Title of article
Pyrrolo-pyrimidones: A novel class of MK2 inhibitors with potent cellular activity
Author/Authors
Achim Schlapbach، نويسنده , , Roland Feifel، نويسنده , , Stuart Hawtin، نويسنده , , Richard Heng، نويسنده , , Guido Koch، نويسنده , , Henrik Moebitz، نويسنده , , Laszlo Revesz، نويسنده , , Clemens Scheufler، نويسنده , , Juraj Velcicky، نويسنده , , Rudolf Waelchli، نويسنده , , Christine Huppertz، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
6142
To page
6146
Abstract
Pyrrolo-pyrimidones of the general structure 1 were synthesized and evaluated for their potential as MK2 inhibitors. Potent derivatives were discovered which inhibit MK2 in the nanomolar range and show potent inhibition of cytokine release from LPS-stimulated monocytes. These derivatives were shown to inhibit phosphorylation of hsp27, a downstream target of MK2 and are modestly selective in a panel of 28 kinases.
Keywords
MK2 , MAPKAPK-2 , TNF? inhibition , inflammation , rheumatoid arthritis
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
800188
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