2abj

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[[Image:2abj.gif|left|200px]]
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{{STRUCTURE_2abj| PDB=2abj | SCENE= }}
{{STRUCTURE_2abj| PDB=2abj | SCENE= }}
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'''Crystal structure of human branched chain amino acid transaminase in a complex with an inhibitor, C16H10N2O4F3SCl, and pyridoxal 5' phosphate.'''
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===Crystal structure of human branched chain amino acid transaminase in a complex with an inhibitor, C16H10N2O4F3SCl, and pyridoxal 5' phosphate.===
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==Overview==
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The inhibition of the cytosolic isoenzyme BCAT that is expressed specifically in neuronal tissue is likely to be useful for the treatment of neurodegenerative and other neurological disorders where glutamatergic mechanisms are implicated. Compound 2 exhibited an IC50 of 0.8 microM in the hBCATc assays; it is an active and selective inhibitor. Inhibitor 2 also blocked calcium influx into neuronal cells following inhibition of glutamate uptake, and demonstrated neuroprotective efficacy in vivo. SAR, pharmacology, and the crystal structure of hBCATc with inhibitor 2 are described.
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(as it appears on PubMed at http://www.pubmed.gov), where 16143519 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16143519}}
==About this Structure==
==About this Structure==
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[[Category: Plp-lys220 schiff base]]
[[Category: Plp-lys220 schiff base]]
[[Category: Pyridoxal-phosphate-dependent aminotransferase]]
[[Category: Pyridoxal-phosphate-dependent aminotransferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 18:51:02 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 19:51:09 2008''

Revision as of 16:51, 28 July 2008

Image:2abj.png

Template:STRUCTURE 2abj

Crystal structure of human branched chain amino acid transaminase in a complex with an inhibitor, C16H10N2O4F3SCl, and pyridoxal 5' phosphate.

Template:ABSTRACT PUBMED 16143519

About this Structure

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

Reference

The design and synthesis of human branched-chain amino acid aminotransferase inhibitors for treatment of neurodegenerative diseases., Hu LY, Boxer PA, Kesten SR, Lei HJ, Wustrow DJ, Moreland DW, Zhang L, Ahn K, Ryder TR, Liu X, Rubin JR, Fahnoe K, Carroll RT, Dutta S, Fahnoe DC, Probert AW, Roof RL, Rafferty MF, Kostlan CR, Scholten JD, Hood M, Ren XD, Schielke GP, Su TZ, Taylor CP, Mistry A, McConnell P, Hasemann C, Ohren J, Bioorg Med Chem Lett. 2006 May 1;16(9):2337-40. Epub 2005 Sep 6. PMID:16143519

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