ArticleThe Journal of biological chemistry2013
Characterization of a Cdc42 protein inhibitor and its use as a molecular probe.
Article in The Journal of biological chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 104 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
104 citing papers in PubMed, 169 citations in OpenAlex.
- A Novel Pharmacologic Activity of Ketorolac for Therapeutic Benefit in Ovarian Cancer Patients.Clinical cancer research : an official journal of the American Association for Cancer Research · 2015Trial
- Functional Specialization of Clathrin-Independent Endocytic Routes: Mechanisms and Cellular Roles.Traffic (Copenhagen, Denmark) · 2026Review
- Heterogeneity in the coordination of delta cells with beta cells is driven by both paracrine signals and low-density Cx36 gap junctions.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- Migrating immune cells globally coordinate protrusive forces.Nature immunology · 2025Article
- Transendothelial migration of the Lyme disease spirochete involves spirochete internalization as an intermediate step through a transcellular pathway that involves Cdc42 and Rac1.Microbiology spectrum · 2025Article
- Structural Dynamics of Rho GTPases.Journal of molecular biology · 2025Review
- Galactin-3 regulation of CDC42 promotes neuronal autophagy following spinal cord injury.Frontiers in cellular neuroscience · 2025Article
- Alveolar macrophage function is impaired following inhalation of berry e-cigarette vapor.Proceedings of the National Academy of Sciences of the United States of America · 2024Article
- Targeting TNF/IL-17/MAPK pathway in hHaematologica · 2024Article
- Targeting F-actin stress fibers to suppress the dedifferentiated phenotype in chondrocytes.European journal of cell biology · 2024Article
- Small GTPases control macropinocytosis of amyloid precursor protein and cleavage to amyloid-β.Heliyon · 2024Article
- A Recipe for Successful Metastasis: Transition and Migratory Modes of Ovarian Cancer Cells.Cancers · 2024Review
- Target-based drug discovery: Applications of fluorescence techniques in high throughput and fragment-based screening.Heliyon · 2024Review
- MRCK activates mouse oocyte myosin II for spindle rotation and male pronucleus centration.The Journal of cell biology · 2023Article
- mTORC2-NDRG1-CDC42 axis couples fasting to mitochondrial fission.Nature cell biology · 2023Article
- Molecular dynamics simulations reveal the inhibition mechanism of Cdc42 by RhoGDI1.Journal of computer-aided molecular design · 2023Article
- Increased cross-presentation by dendritic cells and enhanced anti-tumour therapy using the Arp2/3 inhibitor CK666.British journal of cancer · 2023Article
- Crosstalk between CD4American journal of respiratory and critical care medicine · 2023Article
- Rho GTPase Signaling in Platelet Regulation and Implication for Antiplatelet Therapies.International journal of molecular sciences · 2023Review
- Review
44 more citing papers are in PubMed but not listed here.
Corrections and comments
- Erratum issued
Authors and funding
21 authors at 3 institutions in 1 country.
Funding
Abstract
Cdc42 plays important roles in cytoskeleton organization, cell cycle progression, signal transduction, and vesicle trafficking. Overactive Cdc42 has been implicated in the pathology of cancers, immune diseases, and neuronal disorders. Therefore, Cdc42 inhibitors would be useful in probing molecular pathways and could have therapeutic potential. Previous inhibitors have lacked selectivity and trended toward toxicity. We report here the characterization of a Cdc42-selective guanine nucleotide binding lead inhibitor that was identified by high throughput screening. A second active analog was identified via structure-activity relationship studies. The compounds demonstrated excellent selectivity with no inhibition toward Rho and Rac in the same GTPase family. Biochemical characterization showed that the compounds act as noncompetitive allosteric inhibitors. When tested in cellular assays, the lead compound inhibited Cdc42-related filopodia formation and cell migration. The lead compound was also used to clarify the involvement of Cdc42 in the Sin Nombre virus internalization and the signaling pathway of integrin VLA-4. Together, these data present the characterization of a novel Cdc42-selective allosteric inhibitor and a related analog, the use of which will facilitate drug development targeting Cdc42-related diseases and molecular pathway studies that involve GTPases.
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.