1q1m | pdb_00001q1m
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A Highly Efficient Approach to a Selective and Cell Active PTP1B inhibitors
Overview
Using an NMR-based fragment screening and X-ray crystal structure-based, assembly, starting with millimolar ligands for both the catalytic site and, the second phosphotyrosine binding site, we have identified a, small-molecule inhibitor of protein tyrosine phosphatase 1B with low, micromolar inhibition constant, high selectivity (30-fold) over the highly, homologous T-cell protein tyrosine phosphatase, and good cellular activity, in COS-7 cells.
Disease
Known diseases associated with this structure: Abdominal body fat distribution, modifier of OMIM:[176885], Insulin resistance, susceptibility to OMIM:[176885]
About this Structure
1Q1M is a Single protein structure of sequence from Homo sapiens with 234 as ligand. Active as Protein-tyrosine-phosphatase, with EC number 3.1.3.48 Full crystallographic information is available from OCA.
Reference
Fragment screening and assembly: a highly efficient approach to a selective and cell active protein tyrosine phosphatase 1B inhibitor., Liu G, Xin Z, Pei Z, Hajduk PJ, Abad-Zapatero C, Hutchins CW, Zhao H, Lubben TH, Ballaron SJ, Haasch DL, Kaszubska W, Rondinone CM, Trevillyan JM, Jirousek MR, J Med Chem. 2003 Sep 25;46(20):4232-5. PMID:13678400
Page seeded by OCA on Mon Nov 12 18:49:25 2007
Proteopedia Page Contributors and Editors (what is this?)
- Pages with broken file links
- Homo sapiens
- Protein-tyrosine-phosphatase
- Single protein
- Abad-Zapatero, C.
- Ballaron, S.J.
- Haasch, D.L.
- Hajduk, P.J.
- Hutchins, C.W.
- Jirousek, M.R.
- Kaszubska, W.
- Liu, G.
- Lubben, T.H.
- Pei, Z.
- Rondinone, C.M.
- Trevillyan, J.M.
- Xin, Z.
- Zhao, H.
- 234
- Inhibitors with isoxazole-salicylate pharmacophores
- Protein tyrosine phosphatase 1b
- Ptp1b
