View source for 2c65

[[Image:2c65.gif|left|200px]]<br />
<applet load="2c65" size="450" color="white" frame="true" align="right" spinBox="true" 
caption="2c65, resolution 1.70&Aring;" />
'''MAO INHIBITION BY RASAGILINE ANALOGUES'''<br />

==Overview==
Monoamine oxidases A and B (MAO A and B) catalyze the degradation of, neurotransmitters and represent drug targets for the treatment of, neurodegenerative disorders. Rasagiline is an irreversible, MAO, B-selective inhibitor that has been approved as a novel anti-Parkinson's, drug. In this study, we investigate the inhibition of recombinant human, MAO A and MAO B by several rasagiline analogues. Different substituents, added onto the rasagiline scaffold alter the binding affinity depending on, the position on the aminoindan ring and on the size of the substituent., Compounds with a hydroxyl group on either the C4 or the C6 atom inhibit, both isozymes, whereas a bulkier substituent such as a carbamate is, tolerated only at the C4 position. The 1.7 A crystal structure of MAO B in, complex ... [[http://ispc.weizmann.ac.il/pmbin/getpm?16366596 (full description)]]

==About this Structure==
2C65 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 FAD as [[http://en.wikipedia.org/wiki/ligand ligand]]. Active as [[http://en.wikipedia.org/wiki/Amine_oxidase_(flavin-containing) Amine oxidase (flavin-containing)]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.4.3.4 1.4.3.4]]. Structure known Active Site: AC1. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2C65 OCA]]. 

==Reference==
Binding of rasagiline-related inhibitors to human monoamine oxidases: a kinetic and crystallographic analysis., Binda C, Hubalek F, Li M, Herzig Y, Sterling J, Edmondson DE, Mattevi A, J Med Chem. 2005 Dec 29;48(26):8148-54. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=16366596 16366596]
[[Category: Amine oxidase (flavin-containing)]]
[[Category: Homo sapiens]]
[[Category: Single protein]]
[[Category: Binda, C.]]
[[Category: Edmondson, D.E.]]
[[Category: Herzig, Y.]]
[[Category: Hubalek, F.]]
[[Category: Li, M.]]
[[Category: Mattevi, A.]]
[[Category: Sterling, J.]]
[[Category: FAD]]
[[Category: acetylation]]
[[Category: enantioselectivity]]
[[Category: fad]]
[[Category: flavin]]
[[Category: flavoprotein]]
[[Category: human monoamine oxidase]]
[[Category: inhibitor binding]]
[[Category: mitochondrion]]
[[Category: oxidoreductase]]
[[Category: parkinson]]
[[Category: rasagiline]]
[[Category: transmembrane]]

''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 11:28:59 2007''