Evidence map›Paper›PMID 22034937›Full record

ArticleBioconjugate chemistry2011

Functional fluorescently labeled bithiazole ΔF508-CFTR corrector imaged in whole body slices in mice.

Holly R Davison, Stephanie Taylor, Chris Drake, Puay-Wah Phuan, Nico Derichs, Chenjuan Yao, Ella F Jones, Julie Sutcliffe, A S Verkman, Mark J Kurth

Open access · greenAbstract read
In one paragraph

Article in Bioconjugate chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
1.0field-weighted citation impact, top 21% 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

6 citing papers in PubMed, 13 citations in OpenAlex.

  1. Article
  2. Review
  3. Article
  4. Article
  5. Fluorinated ΔF508-CFTR correctors and potentiators for PET imaging.Bioorganic & medicinal chemistry letters · 2012
    Article
  6. 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

10 authors at 3 institutions in 1 country.

Holly R DavisonDepartment of Chemistry, University of California, Davis, Davis, California 95616, United States.
Stephanie Taylor
Chris Drake
Puay-Wah Phuan
Nico Derichs
Chenjuan Yao
Ella F Jones
Julie Sutcliffe
A S Verkman
Mark J Kurth
University of California, San Francisco · USUniversity of California, Davis · USBerry (United States) · US

Funding

SynthesisP30DK072517 · NIDDK · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI VERKMAN, ALAN S · 2005 to 2022
$18.1M
Complex Heterocycles and Hybrid Strategies for Pilot Scale LibrariesP41GM089153 · NIGMS · UNIVERSITY OF CALIFORNIA AT DAVIS · PI KURTH, MARK J. · 2010 to 2012
$1.1M
NIDDK NIH HHS DK72517NIDDK NIH HHS P30 DK072517NIGMS NIH HHS GM089153NIGMS NIH HHS P41 GM089153
6 · The paper itself

Abstract

We previously reported the identification and structure-activity analysis of bithiazole-based correctors of defective cellular processing of the cystic fibrosis-causing CFTR mutant, ΔF508-CFTR. Here, we report the synthesis and uptake of a functional, fluorescently labeled bithiazole corrector. Following synthesis and functional analysis of four bithiazole-fluorophore conjugates, we found that 5, a bithazole-based BODIPY conjugate, had low micromolar potency for correction of defective ΔF508-CFTR cellular misprocessing, with comparable efficacy to benchmark corrector corr-4a. Intravenous administration of 5 to mice established its stability in extrahepatic tissues for tens of minutes. By fluorescence imaging of whole-body frozen slices, fluorescent corrector 5 was visualized strongly in gastrointestinal organs, with less in lung and liver. Our results provide proof-of-concept for mapping the biodistribution of a ΔF508-CFTR corrector by fluorophore labeling and fluorescence imaging of whole-body slices.

Indexed as

Whole Body ImagingAnimalsBoron CompoundsCystic FibrosisCystic Fibrosis Transmembrane Conductance RegulatorFluorescent DyesMiceMutationThiazoles4,4-difluoro-4-bora-3a,4a-diaza-s-indaceneBoron CompoundsCystic Fibrosis Transmembrane Conductance RegulatorFluorescent DyesThiazoles

Identifiers

PMID22034937
PMCPMC3245868
OpenAlexW2036221498

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.