ArticleThe Journal of biological chemistry2013
Small molecule agonist of very late antigen-4 (VLA-4) integrin induces progenitor cell adhesion.
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. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 29 citations in OpenAlex.
- VLA-4 agonist promotes engraftment and immune reconstitution of allogeneic hematopoietic stem cells.Blood advances · 2026Article
- Liposomal nanoparticles as a drug delivery system for improved treatment of multiple myeloma.RSC advances · 2026Review
- Single-cell profiling of tumor lineage plasticity and the immune microenvironment in transformed small cell lung cancer.Journal of translational medicine · 2026Article
- Analysis of ICAM-1 rs3093030, VCAM-1 rs3783605, and E-Selectin rs1805193 Polymorphisms in African Women Living with HIV and Preeclampsia.International journal of molecular sciences · 2024Article
- 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
- Poly(l-lactic acid) Scaffold Releasing an αACS applied bio materials · 2023Article
- LFA-1 activation enriches tumor-specific T cells in a cold tumor model and synergizes with CTLA-4 blockade.The Journal of clinical investigation · 2022Article
- Peptide Mediated Adhesion to Beta-Lactam Ring of Equine Mesenchymal Stem Cells: A Pilot Study.Animals : an open access journal from MDPI · 2022Article
- New 4-Aminoproline-Based Small Molecule Cyclopeptidomimetics as Potential Modulators of αMolecules (Basel, Switzerland) · 2021Article
- Use of a small molecule integrin activator as a systemically administered vaccine adjuvant in controlling Chagas disease.NPJ vaccines · 2021Article
- AMD3100 and SDF‑1 regulate cellular functions of endothelial progenitor cells and accelerate endothelial regeneration in a rat carotid artery injury model.Molecular medicine reports · 2020Article
- Integrin-Targeting Peptides for the Design of Functional Cell-Responsive Biomaterials.Biomedicines · 2020Review
- Targeted melanoma radiotherapy using ultrasmallBiomaterials · 2020Article
- Novel Ligands Targeting αFrontiers in chemistry · 2019Review
- Article
- Overexpression of VLA-4 in glial-restricted precursors enhances their endothelial docking and induces diapedesis in a mouse stroke model.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2018Article
- Can Integrin Agonists Have Cards to Play against Cancer? A Literature Survey of Small Molecules Integrin Activators.Cancers · 2017Review
- Integrins and integrin-associated proteins in the cardiac myocyte.Circulation research · 2014Review
- Role of integrin alpha4 in drug resistance of leukemia.Frontiers in oncology · 2014Review
Corrections and comments
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Authors and funding
13 authors at 2 institutions in 1 country.
Funding
Abstract
Activation of the integrin family of cell adhesion receptors on progenitor cells may be a viable approach to enhance the effects of stem cell-based therapies by improving cell retention and engraftment. Here, we describe the synthesis and characterization of the first small molecule agonist identified for the integrin α4β1 (also known as very late antigen-4 or VLA-4). The agonist, THI0019, was generated via two structural modifications to a previously identified α4β1 antagonist. THI0019 greatly enhanced the adhesion of cultured cell lines and primary progenitor cells to α4β1 ligands VCAM-1 and CS1 under both static and flow conditions. Furthermore, THI0019 facilitated the rolling and spreading of cells on VCAM-1 and the migration of cells toward SDF-1α. Molecular modeling predicted that the compound binds at the α/β subunit interface overlapping the ligand-binding site thus indicating that the compound must be displaced upon ligand binding. In support of this model, an analog of THI0019 modified to contain a photoreactive group was used to demonstrate that when cross-linked to the integrin, the compound behaves as an antagonist instead of an agonist. In addition, THI0019 showed cross-reactivity with the related integrin α4β7 as well as α5β1 and αLβ2. When cross-linked to αLβ2, the photoreactive analog of THI0019 remained an agonist, consistent with it binding at the α/β subunit interface and not at the ligand-binding site in the inserted ("I") domain of the αL subunit. Co-administering progenitor cells with a compound such as THI0019 may provide a mechanism for enhancing stem cell therapy.
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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.