ArticleThe Journal of biological chemistry2006
A small molecule agonist of an integrin, alphaLbeta2.
Article in The Journal of biological chemistry, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
What it found
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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
21 citing papers in PubMed, 37 citations in OpenAlex.
- Conjecturing about Small-Molecule Agonists and Antagonists of α4β1 Integrin: From Mechanistic Insight to Potential Therapeutic Applications.Biomedicines · 2024Review
- Design and Pharmacological Characterization of αJournal of medicinal chemistry · 2023Article
- Heterotropic roles of divalent cations in the establishment of allostery and affinity maturation of integrin αXβ2.Cell reports · 2022Article
- Integrin-Targeting Peptides for the Design of Functional Cell-Responsive Biomaterials.Biomedicines · 2020Review
- High Density Display of an Anti-Angiogenic Peptide on Micelle Surfaces Enhances Their Inhibition of αvβ3 Integrin-Mediated Neovascularization In Vitro.Nanomaterials (Basel, Switzerland) · 2020Article
- Can Integrin Agonists Have Cards to Play against Cancer? A Literature Survey of Small Molecules Integrin Activators.Cancers · 2017Review
- Integrin Cross-Talk Regulates the Human Neutrophil Response to Fungal β-Glucan in the Context of the Extracellular Matrix: A Prominent Role for VLA3 in the Antifungal Response.Journal of immunology (Baltimore, Md. : 1950) · 2017Article
- Structural basis of blocking integrin activation and deactivation for anti-inflammation.Journal of biomedical science · 2015Review
- Identification and X-ray co-crystal structure of a small-molecule activator of LFA-1-ICAM-1 binding.Angewandte Chemie (International ed. in English) · 2014Article
- Sepsis-induced potentiation of peritoneal macrophage migration is mitigated by programmed cell death receptor-1 gene deficiency.Journal of innate immunity · 2014Article
- SHARPIN regulates uropod detachment in migrating lymphocytes.Cell reports · 2013Article
- Novel automated tracking analysis of particles subjected to shear flow: kindlin-3 role in B cells.Biophysical journal · 2013Article
- Small molecule agonist of very late antigen-4 (VLA-4) integrin induces progenitor cell adhesion.The Journal of biological chemistry · 2013Article
- Regulation of integrin affinity on cell surfaces.The EMBO journal · 2011Article
- Small molecule-mediated activation of the integrin CD11b/CD18 reduces inflammatory disease.Science signaling · 2011Article
- Article
- Identification of novel agonists of the integrin CD11b/CD18.Bioorganic & medicinal chemistry letters · 2009Article
- Lymphocyte crawling and transendothelial migration require chemokine triggering of high-affinity LFA-1 integrin.Immunity · 2009Article
- Article
- Aberrant activation of integrin alpha4beta7 suppresses lymphocyte migration to the gut.The Journal of clinical investigation · 2007Article
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
The binding of integrin alpha(L)beta(2) to its ligand intercellular adhesion molecule-1 is required for immune responses and leukocyte trafficking. Small molecule antagonists of alpha(L)beta(2) are under intense investigation as potential anti-inflammatory drugs. We describe for the first time a small molecule integrin agonist. A previously described alpha/beta I allosteric inhibitor, compound 4, functions as an agonist of alpha(L)beta(2) in Ca(2+) and Mg(2+)and as an antagonist in Mn(2+). We have characterized the mechanism of activation and its competitive and noncompetitive inhibition by different compounds. Although it stimulates ligand binding, compound 4 nonetheless inhibits lymphocyte transendothelial migration. Agonism by compound 4 results in accumulation of alpha(L)beta(2) in the uropod, extreme uropod elongation, and defective de-adhesion. Small molecule integrin agonists open up novel therapeutic possibilities.
Indexed as
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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.