Proto-oncogene serine/threonine-protein kinase
From Proteopedia
(Difference between revisions)
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{{STRUCTURE_3cy2| PDB=3cy2 | SIZE=350| SCENE= |right|CAPTION=Pim-1 (grey) complex with consensus peptide (green), inhibitor and Cl- ion [[3cy2]] }} | {{STRUCTURE_3cy2| PDB=3cy2 | SIZE=350| SCENE= |right|CAPTION=Pim-1 (grey) complex with consensus peptide (green), inhibitor and Cl- ion [[3cy2]] }} | ||
== Function == | == Function == | ||
| - | '''Proto-oncogene serine/threonine-protein kinase (Pim1)''' is the provirus integration site for Moloney murine leukemia virus 1<ref>PMID:15694833</ref>. Pim1 is involved in cell cycle progression, apoptosis, transcriptional activation and signaling pathways. Pim1 phosphorylates and inhibits proapoptotic proteins. | + | '''Proto-oncogene serine/threonine-protein kinase (Pim1)''' is the provirus integration site for Moloney murine leukemia virus 1<ref>PMID:15694833</ref>. Pim1 is involved in cell cycle progression, apoptosis, transcriptional activation and signaling pathways. Pim1 phosphorylates and inhibits proapoptotic proteins. For details see [[Student Project 6 for UMass Chemistry 423 Spring 2015]]. |
== Relevance == | == Relevance == | ||
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Pim-1 plays a pivotal role in several tumor relevant signaling pathways and is relevant to colon carcinoma<ref>PMID:23814490</ref>. | Pim-1 plays a pivotal role in several tumor relevant signaling pathways and is relevant to colon carcinoma<ref>PMID:23814490</ref>. | ||
| - | + | == Structural highlights == | |
| + | Pim1 is phosphorylated on serine 261 (PSer). The consensus peptide (pimtide) ARKRRRHPSGPPTA binds strongly to Pim1<ref>PMID:22136433</ref>. | ||
== 3D Structures of pim-1 == | == 3D Structures of pim-1 == | ||
Revision as of 07:37, 28 July 2016
Contents |
Function
Proto-oncogene serine/threonine-protein kinase (Pim1) is the provirus integration site for Moloney murine leukemia virus 1[1]. Pim1 is involved in cell cycle progression, apoptosis, transcriptional activation and signaling pathways. Pim1 phosphorylates and inhibits proapoptotic proteins. For details see Student Project 6 for UMass Chemistry 423 Spring 2015.
Relevance
Pim1 is a progression marker in diffuse large B-cell lymphoma[2].
Disease
Pim-1 plays a pivotal role in several tumor relevant signaling pathways and is relevant to colon carcinoma[3].
Structural highlights
Pim1 is phosphorylated on serine 261 (PSer). The consensus peptide (pimtide) ARKRRRHPSGPPTA binds strongly to Pim1[4].
3D Structures of pim-1
Updated on 28-July-2016
References
- ↑ Bachmann M, Moroy T. The serine/threonine kinase Pim-1. Int J Biochem Cell Biol. 2005 Apr;37(4):726-30. PMID:15694833 doi:http://dx.doi.org/10.1016/j.biocel.2004.11.005
- ↑ Brault L, Menter T, Obermann EC, Knapp S, Thommen S, Schwaller J, Tzankov A. PIM kinases are progression markers and emerging therapeutic targets in diffuse large B-cell lymphoma. Br J Cancer. 2012 Jul 24;107(3):491-500. doi: 10.1038/bjc.2012.272. Epub 2012 Jun, 21. PMID:22722314 doi:http://dx.doi.org/10.1038/bjc.2012.272
- ↑ Weirauch U, Beckmann N, Thomas M, Grunweller A, Huber K, Bracher F, Hartmann RK, Aigner A. Functional role and therapeutic potential of the pim-1 kinase in colon carcinoma. Neoplasia. 2013 Jul;15(7):783-94. PMID:23814490
- ↑ Huber K, Brault L, Fedorov O, Gasser C, Filippakopoulos P, Bullock AN, Fabbro D, Trappe J, Schwaller J, Knapp S, Bracher F. 7,8-Dichloro-1-oxo-beta-carbolines as a Versatile Scaffold for the Development of Potent and Selective Kinase Inhibitors with Unusual Binding Modes. J Med Chem. 2012 Jan 12;55(1):403-13. Epub 2012 Jan 3. PMID:22136433 doi:10.1021/jm201286z
