SET and MYND domain containing 2

Target id: 2714

Nomenclature: SET and MYND domain containing 2

Family: 2.1.1.43 Histone methyltransferases (HMTs)

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for SET and MYND domain containing 2 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 433 1q32.3 SMYD2 SET and MYND domain containing 2
Mouse - 433 1 H6 Smyd2 SET and MYND domain containing 2
Rat - 433 13q27 Smyd2 SET and MYND domain containing 2
Previous and Unofficial Names
KMT3C
Database Links
BRENDA
CATH/Gene3D
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Structural basis of substrate methylation and Inhibition of SMYD2.
PDB Id:  3S7B
Ligand:  AZ505
Resolution:  2.42Å
Species:  Human
References:  2
Enzyme Reaction
EC Number: 2.1.1.43

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
LLY-507 Hs Inhibition >7.8 pIC50 3
pIC50 >7.8 (IC50 <1.5x10-8 M) [3]
BAY-598 Hs Inhibition 7.6 pIC50 4
pIC50 7.6 (IC50 2.7x10-8 M) [4]
Description: Measuring inhibition of methylation of p53K370 in vitro
AZ505 Hs Inhibition 6.9 pIC50 2
pIC50 6.9 (IC50 1.2x10-7 M) [2]
General Comments
SMYD2 methylates histone and non-histone proteins. The enzyme methylates histone H3 ' at lusine 4 (H3K4me) and dimethylates histone H3 at lysine 36 (H3K36me2) [1]. SMYD2 modulation of chromatin structure is reported to modulate cell proliferation [1].

References

Show »

1. Brown MA, Sims 3rd RJ, Gottlieb PD, Tucker PW. (2006) Identification and characterization of Smyd2: a split SET/MYND domain-containing histone H3 lysine 36-specific methyltransferase that interacts with the Sin3 histone deacetylase complex. Mol. Cancer5: 26. [PMID:16805913]

2. Ferguson AD, Larsen NA, Howard T, Pollard H, Green I, Grande C, Cheung T, Garcia-Arenas R, Cowen S, Wu J et al.. (2011) Structural basis of substrate methylation and inhibition of SMYD2. Structure19 (9): 1262-73. [PMID:21782458]

3. SGC. LLY-507: A chemical probe for SMYD2 protein lysine methyltransferase. Accessed on 03/03/2015. Modified on 03/03/2015. thesgc.org, http://www.thesgc.org/chemical-probes/LLY-507

4. Structural Genomics Consortium. BAY-598 A selective chemical probe for SMYD2. Accessed on 11/12/2015. Modified on 11/12/2015. The Structural Genomics Consortium, http://www.thesgc.org/chemical-probes/BAY-598

How to cite this page

2.1.1.43 Histone methyltransferases (HMTs): SET and MYND domain containing 2. Last modified on 11/12/2015. Accessed on 17/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2714.