2c2z: Difference between revisions

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==Overview==

Aza-peptide Michael acceptors are a novel class of inhibitors that are, potent and specific for caspases-2, -3, -6, -7, -8, -9, and -10. The, second-order rate constants are in the order of 10(6) M(-1) s(-1). The, aza-peptide Michael acceptor inhibitor 18t, (Cbz-Asp-Glu-Val-AAsp-trans-CH=CH-CON(CH(2)-1-Naphth)(2) is the most, potent compound and it inhibits caspase-3 with a k(2) value of 5620000, M(-1) s(-1). The inhibitor 18t is 13700, 190, 6.4, 594, 37500, and, 173-fold more selective for caspase-3 over caspases-2, -6, -7, -8, -9, and, -10, respectively. Aza-peptide Michael acceptors designed with caspase, specific sequences are selective and do not show any cross reactivity with, clan CA cysteine proteases such as papain, cathepsin B, and calpains., High-resolution crystal structures .~~.. [[http://ispc.weizmann.ac.il/pmbin/getpm?16970398 (full description)]]~~

Aza-peptide Michael acceptors are a novel class of inhibitors that are, potent and specific for caspases-2, -3, -6, -7, -8, -9, and -10. The, second-order rate constants are in the order of 10(6) M(-1) s(-1). The, aza-peptide Michael acceptor inhibitor 18t, (Cbz-Asp-Glu-Val-AAsp-trans-CH=CH-CON(CH(2)-1-Naphth)(2) is the most, potent compound and it inhibits caspase-3 with a k(2) value of 5620000, M(-1) s(-1). The inhibitor 18t is 13700, 190, 6.4, 594, 37500, and, 173-fold more selective for caspase-3 over caspases-2, -6, -7, -8, -9, and, -10, respectively. Aza-peptide Michael acceptors designed with caspase, specific sequences are selective and do not show any cross reactivity with, clan CA cysteine proteases such as papain, cathepsin B, and calpains., High-resolution crystal structures of caspase-3 and caspase-8 in complex, with aza-peptide Michael acceptor inhibitors demonstrate the nucleophilic, attack on C2 and provide insight into the selectivity and potency of the, inhibitors with respect to the P1' moiety.

==About this Structure==

2C2Z is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]] with DTD as [[http://en.wikipedia.org/wiki/ligand ligand]]. Structure known Active Site: AC1. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2C2Z OCA]].

2C2Z is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with DTD as [http://en.wikipedia.org/wiki/ligand ligand]. Structure known Active Site: AC1. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2C2Z OCA].

==Reference==

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[[Category: zymogen]]

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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 5 12:47:29 2007''

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@@ Line 5: / Line 5: @@
 ==Overview==
-Aza-peptide Michael acceptors are a novel class of inhibitors that are, potent and specific for caspases-2, -3, -6, -7, -8, -9, and -10. The, second-order rate constants are in the order of 10(6) M(-1) s(-1). The, aza-peptide Michael acceptor inhibitor 18t, (Cbz-Asp-Glu-Val-AAsp-trans-CH=CH-CON(CH(2)-1-Naphth)(2) is the most, potent compound and it inhibits caspase-3 with a k(2) value of 5620000, M(-1) s(-1). The inhibitor 18t is 13700, 190, 6.4, 594, 37500, and, 173-fold more selective for caspase-3 over caspases-2, -6, -7, -8, -9, and, -10, respectively. Aza-peptide Michael acceptors designed with caspase, specific sequences are selective and do not show any cross reactivity with, clan CA cysteine proteases such as papain, cathepsin B, and calpains., High-resolution crystal structures ... [[http://ispc.weizmann.ac.il/pmbin/getpm?16970398 (full description)]]
+Aza-peptide Michael acceptors are a novel class of inhibitors that are, potent and specific for caspases-2, -3, -6, -7, -8, -9, and -10. The, second-order rate constants are in the order of 10(6) M(-1) s(-1). The, aza-peptide Michael acceptor inhibitor 18t, (Cbz-Asp-Glu-Val-AAsp-trans-CH=CH-CON(CH(2)-1-Naphth)(2) is the most, potent compound and it inhibits caspase-3 with a k(2) value of 5620000, M(-1) s(-1). The inhibitor 18t is 13700, 190, 6.4, 594, 37500, and, 173-fold more selective for caspase-3 over caspases-2, -6, -7, -8, -9, and, -10, respectively. Aza-peptide Michael acceptors designed with caspase, specific sequences are selective and do not show any cross reactivity with, clan CA cysteine proteases such as papain, cathepsin B, and calpains., High-resolution crystal structures of caspase-3 and caspase-8 in complex, with aza-peptide Michael acceptor inhibitors demonstrate the nucleophilic, attack on C2 and provide insight into the selectivity and potency of the, inhibitors with respect to the P1' moiety.
 ==About this Structure==
-C2Z is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]] with DTD as [[http://en.wikipedia.org/wiki/ligand ligand]]. Structure known Active Site: AC1. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2C2Z OCA]].
+C2Z is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with DTD as [http://en.wikipedia.org/wiki/ligand ligand]. Structure known Active Site: AC1. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2C2Z OCA].
 ==Reference==
@@ Line 41: / Line 41: @@
 [[Category: zymogen]]
-''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 16:56:07 2007''
+''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov  5 12:47:29 2007''