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Lead compound optimization strategy (7)——modification strategies for peptides
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Jing-jing PENG1, 2, Jiang WANG1, 2, Wen-hao DAI1, Xiong XIE1, 2, Hong LIU1, 2, *
Acta Pharmaceutica Sinica | 2020, 55(3) : 427 - 445
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Acta Pharmaceutica Sinica | 2020, 55(3): 427-445
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Lead compound optimization strategy (7)——modification strategies for peptides
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Jing-jing PENG1, 2, Jiang WANG1, 2, Wen-hao DAI1, Xiong XIE1, 2, Hong LIU1, 2, *
Affiliations
  • 1. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
  • 2. University of Chinese Academy of Sciences, Beijing 100049, China
Published: 2020-03-12 doi: 10.16438/j.0513-4870.2019-0877
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Most peptides have high binding affinity and good selectivity for endogenous receptors and are good lead compounds to develop into drugs. Many approved drugs are derived from the structural optimization of peptide molecules, such as the antihypertensive drug captopril and the anti-hepatitis C drug telaprevir. At present, the main problems in the development of peptide drugs include poor stability, short half-life, and high plasma clearance rate; lack of oral availability and poor patient compliance, a complex production process, and high production cost. Therefore, rational modification of peptides can not only reduce the production cost, but also improve the druggability of the peptides. Here we review structural modification strategies for peptides from the perspective of improving their physicochemical properties. These modification strategies are divided into two parts:one is modification of the peptide backbone, including unnatural amino acid modification, pseudopeptide strategy, inverse-peptide strategy, cyclization strategy, and terminal structure modification. Another is modification of the side chains of peptides, including fatty acid conjugation, polyethylene glycol conjugation, protein fusion strategy, and cholesterol conjugation.

peptide  /  structure optimization  /  drug design  /  lead compound
Jing-jing PENG, Jiang WANG, Wen-hao DAI, Xiong XIE, Hong LIU. Lead compound optimization strategy (7)——modification strategies for peptides[J]. Acta Pharmaceutica Sinica, 2020 , 55 (3) : 427 -445 . DOI: 10.16438/j.0513-4870.2019-0877
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Year 2020 volume 55 Issue 3
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Article Info
doi: 10.16438/j.0513-4870.2019-0877
  • Receive Date：2019-11-06
  • Online Date：2026-01-20
  • Published：2020-03-12
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  • Received：2019-11-06
  • Revised：2019-12-04
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Affiliations
    1. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
    2. University of Chinese Academy of Sciences, Beijing 100049, China
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表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
total species (%)		 属
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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