Hydroxyindole carboxylic acid-based inhibitors for receptor-type protein tyrosine protein phosphatase beta.

ABSTRACT:

Aims

Protein tyrosine phosphatases (PTPs) play an important role in regulating a wide range of cellular processes. Understanding the role of PTPs within these processes has been hampered by a lack of potent and selective PTP inhibitors. Generating potent and selective probes for PTPs remains a significant challenge because of the highly conserved and positively charged PTP active site that also harbors a redox-sensitive Cys residue.

Results

We describe a facile method that uses an appropriate hydroxyindole carboxylic acid to anchor the inhibitor to the PTP active site and relies on the secondary binding elements introduced through an amide-focused library to enhance binding affinity for the target PTP and to impart selectivity against off-target phosphatases. Here, we disclo

SUBMITTER: Zeng LF 

PROVIDER: S-EPMC3995206 | biostudies-literature | 2014 May

REPOSITORIES: biostudies-literature