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Active conformation of an insect neuropeptide family.

作者信息

Nachman R J, Roberts V A, Dyson H J, Holman G M, Tainer J A

机构信息

Veterinary Toxicology and Entomology Research Laboratory, U.S. Department of Agriculture, College Station, TX 77840.

出版信息

Proc Natl Acad Sci U S A. 1991 May 15;88(10):4518-22. doi: 10.1073/pnas.88.10.4518.

DOI:10.1073/pnas.88.10.4518
PMID:2034692
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC51692/
Abstract

To understand the structural and chemical basis for insect neuropeptide activity, we have designed, synthesized, and determined the conformation of a biologically active cyclic analog of the pyrokinins, an insect neuropeptide family that mediates myotropic (visceral muscle contractile) activity. Members of this insect neuropeptide family share the common C-terminal pentapeptide sequence Phe-Xaa-Pro-Arg-Leu-NH2 (Xaa = Ser, Thr, or Val). Circular dichroic, nuclear magnetic resonance, and molecular dynamics analyses of the conformationally restricted cyclic pyrokinin analog cyclo(-Asn-Thr-Ser-Phe-Thr-Pro-Arg-Leu-) indicated the presence of a beta-turn in the active core region encompassing residues Thr-Pro-Arg-Leu. The rigid cyclic analog retains biological activity, suggesting that its C-terminal beta-turn is the active pyrokinin conformation recognized by the myotropic receptor. As individual pyrokinins and pyrokinin-like neuropeptides demonstrate both oviduct-contractile and pheromone-biosynthesis activities in various insects, the biologically active beta-turn structure reported here holds broad significance for many biological processes.

摘要
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67de/51692/a0c0b77d4203/pnas01060-0471-b.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67de/51692/39f06d178b58/pnas01060-0470-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67de/51692/298219829acd/pnas01060-0471-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67de/51692/a0c0b77d4203/pnas01060-0471-b.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67de/51692/39f06d178b58/pnas01060-0470-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67de/51692/298219829acd/pnas01060-0471-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/67de/51692/a0c0b77d4203/pnas01060-0471-b.jpg

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本文引用的文献

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