Peptoid mimics of agouti related protein |
| |
| Authors: | Thompson Darren A Chai Biao-Xin Rood Hilary L E Siani Michael A Douglas Nicholai R Gantz Ira Millhauser Glenn L |
| |
| Affiliation: | Department of Chemistry and Biochemistry, University of California, Santa Cruz 95064, USA. thompson@chemistry.ucsc.edu |
| |
| 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. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ |
