ART (protein product of agouti-related transcript) as an antagonist of MC-3 and MC-4 receptors
TM Fong, C Mao, T MacNeil, R Kalyani, T Smith… - Biochemical and …, 1997 - Elsevier
TM Fong, C Mao, T MacNeil, R Kalyani, T Smith, D Weinberg, MR Tota, LHT Van der Ploeg
Biochemical and biophysical research communications, 1997•ElsevierThe mRNA encoding an agouti related protein (ART) of unknown biochemical function was
previously reported to be up-regulated in the hypothalamus of two genetically obese mouse
strains. We have expressed human ART as a secreted protein in COS-7 cells, and show that
recombinant ART is functionally active in inhibiting the binding of a radiolabeled α-
melanocyte stimulating hormone (α-MSH) analog to the human melanocortin-3 (MC-3) and
melanocortin-4 (MC-4) receptors, while it is not a potent inhibitor of the human melanocortin …
previously reported to be up-regulated in the hypothalamus of two genetically obese mouse
strains. We have expressed human ART as a secreted protein in COS-7 cells, and show that
recombinant ART is functionally active in inhibiting the binding of a radiolabeled α-
melanocyte stimulating hormone (α-MSH) analog to the human melanocortin-3 (MC-3) and
melanocortin-4 (MC-4) receptors, while it is not a potent inhibitor of the human melanocortin …
The mRNA encoding an agouti related protein (ART) of unknown biochemical function was previously reported to be up-regulated in the hypothalamus of two genetically obese mouse strains. We have expressed human ART as a secreted protein in COS-7 cells, and show that recombinant ART is functionally active in inhibiting the binding of a radiolabeled α-melanocyte stimulating hormone (α-MSH) analog to the human melanocortin-3 (MC-3) and melanocortin-4 (MC-4) receptors, while it is not a potent inhibitor of the human melanocortin-5 (MC-5) receptor. ART is an antagonist of the human MC-3 and MC-4 receptors as determined in functional assay. ART appears to be approximately 100-fold more potent than agouti with reference to the MC-3R and MC-4R binding affinity. These data suggest that ART may be a physiological regulator of feeding behavior.
Elsevier
