Over expression of Low Molecular Weight Protein Tyrosine Phosphatase (LMW-PTP) is sufficient to transform cells.   In fact, in human breast, colon, bladder, and kidney tumor samples it has been shown that there is enhanced expression of LMW-PTP.  Pyridoxal 5'-phosphate (PLP) is a known inhibitor and substrate for LMW-PTP.  Non-hydrolysable phosphonate acid analogs of PLP were synthesized, screened for their inhibitory properties against LMW-PTP isoform B in kinetic assays, and their proposed binding examined by molecular modeling.  Structure Activity Relationships (SAR) from this work will be presented.

Rational design of low molecular weight protein tyrosine phosphatase (LMW-PTP) inhibitors

243rd National Meeting (2012)

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