4mpn: Difference between revisions

Line 1:

~~'''Unreleased~~ structure~~'''~~

===Crystal structure of pyruvate dehydrogenase kinase isoform 2 in complex with inhibitor PS10===

~~The entry 4mpn is ON HOLD~~ ~~until Paper Publication~~

==Function==

[[http://www.uniprot.org/uniprot/PDK2_HUMAN PDK2_HUMAN]] Serine/threonine kinase that plays a key role in the regulation of glucose and fatty acid metabolism and homeostasis via phosphorylation of the pyruvate dehydrogenase subunits PDHA1 and PDHA2. This inhibits pyruvate dehydrogenase activity, and thereby regulates metabolite flux through the tricarboxylic acid cycle, down-regulates aerobic respiration and inhibits the formation of acetyl-coenzyme A from pyruvate. Inhibition of pyruvate dehydrogenase decreases glucose utilization and increases fat metabolism. Mediates cellular responses to insulin. Plays an important role in maintaining normal blood glucose levels and in metabolic adaptation to nutrient availability. Via its regulation of pyruvate dehydrogenase activity, plays an important role in maintaining normal blood pH and in preventing the accumulation of ketone bodies under starvation. Plays a role in the regulation of cell proliferation and in resistance to apoptosis under oxidative stress. Plays a role in p53/TP53-mediated apoptosis.<ref>PMID:7499431</ref> <ref>PMID:9787110</ref> <ref>PMID:17222789</ref> <ref>PMID:19833728</ref> <ref>PMID:21283817</ref> <ref>PMID:22123926</ref>

~~Authors~~: ~~Gui, W.J., Tso, S.C., Chuang, J.L., Wu, C.Y., Qi, X., Tambar, U.K., Wynn, R~~.M.~~, Chuang, D~~.T.

==About this Structure==

[[4mpn]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4MPN OCA].

~~Description~~: ~~Crystal structure of pyruvate~~ dehydrogenase ~~kinase isoform~~ 2 ~~in complex with inhibitor PS10~~

==Reference==

[[Category: Chuang, D T.]]

[[Category: Chuang, J L.]]

[[Category: Gui, W J.]]

[[Category: Qi, X.]]

[[Category: Tambar, U K.]]

[[Category: Tso, S C.]]

[[Category: Wu, C Y.]]

[[Category: Wynn, R M.]]

[[Category: Bergerat nucleotide-binding fold]]

[[Category: Cancer]]

[[Category: Ghkl protein kinase]]

[[Category: Hepatic steatosis]]

[[Category: Impaired glucose oxidation]]

[[Category: Mitochondrial protein kinase]]

[[Category: Protein kinase]]

[[Category: Pyruvate dehydrogenase complex]]

[[Category: Transferase]]

[[Category: Type 2 diabetes]]

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@@ Line 1: / Line 1: @@
-'''Unreleased structure'''
+{{STRUCTURE_4mpn|  PDB=4mpn  |  SCENE=  }}
+===Crystal structure of pyruvate dehydrogenase kinase isoform 2 in complex with inhibitor PS10===
+{{ABSTRACT_PUBMED_24356970}}
-The entry 4mpn is ON HOLD  until Paper Publication
+==Function==
+[[http://www.uniprot.org/uniprot/PDK2_HUMAN PDK2_HUMAN]] Serine/threonine kinase that plays a key role in the regulation of glucose and fatty acid metabolism and homeostasis via phosphorylation of the pyruvate dehydrogenase subunits PDHA1 and PDHA2. This inhibits pyruvate dehydrogenase activity, and thereby regulates metabolite flux through the tricarboxylic acid cycle, down-regulates aerobic respiration and inhibits the formation of acetyl-coenzyme A from pyruvate. Inhibition of pyruvate dehydrogenase decreases glucose utilization and increases fat metabolism. Mediates cellular responses to insulin. Plays an important role in maintaining normal blood glucose levels and in metabolic adaptation to nutrient availability. Via its regulation of pyruvate dehydrogenase activity, plays an important role in maintaining normal blood pH and in preventing the accumulation of ketone bodies under starvation. Plays a role in the regulation of cell proliferation and in resistance to apoptosis under oxidative stress. Plays a role in p53/TP53-mediated apoptosis.<ref>PMID:7499431</ref> <ref>PMID:9787110</ref> <ref>PMID:17222789</ref> <ref>PMID:19833728</ref> <ref>PMID:21283817</ref> <ref>PMID:22123926</ref>
-Authors: Gui, W.J., Tso, S.C., Chuang, J.L., Wu, C.Y., Qi, X., Tambar, U.K., Wynn, R.M., Chuang, D.T.
+==About this Structure==
+[[4mpn]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4MPN OCA].
-Description: Crystal structure of pyruvate dehydrogenase kinase isoform 2 in complex with inhibitor PS10
+==Reference==
+<ref group="xtra">PMID:024356970</ref><references group="xtra"/><references/>
+[[Category: Chuang, D T.]]
+[[Category: Chuang, J L.]]
+[[Category: Gui, W J.]]
+[[Category: Qi, X.]]
+[[Category: Tambar, U K.]]
+[[Category: Tso, S C.]]
+[[Category: Wu, C Y.]]
+[[Category: Wynn, R M.]]
+[[Category: Bergerat nucleotide-binding fold]]
+[[Category: Cancer]]
+[[Category: Ghkl protein kinase]]
+[[Category: Hepatic steatosis]]
+[[Category: Impaired glucose oxidation]]
+[[Category: Mitochondrial protein kinase]]
+[[Category: Protein kinase]]
+[[Category: Pyruvate dehydrogenase complex]]
+[[Category: Transferase]]
+[[Category: Type 2 diabetes]]