4jv7: Difference between revisions

Line 1:

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

===Co-crystal structure of MDM2 with inhibitor (2S,5R,6S)-2-benzyl-5,6-bis(4-bromophenyl)-4-methylmorpholin-3-one===

~~The entry 4jv7 is ON HOLD~~

==Disease==

[[http://www.uniprot.org/uniprot/MDM2_HUMAN MDM2_HUMAN]] Note=Seems to be amplified in certain tumors (including soft tissue sarcomas, osteosarcomas and gliomas). A higher frequency of splice variants lacking p53 binding domain sequences was found in late-stage and high-grade ovarian and bladder carcinomas. Four of the splice variants show loss of p53 binding.

~~Authors~~: ~~Huang, X~~.~~, Gonzalez~~-~~Lopez de Turiso~~, F.~~, Sun, D~~.~~, Yosup, R~~.~~, Bartberger, M~~.D.~~, Beck, H~~.P.~~, Cannon, J., Shaffer, P~~.~~, Oliner, J~~.~~D., Olson, S.H., Medina, J.C~~.

==Function==

[[http://www.uniprot.org/uniprot/MDM2_HUMAN MDM2_HUMAN]] E3 ubiquitin-protein ligase that mediates ubiquitination of p53/TP53, leading to its degradation by the proteasome. Inhibits p53/TP53- and p73/TP73-mediated cell cycle arrest and apoptosis by binding its transcriptional activation domain. Also acts as an ubiquitin ligase E3 toward itself and ARRB1. Permits the nuclear export of p53/TP53. Promotes proteasome-dependent ubiquitin-independent degradation of retinoblastoma RB1 protein. Inhibits DAXX-mediated apoptosis by inducing its ubiquitination and degradation. Component of the TRIM28/KAP1-MDM2-p53/TP53 complex involved in stabilizing p53/TP53. Also component of the TRIM28/KAP1-ERBB4-MDM2 complex which links growth factor and DNA damage response pathways. Mediates ubiquitination and subsequent proteasome degradation of DYRK2 in nucleus. Ubiquitinates IGF1R and promotes it to proteasomal degradation.<ref>PMID:12821780</ref> <ref>PMID:15053880</ref> <ref>PMID:15195100</ref> <ref>PMID:16337594</ref> <ref>PMID:15632057</ref> <ref>PMID:17290220</ref> <ref>PMID:19098711</ref> <ref>PMID:19219073</ref> <ref>PMID:19965871</ref> <ref>PMID:20858735</ref> <ref>PMID:20173098</ref>

~~Description~~:

==About this Structure==

[[4jv7]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4JV7 OCA].

==Reference==

[[Category: Homo sapiens]]

[[Category: Bartberger, M D.]]

[[Category: Beck, H P.]]

[[Category: Cannon, J.]]

[[Category: Huang, X.]]

[[Category: Medina, J C.]]

[[Category: Oliner, J D.]]

[[Category: Olson, S H.]]

[[Category: Shaffer, P.]]

[[Category: Sun, D.]]

[[Category: Turiso, F Gonzalez-Lopez de.]]

[[Category: Yosup, R.]]

[[Category: Ligase-ligase inhibitor complex]]

[[Category: P53]]

[[Category: Protein-protein interaction]]

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@@ Line 1: / Line 1: @@
-'''Unreleased structure'''
+{{STRUCTURE_4jv7|  PDB=4jv7  |  SCENE=  }}
+===Co-crystal structure of MDM2 with inhibitor (2S,5R,6S)-2-benzyl-5,6-bis(4-bromophenyl)-4-methylmorpholin-3-one===
+{{ABSTRACT_PUBMED_23597064}}
-The entry 4jv7 is ON HOLD
+==Disease==
+[[http://www.uniprot.org/uniprot/MDM2_HUMAN MDM2_HUMAN]] Note=Seems to be amplified in certain tumors (including soft tissue sarcomas, osteosarcomas and gliomas). A higher frequency of splice variants lacking p53 binding domain sequences was found in late-stage and high-grade ovarian and bladder carcinomas. Four of the splice variants show loss of p53 binding.
-Authors: Huang, X., Gonzalez-Lopez de Turiso, F., Sun, D., Yosup, R., Bartberger, M.D., Beck, H.P., Cannon, J., Shaffer, P., Oliner, J.D., Olson, S.H., Medina, J.C.
+==Function==
+[[http://www.uniprot.org/uniprot/MDM2_HUMAN MDM2_HUMAN]] E3 ubiquitin-protein ligase that mediates ubiquitination of p53/TP53, leading to its degradation by the proteasome. Inhibits p53/TP53- and p73/TP73-mediated cell cycle arrest and apoptosis by binding its transcriptional activation domain. Also acts as an ubiquitin ligase E3 toward itself and ARRB1. Permits the nuclear export of p53/TP53. Promotes proteasome-dependent ubiquitin-independent degradation of retinoblastoma RB1 protein. Inhibits DAXX-mediated apoptosis by inducing its ubiquitination and degradation. Component of the TRIM28/KAP1-MDM2-p53/TP53 complex involved in stabilizing p53/TP53. Also component of the TRIM28/KAP1-ERBB4-MDM2 complex which links growth factor and DNA damage response pathways. Mediates ubiquitination and subsequent proteasome degradation of DYRK2 in nucleus. Ubiquitinates IGF1R and promotes it to proteasomal degradation.<ref>PMID:12821780</ref> <ref>PMID:15053880</ref> <ref>PMID:15195100</ref> <ref>PMID:16337594</ref> <ref>PMID:15632057</ref> <ref>PMID:17290220</ref> <ref>PMID:19098711</ref> <ref>PMID:19219073</ref> <ref>PMID:19965871</ref> <ref>PMID:20858735</ref> <ref>PMID:20173098</ref>
-Description:
+==About this Structure==
+[[4jv7]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4JV7 OCA].
+==Reference==
+<references group="xtra"/><references/>
+[[Category: Homo sapiens]]
+[[Category: Bartberger, M D.]]
+[[Category: Beck, H P.]]
+[[Category: Cannon, J.]]
+[[Category: Huang, X.]]
+[[Category: Medina, J C.]]
+[[Category: Oliner, J D.]]
+[[Category: Olson, S H.]]
+[[Category: Shaffer, P.]]
+[[Category: Sun, D.]]
+[[Category: Turiso, F Gonzalez-Lopez de.]]
+[[Category: Yosup, R.]]
+[[Category: Ligase-ligase inhibitor complex]]
+[[Category: P53]]
+[[Category: Protein-protein interaction]]