1.14.11.- Histone demethylases

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Chromatin modifying enzymes
1.14.11.- Histone demethylases

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

2677

lysine demethylase 1A Show summary »« Hide summary More detailed page go icon to follow link

lysine demethylase 1B Show summary »« Hide summary

lysine demethylase 2A Show summary »« Hide summary More detailed page go icon to follow link

lysine demethylase 2B Show summary »« Hide summary

lysine demethylase 3A Show summary »« Hide summary

lysine demethylase 3B Show summary »« Hide summary

lysine demethylase 4A Show summary »« Hide summary More detailed page go icon to follow link

lysine demethylase 4B Show summary »« Hide summary

lysine demethylase 4C Show summary »« Hide summary

Target Id

2677

Nomenclature

lysine demethylase 4C

Previous and unofficial names

JHDM3C | JMJD2C | Jumonji domain containing 2C | lysine (K)-specific demethylase 4C

Genes

KDM4C (Hs), Kdm4c (Mm), Kdm4c (Rn)

Ensembl ID

ENSG00000107077 (Hs), ENSMUSG00000028397 (Mm), ENSRNOG00000006644 (Rn)

UniProtKB AC

Q9H3R0 (Hs), Q8VCD7 (Mm)

EC number

1.14.11.-

Inhibitors

zavondemstat pIC₅₀ 6.0 – 7.0 [1]

IOX1 pIC₅₀ 6.2 [10]

lysine demethylase 4D Show summary »« Hide summary

lysine demethylase 4E Show summary »« Hide summary More detailed page go icon to follow link

Target Id

2679

Nomenclature

lysine demethylase 4E

Previous and unofficial names

lysine-specific demethylase 4D-like | KDM4DL | JMJD2E | lysine (K)-specific demethylase 4E

Genes

KDM4E (Hs)

Ensembl ID

ENSG00000235268 (Hs)

UniProtKB AC

B2RXH2 (Hs)

Inhibitors

compound 6a [PMID: 18942826] pIC₅₀ 5.8 [7]

lysine demethylase 5A Show summary »« Hide summary More detailed page go icon to follow link

Target Id

2680

Nomenclature

lysine demethylase 5A

Previous and unofficial names

JARID1A | Jumonji/ARID domain-containing protein 1A | lysine (K)-specific demethylase 5A

Genes

KDM5A (Hs), Kdm5a (Mm), Kdm5a (Rn)

Ensembl ID

ENSG00000073614 (Hs), ENSMUSG00000030180 (Mm), ENSRNOG00000010591 (Rn)

UniProtKB AC

P29375 (Hs), Q3UXZ9 (Mm)

Inhibitors

PBIT pIC₅₀ 5.2 [9]

lysine demethylase 5B Show summary »« Hide summary More detailed page go icon to follow link

lysine demethylase 5C Show summary »« Hide summary More detailed page go icon to follow link

Target Id

2682

Nomenclature

lysine demethylase 5C

Previous and unofficial names

Genes

KDM5C (Hs), Kdm5c (Mm), Kdm5c (Rn)

Ensembl ID

ENSG00000126012 (Hs), ENSMUSG00000025332 (Mm), ENSRNOG00000057706 (Rn)

UniProtKB AC

P41229 (Hs), P41230 (Mm)

Inhibitors

PBIT pIC₅₀ 5.3 [9]

Comment

Mutations in this gene are associated with X-linked mental retardation [4,12].

lysine demethylase 5D Show summary »« Hide summary

Target Id	2683
Nomenclature	lysine demethylase 5D
Previous and unofficial names	lysine (K)-specific demethylase 5D
Genes	KDM5D (Hs), Kdm5d (Mm)
Ensembl ID	ENSG00000012817 (Hs), ENSMUSG00000056673 (Mm)
UniProtKB AC	Q9BY66 (Hs), Q62240 (Mm)

lysine demethylase 6A Show summary »« Hide summary More detailed page go icon to follow link

Target Id

2684

Nomenclature

lysine demethylase 6A

Previous and unofficial names

UTX | lysine (K)-specific demethylase 6A | Kdm6a | ubiquitously transcribed tetratricopeptide repeat containing, Y-linked | ubiquitously transcribed tetratricopeptide repeat gene, Y chromosome | ubiquitously transcribed tetratricopeptide repeat gene | ubiquitously transcribed tetratricopeptide repeat containing

Genes

KDM6A (Hs), Kdm6a (Mm), Uty (Rn)

Ensembl ID

ENSG00000147050 (Hs), ENSMUSG00000037369 (Mm), ENSRNOG00000060617 (Rn)

UniProtKB AC

O15550 (Hs), O70546 (Mm)

Inhibitors

GSK-J1 pIC₅₀ 7.3 [2]

GSK-J4 pIC₅₀ 5.2 [2]

KDM5 inhibitor N71 pIC₅₀ <4.2 [3]

lysine demethylase 6B Show summary »« Hide summary More detailed page go icon to follow link

Target Id

2685

Nomenclature

lysine demethylase 6B

Previous and unofficial names

JMJD3 | KDM1 lysine (K)-specific demethylase 6B | lysine (K)-specific demethylase 6B

Genes

KDM6B (Hs), Kdm6b (Mm), Kdm6b (Rn)

Ensembl ID

ENSG00000132510 (Hs), ENSMUSG00000018476 (Mm), ENSRNOG00000037613 (Rn)

UniProtKB AC

O15054 (Hs), Q5NCY0 (Mm)

Inhibitors

GSK-J1 pIC₅₀ 7.2 – 7.6 [2,5]

lysine demethylase 7A Show summary »« Hide summary More detailed page go icon to follow link

Target Id

2686

Nomenclature

lysine demethylase 7A

Previous and unofficial names

lysine (K)-specific demethylase 7A

Genes

KDM7A (Hs), Kdm7a (Mm)

Ensembl ID

ENSG00000006459 (Hs), ENSMUSG00000042599 (Mm)

UniProtKB AC

Q6ZMT4 (Hs)

EC number

1.14.11.-

lysine demethylase 8 Show summary »« Hide summary

PHD finger protein 2 Show summary »« Hide summary

PHD finger protein 8 Show summary »« Hide summary More detailed page go icon to follow link

jumonji domain containing 6, arginine demethylase and lysine hydroxylase C Show summary »« Hide summary More detailed page go icon to follow link

Target Id	2892
Nomenclature	jumonji domain containing 6, arginine demethylase and lysine hydroxylase
Previous and unofficial names	bifunctional arginine demethylase and lysyl-hydroxylase JMJD6 \| jumonji domain containing 6 \| phosphatidylserine receptor \| PSR \| PtdSerR
Genes	JMJD6 (Hs), Jmjd6 (Mm), Jmjd6 (Rn)
Ensembl ID	ENSG00000070495 (Hs), ENSMUSG00000056962 (Mm), ENSRNOG00000000250 (Rn)
UniProtKB AC	Q6NYC1 (Hs), Q9ERI5 (Mm), Q6AYK2 (Rn)
Comment	JMJD6 is the only known histone arginine demethylase in humans.

References

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1. Boloor A, Chen YK, Wallace MB. (2015) Histone demethylase inhibitors. Patent number: WO2015200709A1. Assignee: Quanticel Pharmaceuticals, Inc.. Priority date: 25/06/2015. Publication date: 30/12/2015.

2. Heinemann B, Nielsen JM, Hudlebusch HR, Lees MJ, Larsen DV, Boesen T, Labelle M, Gerlach LO, Birk P, Helin K. (2014) Inhibition of demethylases by GSK-J1/J4. Nature, 514 (7520): E1-2. [PMID:25279926]

3. Horton JR, Woodcock CB, Chen Q, Liu X, Zhang X, Shanks J, Rai G, Mott BT, Jansen DJ, Kales SC et al.. (2018) Structure-Based Engineering of Irreversible Inhibitors against Histone Lysine Demethylase KDM5A. J Med Chem, 61 (23): 10588-10601. [PMID:30392349]

4. Iwase S, Lan F, Bayliss P, de la Torre-Ubieta L, Huarte M, Qi HH, Whetstine JR, Bonni A, Roberts TM, Shi Y. (2007) The X-linked mental retardation gene SMCX/JARID1C defines a family of histone H3 lysine 4 demethylases. Cell, 128 (6): 1077-88. [PMID:17320160]

5. Kruidenier L, Chung CW, Cheng Z, Liddle J, Che K, Joberty G, Bantscheff M, Bountra C, Bridges A, Diallo H et al.. (2012) A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature, 488 (7411): 404-8. [PMID:22842901]

6. Ogasawara D, Suzuki T, Mino K, Ueda R, Khan MN, Matsubara T, Koseki K, Hasegawa M, Sasaki R, Nakagawa H et al.. (2011) Synthesis and biological activity of optically active NCL-1, a lysine-specific demethylase 1 selective inhibitor. Bioorg Med Chem, 19 (12): 3702-8. [PMID:21227703]

7. Rose NR, Ng SS, Mecinović J, Liénard BM, Bello SH, Sun Z, McDonough MA, Oppermann U, Schofield CJ. (2008) Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. J Med Chem, 51 (22): 7053-6. [PMID:18942826]

8. Rose NR, Woon EC, Tumber A, Walport LJ, Chowdhury R, Li XS, King ON, Lejeune C, Ng SS, Krojer T et al.. (2012) Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases. J Med Chem, 55 (14): 6639-43. [PMID:22724510]

9. Sayegh J, Cao J, Zou MR, Morales A, Blair LP, Norcia M, Hoyer D, Tackett AJ, Merkel JS, Yan Q. (2013) Identification of small molecule inhibitors of Jumonji AT-rich interactive domain 1B (JARID1B) histone demethylase by a sensitive high throughput screen. J Biol Chem, 288 (13): 9408-17. [PMID:23408432]

10. Schiller R, Scozzafava G, Tumber A, Wickens JR, Bush JT, Rai G, Lejeune C, Choi H, Yeh TL, Chan MC et al.. (2014) A cell-permeable ester derivative of the JmjC histone demethylase inhibitor IOX1. ChemMedChem, 9 (3): 566-71. [PMID:24504543]

11. SGC. GSK-LSD1 - a chemical probe for LSD1. Accessed on 03/03/2015. Modified on 04/08/2023. thesgc.org, https://www.thesgc.org/chemical-probes/GSK-LSD1

12. Tzschach A, Lenzner S, Moser B, Reinhardt R, Chelly J, Fryns JP, Kleefstra T, Raynaud M, Turner G, Ropers HH et al.. (2006) Novel JARID1C/SMCX mutations in patients with X-linked mental retardation. Hum Mutat, 27 (4): 389. [PMID:16541399]

13. Vazquez-Rodriguez S, Wright M, Rogers CM, Cribbs AP, Velupillai S, Philpott M, Lee H, Dunford JE, Huber KVM, Robers MB et al.. (2019) Design, Synthesis and Characterization of Covalent KDM5 Inhibitors. Angew Chem Int Ed Engl, 58 (2): 515-519. DOI: 10.26434/chemrxiv.7072592.v1 [PMID:30431220]

How to cite this family page

Database page citation:

1.14.11.- Histone demethylases. Accessed on 25/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=869.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Fabbro D, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: Enzymes. Br J Pharmacol. 180 Suppl 2:S289-373.