肽 - 药物缀合物：新型药物设计方法

Title:Peptide-Drug Conjugate: A Novel Drug Design Approach

Volume: 24 Issue: 31

关键词: 肽 - 药物偶联物（PDC），抗体 - 药物共轭物（ADC），肽，接头，有效载荷，药物设计。

摘要: More than 100 years ago, German physician Paul Ehrlich first proposed the concept of selectively delivering “magic bullets” to tumors through targeting agents. The targeting therapy with antibody-drug conjugates (ADCs) and peptide-drug conjugate (PDCs), which are usually composed of monoclonal antibodies or peptides, toxic payloads and cleavage/ noncleavage linkers, has been extensively studied for decades. The conjugates enable selective delivery of cytotoxic payloads to target cells, which results in improved efficacy, reduced systemic toxicity and improved pharmacokinetics (PK)/pharmacodynamics (PD) compared with traditional chemotherapy. PDC and ADC share similar concept, but with vastly different structures and properties. Humanized antibodies introduce high specificity and prolonged half-life, while small molecule weight peptides exhibit higher drug loading and enhanced tissue penetration capacity, and the flexible linear or cyclic peptides are also modified more easily. In this review, the principles of design, synthesis approaches and the latest advances of PDCs are summarized.

Cite this article as:

Peptide-Drug Conjugate: A Novel Drug Design Approach, Current Medicinal Chemistry 2017; 24 (31) . https://dx.doi.org/10.2174/0929867324666170404142840