Discovery of a Novel Superpotent and Selective Melanocortin-4 Receptor Antagonist (HS024): Evaluation in Vitro and in Vivo**This work was supported by grants from the Swedish Medical Research Council (04X-05957), the Swedish Society for Medical Research, and the Estonian Science Foundation (Grant 3267); the Ants ja Maria Silvere ning Sigfried Panti Malestusstipendium Foundation (to A.K.); and the Swedish Institute (to I.M.).

Kask, Ants; Mutulis, Felikss; Muceniece, Ruta; Pähkla, Rein; Mutule, Ilze; E. S. Wikberg, Jarl; Rägo, Lembit; B. Schiöth, Helgi

doi:10.1210/endo.139.12.6352

Public

Discovery of a Novel Superpotent and Selective Melanocortin-4 Receptor Antagonist (HS024): Evaluation in Vitro and in Vivo**This work was supported by grants from the Swedish Medical Research Council (04X-05957), the Swedish Society for Medical Research, and the Estonian Science Foundation (Grant 3267); the Ants ja Maria Silvere ning Sigfried Panti Malestusstipendium Foundation (to A.K.); and the Swedish Institute (to I.M.).

Published in Endocrinology • Dec 1, 1998

Authors:

Ants Kask

Felikss Mutulis

Ruta Muceniece

Abstract

Several novel cyclic MSH analogs were synthesized, and their binding properties were tested on cells transiently expressing the human melanocortin-1 (MC1), MC3, MC4, and MC5 receptors. We discovered a novel substance (HS024) that showed about 20-fold selectivity and very high affinity (Ki = 0.29 nM)...

Subject

Melanocortin

Receptor

Internal medicine

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