Evidence map›Paper›PMID 41576909›Full record

ArticleEuropean journal of medicinal chemistry2026

Discovery of Focal Adhesion Kinase (FAK) activators to promote intestinal mucosal healing.

Ricardo Gallardo-Macias, Qinggang Wang, Ahmed Adham Raafat Elsayed, Guiming Liu, Henry L Wong, Gunda I Georg, Marc D Basson, Vadim J Gurvich

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in European journal of medicinal chemistry, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
–field-weighted citation impact
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

0 citing papers in PubMed.

No citing paper in PubMed yet.

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

8 authors.

Ricardo Gallardo-MaciasInstitute for Therapeutics Discovery and Development and Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, Minneapolis, MN, USA.
Qinggang WangDepartment of Cancer Biology, MD Anderson Cancer Center, Houston, TX, USA.
Ahmed Adham Raafat ElsayedDepartment of Biomedical Sciences, College of Medicine, Northeast Ohio Medical University, Rootstown, OH, USA.
Guiming LiuDepartment of Biomedical Sciences, College of Medicine, Northeast Ohio Medical University, Rootstown, OH, USA.
Henry L WongInstitute for Therapeutics Discovery and Development and Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, Minneapolis, MN, USA.
Gunda I GeorgInstitute for Therapeutics Discovery and Development and Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, Minneapolis, MN, USA.
Marc D BassonDepartment of Biomedical Sciences, College of Medicine, Northeast Ohio Medical University, Rootstown, OH, USA. Electronic address: mbasson@neomed.edu.
Vadim J GurvichInstitute for Therapeutics Discovery and Development and Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, Minneapolis, MN, USA. Electronic address: vadimg@umn.edu.

Funding

University of Minnesota Clinical and Translational Science Institute (UMN CTSI)UL1TR000114 · NCATS · UNIVERSITY OF MINNESOTA · PI BLAZAR, BRUCE R · 2012 to 2015
$35.0M
University of Minnesota Clinical and Translational Science Institute (UMN CTSI)UL1TR002494 · NCATS · UNIVERSITY OF MINNESOTA · PI BLAZAR, BRUCE R, WEISDORF, DANIEL J · 2018 to 2022
$34.9M
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 COMBS, COLIN K · 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
NCATS NIH HHS UL1 TR000114NCATS NIH HHS UL1 TR002494NHLBI NIH HHS U01 HL152410NIGMS NIH HHS P20 GM113123NIGMS NIH HHS U54 GM128729
6 · The paper itself

Abstract

Chronic use of nonsteroidal anti-inflammatory drugs (NSAIDs) causes injuries in the gastrointestinal mucosa. Proton pump inhibitors are the most common drugs prescribed to decrease upper gastrointestinal side effects caused by NSAIDs. However, they worsen the lower GI injuries caused by NSAIDs and do not directly promote restitution of the epithelial mucosa. Focal adhesion kinase (FAK) is essential in wound healing and epithelial sheet migration, making it an attractive pharmacological target. We have designed, synthesized, and evaluated a series of novel, specific FAK activators that increase FAK phosphorylation at Tyr-397 and promote mucosal healing in a Caco-2 model. We found that novel analogs 10bHCl, 10kHCl, and our original lead 5aHCl are preclinical candidates for further studies towards mucosal wound healing. For lead 5aHCl, which had previously shown healing in a mouse model, we performed a pharmacokinetic study. There are currently no therapeutics that promote mucosal healing, and no specific FAK activators beyond our work.

Indexed as

Drug DiscoveryEnzyme ActivatorsFocal Adhesion Kinase 1Focal Adhesion Protein-Tyrosine KinasesIntestinal MucosaWound HealingAnimalsAnti-Inflammatory Agents, Non-SteroidalCaco-2 CellsDose-Response Relationship, DrugHumansMolecular StructurePhosphorylationStructure-Activity RelationshipAnti-Inflammatory Agents, Non-SteroidalEnzyme ActivatorsFocal Adhesion Kinase 1Focal Adhesion Protein-Tyrosine KinasesCaco-2 FAKFocal adhesion kinaseKinase activatorNonsteroidal anti-inflammatory drugsPhosphorylationStructure-activity relationshipWound healing

Identifiers

PMID41576909
PMCPMC12866986

What OpenQuestion holds

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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.