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SET and MYND domain containing 2

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Target id: 2714

Nomenclature: SET and MYND domain containing 2

Family: 2.1.1.43 Histone methyltransferases (HMTs)

Contents:

Gene and Protein Information Click here for help
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 Click here for help
KMT3C
Database Links Click here for help
Alphafold Q9NRG4 (Hs), Q8R5A0 (Mm), Q7M6Z3 (Rn)
BRENDA 2.1.1.43
CATH/Gene3D 1.25.40.10
ChEMBL Target CHEMBL2169716 (Hs)
Ensembl Gene ENSG00000143499 (Hs), ENSMUSG00000026603 (Mm), ENSRNOG00000003583 (Rn)
Entrez Gene 56950 (Hs), 226830 (Mm), 289372 (Rn)
Human Protein Atlas ENSG00000143499 (Hs)
KEGG Enzyme 2.1.1.43
KEGG Gene hsa:56950 (Hs), mmu:226830 (Mm), rno:289372 (Rn)
OMIM 610663 (Hs)
Pharos Q9NRG4 (Hs)
RefSeq Nucleotide NM_020197 (Hs), NM_026796 (Mm), NM_206851 (Rn)
RefSeq Protein NP_064582 (Hs), NP_081072 (Mm), NP_996733 (Rn)
SynPHARM 79343 (in complex with AZ505)
83226 (in complex with BAY-598)
81854 (in complex with LLY-507)
UniProtKB Q9NRG4 (Hs), Q8R5A0 (Mm), Q7M6Z3 (Rn)
Wikipedia SMYD2 (Hs)
Selected 3D Structures Click here for help
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 Click here for help
EC Number: 2.1.1.43

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
LLY-507 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition >7.8 pIC50 4
⤷ pIC50 >7.8 (IC50 <1.5x10-8 M) [4]
BAY-598 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 7.6 pIC50 3
⤷ pIC50 7.6 (IC50 2.7x10-8 M) [3]
Description: Measuring inhibition of methylation of p53K370 in vitro
AZ505 Small molecule or natural product Ligand has a PDB structure 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

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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 Cancer, 5: 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. Structure, 19 (9): 1262-73. [PMID:21782458]

3. SGC. BAY-598 A selective chemical probe for SMYD2. Accessed on 11/12/2015. Modified on 04/08/2023. thesgc.org, https://www.thesgc.org/chemical-probes/BAY-598

4. SGC. LLY-507: A chemical probe for SMYD2 protein lysine methyltransferase. Accessed on 03/03/2015. Modified on 04/08/2023. thesgc.org, https://www.thesgc.org/chemical-probes/LLY-507

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 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2714.