2ofu

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[[Image:2ofu.gif|left|200px]]
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{{STRUCTURE_2ofu| PDB=2ofu | SCENE= }}
{{STRUCTURE_2ofu| PDB=2ofu | SCENE= }}
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'''x-ray crystal structure of 2-aminopyrimidine carbamate 43 bound to Lck'''
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===x-ray crystal structure of 2-aminopyrimidine carbamate 43 bound to Lck===
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==Overview==
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The lymphocyte-specific kinase (Lck) is a cytoplasmic tyrosine kinase of the Src family expressed in T cells and NK cells. Genetic evidence in both mice and humans demonstrates that Lck kinase activity is critical for signaling mediated by the T cell receptor (TCR), which leads to normal T cell development and activation. A small molecule inhibitor of Lck is expected to be useful in the treatment of T cell-mediated autoimmune and inflammatory disorders and/or organ transplant rejection. In this paper, we describe the synthesis, structure-activity relationships, and pharmacological characterization of 2-aminopyrimidine carbamates, a new class of compounds with potent and selective inhibition of Lck. The most promising compound of this series, 2,6-dimethylphenyl 2-((3,5-bis(methyloxy)-4-((3-(4-methyl-1-piperazinyl)propyl)oxy)phenyl)ami no)-4-pyrimidinyl(2,4-bis(methyloxy)phenyl)carbamate (43) exhibits good activity when evaluated in in vitro assays and in an in vivo model of T cell activation.
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(as it appears on PubMed at http://www.pubmed.gov), where 16884310 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16884310}}
==Disease==
==Disease==
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[[Category: Kinase domain]]
[[Category: Kinase domain]]
[[Category: Lck]]
[[Category: Lck]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 10:49:11 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 18:41:18 2008''

Revision as of 15:41, 27 July 2008

Image:2ofu.png

Template:STRUCTURE 2ofu

Contents

x-ray crystal structure of 2-aminopyrimidine carbamate 43 bound to Lck

Template:ABSTRACT PUBMED 16884310

Disease

Known disease associated with this structure: SCID due to LCK deficiency OMIM:[153390]

About this Structure

2OFU is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity., Martin MW, Newcomb J, Nunes JJ, McGowan DC, Armistead DM, Boucher C, Buchanan JL, Buckner W, Chai L, Elbaum D, Epstein LF, Faust T, Flynn S, Gallant P, Gore A, Gu Y, Hsieh F, Huang X, Lee JH, Metz D, Middleton S, Mohn D, Morgenstern K, Morrison MJ, Novak PM, Oliveira-dos-Santos A, Powers D, Rose P, Schneider S, Sell S, Tudor Y, Turci SM, Welcher AA, White RD, Zack D, Zhao H, Zhu L, Zhu X, Ghiron C, Amouzegh P, Ermann M, Jenkins J, Johnston D, Napier S, Power E, J Med Chem. 2006 Aug 10;49(16):4981-91. PMID:16884310

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