Title of article
A phosphorylated prodrug for the inhibition of Pin1
Author/Authors
Song Zhao، نويسنده , , Felicia A. Etzkorn، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
4
From page
6615
To page
6618
Abstract
Fmoc-pSer-Ψ[(Z)CH C]-Pro-(2)-N-(3)-ethylaminoindole 1, showed moderate inhibition towards the mitotic regulator, Pin1 (IC50 = 28.3 μM). To improve the cell permeability, the charged phosphate was masked as the bis-pivaloyloxymethyl (POM) phosphate in Fmoc-(bisPOM)-pSer-Ψ[(Z)CH C]-Pro-(2)-N-(3)-ethylaminoindole 2. Antiproliferative activity towards A2780 ovarian cancer cells of 1 (IC50 = 46.2 μM) was improved significantly in 2 (IC50 = 26.9 μM), comparable to the IC50 of 1 towards Pin1 enzymatic activity.
Keywords
Pin1 , inhibitor , peptidyl-prolyl isomerase , Bis-pivaloyloxymethyl (POM) , Cis-proline isostere , Cell permeability
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798855
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