View source for 2q1q

[[Image:2q1q.jpg|left|200px]]<br /><applet load="2q1q" size="350" color="white" frame="true" align="right" spinBox="true" 
caption="2q1q, resolution 1.90&Aring;" />
'''Carbonic anhydrase inhibitors. Interaction of the antiepileptic drug sulthiame with twelve mammalian isoforms: kinetic and X-Ray crystallographic studies'''<br />

==Overview==
Sulthiame, a clinically used antiepileptic, was investigated for its, interaction with 12 catalytically active mammalian carbonic anhydrase (CA, EC 4.2.1.1) isoforms. The drug is a potent inhibitor of CA II, VII, IX, and XII (K(I)s of 6-56nM), and a medium potency inhibitor against CA IV, VA, VB, and VI (K(I)s of 81-134nM). The high resolution crystal structure, of the hCA II-sulthiame adduct revealed a large number of favorable, interactions between the drug and the enzyme which explain its strong low, nanomolar affinity for this isoform and may also be exploited for the, design of effective inhibitors incorporating sultam moieties.

==About this Structure==
2Q1Q is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/ ] with <scene name='pdbligand=ZN:'>ZN</scene>, <scene name='pdbligand=HG:'>HG</scene> and <scene name='pdbligand=OSP:'>OSP</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Carbonate_dehydratase Carbonate dehydratase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=4.2.1.1 4.2.1.1] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Q1Q OCA]. 

==Reference==
Carbonic anhydrase inhibitors. Interaction of the antiepileptic drug sulthiame with twelve mammalian isoforms: Kinetic and X-ray crystallographic studies., Temperini C, Innocenti A, Mastrolorenzo A, Scozzafava A, Supuran CT, Bioorg Med Chem Lett. 2007 Sep 1;17(17):4866-72. Epub 2007 Jun 14. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17588751 17588751]
[[Category: Carbonate dehydratase]]
[[Category: Single protein]]
[[Category: Innocenti, A.]]
[[Category: Mastrolorenzo, A.]]
[[Category: Scozzafava, A.]]
[[Category: Supuran, C.T.]]
[[Category: Temperini, C.]]
[[Category: HG]]
[[Category: OSP]]
[[Category: ZN]]
[[Category: antiepileptic]]
[[Category: carbonic anhydrase]]
[[Category: crystal structure]]
[[Category: inhibitors]]
[[Category: lyase]]

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