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作 者:崔娜 史亚军[1] 白敏 王胜正 丁一 CUI Na;SHI Yajun;BAI Min;WANG Shengzheng;DING Yi(School of Pharmacy,Shaanxi University of Traditional Chinese Medicine,Xianyang 712046,China;Department of Pharmacy,First Affiliated Hospital of Air Force Medical University,Xi'an 710032,China;Department of Medicinal Chemistry and Pharmaceutical Analysis,School of Pharmacy,Air Force Medical University,Xi'an 710032,China)
机构地区:[1]陕西中医药大学药学院,陕西咸阳712046 [2]空军军医大学第一附属医院药剂科,西安710032 [3]空军军医大学药学系药物化学与药物分析学教研室,西安710032
出 处:《中国药学杂志》2024年第9期768-775,共8页Chinese Pharmaceutical Journal
基 金:国家自然科学基金项目资助(82274313);陕西省重点研发计划项目资助(2023GHZD43)
摘 要:中枢神经系统(central nervous system,CNS)疾病严重危害人类的生命健康。但由于血脑屏障(blood-brain barrier,BBB)的存在,缺乏将药物输送到大脑的有效技术,这严重影响CNS疾病相关药物的开发成功率,致使治疗效果往往不尽如人意。因此,迫切需要一种新技术解决上述问题。脑靶向肽偶联药物由脑靶向肽、连接基团和有效载荷3部分组成,其利用生物相关的内源性转运机制使生物活性分子透过BBB,并到达脑实质,已成为一种有前景的CNS药物。本文简要介绍了脑靶向肽偶联药物中脑靶向肽、连接基团和有效载荷的种类及特征等,并列举了一些常见的脑靶向肽偶联药物,以及此类药物面临的挑战和改进的方法,以期为后续CNS药物的设计和开发提供新思路。Central nervous system(CNS)diseases are a serious threat to human health.However,due to the existence of blood-brain barrier(BBB),there is a lack of effective technology to deliver drugs to the brain,which seriously affects the success rate of drug development related to CNS diseases,resulting in treatment results that are often unsatisfactory.Therefore,a new technology is urgently needed to solve the above problems.Brain targeted peptide-drug conjugates,which consist of a brain targeted peptide,a linker,and a payload,have become a promising CNS drug by enabling bioactive molecules to cross the BBB and reach the brain parenchyma by using biologically relevant endogenous transport mechanisms.In this review,the types and characteristics of brain targeting peptides,linkers,and payloads are briefly introduced,and some common brain targeting peptide-drug conjugates are listed,as well as the challenges faced by such drugs and the improvement methods,in order to provide ideas for the design and development of drugs for CNS diseases.
关 键 词:多肽偶联药物 脑靶向肽 连接基团 有效载荷 中枢神经系统 血脑屏障
分 类 号:R945[医药卫生—微生物与生化药学]
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