Bioactivity and Structure of Analogues of Exendin-4

Chem. J. Chinese Universities

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Bioactivity and Structure of Analogues of Exendin-4

SONG Xiang-Wei¹, WANG Xue-Li², XIONG Xin-Hui¹, NIU Jian-Li¹ , WANG Shi-Qing³, WANG Li-Ping¹*, LI Wei¹

1. College of Life Science, Jilin University,
2. Key Laboratory for Molecular Enzymology and Engineering of the Ministry of Education, Jilin University, Changchun 130021, China;
3. School of Biological and Agricultural Engineering, Jilin University, Changchun 130022, China

Received:2007-12-06 Revised:1900-01-01 Online:2008-06-10 Published:2008-06-10
Contact: WANG Li-Ping

Abstract

Abstract: Exendin-4 is an incretin mimetic that has been studied as a potent drug for the treatment of the type 2 diabetes. To screen the shorter analogues of Exendin-4 that have the same bioactivity, we designed two analogues of Exendin-4: Ex1, deleting this sequence and Ex2, replacing this sequence with three Alas. The proliferation assay of RINm-5F cell using MTT suggested the bioactivity of Ex1 and Ex2 was lower compared to that of Exendin-4 caused by the deletion of LSKQMEEEA. Ex1 and Ex2 had the same strong stability against DPPⅣ with Exendin-4. CD data suggested the helix content of Ex1 had a significant lost, but the helix content of Ex2 was the same as that of Exendin-4. The emission maximum of Ex1 was red-shifted of 3 nm relative to Exendin-4, the absence of this sequence made Trp25 more apt to hydrophilic and the Trp-cage became looser. So we have designed Ex2, the mimetic of Exendin-4 that had the same bioactivity and strong stability against DPPⅣ with Exendin-4 successfully. It became a solid foundation for designing shorter analogues of Exendin-4 for oral drug of diabetes.

Key words: Exendin-4 analogue, Helix structure, Stability, Bioactivity

CLC Number:

O629

TrendMD:

SONG Xiang-Wei¹, WANG Xue-Li², XIONG Xin-Hui¹, NIU Jian-Li¹ , WANG Shi-Qing³, WANG Li-Ping¹*, LI Wei¹. Bioactivity and Structure of Analogues of Exendin-4[J]. Chem. J. Chinese Universities, doi: .

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Bioactivity and Structure of Analogues of Exendin-4

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