Journal
BIOORGANIC CHEMISTRY
Volume 37, Issue 1-3, Pages 90-95Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2009.04.001
Keywords
Benzodiazepine; Combinatorial synthesis; Peptidomimetics; Melanocortin 4 receptors
Funding
- institute of Medical System Engineering (iMSE)
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As an effective strategy of the drug discovery for peptide-binding GPCRs based on the natural ligands, beta-turn peptidomimetic compound library with benzodiazepine skeleton was constructed using solid and solution phase parallel synthesis with four different scaffolds containing Phe, Lys, Ser and Glu, respectively. The usefulness of 162 library compounds was evaluated by the cell based screening at melanocortin 4 receptor in CHO-k1 cells, to find hit compounds showing agonistic effect at the receptor. The screening of library afforded three hit compounds including the most effective analog, (S)-3-benzyl-7-(4-fluorobenzyloxy)-4-(4-methoxyphenethyl)-4,5-dihydro-1H-benzo[e][1,4]diazepin-2(3H)-one, 13aiE, of which EC50 was determined as 13 mu M. (C) 2009 Elsevier Inc. All rights reserved.
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