Peptide-Drug Conjugate: A Novel Drug Design Approach

Author(s): Liang Ma, Chao Wang, Zihao He, Biao Cheng, Ling Zheng, Kun Huang*

Journal Name: Current Medicinal Chemistry

Volume 24 , Issue 31 , 2017

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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.

Keywords: Peptide-drug conjugates (PDCs), antibody-drug conjugates (ADCs), peptide, linker, payloads, drug design.

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Article Details

Year: 2017
Page: [3373 - 3396]
Pages: 24
DOI: 10.2174/0929867324666170404142840
Price: $65

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