Evidence map›Paper›PMID 36632414›Full record

ArticleCurrent research in pharmacology and drug discovery2023

A novel drug-like water-soluble small molecule Focal Adhesion Kinase (FAK) activator promotes intestinal mucosal healing.

Qinggang Wang, Ricardo Gallardo-Macias, Emilie E Vomhof-DeKrey, Rashmi Gupta, Svetlana A Golovko, Mikhail Y Golovko, Sema Oncel, Vadim J Gurvich, Marc D Basson

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

Article in Current research in pharmacology and drug discovery, 2023. 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 27% 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, 8 citations in OpenAlex.

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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 3 institutions in 1 country.

Qinggang WangDepartment of Surgery, University of North Dakota School of Medicine and Health Sciences, USA.
Ricardo Gallardo-MaciasInstitute for Therapeutics Discovery and Development and Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, USA.
Emilie E Vomhof-DeKreyDepartment of Surgery, University of North Dakota School of Medicine and Health Sciences, USA.
Rashmi GuptaCurrently at Department of Biology, University of Maryland, USA.
Svetlana A GolovkoDepartment of Biomedical Sciences, University of North Dakota School of Medicine and Health Sciences, USA.
Mikhail Y GolovkoDepartment of Biomedical Sciences, University of North Dakota School of Medicine and Health Sciences, USA.
Sema OncelDepartment of Biomedical Sciences, University of North Dakota School of Medicine and Health Sciences, USA.
Vadim J GurvichInstitute for Therapeutics Discovery and Development and Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, USA.
Marc D BassonDepartments of Surgery, Biomedical Sciences, and Pathology, University of North Dakota School of Medicine and Health Sciences, USA.
University of North Dakota · USUniversity of Minnesota · USUniversity of Maryland, College Park · US

Funding

Tracking and Evaluation CoreU54GM128729 · NIGMS · UNIVERSITY OF NORTH DAKOTA · PI BASSON, MARC D. · 2018 to 2022
$20.3M
Yersina perstis interactions with macrophagesP20GM113123 · NIGMS · UNIVERSITY OF NORTH DAKOTA · PI BRADLEY, DAVID S. · 2016 to 2025
$19.9M
Midwest Biomedical Accelerator Consortium: MBArCU01HL152410 · NHLBI · UNIVERSITY OF MISSOURI-COLUMBIA · PI FAY, WILLIAM P, GRANT, SHEILA ANN · 2019 to 2023
$5.6M
NHLBI NIH HHS U01 HL152410NIGMS NIH HHS P20 GM113123NIGMS NIH HHS U54 GM128729
6 · The paper itself

Abstract

Non-steroidal anti-inflammatory drugs (NSAIDs) injure the proximal and distal gut by different mechanisms. While many drugs reduce gastrointestinal injury, no drug directly stimulates mucosal wound healing. Focal adhesion kinase (FAK), a non-receptor tyrosine kinase, induces epithelial sheet migration. We synthesized and evaluated a water-soluble FAK-activating small molecule, M64HCl, with drug-like properties. Monolayer wound closure and Western blots measured migration and FAK phosphorylation in Caco-2 ​cells, in vitro kinase assays established FAK activation, and pharmacologic tests assessed drug-like properties. 30 ​mg/kg/day M64HCl was administered in two murine small intestine injury models for 4 days. M64HCl (0.1-1000 ​nM) dose-dependently increased Caco-2 FAK-Tyr 397 phosphorylation, without activating Pyk2 and accelerated Caco-2 monolayer wound closure. M64HCl dose-responsively activates the FAK kinase domain vs. the non-salt M64, increasing the V

Indexed as

Focal adhesion kinaseMucosal healingNon-steroidal anti-inflammatory drugsSmall intestineUlcer

Identifiers

PMID36632414
PMCPMC9827036
OpenAlexW4313570078

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC-ND
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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.