journal:  EJNMMI Radiopharm Chem       Date:  2019-11-29
  1 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.