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Research Progress in Brain Targeting Peptide-Drug Conjugates
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Na CUI1, 2, Yajun SHI1, *, Min BAI1, 2, Shengzheng WANG3, Yi DING2, *
Chinese Pharmaceutical Journal | 2024, 59(9) : 768 - 775
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Chinese Pharmaceutical Journal | 2024, 59(9): 768-775
Research Progress in Brain Targeting Peptide-Drug Conjugates
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Na CUI1, 2, Yajun SHI1, *, Min BAI1, 2, Shengzheng WANG3, Yi DING2, *
Affiliations
  • 1 School of Pharmacy, Shaanxi University of Traditional Chinese Medicine, Xianyang 712046, China
  • 2 Department of Pharmacy, First Affiliated Hospital of Air Force Medical University, Xi'an 710032, China
  • 3 Department of Medicinal Chemistry and Pharmaceutical Analysis, School of Pharmacy, Air Force Medical University, Xi'an 710032, China
Published: 2024-05-08 doi: 10.11669/cpj.2024.09.002
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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.

peptide-drug conjugate  /  brain targeting peptide  /  linker  /  payload  /  central nervous system  /  blood-brain barrier
Na CUI, Yajun SHI, Min BAI, Shengzheng WANG, Yi DING. Research Progress in Brain Targeting Peptide-Drug Conjugates[J]. Chinese Pharmaceutical Journal, 2024 , 59 (9) : 768 -775 . DOI: 10.11669/cpj.2024.09.002
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Article Info
doi: 10.11669/cpj.2024.09.002
  • Receive Date：2023-02-28
  • Online Date：2025-11-25
  • Published：2024-05-08
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  • Received：2023-02-28
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Affiliations
    1 School of Pharmacy, Shaanxi University of Traditional Chinese Medicine, Xianyang 712046, China
    2 Department of Pharmacy, First Affiliated Hospital of Air Force Medical University, Xi'an 710032, China
    3 Department of Medicinal Chemistry and Pharmaceutical Analysis, School of Pharmacy, Air Force Medical University, Xi'an 710032, China
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https://castjournals.cast.org.cn/joweb/zgyxzz/EN/10.11669/cpj.2024.09.002
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