Innovations in Integrin-Targeted Drug Delivery: From Peptide Conjugates to Dual-Action Therapeutics

Dear Colleagues,

Targeted therapy represents an emerging paradigm in biomedical research today. The selective delivery of drugs to diseased tissues can improve therapeutic efficiency, overcome drug resistance, and minimize off-target effects.

Integrin receptors are an ideal option for targeted delivery because they have extracellular binding domains and they can promote drug internalization. Furthermore, certain integrin receptors have been shown to be upregulated in many disease states.

Therefore, peptides that recognize integrins are ideal for creating covalent conjugates for use as drug delivery systems. Using peptides instead of other compounds (i.e., antibodies) has several advantages, such as easy accessibility through chemical synthesis, increasing the pharmacokinetic properties of the payload drug and reducing the immunogenicity. Additionally, the peptide used as the targeting unit may have biological activity (e.g., as an integrin antagonist), which could have a synergistic effect with the payload drug, making the peptide–drug conjugate a potential dual-action therapeutic.

The Pharmaceuticals journal invites reviews and original articles that shed light on the challenges and opportunities of using integrin-targeted peptide–drug conjugates (PDCs). Topics include the design and chemical synthesis of constructs, new methodologies in conjugation chemistry, and in vivo/in vitro studies of PDCs.

Dr. Kelly Bugatti
Dr. Lucia Battistini
Dr. Andrea Sartori
Guest Editors

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