Detail of "16599-33-0"

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MTSEA prevents ligand binding to the human melanocortin-4 receptor by modification of cysteine 130 in transmembrane helix 3

MTSEA prevents ligand binding to the human melanocortin-4 receptor by modification of cysteine 130 in transmembrane helix 3. Cox, Alan; Donnelly, Dan; Kaur, Manminder; Cheetham, Sharon C.; Cockcroft, Victor B.; Findlay, John B. C. (School of Biochemistry and Microbiology, University of Leeds, Leeds LS2 9JT, UK). FEBS Letters, 579(1), 285-291 (English) 2005 Elsevier B.V. CODEN: FEBLAL. ISSN: 0014-5793. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) We have investigated the effect of the sulfhydryl-reactive reagent, Me thiosulfonate ethylammonium (MTSEA), on ligand binding to the human melanocortin-4 (MC4) receptor stably expressed in HEK-293 cells. MTSEA inhibited binding of the agonist, 125I-NDPa-MSH, and the antagonist, 125I-SHU9119, in a concn.-dependent manner. Pre-incubation of cells with either the agonist or antagonist protected from subsequent MTSEA inhibition of radioligand binding. Mutation of Cys130 in transmembrane helix 3 to alanine, while not affecting ligand binding, led to a complete loss of the inhibitory effect of MTSEA. Since other types of sulfhydryl-reactive reagents had no effect on ligand binding, we conclude that covalent modification of Cys130 by MTSEA disrupts ligand binding by neutralizing a close-by neg. charge, most likely on Asp126.Except for chemicals metioned above, 52-90-4 and 16599-33-0 are also used. .