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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).
lysine demethylase 1A Show summary »« Hide summary More detailed page
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lysine demethylase 1B Show summary »« Hide summary
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lysine demethylase 2A Show summary »« Hide summary More detailed page
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lysine demethylase 2B Show summary »« Hide summary
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lysine demethylase 3A Show summary »« Hide summary
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lysine demethylase 3B Show summary »« Hide summary
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lysine demethylase 4A Show summary »« Hide summary More detailed page
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lysine demethylase 4B Show summary »« Hide summary
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lysine demethylase 4C Show summary »« Hide summary
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lysine demethylase 4D Show summary »« Hide summary
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lysine demethylase 4E Show summary »« Hide summary More detailed page
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lysine demethylase 5A Show summary »« Hide summary More detailed page
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lysine demethylase 5B Show summary »« Hide summary More detailed page
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lysine demethylase 5C Show summary »« Hide summary More detailed page
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lysine demethylase 5D Show summary »« Hide summary
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lysine demethylase 6A Show summary »« Hide summary More detailed page
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lysine demethylase 6B Show summary »« Hide summary More detailed page
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lysine demethylase 7A Show summary »« Hide summary More detailed page
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lysine demethylase 8 Show summary »« Hide summary
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PHD finger protein 2 Show summary »« Hide summary
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PHD finger protein 8 Show summary »« Hide summary More detailed page
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jumonji domain containing 6, arginine demethylase and lysine hydroxylase C Show summary »« Hide summary More detailed page
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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]
Database page citation:
1.14.11.- Histone demethylases. Accessed on 11/12/2024. 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.
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