Author/Authors :
Brent Douty، نويسنده , , Brian Wayland، نويسنده , , Paul J. Ala، نويسنده , , Michael J. Bower، نويسنده , , James Pruitt، نويسنده , , Lori Bostrom، نويسنده , , Min Wei، نويسنده , , Ronald Klabe، نويسنده , , Lucie Gonneville، نويسنده , , Richard Wynn، نويسنده , , Timothy C. Burn، نويسنده , , Phillip C.C. Liu، نويسنده , , Andrew P. Combs، نويسنده , , Eddy W. Yue، نويسنده ,
Abstract :
The structure-based design and synthesis of isothiazolidinone (IZD) inhibitors of PTP1B containing imidazoles and imidazolines and their modification to interact with the B site of PTP1B are described here. The X-ray crystal structures of 3I and 4I complexed with PTP1B were solved and revealed the inhibitors are interacting extensively with the B site of the enzyme.
Keywords :
PTP1B , Isothiazolidinone , Phosphotyrosine , protein tyrosine phosphatase
