Evidence map›Paper›PMID 35114895›Full record

ReviewChannels (Austin, Tex.)2022

A SWELL time to develop the molecular pharmacology of the volume-regulated anion channel (VRAC).

Eric E Figueroa, Jerod S Denton

Open access · goldAbstract readReview
In one paragraph

Review in Channels (Austin, Tex.), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.

0numbers the graph read from it
0cells of the map it votes in
16citing papers in PubMed
1.6field-weighted citation impact, top 17% 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

16 citing papers in PubMed, 19 citations in OpenAlex.

  1. Article
  2. Article
  3. Exploring the selective inhibitory effects of Flavoxate and its analogues on two chloride channels and neuronal action potentials.The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology · 2026
    Article
  4. Article
  5. Review
  6. Article
  7. Review
  8. Review
  9. Review
  10. Article
  11. Review
  12. Article
  13. Article
  14. Structure of a volume-regulated heteromeric LRRC8A/C channel.Nature structural & molecular biology · 2023
    Article
  15. Article
  16. Review
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

2 authors at 1 institution in 1 country.

Eric E FigueroaDepartment of Physiology, University of California San Francisco, San Francisco, CA, USA.
Jerod S DentonDepartment of Pharmacology, Vanderbilt University, Vanderbilt Institute of Chemical Biology, Nashville, TN, USA.
Vanderbilt University · US

Funding

UCSF IRACDA Scholars ProgramK12GM081266 · NIGMS · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI Raymond M. Esquerra, HOLLY A. INGRAHAM · 2007 to 2026
$19.4M
Structure-function analysis of the volume-regulated anion channel VRAC using novel LRRC8 chimerasR01DK051610 · NIDDK · VANDERBILT UNIVERSITY MEDICAL CENTER · PI DENTON, JEROD S. · 1996 to 2025
$8.9M
Molecular pharmacology of LRRC8 volume-regulated anion channelsF31DK120225 · NIDDK · VANDERBILT UNIVERSITY · PI FIGUEROA, ERIC · 2018 to 2020
$69k
NIDDK NIH HHS F31 DK120225NIDDK NIH HHS R01 DK051610NIGMS NIH HHS K12 GM081266
6 · The paper itself

Abstract

Newly emerging roles of LRRC8 volume-regulated anion channels (VRAC) raise important questions about the therapeutic potential of VRAC in the treatment of epilepsy, type 2 diabetes, and other human diseases. A critical barrier to evaluating whether VRAC represents a viable drug target is the lack of potent and specific small-molecule inhibitors and activators of the channel. Here we review recent progress in developing the molecular pharmacology of VRAC made by screening a library of FDA-approved drugs for novel channel modulators. We discuss the discovery and characterization of cysteinyl leukotriene receptor antagonists Pranlukast and Zafirlukast as novel VRAC inhibitors, and zinc pyrithione (ZPT), which apparently activates VRAC through a reactive oxygen species (ROS)-dependent mechanism. These ongoing efforts set the stage for developing a pharmacological toolkit for probing the integrative physiology, molecular pharmacology, and therapeutic potential of VRAC.

Indexed as

Diabetes Mellitus, Type 2Membrane ProteinsAnionsHumansReactive Oxygen SpeciesAnionsMembrane ProteinsReactive Oxygen SpeciesLRRC8PranlukastVRACZafirlukastzinc pyrithione

Identifiers

PMID35114895
PMCPMC8820792
OpenAlexW4212836368

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.