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Combinatorial synthesis and biological evaluation of peptide-binding GPCR-targeted library.

Abstract：

: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 EC(50) was determined as 13 microM.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Lee JY,Im I,Webb TR,McGrath D,Song MR,Kim YC

doi

10.1016/j.bioorg.2009.04.001

subject

Has Abstract

pub_date

2009-06-01 00:00:00

pages

90-5

issue

3

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(09)00018-2

journal_volume

37

pub_type

杂志文章

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