Peptide Conjugates as Therapeutic, Diagnostic and Theranostic Agents

Dear Colleagues,

There is currently a very active revival of interest in the exploitation of peptides as core tools to develop novel drugs, diagnostics, and theranostics for new high value-added products to address unmet medical needs. This emanates from their biocompatibility, enhanced biochemical characteristics with respect to targeted delivery, and ease in rational design and production. In particular, Peptide–Drug Conjugates (PDCs) are arguably an inextricable accessory in our armamentarium against cancer and are continuously gaining attention as a viable approach to selectively target malignant cells. Besides, conjugation of a bioimaging agent, a drug, or of both modalities to a peptide that targets a specific biomarker expressed in a diseased location in a tissue can result in a potent diagnostic, therapeutic, or theranostic agent. This Special Issue will collect recent advances and developments in the field of peptide conjugation to drugs (PDCs), imaging (diagnostic), or dual modalities (theranostics) against cancer and other diseases, including the rational design and novel methodologies for the synthesis (e.g., rapid click chemistry reactions) of novel peptide conjugates. The contributions will also be focused on the impact of the linker in the overall pharmaceutical profile of peptide conjugates, the interactions with the targeted biomarker, the discovery of novel targets, and the possible side-product formation that may occur during such conjugations.

PDCs consist of three building blocks: the tumor-targeting peptide, the cytotoxic drug, and the biodegradable tether (linker). This Special Issue will collect recent advances in the field of peptide–drug conjugation against cancer, mainly including the rational design of novel peptide–drug conjugates and novel methodologies for their synthesis (e.g., the development of rapid click reactions). The contributions will also be focused on the impact of the linker in the overall pharmaceutical profile of PDCs, the receptor binding interactions, the discovery of novel molecular targets, and the possible side-product formation that may occur during such conjugations.

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• peptide–drug conjugates
• peptide-based diagnostics
• peptide-based theranostics
• rational design
• cancer research