Molecular and functional characterization of adipokinetic hormone receptor and its peptide ligands in Bombyx mori

Zhu, Chenggang; Huang, Haishan; Hua, Rongsheng; Li, Guo; Yang, Dong; Luo, Jiansong; Zhang, Cunxin; Shi, Liangen; Benovic, Jeffrey L.; Zhou, Naiming

doi:10.1016/j.febslet.2009.03.060

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Volume 583, Issue 9 , Pages 1463-1468, 6 May 2009

Molecular and functional characterization of adipokinetic hormone receptor and its peptide ligands in Bombyx mori

Edited by Jesus Avila

Chenggang Zhu
- Institute of Biochemistry, College of Life Sciences, Zijingang Campus, Zhejiang University, Hangzhou, Zhejiang 310058, China
- Both authors contributed equally to this work.
Haishan Huang
- Institute of Biochemistry, College of Life Sciences, Zijingang Campus, Zhejiang University, Hangzhou, Zhejiang 310058, China
- Both authors contributed equally to this work.
Rongsheng Hua
- College of Animal Sciences, Huajia Pond Campus, Zhejiang University, Hangzhou, Zhejiang 310029, China
Guo Li
- Institute of Biochemistry, College of Life Sciences, Zijingang Campus, Zhejiang University, Hangzhou, Zhejiang 310058, China
Dong Yang
- Institute of Biochemistry, College of Life Sciences, Zijingang Campus, Zhejiang University, Hangzhou, Zhejiang 310058, China
Jiansong Luo
- Department of Biochemistry, Kimmel Cancer Center, Thomas Jefferson University, Philadelphia, PA 19107, USA
Cunxin Zhang
- Institute of Biochemistry, College of Life Sciences, Zijingang Campus, Zhejiang University, Hangzhou, Zhejiang 310058, China
Liangen Shi
- College of Animal Sciences, Huajia Pond Campus, Zhejiang University, Hangzhou, Zhejiang 310029, China
Jeffrey L. Benovic
- Department of Biochemistry, Kimmel Cancer Center, Thomas Jefferson University, Philadelphia, PA 19107, USA
Naiming Zhou
- Institute of Biochemistry, College of Life Sciences, Zijingang Campus, Zhejiang University, Hangzhou, Zhejiang 310058, China
- Corresponding author. Fax: +86 0571 88206134x8000.

Received 20 February 2009; received in revised form 25 March 2009; accepted 26 March 2009. published online 02 April 2009.

Abstract

Neuropeptides of the adipokinetic hormone (AKH) family are among the best studied hormone peptides, but its signaling pathways remain to be elucidated. In this study, we molecularly characterized the signaling of Bombyx AKH receptor (AKHR) and its peptide ligands in HEK293 cells. In HEK293 cells stably expressing AKHR, AKH1 stimulation not only led to a ligand concentration dependent mobilization of intracellular Ca²⁺ and cAMP accumulation, but also elicited transient activation of extracellular signal-regulated kinase 1/2 (ERK1/2) pathway. We observed that AKH receptor was rapidly internalized after AKH1 stimulation. We further demonstrated that AKH2 exhibited high activities in cAMP accumulation and ERK1/2 activation on AKHR comparable to AKH1, whereas AKH3 was much less effective.

Abbreviations: GPCR, G protein-coupled receptor, AKH, adipokinetic hormone, Hez-HrTH, Heliothis zea hypertrehalosaemic hormone, MAPK, mitogen-activated protein kinase, ERK1/2, extracellular signal-regulated kinase1/2, PTX, pertussis toxin, CTX, cholera toxin