View source for 2dxs

[[Image:2dxs.jpg|left|200px]]<br /><applet load="2dxs" size="350" color="white" frame="true" align="right" spinBox="true" 
caption="2dxs, resolution 2.20&Aring;" />
'''Crystal structure of HCV NS5B RNA polymerase complexed with a tetracyclic inhibitor'''<br />

==Overview==
We report a new series of hepatitis C virus NS5B RNA polymerase inhibitors, containing a conformationally constrained tetracyclic scaffold. SAR, studies led to the identification of, 6,7-dihydro-5H-benzo[5,6][1,4]diazepino[7,1-a]indoles (19 and 20) bearing, a basic pendent group with high biochemical and cellular potencies. These, compounds displayed a very small shift in cellular potency when the, replicon assay was performed in the presence of human serum albumin.

==About this Structure==
2DXS is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Hepatitis_c_virus Hepatitis c virus] with <scene name='pdbligand=JTP:'>JTP</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/RNA-directed_RNA_polymerase RNA-directed RNA polymerase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.7.48 2.7.7.48] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2DXS OCA]. 

==Reference==
Discovery of conformationally constrained tetracyclic compounds as potent hepatitis C virus NS5B RNA polymerase inhibitors., Ikegashira K, Oka T, Hirashima S, Noji S, Yamanaka H, Hara Y, Adachi T, Tsuruha J, Doi S, Hase Y, Noguchi T, Ando I, Ogura N, Ikeda S, Hashimoto H, J Med Chem. 2006 Nov 30;49(24):6950-3. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17125247 17125247]
[[Category: Hepatitis c virus]]
[[Category: RNA-directed RNA polymerase]]
[[Category: Single protein]]
[[Category: Adachi, T.]]
[[Category: Doi, S.]]
[[Category: Ikegashira, K.]]
[[Category: Kamada, M.]]
[[Category: Murase, K.]]
[[Category: Nomura, A.]]
[[Category: Orita, T.]]
[[Category: Tsuruha, J.]]
[[Category: Uehara, K.]]
[[Category: Watanabe, S.]]
[[Category: JTP]]
[[Category: hcv]]
[[Category: ns5b]]
[[Category: rna polymerase]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jan 29 19:14:22 2008''