Design and Synthesis of Novel Helix Mimetics Based on the Covalent H-Bond Replacement and Amide Surrogate

被引:0
|
作者
Liu, Junyang [1 ]
Tang, Shoubin [1 ,2 ]
Yan, Jia-Lei [1 ]
Ye, Tao [2 ,3 ]
机构
[1] Wuyi Univ, Innovat Ctr Marine Biotechnol & Pharmaceut, Sch Biotechnol & Hlth Sci, Jiangmen 529020, Peoples R China
[2] QianYan Shenzhen Pharmatech Ltd, 5th Floor East,Bldg 3,Longcheng Ind Pk, Shenzhen 518172, Peoples R China
[3] Peking Univ, Shenzhen Grad Sch, State Key Lab Chem Oncogen, Shenzhen 518055, Peoples R China
来源
MOLECULES | 2023年 / 28卷 / 02期
关键词
synthesis; helix mimetics; protein-protein interactions; PCNA; PROTEIN-PROTEIN INTERACTIONS; SMALL-MOLECULE INHIBITORS; ALPHA-HELIX; STEREOCHEMICAL ASSIGNMENT; MDM2; P53; MODULATORS; STABILITY; PEPTIDES; STATINE;
D O I
10.3390/molecules28020780
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
A novel hydrogen bond surrogate-based (HBS) alpha-helix mimetic was designed by the combination of covalent H-bond replacement and the use of an ether linkage to substitute an amide bond within a short peptide sequence. The new helix template could be placed in position other than the N-terminus of a short peptide, and the CD studies demonstrate that the template adopts stable conformations in aqueous buffer at exceptionally high temperatures.
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页数:14
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