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XMetD is a negative allosteric modulator (NAM) of the INSR. Studies were performed in cultured CHO cells engineered to express the human INSR. (A) XMetD decreased insulin binding to the INSR. (B) XMetD markedly decreased insulin-induced INSR autophosphorylation. (C) XMetD markedly decreased insulin-induced pAkt phosphorylation. (D) XMetS decreased insulin-induced glucose uptake.
