Quiescent affinity inactivators of protein tyrosine phosphatases

✍ Scribed by William P. Taylor; Zhong-Yin Zhang; Theodore S. Widlanski

• Book ID: 103992346
• Publisher: Elsevier Science
• Year: 1996
• Tongue: English
• Weight: 448 KB
• Volume: 4
• Category: Article
• ISSN: 0968-0896
• DOI: 10.1016/0968-0896(96)00144-7

✦ Synopsis

alpha-Halobenzylphosphonates were investigated as possible inactivators of protein tyrosine phosphatases (PTPases). These compounds inactivate the Yersinia PTPase (Yop51*delta 162) in a time- and concentration-dependent fashion. This inactivation is active-site directed and irreversible, and is surprisingly rapid in light of the stability of the alpha-halobenzylphosphonates toward nucleophiles in solution. The potential of these molecules for probing the stereochemistry of PTPase inactivation, as well as for providing a useful paradigm for the design of more potent PTPase inhibitors is discussed.