2q1j: Difference between revisions

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==Overview==

Herein, we report on the identification of three potent glycine and, related amino acid-based series of FXa inhibitors containing a neutral P1, chlorophenyl pharmacophore. A X-ray crystal structure has shown that, constrained glycine derivatives with optimized N-substitution can greatly, increase hydrophobic interactions in the FXa active site. Also, the, substitution of a pyridone ring for a phenylsulfone ring in the P4, sidechain resulted in an inhibitor with enhanced oral bioavailability.

Herein, we report on the identification of three potent glycine and related amino acid-based series of FXa inhibitors containing a neutral P1 chlorophenyl pharmacophore. A X-ray crystal structure has shown that constrained glycine derivatives with optimized N-substitution can greatly increase hydrophobic interactions in the FXa active site. Also, the substitution of a pyridone ring for a phenylsulfone ring in the P4 sidechain resulted in an inhibitor with enhanced oral bioavailability.

==Disease==

Known disease associated with this structure: Factor X deficiency OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=227600 227600]]

==About this Structure==

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[[Category: Homo sapiens]]

[[Category: Protein complex]]

[[Category: Bigge, C.F.]]

[[Category: Bigge, C F.]]

[[Category: Cody, W.L.]]

[[Category: Cody, W L.]]

[[Category: Filipski, K.J.]]

[[Category: Filipski, K J.]]

[[Category: Finzel, B.C.]]

[[Category: Finzel, B C.]]

[[Category: Kohrt, J.T.]]

[[Category: Kohrt, J T.]]

[[Category: Zhang, E.]]

[[Category: CA]]

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[[Category: zymogen]]

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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:35:05 2008''

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@@ Line 4: / Line 4: @@
 ==Overview==
-Herein, we report on the identification of three potent glycine and, related amino acid-based series of FXa inhibitors containing a neutral P1, chlorophenyl pharmacophore. A X-ray crystal structure has shown that, constrained glycine derivatives with optimized N-substitution can greatly, increase hydrophobic interactions in the FXa active site. Also, the, substitution of a pyridone ring for a phenylsulfone ring in the P4, sidechain resulted in an inhibitor with enhanced oral bioavailability.
+Herein, we report on the identification of three potent glycine and related amino acid-based series of FXa inhibitors containing a neutral P1 chlorophenyl pharmacophore. A X-ray crystal structure has shown that constrained glycine derivatives with optimized N-substitution can greatly increase hydrophobic interactions in the FXa active site. Also, the substitution of a pyridone ring for a phenylsulfone ring in the P4 sidechain resulted in an inhibitor with enhanced oral bioavailability.
+==Disease==
+Known disease associated with this structure: Factor X deficiency OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=227600 227600]]
 ==About this Structure==
@@ Line 14: / Line 17: @@
 [[Category: Homo sapiens]]
 [[Category: Protein complex]]
-[[Category: Bigge, C.F.]]
+[[Category: Bigge, C F.]]
-[[Category: Cody, W.L.]]
+[[Category: Cody, W L.]]
-[[Category: Filipski, K.J.]]
+[[Category: Filipski, K J.]]
-[[Category: Finzel, B.C.]]
+[[Category: Finzel, B C.]]
-[[Category: Kohrt, J.T.]]
+[[Category: Kohrt, J T.]]
 [[Category: Zhang, E.]]
 [[Category: CA]]
@@ Line 36: / Line 39: @@
 [[Category: zymogen]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 14:13:01 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:35:05 2008''