1ijr
From Proteopedia
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==Overview== | ==Overview== | ||
| - | The novel phosphotyrosine (pTyr) mimetic | + | The novel phosphotyrosine (pTyr) mimetic 4'-carboxymethyloxy-3'-phosphonophenylalanine (Cpp) has been designed and incorporated into a series of nonpeptide inhibitors of the SH2 domain of pp60(c-Src) (Src) tyrosine kinase. A 2.2 A X-ray crystal structure of 1a bound to a mutant form of Lck SH2 domain provides insight regarding the structure-activity relationships and supports the design concept of this new pTyr mimetic. |
==Disease== | ==Disease== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Transferase]] | [[Category: Transferase]] | ||
| - | [[Category: Kawahata, N | + | [[Category: Kawahata, N H.]] |
| - | [[Category: Luke, G | + | [[Category: Luke, G P.]] |
| - | [[Category: Shakespeare, W | + | [[Category: Shakespeare, W C.]] |
[[Category: Sundaramoorthi, R.]] | [[Category: Sundaramoorthi, R.]] | ||
| - | [[Category: Yang, M | + | [[Category: Yang, M H.]] |
[[Category: CC0]] | [[Category: CC0]] | ||
[[Category: tyrosine-protein kinase]] | [[Category: tyrosine-protein kinase]] | ||
| - | ''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 13:12:41 2008'' |
Revision as of 11:12, 21 February 2008
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Crystal structure of LCK SH2 complexed with nonpeptide phosphotyrosine mimetic
Contents |
Overview
The novel phosphotyrosine (pTyr) mimetic 4'-carboxymethyloxy-3'-phosphonophenylalanine (Cpp) has been designed and incorporated into a series of nonpeptide inhibitors of the SH2 domain of pp60(c-Src) (Src) tyrosine kinase. A 2.2 A X-ray crystal structure of 1a bound to a mutant form of Lck SH2 domain provides insight regarding the structure-activity relationships and supports the design concept of this new pTyr mimetic.
Disease
Known disease associated with this structure: SCID due to LCK deficiency OMIM:[153390]
About this Structure
1IJR is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Transferase, with EC number and 2.7.10.2 2.7.10.1 and 2.7.10.2 Full crystallographic information is available from OCA.
Reference
A novel phosphotyrosine mimetic 4'-carboxymethyloxy-3'-phosphonophenylalanine (Cpp): exploitation in the design of nonpeptide inhibitors of pp60(Src) SH2 domain., Kawahata N, Yang MG, Luke GP, Shakespeare WC, Sundaramoorthi R, Wang Y, Johnson D, Merry T, Violette S, Guan W, Bartlett C, Smith J, Hatada M, Lu X, Dalgarno DC, Eyermann CJ, Bohacek RS, Sawyer TK, Bioorg Med Chem Lett. 2001 Sep 3;11(17):2319-23. PMID:11527723
Page seeded by OCA on Thu Feb 21 13:12:41 2008
