Histone methyltransferase
From Proteopedia
(Difference between revisions)
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| - | <StructureSection load='1o9s' size='350' side='right' caption='Human histone-lysine N-methyltrasferase | + | <StructureSection load='1o9s' size='350' side='right' caption='Human histone-lysine N-methyltrasferase (grey, green) complex with methylated lysine histone H3 peptide (rust, aqua) and S-adenosyl homocysteine (SAH) (PDB entry [[1o9s]])' scene=''> |
== Function == | == Function == | ||
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== Relevance == | == Relevance == | ||
| - | Inhibitors of the histone-lysine N-methyltransferase SMYD2 which represses the tumor-suppressing activities of p53 are studied as cancer therapy | + | Inhibitors of the histone-lysine N-methyltransferase SMYD2 which represses the tumor-suppressing activities of p53 are studied as cancer therapy drug<ref>PMID:21782458</ref>.s. |
== Disease == | == Disease == | ||
Aberrant HMT plays a role in cancer, intellectual disability syndromes and regulation of tissue aging<ref>PMID:22473383</ref>. | Aberrant HMT plays a role in cancer, intellectual disability syndromes and regulation of tissue aging<ref>PMID:22473383</ref>. | ||
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| + | == Structural highlights == | ||
| + | Human KHMT binds SAH in the peptide binding groove with the histone H3 peptide assuming an extended conformation and the methylated lysine inserted in a hydrophobic environment<ref>PMID:12540855</ref>. | ||
| + | </StructureSection> | ||
== 3D Structures of histone methyltransferase == | == 3D Structures of histone methyltransferase == | ||
Revision as of 09:38, 24 March 2016
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3D Structures of histone methyltransferase
Updated on 24-March-2016
References
- ↑ Trievel RC. Structure and function of histone methyltransferases. Crit Rev Eukaryot Gene Expr. 2004;14(3):147-69. PMID:15248813
- ↑ Ferguson AD, Larsen NA, Howard T, Pollard H, Green I, Grande C, Cheung T, Garcia-Arenas R, Cowen S, Wu J, Godin R, Chen H, Keen N. Structural Basis of Substrate Methylation and Inhibition of SMYD2. Structure. 2011 Jul 20. PMID:21782458 doi:10.1016/j.str.2011.06.011
- ↑ Greer EL, Shi Y. Histone methylation: a dynamic mark in health, disease and inheritance. Nat Rev Genet. 2012 Apr 3;13(5):343-57. doi: 10.1038/nrg3173. PMID:22473383 doi:http://dx.doi.org/10.1038/nrg3173
- ↑ Xiao B, Jing C, Wilson JR, Walker PA, Vasisht N, Kelly G, Howell S, Taylor IA, Blackburn GM, Gamblin SJ. Structure and catalytic mechanism of the human histone methyltransferase SET7/9. Nature. 2003 Feb 6;421(6923):652-6. Epub 2003 Jan 22. PMID:12540855 doi:10.1038/nature01378
