1nz7: Difference between revisions
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==Overview== | ==Overview== | ||
We have previously reported a novel series of oxalyl-aryl-amino benzoic | 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. | ||
==Disease== | ==Disease== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Abad-Zapatero, C.]] | [[Category: Abad-Zapatero, C.]] | ||
[[Category: Ballaron, S | [[Category: Ballaron, S J.]] | ||
[[Category: Hajduk, P | [[Category: Hajduk, P J.]] | ||
[[Category: Hutchins, C | [[Category: Hutchins, C W.]] | ||
[[Category: Jirousek, M | [[Category: Jirousek, M R.]] | ||
[[Category: Liu, G.]] | [[Category: Liu, G.]] | ||
[[Category: Lubben, T.]] | [[Category: Lubben, T.]] | ||
[[Category: Oost, T | [[Category: Oost, T K.]] | ||
[[Category: Pei, Z.]] | [[Category: Pei, Z.]] | ||
[[Category: Stashko, M | [[Category: Stashko, M A.]] | ||
[[Category: Szczepankiewicz, B | [[Category: Szczepankiewicz, B G.]] | ||
[[Category: Trevillyan, J | [[Category: Trevillyan, J M.]] | ||
[[Category: Xin, Z.]] | [[Category: Xin, Z.]] | ||
[[Category: 901]] | [[Category: 901]] | ||
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[[Category: protein tyrosine phosphatase fold]] | [[Category: protein tyrosine phosphatase fold]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:11:37 2008'' | ||
Revision as of 15:11, 21 February 2008
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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.
DiseaseDisease
Known diseases associated with this structure: Abdominal body fat distribution, modifier of OMIM:[176885], Insulin resistance, susceptibility to OMIM:[176885]
About this StructureAbout this Structure
1NZ7 is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Protein-tyrosine-phosphatase, with EC number 3.1.3.48 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
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Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)
OCA- Pages with broken file links
- 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.
- 901
- Oxamic acid inhibitor bound to p-loop
- Protein tyrosine phosphatase fold