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2.1.1.43 Histone methyltransferases (HMTs)

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Enzymes

2652
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ASH1 like histone lysine methyltransferase Show summary »

DOT1 like histone lysine methyltransferase Show summary » More detailed page go icon to follow link

euchromatic histone lysine methyltransferase 1 Show summary »

euchromatic histone lysine methyltransferase 2 Show summary »


Target Id 2652
Nomenclature euchromatic histone lysine methyltransferase 2
Previous and unofficial names G9a | KMT1C | euchromatic histone-lysine N-methyltransferase 2 | euchromatic histone lysine N-methyltransferase 2
Genes EHMT2 (Hs), Ehmt2 (Mm), Ehmt2 (Rn)
Ensembl ID ENSG00000236759 (Hs), ENSMUSG00000013787 (Mm), ENSRNOG00000030630 (Rn)
UniProtKB AC Q96KQ7 (Hs), Q9Z148 (Mm)
Inhibitors
UNC0321 pKi 10.2 [19]
UNC0638 pKi 8.5 [35]
UNC0642 pIC50 >8.6 [18]
A-366 pIC50 8.5 [28,34]
UNC0638 pIC50 >7.8 [35]
BIX-01294 pIC50 5.8 [16]
BRD9539 pIC50 5.2 [40]
Comment Pharmacological inhibition of EHMT2 (G9a) re-activates production of fetal haemoglobin in adult erythrocytes in vitro [15,27]. This effect is predicted to offer disease-modifying benefit for patients with β-globinopathies such as sickle cell disease and β-thalassemia. A first-in-class EHMT2 inhibitor, EZM8266, is being developed as a novel therapeutic for sickle cell disease.

EZH1 (enhancer of zeste 1 polycomb repressive complex 2 subunit) Show summary » More detailed page go icon to follow link

EZH2 (enhancer of zeste 2 polycomb repressive complex 2 subunit) Show summary » More detailed page go icon to follow link

lysine methyltransferase 2B Show summary »

lysine methyltransferase 2A Show summary »

lysine methyltransferase 2C Show summary »

lysine methyltransferase 2D Show summary »

lysine methyltransferase 2E (inactive) Show summary »

lysine methyltransferase 5A Show summary »

lysine methyltransferase 5B Show summary »

lysine methyltransferase 5C Show summary »

nuclear receptor binding SET domain protein 1 Show summary »

PR/SET domain 2 Show summary »

SET domain containing 1A, histone lysine methyltransferase Show summary »

SET domain containing 1B, histone lysine methyltransferase Show summary »

SET domain containing 2, histone lysine methyltransferase Show summary »

SET domain containing 7, histone lysine methyltransferase Show summary » More detailed page go icon to follow link

SET domain bifurcated histone lysine methyltransferase 1 Show summary »

SET domain bifurcated histone lysine methyltransferase 2 Show summary »

SET and MYND domain containing 2 Show summary » More detailed page go icon to follow link

suppressor of variegation 3-9 homolog 1 Show summary »

suppressor of variegation 3-9 homolog 2 Show summary »

References

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How to cite this family page

Database page citation:

2.1.1.43 Histone methyltransferases (HMTs). Accessed on 04/08/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=871.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Fabbro D, Kelly E, Mathie A, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Davies JA; CGTP Collaborators. (2019) The Concise Guide to PHARMACOLOGY 2019/20: Enzymes. Br J Pharmacol. 176 Issue S1: S297-S396.