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. 2003 Apr 17;13(8):1409-13.
doi: 10.1016/s0960-894x(03)00164-1.

Peptoid mimics of agouti related protein

Darren A Thompson  1 , Biao-Xin Chai, Hilary L E Rood, Michael A Siani, Nicholai R Douglas, Ira Gantz, Glenn L Millhauser
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Peptoid mimics of agouti related protein

Darren A Thompson et al. Bioorg Med Chem Lett. .

Abstract

The Agouti Related Protein (AGRP) is an endogenous antagonist of melanocortin-3 and -4 receptors, each of which plays a key role in body weight homeostasis. We designed a peptoid trimer based on AGRP 111-113 in which a single chiral atom is used to partially restrain the backbone structure. Peptoid 5 displaced both radiolabeled Nle4-alpha-MSH (IC(50)=3.1 microM) and AGRP (86-132) (IC(50)=1.9 microM) from the human melanocortin-4 receptor and functioned as an antagonist of alpha-MSH stimulated cAMP generation, thus providing an important lead in the development of AGRP mimetics.

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