ArticleProceedings of the National Academy of Sciences of the United States of America2009
Small-molecule inhibitors of integrin alpha2beta1 that prevent pathological thrombus formation via an allosteric mechanism.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 39 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
39 citing papers in PubMed, 86 citations in OpenAlex.
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- Structural and theoretical study of π-stacking interactions in new complexes based on CuClJournal of molecular modeling · 2023Article
- The effects of inhibition and siRNA knockdown of collagen-binding integrins on human umbilical vein endothelial cell migration and tube formation.Scientific reports · 2022Article
- Perspectives on pediatric congenital aortic valve stenosis: Extracellular matrix proteins, post translational modifications, and proteomic strategies.Frontiers in cardiovascular medicine · 2022Review
- Selectivity of the collagen-binding integrin inhibitors, TC-I-15 and obtustatin.Toxicology and applied pharmacology · 2021Article
- Integrin α2β1 regulates collagen I tethering to modulate hyperresponsiveness in reactive airway disease models.The Journal of clinical investigation · 2021Article
- Hsp47 promotes cancer metastasis by enhancing collagen-dependent cancer cell-platelet interaction.Proceedings of the National Academy of Sciences of the United States of America · 2020Article
- Structure-guided design of pure orthosteric inhibitors of αIIbβ3 that prevent thrombosis but preserve hemostasis.Nature communications · 2020Article
- The Role of Tenascin-C in Tissue Injury and Repair After Stroke.Frontiers in immunology · 2020Review
- Extracellular vesicles of carcinoma-associated fibroblasts creates a pre-metastatic niche in the lung through activating fibroblasts.Molecular cancer · 2019Article
- Proximity proteomics identifies cancer cell membrane cis-molecular complex as a potential cancer target.Cancer science · 2019Article
- Review
- Linking prostate cancer cell AR heterogeneity to distinct castration and enzalutamide responses.Nature communications · 2018Article
- A Nociceptive Role for Integrin Signaling in Pain After Mechanical Injury to the Spinal Facet Capsular Ligament.Annals of biomedical engineering · 2017Article
- ExploringACS medicinal chemistry letters · 2016Article
- αv integrins: key regulators of tissue fibrosis.Cell and tissue research · 2016Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
11 authors at 3 institutions in 2 countries.
Funding
Abstract
There is a grave need for safer antiplatelet therapeutics to prevent heart attack and stroke. Agents targeting the interaction of platelets with the diseased vessel wall could impact vascular disease with minimal effects on normal hemostasis. We targeted integrin alpha(2)beta(1), a collagen receptor, because its overexpression is associated with pathological clot formation whereas its absence does not cause severe bleeding. Structure-activity studies led to highly potent and selective small-molecule inhibitors. Responses of integrin alpha(2)beta(1) mutants to these compounds are consistent with a computational model of their mode of inhibition and shed light on the activation mechanism of I-domain-containing integrins. A potent compound was proven efficacious in an animal model of arterial thrombosis, which demonstrates in vivo efficacy for inhibition of this platelet receptor. These results suggest that targeting integrin alpha(2)beta(1) could be a potentially safe, effective approach to long-term therapy for cardiovascular disease.
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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.