2qe2: Difference between revisions

Line 4:

==Overview==

A series of potent anthranilic acid-based inhibitors of the hepatitis C, NS5B polymerase has been identified. The inhibitors bind to a site on NS5B, between the thumb and palm regions adjacent to the active site as, determined by X-ray crystallography of the enzyme-inhibitor complex., Guided by both molecular modeling and traditional SAR, the enzyme activity, of the initial hit was improved by approximately 100-fold, yielding a, series of potent and selective NS5B inhibitors with IC50 values as low as, 10 nM. These compounds were also inhibitors of the HCV replicon in, cultured HUH7 cells.

A series of potent anthranilic acid-based inhibitors of the hepatitis C NS5B polymerase has been identified. The inhibitors bind to a site on NS5B between the thumb and palm regions adjacent to the active site as determined by X-ray crystallography of the enzyme-inhibitor complex. Guided by both molecular modeling and traditional SAR, the enzyme activity of the initial hit was improved by approximately 100-fold, yielding a series of potent and selective NS5B inhibitors with IC50 values as low as 10 nM. These compounds were also inhibitors of the HCV replicon in cultured HUH7 cells.

==About this Structure==

Line 20:

[[Category: transferase]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Wed Jan 23 13~~:21:04 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:38:33 2008''

Navigation menu

Page actions

Page actions

Personal tools

Navigation

Search

Tools

@@ Line 4: / Line 4: @@
 ==Overview==
-A series of potent anthranilic acid-based inhibitors of the hepatitis C, NS5B polymerase has been identified. The inhibitors bind to a site on NS5B, between the thumb and palm regions adjacent to the active site as, determined by X-ray crystallography of the enzyme-inhibitor complex., Guided by both molecular modeling and traditional SAR, the enzyme activity, of the initial hit was improved by approximately 100-fold, yielding a, series of potent and selective NS5B inhibitors with IC50 values as low as, 10 nM. These compounds were also inhibitors of the HCV replicon in, cultured HUH7 cells.
+A series of potent anthranilic acid-based inhibitors of the hepatitis C NS5B polymerase has been identified. The inhibitors bind to a site on NS5B between the thumb and palm regions adjacent to the active site as determined by X-ray crystallography of the enzyme-inhibitor complex. Guided by both molecular modeling and traditional SAR, the enzyme activity of the initial hit was improved by approximately 100-fold, yielding a series of potent and selective NS5B inhibitors with IC50 values as low as 10 nM. These compounds were also inhibitors of the HCV replicon in cultured HUH7 cells.
 ==About this Structure==
@@ Line 20: / Line 20: @@
 [[Category: transferase]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 13:21:04 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:38:33 2008''