2h03
From Proteopedia
(New page: 200px<br /> <applet load="2h03" size="450" color="white" frame="true" align="right" spinBox="true" caption="2h03, resolution 1.650Å" /> '''Structural studies...) |
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| - | [[Image:2h03.gif|left|200px]]<br /> | + | [[Image:2h03.gif|left|200px]]<br /><applet load="2h03" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2h03" size=" | + | |
caption="2h03, resolution 1.650Å" /> | caption="2h03, resolution 1.650Å" /> | ||
'''Structural studies of protein tyrosine phosphatase beta catalytic domain in complex with inhibitors'''<br /> | '''Structural studies of protein tyrosine phosphatase beta catalytic domain in complex with inhibitors'''<br /> | ||
==Overview== | ==Overview== | ||
| - | The sulfamic acid phosphotyrosine mimetic was coupled with a previously | + | The sulfamic acid phosphotyrosine mimetic was coupled with a previously known malonate template to obtain highly selective and potent inhibitors of HPTPbeta. Potentially hydrolyzable malonate ester functionalities were replaced with 1,2,4-oxadiazoles without a significant effect on HPTPbeta potency. |
==About this Structure== | ==About this Structure== | ||
| - | 2H03 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with CL, MG and 3UN as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Protein-tyrosine-phosphatase Protein-tyrosine-phosphatase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.3.48 3.1.3.48] Full crystallographic information is available from [http:// | + | 2H03 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=CL:'>CL</scene>, <scene name='pdbligand=MG:'>MG</scene> and <scene name='pdbligand=3UN:'>3UN</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Protein-tyrosine-phosphatase Protein-tyrosine-phosphatase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.3.48 3.1.3.48] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2H03 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Protein-tyrosine-phosphatase]] | [[Category: Protein-tyrosine-phosphatase]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Amarasinghe, K | + | [[Category: Amarasinghe, K D.]] |
| - | [[Category: Clark, C | + | [[Category: Clark, C M.]] |
| - | [[Category: Evdokimov, A | + | [[Category: Evdokimov, A G.]] |
| - | [[Category: Gray, J | + | [[Category: Gray, J L.]] |
| - | [[Category: Maier, M | + | [[Category: Maier, M B.]] |
[[Category: Mekel, M.]] | [[Category: Mekel, M.]] | ||
[[Category: Nichols, R.]] | [[Category: Nichols, R.]] | ||
| - | [[Category: Peters, K | + | [[Category: Peters, K G.]] |
| - | [[Category: Pokross, M | + | [[Category: Pokross, M E.]] |
| - | [[Category: Walter, R | + | [[Category: Walter, R L.]] |
[[Category: 3UN]] | [[Category: 3UN]] | ||
[[Category: CL]] | [[Category: CL]] | ||
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[[Category: wpd-loop]] | [[Category: wpd-loop]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:36:47 2008'' |
Revision as of 15:36, 21 February 2008
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Structural studies of protein tyrosine phosphatase beta catalytic domain in complex with inhibitors
Overview
The sulfamic acid phosphotyrosine mimetic was coupled with a previously known malonate template to obtain highly selective and potent inhibitors of HPTPbeta. Potentially hydrolyzable malonate ester functionalities were replaced with 1,2,4-oxadiazoles without a significant effect on HPTPbeta potency.
About this Structure
2H03 is a Single protein structure of sequence from Homo sapiens with , and as ligands. Active as Protein-tyrosine-phosphatase, with EC number 3.1.3.48 Full crystallographic information is available from OCA.
Reference
Design and synthesis of potent, non-peptidic inhibitors of HPTPbeta., Amarasinghe KK, Evidokimov AG, Xu K, Clark CM, Maier MB, Srivastava A, Colson AO, Gerwe GS, Stake GE, Howard BW, Pokross ME, Gray JL, Peters KG, Bioorg Med Chem Lett. 2006 Aug 15;16(16):4252-6. Epub 2006 Jun 12. PMID:16759857
Page seeded by OCA on Thu Feb 21 17:36:47 2008
Categories: Homo sapiens | Protein-tyrosine-phosphatase | Single protein | Amarasinghe, K D. | Clark, C M. | Evdokimov, A G. | Gray, J L. | Maier, M B. | Mekel, M. | Nichols, R. | Peters, K G. | Pokross, M E. | Walter, R L. | 3UN | CL | MG | Drug design | Inhibitor | Phosphatase | Protein tyrosine phosphatase | Sulfamic acid | Wpd-loop
