Evidence map›Paper›PMID 34365128›Full record

ArticleEuropean journal of medicinal chemistry2021

Gemfibrozil derivatives as activators of soluble guanylyl cyclase - A structure-activity study.

Kevin M Gayler, Jeremy M Quintana, Jordan Mattke, Michael A Plunk, Jessica H Kostyo, Johann W Karunananthan, Harold Nguyen, Mina Shuda, Liam D Ferreira, Hannah Baker and 4 more

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in European journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
0.5field-weighted citation impact, top 37% 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

1 citing paper in PubMed, 9 citations in OpenAlex.

  1. 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

14 authors at 3 institutions in 1 country.

Kevin M GaylerDepartment of Chemistry and Biochemistry, Institute of Biomedical Studies, Baylor University, Baylor University, Waco, TX, 76798, USA.
Jeremy M QuintanaDepartment of Chemistry and Biochemistry, Institute of Biomedical Studies, Baylor University, Baylor University, Waco, TX, 76798, USA.
Jordan MattkeDepartment of Chemistry and Biochemistry, Institute of Biomedical Studies, Baylor University, Baylor University, Waco, TX, 76798, USA.
Michael A PlunkDepartment of Chemistry and Biochemistry, Institute of Biomedical Studies, Baylor University, Baylor University, Waco, TX, 76798, USA.
Jessica H KostyoDepartment of Chemistry and Biochemistry, Institute of Biomedical Studies, Baylor University, Baylor University, Waco, TX, 76798, USA.
Johann W KarunananthanDepartment of Chemistry and Biochemistry, Institute of Biomedical Studies, Baylor University, Baylor University, Waco, TX, 76798, USA.
Harold NguyenDepartment of Chemistry and Biochemistry, Institute of Biomedical Studies, Baylor University, Baylor University, Waco, TX, 76798, USA.
Mina ShudaDepartment of Chemistry and Biochemistry, Institute of Biomedical Studies, Baylor University, Baylor University, Waco, TX, 76798, USA.
Liam D FerreiraDepartment of Chemistry and Biochemistry, Institute of Biomedical Studies, Baylor University, Baylor University, Waco, TX, 76798, USA.
Hannah BakerDepartment of Chemistry and Biochemistry, Institute of Biomedical Studies, Baylor University, Baylor University, Waco, TX, 76798, USA.
Alexandra L StinchcombDepartment of Chemistry and Biochemistry, Institute of Biomedical Studies, Baylor University, Baylor University, Waco, TX, 76798, USA.
Iraida SharinaDepartment of Internal Medicine, Division of Cardiology, the University of Texas Health Science Center in Houston, McGoven Medical School, 1941 East Road, Houston, TX, 77054, USA.
Robert R KaneDepartment of Chemistry and Biochemistry, Institute of Biomedical Studies, Baylor University, Baylor University, Waco, TX, 76798, USA. Electronic address: Bob_kane@Baylor.edu.
Emil MartinDepartment of Internal Medicine, Division of Cardiology, the University of Texas Health Science Center in Houston, McGoven Medical School, 1941 East Road, Houston, TX, 77054, USA. Electronic address: emil.martin@uth.tmc.edu.
Baylor University · USThe University of Texas Health Science Center · USThe University of Texas Health Science Center at Houston · US

Funding

Regulation of sGC vascular function by the Activator of G-protein Signaling 3R01HL139838 · NHLBI · UNIVERSITY OF TEXAS HLTH SCI CTR HOUSTON · PI MARTIN, EMIL · 2018 to 2021
$1.5M
NHLBI NIH HHS R01 HL139838
6 · The paper itself

Abstract

Previous studies demonstrated that anti-hyperlipidemic drug gemfibrozil acts as NO- and heme-independent activator of NO receptor soluble guanylyl cyclase. A series of new gemfibrozil derivatives were synthesized and evaluated for sGC activation. The structure-activity relationship study identified the positions in gemfibrozil's scaffold that are detrimental for sGC activation and those that are amendable for optimizing modifications. Compared with gemfibrozil, compounds 7c and 15b were more potent activators of cGMP-forming activity of purified sGC and exhibited enhanced relaxation of preconstricted mouse thoracic aorta rings. These studies established the overall framework needed for futher improvement of sGC activators based on gemfibrozil scaffold.

Indexed as

AnimalsGemfibrozilHumansMiceNitric OxideSoluble Guanylyl CyclaseStructure-Activity RelationshipGemfibrozilNitric OxideSoluble Guanylyl CyclaseBiochemistryGemfibrozilMedicinal chemistrySoluble guanylyl cyclase

Identifiers

PMID34365128
PMCPMC8511081
OpenAlexW3188266779

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.