摘要
A single peptide–drug conjugate molecule achieves multiple biological functions, which is proposed as a novel drug delivery system, the molecular drug delivery system. Recently, peptide–drug conjugates have been introduced as potential diagnostics and anticancer drugs in the clinic. Aminopeptidase N, integrins, the somatostatin receptor, and several other receptors are major molecular targeting receptors for current peptide–drug conjugate-based molecular drug delivery systems. Solving the problem of oral administration will greatly promote the development of peptide–drug conjugate 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. 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. a chemotherapy medication used to treat chronic lymphocytic leukemia (CLL), Hodgkin lymphoma, and non-Hodgkin lymphoma. the rate of application of a dose, which means quantity (in units of energy/mass) in the fields of nutrition, and medicine, although in common and imprecise usage the words are sometimes used synonymously. formulation technologies for transporting active pharmaceutical ingredients in the body as needed to safely achieve the desired therapeutic or diagnostic effects. engineered technologies that use nanoscale particles for the targeted delivery and controlled release of active pharmaceutical ingredients. gives companies researching cures for rare diseases a 7-year window of tax reductions and the exclusive right to develop a cure for a specific condition. active pharmaceutical ingredients, which can be effectively used for diagnosis/treatment in patients. a small, protein-like chain designed to mimic a peptide. tomography in which a computer-generated image of a biological activity in the body is produced through the detection of gamma-rays that are emitted when introduced radionuclides decay and release positrons. a peptide hormone that regulates the endocrine system and affects neurotransmission and cell proliferation via interaction with G protein-coupled somatostatin receptors and inhibition of the release of numerous secondary hormones. a short peptide, typically in an α-helical conformation, that is constrained by a synthetic brace as a staple.