1fpc: Difference between revisions

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==Overview==

The structures of two mimetic inhibitor complexes of human alpha-thrombin, have been determined by X-ray crystallography. One mimics a beta-turn with, a bicyclic ring system; the other mimics two different active-site binding, modes. The beta-turn mimetic is used to approximate a turn found in the, conformation of fibrinopeptide A, which is catalytically released by, thrombin in the activation of fibrinogen to fibrin. The binding of the, second mimetic is a hybrid between normal substrate and the abnormal, binding of the potent natural leech inhibitor hirudin. The binding of the, beta-turn mimetic is tenuous, because it is like a substrate, while that, of the substrate-hirudin hybrid is that of a tenacious inhibitor (which it, is). Structurally retrospect modifications for rational design and, improvement of both mimetic inhibitors are proposed.

The structures of two mimetic inhibitor complexes of human alpha-thrombin have been determined by X-ray crystallography. One mimics a beta-turn with a bicyclic ring system; the other mimics two different active-site binding modes. The beta-turn mimetic is used to approximate a turn found in the conformation of fibrinopeptide A, which is catalytically released by thrombin in the activation of fibrinogen to fibrin. The binding of the second mimetic is a hybrid between normal substrate and the abnormal binding of the potent natural leech inhibitor hirudin. The binding of the beta-turn mimetic is tenuous, because it is like a substrate, while that of the substrate-hirudin hybrid is that of a tenacious inhibitor (which it is). Structurally retrospect modifications for rational design and improvement of both mimetic inhibitors are proposed.

==Disease==

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[[Category: Single protein]]

[[Category: Thrombin]]

[[Category: Mathews, I.I.]]

[[Category: Mathews, I I.]]

[[Category: Tulinsky, A.]]

[[Category: ANS]]

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[[Category: complex (serine protease/inhibitor)]]

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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 12:41:08 2008''

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@@ Line 4: / Line 4: @@
 ==Overview==
-The structures of two mimetic inhibitor complexes of human alpha-thrombin, have been determined by X-ray crystallography. One mimics a beta-turn with, a bicyclic ring system; the other mimics two different active-site binding, modes. The beta-turn mimetic is used to approximate a turn found in the, conformation of fibrinopeptide A, which is catalytically released by, thrombin in the activation of fibrinogen to fibrin. The binding of the, second mimetic is a hybrid between normal substrate and the abnormal, binding of the potent natural leech inhibitor hirudin. The binding of the, beta-turn mimetic is tenuous, because it is like a substrate, while that, of the substrate-hirudin hybrid is that of a tenacious inhibitor (which it, is). Structurally retrospect modifications for rational design and, improvement of both mimetic inhibitors are proposed.
+The structures of two mimetic inhibitor complexes of human alpha-thrombin have been determined by X-ray crystallography. One mimics a beta-turn with a bicyclic ring system; the other mimics two different active-site binding modes. The beta-turn mimetic is used to approximate a turn found in the conformation of fibrinopeptide A, which is catalytically released by thrombin in the activation of fibrinogen to fibrin. The binding of the second mimetic is a hybrid between normal substrate and the abnormal binding of the potent natural leech inhibitor hirudin. The binding of the beta-turn mimetic is tenuous, because it is like a substrate, while that of the substrate-hirudin hybrid is that of a tenacious inhibitor (which it is). Structurally retrospect modifications for rational design and improvement of both mimetic inhibitors are proposed.
 ==Disease==
@@ Line 17: / Line 17: @@
 [[Category: Single protein]]
 [[Category: Thrombin]]
-[[Category: Mathews, I.I.]]
+[[Category: Mathews, I I.]]
 [[Category: Tulinsky, A.]]
 [[Category: ANS]]
@@ Line 23: / Line 23: @@
 [[Category: complex (serine protease/inhibitor)]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 15:48:36 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 12:41:08 2008''