title: Marine Antibody-Drug Conjugates: Design Strategies and Research Progress.
abstract: Antibody-drug conjugates (ADCs), constructed with monoclonal antibodies (mAbs), linkers, and natural cytotoxins, are innovative drugs developed for oncotherapy. Owing to the distinctive advantages of both chemotherapy drugs and antibody drugs, ADCs have obtained enormous success during the past several years. The development of highly specific antibodies, novel marine toxins' applications, and innovative linker technologies all accelerate the rapid R&amp;D of ADCs. Meanwhile, some challenges remain to be solved for future ADCs. For instance, varieties of site-specific conjugation have been proposed for solving the inhomogeneity of DARs (Drug Antibody Ratios). In this review, the usages of various natural toxins, especially marine cytotoxins, and the development strategies for ADCs in the past decade are summarized. Representative ADCs with marine cytotoxins in the pipeline are introduced and characterized with their new features, while perspective comments for future ADCs are proposed.
authors.affiliation: Department of Biochemistry and Molecular Biology, Second Military Medical University, Shanghai 200433, China. wyjcherish@163.com.|Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China. wyjcherish@163.com.
authors.forename: Yu-Jie
authors.initials: YJ
authors.lastname: Wang
authors.affiliation: Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China. yuyanli@cpu.edu.cn.
authors.forename: Yu-Yan
authors.initials: YY
authors.lastname: Li
authors.affiliation: Department of Biochemistry and Molecular Biology, Second Military Medical University, Shanghai 200433, China. biolxy@163.com.
authors.forename: Xiao-Yu
authors.initials: XY
authors.lastname: Liu
authors.affiliation: Department of Biochemistry and Molecular Biology, Second Military Medical University, Shanghai 200433, China. luxiaoling80@126.com.
authors.forename: Xiao-Ling
authors.initials: XL
authors.lastname: Lu
authors.affiliation: Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, China. caoxin@sioc.ac.cn.
authors.forename: Xin
authors.initials: X
authors.lastname: Cao
authors.affiliation: Department of Biochemistry and Molecular Biology, Second Military Medical University, Shanghai 200433, China. bhjiao@smmu.edu.cn.
authors.forename: Bing-Hua
authors.initials: BH
authors.lastname: Jiao
mesh_terms: D000818:Animals; D000911:Antibodies, Monoclonal / Q000737:chemistry* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D003603:Cytotoxins / Q000737:chemistry / Q000494:pharmacology; D055808:Drug Discovery / Q000379:methods; D006801:Humans; D018796:Immunoconjugates / Q000737:chemistry* / Q000494:pharmacology; D009369:Neoplasms / Q000188:drug therapy; D012106:Research
chemical_list: D000911:Antibodies, Monoclonal; D000970:Antineoplastic Agents; D003603:Cytotoxins; D018796:Immunoconjugates
keywords: antibody–drug conjugates; marine toxins; monoclonal antibody; targeted therapy