文献类型：期刊文献

英文题名：Molecular cloning, tissue distribution, and pharmacological characterization of melanocortin-4 receptor in spotted scat, Scatophagus argus

作者：Li, Jian-Tao[1,2];Yang, Zhao[3];Chen, Hua-Pu[1,2];Zhu, Chun-Hua[1,2];Deng, Si-Ping[1,2];Li, Guang-Li[1,2];Tao, Ya-Xiong[3]

机构：[1]Guangdong Ocean Univ, Coll Fisheries, Zhanjiang 524088, Peoples R China;[2]Guangdong Ocean Univ, Key Lab Aquaculture South China Sea Aquat Econ An, Zhanjiang 524088, Peoples R China;[3]Auburn Univ, Coll Vet Med, Dept Anat Physiol & Pharmacol, Auburn, AL 36849 USA

年份：2016

卷号：230

起止页码：143

外文期刊名：GENERAL AND COMPARATIVE ENDOCRINOLOGY

收录：SCI-EXPANDED(收录号：WOS:000377051200013)、、Scopus(收录号：2-s2.0-84982267587)、WOS

基金：This study was supported by a Foundation Grant from Agricultural Experiment Station of Guangdong Province, Sail Projects of Guangdong Province (2014.1), Marine Fishery Science and Technology Extension Projects of Guangdong Province (A201408A06) (to G-L L). This study was also partially supported by Auburn University Intramural Grant Program and Animal Health and Disease Research Program of College of Veterinary Medicine at Auburn University (to Y.-X. T).

语种：英文

外文关键词：Melanocortin-4 receptor; Tissue distribution; Ligand binding; Signaling; Spotted scat

外文摘要：Melanocortin-4 receptor (MC4R) plays an important role in the regulation of food intake and energy expenditure in mammals. The functions of the MC4R in fish have not been investigated extensively. We herein reported on the cloning, tissue distribution, and pharmacological characterization of spotted scat (Scatophagus argus) MC4R (SAMC4R). It consisted of a 984 bp open reading frame predicted to encode a protein of 327 amino acids. Sequence analysis revealed that SAMC4R was highly homologous (>80%) at amino acid levels to several teleost MC4Rs. Phylogenetic analyses showed that SAMC4R was closely related to piscine MC4R Using RT-PCR, we showed that in addition to brain, pituitary, and gonads, mc4r mRNA was also widely expressed in peripheral tissues of spotted scat in sexually divergent pattern. With human MC4R (hMC4R) as a control, several agonists including a-melanocyte stimulating hormone (alpha-MSH), [Nle(4), D-Phe(7)]-alpha-MSH (NDP-MSH), adrenocorticotropic hormone (ACM) and THIQ (N-[(3R)-1,2,3,4-tetrahydroisoquinolinium3-ylcarbony1]-(1R)-1-(4-chlorobenzyl)-2-[4-cyclohexyl-4-(1H-1,2,4-triazol-1-ylmethyl)piperidin-1-yl]-2-oxoethylamine), were used to investigate the binding and signaling properties of SAMC4R The results showed that SAMC4R bound NDP-MSH with the highest affinity followed by ACTH (1-24) and alpha-MSH. Similar ranking was also found for hMC4R, although SAMC4R had two to five-fold higher affinities for these ligands. THIQ did not displace NDP-MSH from SAMC4R, different from hMC4R. alpha-MSH, NDP-MSH, and ACTH (1-24) were identified as potent agonists to stimulate cAMP generation followed by THIQ in SAMC4R. The availability of SAMC4R and its pharmacological characteristics will facilitate the investigation of its function in regulating diverse physiological processes in spotted scat. (C) 2016 Elsevier Inc. All rights reserved.