Gonadotropin releasing hormone activation is mediated by dimerization of occupied receptors |
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| Authors: | E Hazum D Keinan |
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| Affiliation: | 1. UFZ – Helmholtz Centre for Environmental Research, Effect-Directed Analysis, 04318 Leipzig, Germany;2. RWTH Aachen University, Institute for Environmental Research (Biology V), Department of Ecosystem Analysis (ESA), Worringer Weg 1, D-52074 Aachen, Germany;3. UFZ – Helmholtz Centre for Environmental Research, Cell Toxicology, 04318 Leipzig, Germany;4. Eberhard Karls University Tübingen, Environmental Toxicology, Center for Applied Geoscience, 72074 Tübingen, Germany;5. University of Novi Sad, Faculty of Sciences, Trg Dositeja Obradovica 2, 21000 Novi Sad, Serbia |
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| Abstract: | A dinitrophenyl (DNP)-derivative of a gonadotropin releasing hormone (GnRH) antagonist was prepared by chemical modification of the epsilon amino group in position 6 of [D-pGlu1,D-Phe2,D-Trp3,D-Lys6]GnRH with 1-fluoro-2, 4-dinitrobenzene. The DNP-antagonist D-pGlu-D-Phe-D-Trp-Ser-Tyr-D-Lys(N epsilon-DNP)-Leu-Arg-Pro-Gly-NH2, retained high affinity binding to the GnRH receptor of pituitary membrane preparations and exhibited antagonistic activity when assayed in cultured pituitary cells. Both antibodies against DNP and their Fab fragments were able to bind the DNP-antagonist. However, only the addition of bivalent antibodies (and not the Fab fragments) converted the DNP-antagonist to an agonist. These results suggest that divalency is a critical factor in GnRH action. |
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