Reference on EC 1.14.99.66 - [histone H3]-N6,N6-dimethyl-L-lysine4 FAD-dependent demethylase
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REF. 
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Lee, M.G.; Wynder, C.; Schmidt, D.M.; McCafferty, D.G.; Shiekhattar, R.
Histone H3 lysine 4 demethylation is a target of nonselective antidepressive medications
Chem. Biol.
13
563-567
2006
Mus musculus
Forneris, F.; Binda, C.; Vanoni, M.A.; Mattevi, A.; Battaglioli, E.
Histone demethylation catalysed by LSD1 is a flavin-dependent oxidative process
FEBS Lett.
579
2203-2207
2005
Homo sapiens
Chen, Y.; Yang, Y.; Wang, F.; Wan, K.; Yamane, K.; Zhang, Y.; Lei, M.
Crystal structure of human histone lysine-specific demethylase 1 (LSD1)
Proc. Natl. Acad. Sci. USA
103
13956-13961
2006
Homo sapiens
Mimasu, S.; Sengoku, T.; Fukuzawa, S.; Umehara, T.; Yokoyama, S.
Crystal structure of histone demethylase LSD1 and tranylcypromine at 2.25 A
Biochem. Biophys. Res. Commun.
366
15-22
2008
Homo sapiens (O60341)
Spedaletti, V.; Polticelli, F.; Capodaglio, V.; Schinina, M.E.; Stano, P.; Federico, R.; Tavladoraki, P.
Characterization of a lysine-specific histone demethylase from Arabidopsis thaliana
Biochemistry
47
4936-4947
2008
Arabidopsis thaliana (Q8VXV7), Arabidopsis thaliana
Katz, D.J.; Edwards, T.M.; Reinke, V.; Kelly, W.G.
A C. elegans LSD1 demethylase contributes to germline immortality by reprogramming epigenetic memory
Cell
137
308-320
2009
Caenorhabditis elegans
Reddy, M.A.; Villeneuve, L.M.; Wang, M.; Lanting, L.; Natarajan, R.
Role of the lysine-specific demethylase 1 in the proinflammatory phenotype of vascular smooth muscle cells of diabetic mice
Circ. Res.
103
615-623
2008
Mus musculus
Forneris, F.; Battaglioli, E.; Mattevi, A.; Binda, C.
New roles of flavoproteins in molecular cell biology: histone demethylase LSD1 and chromatin
FEBS J.
276
4304-4312
2009
Arabidopsis thaliana, Caenorhabditis elegans, Drosophila melanogaster, Homo sapiens
Magerl, C.; Ellinger, J.; Braunschweig, T.; Kremmer, E.; Koch, L.K.; Hoeller, T.; Buettner, R.; Luescher, B.; Guetgemann, I.
H3K4 dimethylation in hepatocellular carcinoma is rare compared with other hepatobiliary and gastrointestinal carcinomas and correlates with expression of the methylase Ash2 and the demethylase LSD1
Hum. Pathol.
41
181-189
2009
Homo sapiens
Karytinos, A.; Forneris, F.; Profumo, A.; Ciossani, G.; Battaglioli, E.; Binda, C.; Mattevi, A.
A novel mammalian flavin-dependent histone demethylase
J. Biol. Chem.
284
17775-17782
2009
Mus musculus
Chau, C.M.; Deng, Z.; Kang, H.; Lieberman, P.M.
Cell cycle association of the retinoblastoma protein Rb and the histone demethylase LSD1 with the Epstein-Barr virus latency promoter Cp
J. Virol.
82
3428-3437
2008
Homo sapiens
Yokoyama, A.; Takezawa, S.; Schuele, R.; Kitagawa, H.; Kato, S.
Transrepressive function of TLX requires the histone demethylase LSD1
Mol. Cell. Biol.
28
3995-4003
2008
Homo sapiens
Tsai, W.W.; Nguyen, T.T.; Shi, Y.; Barton, M.C.
p53-targeted LSD1 functions in repression of chromatin structure and transcription in vivo
Mol. Cell. Biol.
28
5139-5146
2008
Mus musculus
Ciccone, D.N.; Su, H.; Hevi, S.; Gay, F.; Lei, H.; Bajko, J.; Xu, G.; Li, E.; Chen, T.
KDM1B is a histone H3K4 demethylase required to establish maternal genomic imprints
Nature
461
415-418
2009
Mus musculus
Hu, X.; Li, X.; Valverde, K.; Fu, X.; Noguchi, C.; Qiu, Y.; Huang, S.
LSD1-mediated epigenetic modification is required for TAL1 function and hematopoiesis
Proc. Natl. Acad. Sci. USA
106
10141-10146
2009
Mus musculus
Forneris, F.; Binda, C.; Battaglioli, E.; Mattevi, A.
LSD1: oxidative chemistry for multifaceted functions in chromatin regulation
Trends Biochem. Sci.
33
181-189
2008
Drosophila melanogaster, Homo sapiens (O75164)
Huang, Y.; Stewart, T.M.; Wu, Y.; Baylin, S.B.; Marton, L.J.; Perkins, B.; Jones, R.J.; Woster, P.M.; Casero, R.A.
Novel oligoamine analogues inhibit lysine-specific demethylase 1 and induce reexpression of epigenetically silenced genes
Clin. Cancer Res.
15
7217-7228
2009
Homo sapiens
Sharma, S.K.; Wu, Y.; Steinbergs, N.; Crowley, M.L.; Hanson, A.S.; Casero, R.A.; Woster, P.M.
(Bis)urea and (bis)thiourea inhibitors of lysine-specific demethylase 1 as epigenetic modulators
J. Med. Chem.
53
5197-5212
2010
Homo sapiens
Luka, Z.; Moss, F.; Loukachevitch, L.V.; Bornhop, D.J.; Wagner, C.
Histone demethylase LSD1 is a folate-binding protein
Biochemistry
50
4750-4756
2011
Homo sapiens
Liu, L.; Souto, J.; Liao, W.; Jiang, Y.; Li, Y.; Nishinakamura, R.; Huang, S.; Rosengart, T.; Yang, V.; Schuster, M.; Ma, Y.; Yang, J.
Histone demethylase LSD1 is involved in SALL4 mediated transcriptional repression in hematopoietic stem cells
J. Biol. Chem.
288
34719-34728
2013
Mus musculus, Mus musculus C57/BL6J
Mosammaparast, N.; Kim, H.; Laurent, B.; Zhao, Y.; Lim, H.J.; Majid, M.C.; Dango, S.; Luo, Y.; Hempel, K.; Sowa, M.E.; Gygi, S.P.; Steen, H.; Harper, J.W.; Yankner, B.; Shi, Y.
The histone demethylase LSD1/KDM1A promotes the DNA damage response
J. Cell Biol.
203
457-470
2013
Homo sapiens
Nair, V.D.; Ge, Y.; Balasubramaniyan, N.; Kim, J.; Okawa, Y.; Chikina, M.; Troyanskaya, O.; Sealfon, S.C.
Involvement of histone demethylase LSD1 in short-time-scale gene expression changes during cell cycle progression in embryonic stem cells
Mol. Cell. Biol.
32
4861-4876
2012
Mus musculus
Burg, J.M.; Gonzalez, J.J.; Maksimchuk, K.R.; McCafferty, D.G.
Lysine-specific demethylase 1A (KDM1A/LSD1) product recognition and kinetic analysis of full-length histones
Biochemistry
55
1652-1662
2016
Homo sapiens (O60341)
Amano, Y.; Kikuchi, M.; Sato, S.; Yokoyama, S.; Umehara, T.; Umezawa, N.; Higuchi, T.
Development and crystallographic evaluation of histone H3 peptide with N-terminal serine substitution as a potent inhibitor of lysine-specific demethylase 1
Bioorg. Med. Chem.
25
2617-2624
2017
Homo sapiens (O60341)
Liu, Y.W.; Xia, R.; Lu, K.; Xie, M.; Yang, F.; Sun, M.; De, W.; Wang, C.; Ji, G.
LincRNAFEZF1-AS1 represses p21 expression to promote gastric cancer proliferation through LSD1-mediated H3K4me2 demethylation
Mol. Cancer
16
39
2017
Homo sapiens (O60341)
Vyas, R.N.; Meredith, D.; Lane, R.P.
Lysine-specific demethylase-1 (LSD1) depletion disrupts monogenic and monoallelic odorant receptor (OR) expression in an olfactory neuronal cell line
Mol. Cell. Neurosci.
82
1-11
2017
Mus musculus (Q6ZQ88)
Popova, E.Y.; Pinzon-Guzman, C.; Salzberg, A.C.; Zhang, S.S.; Barnstable, C.J.
LSD1-mediated demethylation of H3K4me2 is required for the transition from late progenitor to differentiated mouse rod photoreceptor
Mol. Neurobiol.
53
4563-4581
2016
Mus musculus (Q6ZQ88), Mus musculus
Mimasu, S.; Sengoku, T.; Fukuzawa, S.; Umehara, T.; Yokoyama, S.
Crystal structure of histone demethylase LSD1 and tranylcypromine at 2.25 A
Biochem. Biophys. Res. Commun.
366
15-22
2008
Homo sapiens (O60341)
Janzer, A.; Lim, S.; Fronhoffs, F.; Niazy, N.; Buettner, R.; Kirfel, J.
Lysine-specific demethylase 1 (LSD1) and histone deacetylase 1 (HDAC1) synergistically repress proinflammatory cytokines and classical complement pathway components
Biochem. Biophys. Res. Commun.
421
665-670
2012
Homo sapiens (O60341)
Yang, M.; Culhane, J.C.; Szewczuk, L.M.; Jalili, P.; Ball, H.L.; Machius, M.; Cole, P.A.; Yu, H.
Structural basis for the inhibition of the LSD1 histone demethylase by the antidepressant trans-2-phenylcyclopropylamine
Biochemistry
46
8058-8065
2007
Homo sapiens (O60341)
Gaweska, H.; Henderson Pozzi, M.; Schmidt, D.M.; McCafferty, D.G.; Fitzpatrick, P.F.
Use of pH and kinetic isotope effects to establish chemistry as rate-limiting in oxidation of a peptide substrate by LSD1
Biochemistry
48
5440-5445
2009
Homo sapiens (O60341)
Luka, Z.; Moss, F.; Loukachevitch, L.V.; Bornhop, D.J.; Wagner, C.
Histone demethylase LSD1 is a folate-binding protein
Biochemistry
50
4750-4756
2011
Homo sapiens (O60341)
Marmorstein, R.; Trievel, R.C.
Histone modifying enzymes structures, mechanisms, and specificities
Biochim. Biophys. Acta
1789
58-68
2009
Homo sapiens (O60341)
Costa, R.; Arrigoni, G.; Cozza, G.; Lolli, G.; Battistutta, R.; Izpisua Belmonte, J.C.; Pinna, L.A.; Sarno, S.
The lysine-specific demethylase 1 is a novel substrate of protein kinase CK2
Biochim. Biophys. Acta
1844
722-729
2014
Homo sapiens (O60341)
Gupta, J.; Kumar, S.; Li, J.; Krishna Murthy Karuturi, R.; Tikoo, K.
Histone H3 lysine 4 monomethylation (H3K4me1) and H3 lysine 9 monomethylation (H3K9me1) distribution and their association in regulating gene expression under hyperglycaemic/hyperinsulinemic conditions in 3T3 cells
Biochimie
94
2656-2664
2012
Mus musculus (Q8CIG3)
Duan, Y.; Qin, W.; Suo, F.; Zhai, X.; Guan, Y.; Wang, X.; Zheng, Y.; Liu, H.
Design, synthesis and in vitro evaluation of stilbene derivatives as novel LSD1 inhibitors for AML therapy
Bioorg. Med. Chem.
26
6000-6014
2018
Homo sapiens (O60341)
Kakizawa, T.; Ota, Y.; Itoh, Y.; Suzuki, T.
Histone H3 peptides incorporating modified lysine residues as lysine-specific demethylase 1 inhibitors
Bioorg. Med. Chem. Lett.
28
167-169
2018
Homo sapiens (O60341)
Schulte, J.H.; Lim, S.; Schramm, A.; Friedrichs, N.; Koster, J.; Versteeg, R.; Ora, I.; Pajtler, K.; Klein-Hitpass, L.; Kuhfittig-Kulle, S.; Metzger, E.; Schuele, R.; Eggert, A.; Buettner, R.; Kirfel, J.
Lysine-specific demethylase 1 is strongly expressed in poorly differentiated neuroblastoma implications for therapy
Cancer Res.
69
2065-2071
2009
Homo sapiens (O60341)
Huang, Y.; Stewart, T.M.; Wu, Y.; Baylin, S.B.; Marton, L.J.; Perkins, B.; Jones, R.J.; Woster, P.M.; Casero, R.A.
Novel oligoamine analogues inhibit lysine-specific demethylase 1 and induce reexpression of epigenetically silenced genes
Clin. Cancer Res.
15
7217-7228
2009
Homo sapiens (O60341)
Lan, F.; Nottke, A.C.; Shi, Y.
Mechanisms involved in the regulation of histone lysine demethylases
Curr. Opin. Cell Biol.
20
316-325
2008
Mus musculus (Q6ZQ88), Drosophila melanogaster (Q9VMJ7), Caenorhabditis elegans (Q9XWP6), Mus musculus C57BL/6J (Q6ZQ88)
Brasacchio, D.; Okabe, J.; Tikellis, C.; Balcerczyk, A.; George, P.; Baker, E.K.; Calkin, A.C.; Brownlee, M.; Cooper, M.E.; El-Osta, A.
Hyperglycemia induces a dynamic cooperativity of histone methylase and demethylase enzymes associated with gene-activating epigenetic marks that coexist on the lysine tail
Diabetes
58
1229-1236
2009
Homo sapiens (O60341), Homo sapiens, Mus musculus (Q6ZQ88), Mus musculus C57BL/6 (Q6ZQ88)
Schulz-Fincke, J.; Hau, M.; Barth, J.; Robaa, D.; Willmann, D.; Kuerner, A.; Haas, J.; Greve, G.; Haydn, T.; Fulda, S.; Luebbert, M.; Luedeke, S.; Berg, T.; Sippl, W.; Schuele, R.; Jung, M.
Structure-activity studies on N-substituted tranylcypromine derivatives lead to selective inhibitors of lysine specific demethylase 1 (LSD1) and potent inducers of leukemic cell differentiation
Eur. J. Med. Chem.
144
52-67
2018
Homo sapiens (O60341)
Forneris, F.; Binda, C.; Vanoni, M.A.; Mattevi, A.; Battaglioli, E.
Histone demethylation catalysed by LSD1 is a flavin-dependent oxidative process
FEBS Lett.
579
2203-2207
2005
Homo sapiens (O60341)
Hirano, K.; Namihira, M.
FAD influx enhances neuronal differentiation of human neural stem cells by facilitating nuclear localization of LSD1
FEBS open bio
7
1932-1942
2017
Homo sapiens (O60341)
Tan, A.H.Y.; Tu, W.; McCuaig, R.; Hardy, K.; Donovan, T.; Tsimbalyuk, S.; Forwood, J.K.; Rao, S.
Lysine-specific histone demethylase 1A regulates macrophage polarization and checkpoint molecules in the tumor microenvironment of triple-negative breast cancer
Front. Immunol.
10
1351
2019
Mus musculus (Q6ZQ88), Mus musculus
Culhane, J.C.; Szewczuk, L.M.; Liu, X.; Da, G.; Marmorstein, R.; Cole, P.A.
A mechanism-based inactivator for histone demethylase LSD1
J. Am. Chem. Soc.
128
4536-4537
2006
Homo sapiens (O60341)
Lee, M.G.; Wynder, C.; Bochar, D.A.; Hakimi, M.A.; Cooch, N.; Shiekhattar, R.
Functional interplay between histone demethylase and deacetylase enzymes
Mol. Cell. Biol.
26
6395-6402
2006
Homo sapiens (O60341)
Hino, S.; Sakamoto, A.; Nagaoka, K.; Anan, K.; Wang, Y.; Mimasu, S.; Umehara, T.; Yokoyama, S.; Kosai, K.; Nakao, M.
FAD-dependent lysine-specific demethylase-1 regulates cellular energy expenditure
Nat. Commun.
3
758
2012
Mus musculus (Q6ZQ88)
Liang, Y.; Vogel, J.; Narayanan, A.; Peng, H.; Kristie, T.
Inhibition of the histone demethylase LSD1 blocks alpha-herpesvirus lytic replication and reactivation from latency
Nat. Med.
15
1312-1317
2009
Homo sapiens (O60341)
Matsuda, S.; Baba, R.; Oki, H.; Morimoto, S.; Toyofuku, M.; Igaki, S.; Kamada, Y.; Iwasaki, S.; Matsumiya, K.; Hibino, R.; Kamada, H.; Hirakawa, T.; Iwatani, M.; Tsuchida, K.; Hara, R.; Ito, M.; Kimura, H.
T-448, a specific inhibitor of LSD1 enzyme activity, improves learning function without causing thrombocytopenia in mice
Neuropsychopharmacology
44
1505-1512
2019
Mus musculus (Q6ZQ88)
Lloret-Llinares, M.; Carre, C.; Vaquero, A.; de Olano, N.; Azorin, F.
Characterization of Drosophila melanogaster JmjC+N histone demethylases
Nucleic Acids Res.
36
2852-2863
2008
Drosophila melanogaster (Q9VMJ7)
Zhu, Q.; Liu, C.; Ge, Z.; Fang, X.; Zhang, X.; Straat, K.; Bjoerkholm, M.; Xu, D.
Lysine-specific demethylase 1 (LSD1) is required for the transcriptional repression of the telomerase reverse transcriptase (hTERT) gene
PLoS ONE
3
e1446
2008
Homo sapiens (O60341)
Kong, X.; Ouyang, S.; Liang, Z.; Lu, J.; Chen, L.; Shen, B.; Li, D.; Zheng, M.; Li, K.K.; Luo, C.; Jiang, H.
Catalytic mechanism investigation of lysine-specific demethylase 1 (LSD1) a computational study
PLoS ONE
6
e25444
2011
Homo sapiens (O60341)
Huang, Y.; Greene, E.; Murray Stewart, T.; Goodwin, A.C.; Baylin, S.B.; Woster, P.M.; Casero, R.A.
Inhibition of lysine-specific demethylase 1 by polyamine analogues results in reexpression of aberrantly silenced genes
Proc. Natl. Acad. Sci. USA
104
8023-8028
2007
Homo sapiens (O60341)
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