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Peptide-drug conjugate-based novel molecular drug delivery system in cancer

期刊

TRENDS IN PHARMACOLOGICAL SCIENCES
卷 42, 期 10, 页码 857-869

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CELL PRESS
DOI: 10.1016/j.tips.2021.07.001

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  1. Key Project of Social Development of Jiangsu Province [BE2019736]

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Peptide-drug conjugates act as integrated drug delivery systems, targeting tumor cells through tumor-targeting peptides and connecting with payloads for therapeutic effects. Exploration of clinical work on these conjugates reveals binding mechanisms and limitations in molecular drug delivery systems.
Drug delivery systems are generally believed to comprise drugs and excipients. A peptide-drug conjugate is a single molecule that can simultaneously play multiple roles in a drug delivery system, such as in vivo drug distribution, targeted release, and bioactivity functions. This molecule can be regarded as an integrated drug delivery system, so it is called a molecular drug delivery system. In the context of cancer therapy, a peptide-drug conjugate comprises a tumor-targeting peptide, a payload, and a linker. Tumor-targeting peptides specifically identify membrane receptors on tumor cells, improve drug-targeted therapeutic effects, and reduce toxic and side effects. Payloads with bioactive functions connect to tumor-targeting peptides through linkers. In this review, we explored ongoing clinical work on peptide-drug conjugates targeting various receptors. We discuss the binding mechanisms of tumor-targeting peptides and related receptors, as well as the limiting factors for peptide-drug conjugate-based molecular drug delivery systems.

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