Evidence map›Paper›PMID 26985318›Full record

ArticleACS medicinal chemistry letters2016

Identification of a Small Molecule Cyclophilin D Inhibitor for Rescuing Aβ-Mediated Mitochondrial Dysfunction.

Koteswara Rao Valasani, Qinru Sun, Du Fang, Zhihua Zhang, Qing Yu, Yaopeng Guo, Jianping Li, Anuradha Roy, Shirley ShiDu Yan

Open access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.

0numbers the graph read from it
0cells of the map it votes in
25citing papers in PubMed
3.0field-weighted citation impact, top 9% 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

25 citing papers in PubMed, 42 citations in OpenAlex.

  1. Review
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  8. Non-Immunosuppressive Cyclophilin Inhibitors.Angewandte Chemie (International ed. in English) · 2022
    Review
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  13. Anxiety and task performance changes in an aging mouse model.Biochemical and biophysical research communications · 2019
    Article
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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

9 authors at 2 institutions in 2 countries.

Koteswara Rao ValasaniDepartment of Pharmacology & Toxicology and Higuchi Bioscience Center, School of Pharmacy, University of Kansas , Lawrence, Kansas 66047, United States.
Qinru SunDepartment of Pharmacology & Toxicology and Higuchi Bioscience Center, School of Pharmacy, University of Kansas, Lawrence, Kansas 66047, United States; College of Medicine and Forensics, Xi'an Jiaotong University Health Science Center, Xi'an, Shaanxi 710061, China.
Du FangDepartment of Pharmacology & Toxicology and Higuchi Bioscience Center, School of Pharmacy, University of Kansas , Lawrence, Kansas 66047, United States.
Zhihua ZhangDepartment of Pharmacology & Toxicology and Higuchi Bioscience Center, School of Pharmacy, University of Kansas , Lawrence, Kansas 66047, United States.
Qing YuDepartment of Pharmacology & Toxicology and Higuchi Bioscience Center, School of Pharmacy, University of Kansas , Lawrence, Kansas 66047, United States.
Yaopeng GuoDepartment of Pharmacology & Toxicology and Higuchi Bioscience Center, School of Pharmacy, University of Kansas , Lawrence, Kansas 66047, United States.
Jianping LiDepartment of Pharmacology & Toxicology and Higuchi Bioscience Center, School of Pharmacy, University of Kansas , Lawrence, Kansas 66047, United States.
Anuradha RoyHigh Throughput Screening Laboratory, University of Kansas , Lawrence, Kansas 66047, United States.
Shirley ShiDu YanDepartment of Pharmacology & Toxicology and Higuchi Bioscience Center, School of Pharmacy, University of Kansas , Lawrence, Kansas 66047, United States.
University of Kansas · USXi'an Jiaotong University · CN

Funding

Synthetic Chemical Biology CoreP20GM113117 · NIGMS · UNIVERSITY OF KANSAS LAWRENCE · PI OROZCO, ROBIN C. · 2016 to 2025
$23.9M
University of Kansas Alzheimer's Disease Core CentersP30AG035982 · NIA · UNIVERSITY OF KANSAS MEDICAL CENTER · PI SWERDLOW, RUSSELL H. · 2011 to 2020
$16.6M
Role of Cyclophilin D in Abeta-induced synaptic injuryR37AG037319 · NIA · UNIVERSITY OF KANSAS LAWRENCE · PI YAN, SHIRLEY SHIDU · 2010 to 2019
$3.1M
Mitochondrial degrading enzyme, synaptic mitochondrial function in AD mouse modelR01AG044793 · NIA · UNIVERSITY OF KANSAS LAWRENCE · PI YAN, SHIRLEY SHIDU · 2014 to 2018
$1.9M
Role of LRG-47 (Irgm1) in EAER01NS065482 · NINDS · UNIVERSITY OF KANSAS LAWRENCE · PI YAN, SHIRLEY SHIDU · 2010 to 2014
$1.6M
Structural and Functional Properties of cyclophilin D and Abeta interaction.R01GM095355 · NIGMS · UNIVERSITY OF KANSAS LAWRENCE · PI YAN, SHIRLEY SHIDU · 2010 to 2013
$1.5M
NIA NIH HHS P30 AG035982NIA NIH HHS R01 AG044793NIA NIH HHS R37 AG037319NIGMS NIH HHS P20 GM113117NIGMS NIH HHS R01 GM095355NINDS NIH HHS R01 NS065482
6 · The paper itself

Abstract

Cyclophilin D (CypD), a peptidylprolyl isomerase F (PPIase), plays a central role in opening the mitochondrial membrane permeability transition pore leading to cell death. CypD resides in the mitochondrial matrix, associates with the inner mitochondrial membrane, interacts with amyloid beta to exacerbate mitochondrial and neuronal stress and has been linked to Alzheimer's disease (AD). We report the biological activity of a small-molecule CypD inhibitor (C-9), which binds strongly to CypD and attenuates mitochondrial and cellular perturbation insulted by Aβ and calcium stress. Binding affinities for C-9 were determined using in vitro surface plasmon resonance. This compound antagonized calcium-mediated mitochondrial swelling, abolished Aβ-induced mitochondrial dysfunction as shown by increased cytochrome c oxidase activity and adenosine-5'-triphosphate levels, and inhibited CypD PPIase enzymatic activity by real-time fluorescence capture assay using Hamamatsu FDSS 7000. Compound C-9 seems a good candidate for further investigation as an AD drug.

Indexed as

amyloid βCypDmitochondrial dysfunctionmPTPsmall molecules

Identifiers

PMID26985318
PMCPMC4789676
OpenAlexW2223371805

What OpenQuestion holds

Textmetadata
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.