2o0u: Difference between revisions

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[[Image:2o0u.~~gif~~|left|200px]]

[[Image:2o0u.png|left|200px]]

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~~'''~~Crystal structure of human JNK3 complexed with N-{3-cyano-6-[3-(1-piperidinyl)propanoyl]-4,5,6,7-tetrahydrothieno[2,3-c]pyridin-2-yl}-1-naphthalenecarboxamide~~'''~~

===Crystal structure of human JNK3 complexed with N-{3-cyano-6-[3-(1-piperidinyl)propanoyl]-4,5,6,7-tetrahydrothieno[2,3-c]pyridin-2-yl}-1-naphthalenecarboxamide===

~~==Overview==~~

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The ~~identification and exploration of a novel~~, ~~potent and selective series of N-~~(~~3-cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amide inhibitors of JNK2 and JNK3 kinases is described. Compounds 5a and 11a were identified~~ as ~~potent inhibitors of JNK3 (pIC50 6~~.~~7 and 6~~.~~6, respectively~~), ~~with essentially equal potency against JNK2 (pIC50 6.5). Selectivity within~~ the ~~mitogen-activated protein kinase (MAPK) family, against JNK1, p38alpha and ERK2, was observed for the series~~. X-~~ray crystallography of 5e and 8a in JNK3 revealed a unique binding mode, with the 3~~-~~cyano substituent forming an H-bond acceptor interaction with the hinge region of the ATP-binding site.~~

The line below this paragraph, {{ABSTRACT_PUBMED_17194588}}, adds the Publication Abstract to the page

(as it appears on PubMed at http://www.pubmed.gov), where 17194588 is the PubMed ID number.

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==About this Structure==

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[[Category: Somers, D.]]

[[Category: Kinase fold]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun ~~May 4 10~~:09:53 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 19:34:42 2008''

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-[[Image:2o0u.gif|left|200px]]
+{{Seed}}
+[[Image:2o0u.png|left|200px]]
 <!--
@@ Line 9: / Line 10: @@
 {{STRUCTURE_2o0u|  PDB=2o0u  |  SCENE=  }}
-'''Crystal structure of human JNK3 complexed with N-{3-cyano-6-[3-(1-piperidinyl)propanoyl]-4,5,6,7-tetrahydrothieno[2,3-c]pyridin-2-yl}-1-naphthalenecarboxamide'''
+===Crystal structure of human JNK3 complexed with N-{3-cyano-6-[3-(1-piperidinyl)propanoyl]-4,5,6,7-tetrahydrothieno[2,3-c]pyridin-2-yl}-1-naphthalenecarboxamide===
-==Overview==
+<!--
-The identification and exploration of a novel, potent and selective series of N-(3-cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amide inhibitors of JNK2 and JNK3 kinases is described. Compounds 5a and 11a were identified as potent inhibitors of JNK3 (pIC50 6.7 and 6.6, respectively), with essentially equal potency against JNK2 (pIC50 6.5). Selectivity within the mitogen-activated protein kinase (MAPK) family, against JNK1, p38alpha and ERK2, was observed for the series. X-ray crystallography of 5e and 8a in JNK3 revealed a unique binding mode, with the 3-cyano substituent forming an H-bond acceptor interaction with the hinge region of the ATP-binding site.
+The line below this paragraph, {{ABSTRACT_PUBMED_17194588}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 17194588 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_17194588}}
 ==About this Structure==
@@ Line 26: / Line 30: @@
 [[Category: Somers, D.]]
 [[Category: Kinase fold]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 10:09:53 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 19:34:42 2008''