1nz7
POTENT, SELECTIVE INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE 1B USING A SECOND PHOSPHOTYROSINE BINDING SITE, complexed with compound 19.
OverviewOverview
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.
About this StructureAbout this Structure
1NZ7 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
ReferenceReference
Potent, selective inhibitors of protein tyrosine phosphatase 1B., Xin Z, Oost TK, Abad-Zapatero C, Hajduk PJ, Pei Z, Szczepankiewicz BG, Hutchins CW, Ballaron SJ, Stashko MA, Lubben T, Trevillyan JM, Jirousek MR, Liu G, Bioorg Med Chem Lett. 2003 Jun 2;13(11):1887-90. PMID:12749891 Page seeded by OCA on Sat May 3 03:09:55 2008
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- Homo sapiens
- Protein-tyrosine-phosphatase
- Single protein
- Abad-Zapatero, C.
- Ballaron, S J.
- Hajduk, P J.
- Hutchins, C W.
- Jirousek, M R.
- Liu, G.
- Lubben, T.
- Oost, T K.
- Pei, Z.
- Stashko, M A.
- Szczepankiewicz, B G.
- Trevillyan, J M.
- Xin, Z.
- Oxamic acid inhibitor bound to p-loop
- Protein tyrosine phosphatase fold