ArticleExperimental & molecular medicine2016
Small molecules that allosterically inhibit p21-activated kinase activity by binding to the regulatory p21-binding domain.
Article in Experimental & molecular medicine, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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.
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.
Who cites it
18 citing papers in PubMed.
- Endothelial β-PIX (ARHGEF7) supports actomyosin mediated expulsion of VWF through dynamic reorganization of the cytoskeleton.Molecular biology of the cell · 2026Article
- Regulation of Vascular Injury and Repair by P21-Activated Kinase 1 and P21-Activated Kinase 2: Therapeutic Potential and Challenges.Biomolecules · 2024Review
- Review
- Review
- PAK1 Is Involved in the Spindle Assembly during the First Meiotic Division in Porcine Oocytes.International journal of molecular sciences · 2023Article
- Development and Utility of a PAK1-Selective Degrader.Journal of medicinal chemistry · 2022Article
- Naphthoquinone as a New Chemical Scaffold for Leishmanicidal Inhibitors ofBiomedicines · 2022Article
- p21-Activated kinases as promising therapeutic targets in hematological malignancies.Leukemia · 2022Review
- Cdc42/Rac Interactive Binding Containing Effector Proteins in Unicellular Protozoans With Reference to Human Host: Locks of the Rho Signaling.Frontiers in genetics · 2022Review
- Liposomes Targeting P21 Activated Kinase-1 (PAK-1) and Selective for Secretory Phospholipase AInternational journal of molecular sciences · 2020Article
- Identification of a novel PAK1 inhibitor to treat pancreatic cancer.Acta pharmaceutica Sinica. B · 2020Article
- Effect of PAK Inhibition on Cell Mechanics Depends on Rac1.Frontiers in cell and developmental biology · 2020Article
- P21-Activated Kinase 1: Emerging biological functions and potential therapeutic targets in Cancer.Theranostics · 2020Review
- Modulation of store-operated calcium entry and nascent adhesion by p21-activated kinase 1.Experimental & molecular medicine · 2018Article
- Computer-aided drug design, synthesis and identification of disulfide compounds as novel and potential allosteric PAK1 inhibitors.RSC advances · 2018Article
- Article
- Targeting PAK1.Biochemical Society transactions · 2017Review
- p21-Activated Kinase 4 Promotes Intimal Hyperplasia and Vascular Smooth Muscle Cells Proliferation during Superficial Femoral Artery Restenosis after Angioplasty.BioMed research international · 2017Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
12 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
p21-activated kinases (PAKs) are key regulators of actin dynamics, cell proliferation and cell survival. Deregulation of PAK activity contributes to the pathogenesis of various human diseases, including cancer and neurological disorders. Using an ELISA-based screening protocol, we identified naphtho(hydro)quinone-based small molecules that allosterically inhibit PAK activity. These molecules interfere with the interactions between the p21-binding domain (PBD) of PAK1 and Rho GTPases by binding to the PBD. Importantly, they inhibit the activity of full-length PAKs and are selective for PAK1 and PAK3 in vitro and in living cells. These compounds may potentially be useful for determining the details of the PAK signaling pathway and may also be used as lead molecules in the development of more selective and potent PAK inhibitors.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
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.