AI 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 Abstract
We have previously reported a novel series of oxalyl-aryl-amino benzoic acid-based, catalytic site-directed, competitive, reversible protein tyrosine phosphatase 1B (PTP1B) inhibitors. With readily access to key intermediates, we utilized a solution phase parallel synthesis approach and rapidly identified a highly potent PTP1B inhibitor (19, K(i)=76 nM) with moderate selectivity (5-fold) over T-cell PTPase (TCPTP) through interacting with a second phosphotyrosine binding site (site 2) in the close proximity to the catalytic site.
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| http://dx.doi.org/10.1016/s0960-894x(03)00302-0 | DOI Listing |
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