Integrin-Targeting Strategies in Allergic Inflammation
Summary
Integrin‐targeting approaches aim to modulate the migration and activation of immune cells that drive allergic inflammation. Central to these efforts are integrins such as α4β1 (very late antigen-4) and β2 family members (including lymphocyte function-associated antigen-1), which orchestrate the cascade of leukocyte rolling, adhesion and extravasation at sites of allergic insult. Strategies have evolved from early RGD- and LDV-based peptides to novel peptidomimetics and cyclopeptides engineered for enhanced stability and affinity, as well as small molecules designed to bind orthosteric or allosteric sites. These ligands may function as antagonists, preventing integrin activation, or as agonists, stabilising inactive conformers and inhibiting leukocyte release. Integration of computational docking, molecular dynamics and structural analysis has refined our understanding of ligand–receptor interactions, guiding the rational design of compounds with improved specificity. Parallel developments in drug delivery—such as nanoparticle conjugation and smart biomaterials—are advancing targeted therapeutic and diagnostic applications. Collectively, these integrin-targeting modalities hold promise for precise control of immune cell trafficking in asthma, atopic dermatitis and other allergic pathologies.
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Integrin-Targeting Strategies in Allergic Inflammation publication trend
The graph below shows the total number of articles in integrin-targeting strategies in allergic inflammation across all publications each year (not limited to Nature Index journals).
Technical terms
Integrin: Heterodimeric transmembrane receptor that mediates cell adhesion and bidirectional signalling.
α4β1 integrin: Leukocyte integrin (very late antigen-4) critical for firm adhesion during immune cell extravasation.
Peptidomimetic: Synthetic molecule designed to mimic the structure and function of a peptide ligand.
Cyclopeptide: Cyclic peptide structure with enhanced conformational stability used to regulate receptor activity.
Allosteric site: Distinct receptor region where ligand binding induces conformational changes without occupying the primary site.
Extravasation: Process by which leukocytes migrate from the bloodstream into surrounding tissues at sites of inflammation.
References
- Design, Pharmacological Characterization, and Molecular Docking of Minimalist Peptidomimetic Antagonists of α4β1 Integrin. International Journal of Molecular Sciences (2023).
- Design and Pharmacological Characterization of α4β1 Integrin Cyclopeptide Agonists: Computational Investigation of Ligand Determinants for Agonism versus Antagonism. Journal of Medicinal Chemistry (2023).
- Analysis of α4 β1integrin specific antagonists binding modes: structural insights by molecular docking, molecular dynamics and linear interaction energy method for free energy calculations. Journal of the Brazilian Chemical Society (2010).
- Integrin-Targeting Peptides for the Design of Functional Cell-Responsive Biomaterials. Biomedicines (2020).
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