Title of article :
2-Aryl-3,3,3-trifluoro-2-hydroxypropionic acids: A new class of protein tyrosine phosphatase 1B inhibitors
Author/Authors :
David R. Adams، نويسنده , , Achamma Abraham، نويسنده , , Jun Asano، نويسنده , , Catherine Breslin، نويسنده , , Colin A.J. Dick، نويسنده , , Ulrich Ixkes، نويسنده , , Blair F. Johnston، نويسنده , , Derek Johnston، نويسنده , , Justin Kewnay، نويسنده , , Simon P. MacKay، نويسنده , , Simon J. MacKenzie، نويسنده , , Morag McFarlane، نويسنده , , Lee Mitchell، نويسنده , , Daniel Spinks، نويسنده , , Yasuo Takano، نويسنده ,
Abstract :
A new series of non-peptidic, mono-acid protein tyrosine phosphatase 1B (PTP1B) inhibitors has been identified by structure-based design. Compounds with 2-(indol-3-yl)- and 2-phenyl-3,3,3-trifluoro-2-hydroxypropionic acid core units targeted at the enzyme’s primary site and a hydrophobic chlorophenylthiazole extension in its 2° site exhibit 3–60 μM IC50s for PTP1B inhibition in an Sf9 cell-based assay.
Keywords :
Protein tyrosine phosphatase 1B , PTP1B , inhibitor , obesity , structure-based design , insulin resistance , Indole , Thiazole , Phospho-tyrosine , insulin sensitivity , Diabetes
