1q1m: Difference between revisions

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==Overview==
==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.
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==
==Disease==
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[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Abad-Zapatero, C.]]
[[Category: Abad-Zapatero, C.]]
[[Category: Ballaron, S.J.]]
[[Category: Ballaron, S J.]]
[[Category: Haasch, D.L.]]
[[Category: Haasch, D L.]]
[[Category: Hajduk, P.J.]]
[[Category: Hajduk, P J.]]
[[Category: Hutchins, C.W.]]
[[Category: Hutchins, C W.]]
[[Category: Jirousek, M.R.]]
[[Category: Jirousek, M R.]]
[[Category: Kaszubska, W.]]
[[Category: Kaszubska, W.]]
[[Category: Liu, G.]]
[[Category: Liu, G.]]
[[Category: Lubben, T.H.]]
[[Category: Lubben, T H.]]
[[Category: Pei, Z.]]
[[Category: Pei, Z.]]
[[Category: Rondinone, C.M.]]
[[Category: Rondinone, C M.]]
[[Category: Trevillyan, J.M.]]
[[Category: Trevillyan, J M.]]
[[Category: Xin, Z.]]
[[Category: Xin, Z.]]
[[Category: Zhao, H.]]
[[Category: Zhao, H.]]
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[[Category: ptp1b]]
[[Category: ptp1b]]


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