Evidence map›Paper›PMID 26227776›Full record

ArticleBioorganic & medicinal chemistry letters2015

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

Open access · greenAbstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
0.4field-weighted citation impact, top 39% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

3 citing papers in PubMed, 8 citations in OpenAlex.

  1. MedComm · 2023
    Review
  2. Review
  3. Improved synthesis of SV2A targeting radiotracer [EJNMMI radiopharmacy and chemistry · 2019
    Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

7 authors at 2 institutions in 1 country.

Hui WangInstitute for Chemical Biology and Drug Discovery, Department of Chemistry, Stony Brook University, Stony Brook, NY 11794-3400, United States.
Li LiuInstitute for Chemical Biology and Drug Discovery, Department of Chemistry, Stony Brook University, Stony Brook, NY 11794-3400, United States.
Yang LuInstitute for Chemical Biology and Drug Discovery, Department of Chemistry, Stony Brook University, Stony Brook, NY 11794-3400, United States.
Pan PanInstitute for Chemical Biology and Drug Discovery, Department of Chemistry, Stony Brook University, Stony Brook, NY 11794-3400, United States.
Jacob M HookerBiological, Environmental and Climate Sciences Department, Brookhaven National Laboratory, Upton, NY 11973, United States.
Joanna S FowlerBiological, Environmental and Climate Sciences Department, Brookhaven National Laboratory, Upton, NY 11973, United States.
Peter J TongeInstitute for Chemical Biology and Drug Discovery, Department of Chemistry, Stony Brook University, Stony Brook, NY 11794-3400, United States. Electronic address: peter.tonge@stonybrook.edu.
Stony Brook University · USBrookhaven National Laboratory · US

Funding

Mechanism of Slow Onset Enzyme Inhibition and Translation to Time-Dependent Drug ActivityR01GM102864 · NIGMS · STATE UNIVERSITY NEW YORK STONY BROOK · PI TONGE, PETER J · 2012 to 2021
$2.6M
NIGMS NIH HHS GM102864NIGMS NIH HHS R01 GM102864
6 · The paper itself

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.

Indexed as

Positron-Emission TomographyAnimalsAnti-Bacterial AgentsAntirheumatic AgentsBacterial ProteinsDisease Models, AnimalDose-Response Relationship, DrugEnzyme InhibitorsMiceMicrobial Sensitivity TestsMolecular StructureMycobacterium tuberculosisOxidoreductasesPapioPhenyl EthersStructure-Activity Relationship2-(2-tolyloxy)-5-hexylphenolAnti-Bacterial AgentsAntirheumatic AgentsBacterial ProteinsEnzyme InhibitorsInhA protein, MycobacteriumOxidoreductasesPhenyl EthersCarbon-11InhA enoyl-ACP reductasePK–PDPositron emission tomographyResidence time

Identifiers

PMID26227776
PMCPMC4607644
OpenAlexW915639078

What OpenQuestion holds

Textmetadata
LicenceTDM
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.