Ring size in cyclic endomorphin-2 analogs modulates receptor binding affinity and selectivity

Author:

Piekielna Justyna12345,Kluczyk Alicja6785,Gentilucci Luca9101112,Cerlesi Maria Camilla1314151617,Calo’ Girolamo1314151617,Tomböly Csaba18192021,Łapiński Krzysztof22235,Janecki Tomasz2425265,Janecka Anna12345

Affiliation:

1. Department of Biomolecular Chemistry

2. Faculty of Medicine

3. Medical University of Lodz

4. Lodz

5. Poland

6. Faculty of Chemistry

7. University of Wroclaw

8. Wroclaw

9. Department of Chemistry ‘G. Ciamician’

10. University of Bologna

11. 40126 Bologna

12. Italy

13. Department of Medical Science

14. Section of Pharmacology

15. and National Institute of Neuroscience

16. University of Ferrara

17. 44121 Ferrara

18. Institute of Biochemistry

19. Biological Research Centre of Hungarian Academy of Sciences

20. Szeged

21. Hungary

22. TriMen Chemicals Ltd

23. 92-318 Lodz

24. Institute of Organic Chemistry

25. Lodz University of Technology

26. 90-924 Lodz

Abstract

A series of endomorphin-2 cyclic analogs with 17- to 14-membered rings was synthesized and evaluated in terms of opioid affinity and selectivity. Conformational studies enabled us to rationalize biological results.

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Physical and Theoretical Chemistry,Biochemistry

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