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Article

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

by
Junyang Liu
1,*,†,
Shoubin Tang
1,2,†,
Jia-Lei Yan
1 and
Tao Ye
2,3,*
1
Innovation Center of Marine Biotechnology and Pharmaceuticals, School of Biotechnology and Health Sciences, Wuyi University, Jiangmen 529020, China
2
QianYan (Shenzhen) Pharmatech. Ltd., 5th Floor East, Building-3, Longcheng Industrial Park, Qinglin Roas West, Longgang District, Shenzhen 518172, China
3
State Key Laboratory of Chemical Oncogenomics, Peking University Shenzhen Graduate School, University Town, Xili, Shenzhen 518055, China
*
Authors to whom correspondence should be addressed.
†
These authors contributed equally to this work.
Molecules 2023, 28(2), 780; https://doi.org/10.3390/molecules28020780
Submission received: 17 November 2022 / Revised: 27 December 2022 / Accepted: 10 January 2023 / Published: 12 January 2023
(This article belongs to the Special Issue Small Molecules and Peptides: New Advancing Trends in Molecular Targets and Drug Discovery)
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Abstract

A novel hydrogen bond surrogate-based (HBS) α-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.
Keywords: synthesis; helix mimetics; protein–protein interactions; PCNA synthesis; helix mimetics; protein–protein interactions; PCNA

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MDPI and ACS Style

Liu, J.; Tang, S.; Yan, J.-L.; Ye, T. Design and Synthesis of Novel Helix Mimetics Based on the Covalent H-Bond Replacement and Amide Surrogate. Molecules 2023, 28, 780. https://doi.org/10.3390/molecules28020780

AMA Style

Liu J, Tang S, Yan J-L, Ye T. Design and Synthesis of Novel Helix Mimetics Based on the Covalent H-Bond Replacement and Amide Surrogate. Molecules. 2023; 28(2):780. https://doi.org/10.3390/molecules28020780

Chicago/Turabian Style

Liu, Junyang, Shoubin Tang, Jia-Lei Yan, and Tao Ye. 2023. "Design and Synthesis of Novel Helix Mimetics Based on the Covalent H-Bond Replacement and Amide Surrogate" Molecules 28, no. 2: 780. https://doi.org/10.3390/molecules28020780

APA Style

Liu, J., Tang, S., Yan, J.-L., & Ye, T. (2023). Design and Synthesis of Novel Helix Mimetics Based on the Covalent H-Bond Replacement and Amide Surrogate. Molecules, 28(2), 780. https://doi.org/10.3390/molecules28020780

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