This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.
Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.
1q1m
From Proteopedia
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.
About this Structure
1Q1M is a Single protein structure of sequence from Homo sapiens. 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 Sat May 3 05:45:19 2008
Categories: 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. | Inhibitors with isoxazole-salicylate pharmacophore | Protein tyrosine phosphatase 1b | Ptp1b
