Publications by authors named "Mike A Stashko"
Bioorg Med Chem Lett
June 2003
Article Synopsis
- A novel series of oxalyl-aryl-amino benzoic acid-based inhibitors for PTP1B was developed.
- Using a solution phase parallel synthesis method, researchers quickly identified a potent inhibitor with a dissociation constant (K(i)) of 76 nM.
- The inhibitor showed moderate selectivity for PTP1B over TCPTP, acting by binding to a secondary phosphotyrosine site near the catalytic site.
Article Synopsis
- Protein Tyrosine phosphatase 1B (PTP1B) negatively regulates insulin and leptin signaling, making it a target for diabetes and obesity treatments.
- An NMR-based screening identified a compound, 2,3-dimethylphenyloxalylaminobenzoic acid, as a reversible and competitive inhibitor of PTP1B.
- Structure-based drug design led to the development of potent PTP1B inhibitors, with one compound showing promise by lowering plasma glucose levels in obese mice.
