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Research progress in bicyclic peptide-based radiopharmaceuticals
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Xin GAO1, Yuan MIAO1, 2, Si-qi ZHANG1, Dun WANG2, Rui WANG1, *, Kuan HU1, *
Acta Pharmaceutica Sinica | 2025, 60(4) : 864 - 874
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Acta Pharmaceutica Sinica | 2025, 60(4): 864-874
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Research progress in bicyclic peptide-based radiopharmaceuticals
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Xin GAO1, Yuan MIAO1, 2, Si-qi ZHANG1, Dun WANG2, Rui WANG1, *, Kuan HU1, *
Affiliations
  • 1State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
  • 2School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China
Published: 2025-04-12 doi: 10.16438/j.0513-4870.2024-0943
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Radiopharmaceuticals play a crucial role in nuclear medicine, with the development of radioligands being a key focus in this field. Peptide-based radiopharmaceuticals have shown significant advantages in clinical applications, with the majority of FDA-approved targeting radiopharmaceuticals since 2018 being derived from peptides or peptidomimetics. Bicyclic peptides have emerged as a promising targeting moiety in radioligands, offering improved biophysical properties compared to linear or monocyclic peptide ligands. This article provides an overview of the methods for obtaining bicyclic peptide ligands, as well as highlighting the major clinical and preclinical advancements in bicyclic peptide-based radiopharmaceuticals. The review also discusses the future prospects of bicyclic peptide-based radiopharmaceuticals, offering insights for practitioners in the field of pharmaceutical science and nuclear medicine to keep up with the latest developments in radiopharmaceutical innovation.

targeted radiopharmaceutical  /  bicyclic peptide  /  PET imaging  /  high-throughput screening  /  natural peptide
Xin GAO, Yuan MIAO, Si-qi ZHANG, Dun WANG, Rui WANG, Kuan HU. Research progress in bicyclic peptide-based radiopharmaceuticals[J]. Acta Pharmaceutica Sinica, 2025 , 60 (4) : 864 -874 . DOI: 10.16438/j.0513-4870.2024-0943
Year 2025 volume 60 Issue 4
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Article Info
doi: 10.16438/j.0513-4870.2024-0943
  • Receive Date:2024-09-10
  • Online Date:2025-10-29
  • Published:2025-04-12
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  • Received:2024-09-10
  • Revised:2024-12-13
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Affiliations
    1State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
    2School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China
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表12种不同金属材料的力学参数

Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)

Genus
种数
Number of
species
占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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