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Unacylated ghrelin is active on the INS-1E rat insulinoma cell line independently of the growth hormone secretagogue receptor type 1a and the corticotropin releasing factor 2 receptor.
Mol Cell Endocrinol. 2006 Jun 07; 251(1-2):103-11.MC

Abstract

Both unacylated ghrelin (UAG) and acylated ghrelin (AG) exert metabolic effects. To investigate the interactions between AG and UAG on ghrelin receptors we evaluated the effects of AG and UAG on INS-1E rat insulinoma cells, using insulin secretion after 30min static incubation as a read-out. A possible involvement of the growth hormone secretagogue receptor type 1a (GHS-R1a) or the corticotropin-releasing factor 2 (CRF2) receptor (CRF2R), as a putative receptor for UAG, was also studied determining their mRNA expression and the functional effects of receptor antagonists on insulin release. Both UAG and AG stimulated insulin release dose-dependently in the nanomolar range. The AG-induced insulin output was antagonized by two GHS-R1a antagonists ([d-Lys(3)]GHRP-6 and BIM28163), which did not block UAG actions. These effects occurred in the presence of low levels of GHS-R1a mRNA. Neither CRF2R expression nor effects of the CRF2R antagonist (astressin(2)B) on insulin output were observed. In conclusion, we provide a sensitive and reproducible assay for specific effects of UAG, which in this study is responsible for insulin release by INS-1E cells. Our data support the existence of a specific receptor for UAG, other than the CRF2R and GHS-R1a. The stimulatory effect on insulin secretion by AG in this cell line is mediated by the GHS-R1a.

Authors+Show Affiliations

Division of Endocrinology, Department of Internal Medicine, Erasmus MC, Dr Molewaterplein 50, 3015 GE, Rotterdam, The Netherlands. c.gauna@erasmusmc.nlNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

16647196

Citation

Gauna, Carlotta, et al. "Unacylated Ghrelin Is Active On the INS-1E Rat Insulinoma Cell Line Independently of the Growth Hormone Secretagogue Receptor Type 1a and the Corticotropin Releasing Factor 2 Receptor." Molecular and Cellular Endocrinology, vol. 251, no. 1-2, 2006, pp. 103-11.
Gauna C, Delhanty PJ, van Aken MO, et al. Unacylated ghrelin is active on the INS-1E rat insulinoma cell line independently of the growth hormone secretagogue receptor type 1a and the corticotropin releasing factor 2 receptor. Mol Cell Endocrinol. 2006;251(1-2):103-11.
Gauna, C., Delhanty, P. J., van Aken, M. O., Janssen, J. A., Themmen, A. P., Hofland, L. J., Culler, M., Broglio, F., Ghigo, E., & van der Lely, A. J. (2006). Unacylated ghrelin is active on the INS-1E rat insulinoma cell line independently of the growth hormone secretagogue receptor type 1a and the corticotropin releasing factor 2 receptor. Molecular and Cellular Endocrinology, 251(1-2), 103-11.
Gauna C, et al. Unacylated Ghrelin Is Active On the INS-1E Rat Insulinoma Cell Line Independently of the Growth Hormone Secretagogue Receptor Type 1a and the Corticotropin Releasing Factor 2 Receptor. Mol Cell Endocrinol. 2006 Jun 7;251(1-2):103-11. PubMed PMID: 16647196.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Unacylated ghrelin is active on the INS-1E rat insulinoma cell line independently of the growth hormone secretagogue receptor type 1a and the corticotropin releasing factor 2 receptor. AU - Gauna,Carlotta, AU - Delhanty,Patric J D, AU - van Aken,Maarten O, AU - Janssen,Joop A M J L, AU - Themmen,Axel P N, AU - Hofland,Leo J, AU - Culler,Michael, AU - Broglio,Fabio, AU - Ghigo,Ezio, AU - van der Lely,Aart Jan, Y1 - 2006/04/27/ PY - 2006/03/03/received PY - 2006/03/28/revised PY - 2006/03/28/accepted PY - 2006/5/2/pubmed PY - 2006/8/19/medline PY - 2006/5/2/entrez SP - 103 EP - 11 JF - Molecular and cellular endocrinology JO - Mol Cell Endocrinol VL - 251 IS - 1-2 N2 - Both unacylated ghrelin (UAG) and acylated ghrelin (AG) exert metabolic effects. To investigate the interactions between AG and UAG on ghrelin receptors we evaluated the effects of AG and UAG on INS-1E rat insulinoma cells, using insulin secretion after 30min static incubation as a read-out. A possible involvement of the growth hormone secretagogue receptor type 1a (GHS-R1a) or the corticotropin-releasing factor 2 (CRF2) receptor (CRF2R), as a putative receptor for UAG, was also studied determining their mRNA expression and the functional effects of receptor antagonists on insulin release. Both UAG and AG stimulated insulin release dose-dependently in the nanomolar range. The AG-induced insulin output was antagonized by two GHS-R1a antagonists ([d-Lys(3)]GHRP-6 and BIM28163), which did not block UAG actions. These effects occurred in the presence of low levels of GHS-R1a mRNA. Neither CRF2R expression nor effects of the CRF2R antagonist (astressin(2)B) on insulin output were observed. In conclusion, we provide a sensitive and reproducible assay for specific effects of UAG, which in this study is responsible for insulin release by INS-1E cells. Our data support the existence of a specific receptor for UAG, other than the CRF2R and GHS-R1a. The stimulatory effect on insulin secretion by AG in this cell line is mediated by the GHS-R1a. SN - 0303-7207 UR - https://www.unboundmedicine.com/medline/citation/16647196/Unacylated_ghrelin_is_active_on_the_INS_1E_rat_insulinoma_cell_line_independently_of_the_growth_hormone_secretagogue_receptor_type_1a_and_the_corticotropin_releasing_factor_2_receptor_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0303-7207(06)00163-8 DB - PRIME DP - Unbound Medicine ER -