ArticleThe Journal of clinical investigation1997
A peptidomimetic antagonist of the alpha(v)beta3 integrin inhibits bone resorption in vitro and prevents osteoporosis in vivo.
Article in The Journal of clinical investigation, 1997. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 57 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.
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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.
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Who cites it
57 citing papers in PubMed, 287 citations in OpenAlex.
- Novel bioactive compounds in the treatment of osteoporosis: chemistry-driven discovery from preclinical validation to clinical translation.Frontiers in chemistry · 2026Review
- Orphan Three-Finger Toxins from Snake Venoms: Unexplored Library of Novel Biological Ligands with Potential New Structures and Functions.International journal of molecular sciences · 2025Review
- Targeting strategies for bone diseases: signaling pathways and clinical studies.Signal transduction and targeted therapy · 2023Review
- Roles of focal adhesion proteins in skeleton and diseases.Acta pharmaceutica Sinica. B · 2023Review
- Plasma Membrane Receptors Involved in the Binding and Response of Osteoclasts to Noncellular Components of the Bone.International journal of molecular sciences · 2021Review
- Regulatory properties of vitronectin and its glycosylation in collagen fibril formation and collagen-degrading enzyme cathepsin K activity.Scientific reports · 2021Article
- Mechanistic Insight Into the Roles of Integrins in Osteoarthritis.Frontiers in cell and developmental biology · 2021Review
- Novel Pure αVβ3 Integrin Antagonists That Do Not Induce Receptor Extension, Prime the Receptor, or Enhance Angiogenesis at Low Concentrations.ACS pharmacology & translational science · 2019Article
- Integrins in Osteocyte Biology and Mechanotransduction.Current osteoporosis reports · 2019Review
- Specialized Roles for Actin in Osteoclasts: Unanswered Questions and Therapeutic Opportunities.Biomolecules · 2019Review
- Anemonin Attenuates RANKL-Induced Osteoclastogenesis and Ameliorates LPS-Induced Inflammatory Bone Loss in MiceFrontiers in pharmacology · 2019Article
- The effect of surface immobilized NBD peptide on osteoclastogenesis of rough titanium platesRSC advances · 2018Article
- Macrophage integrins modulate response to ultra-high molecular weight polyethylene particles and direct particle-induced osteolysis.Biomaterials · 2017Article
- A dose escalating phase I study of GLPG0187, a broad spectrum integrin receptor antagonist, in adult patients with progressive high-grade glioma and other advanced solid malignancies.Investigational new drugs · 2016Article
- Proteomic Analysis of Estrogen-Mediated Signal Transduction in Osteoclasts Formation.BioMed research international · 2015Article
- Targeting integrins to promote bone formation and repair.Nature reviews. Endocrinology · 2013Review
- RNA therapeutics targeting osteoclast-mediated excessive bone resorption.Advanced drug delivery reviews · 2012Review
- Anti-RANKL therapy for bone tumours: Basic, pre-clinical and clinical evidences.Journal of bone oncology · 2012Review
- Contribution of bone tissue modulus to breast cancer metastasis to bone.Cancer microenvironment : official journal of the International Cancer Microenvironment Society · 2011Article
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8 authors at 3 institutions in 3 countries.
Funding
Abstract
Osteoclastic bone degradation requires intimacy between the matrix and the resorptive cell. While the precise role the integrin alpha(v)beta3 plays in the process is not yet understood, occupancy of the heterodimer by soluble ligand or by blocking antibody effectively inhibits bone resorption in vitro and in vivo, suggesting that alpha(v)beta3 blockade may prevent postmenopausal osteoporosis. Thus, we identified a synthetic chemical peptide mimetic, beta-[2-[[5-[(aminoiminomethyl)amino]-1-oxopentyl]amino]-1-+ ++oxoethyl]amino-3-pyridinepropanoic acid, bistrifluoroacetate (SC56631) based upon the alpha(v)beta3 ligand, Arg-Gly-Asp (RGD), which recognizes the isolated integrin, and its relative, alpha(v)beta5, as effectively as does the natural peptide. The mimetic dampens osteoclastic bone resorption in vitro and in vivo. Most importantly, intravenous administration of the mimetic prevents the 55% loss of trabecular bone sustained by rats within 6 wk of oophorectomy. Histological examination of bones taken from SC56631-treated, oophorectomized animals also demonstrates the compound's bone sparing properties and its capacity to decrease osteoclast number. Thus, an RGD mimetic prevents the rapid bone loss that accompanies estrogen withdrawal.
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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.