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Crystal structure and mechanism of human lysine-specific demethylase-1.

Stavropoulos P., Blobel G., Hoelz A.

Nat. Struct. Mol. Biol. 13:626-632(2006) GeneRIF 23028 PDB 2H94 · Mapped (2)
Crystal structure of LSD1 at 2.9-A resolution. LSD1 forms a highly asymmetric closely packed domain structure from which a long helical 'tower' domain protrudes. GeneRIF 23028

Functional interplay between histone demethylase and deacetylase enzymes.

Lee M.G., Wynder C., Bochar D.A., Hakimi M.A., Cooch N., Shiekhattar R.

Mol. Cell. Biol. 26:6395-6402(2006) GeneRIF 23028 · Mapped (10)
These studies reveal an intimate link between the histone demethylase and deacetylase enzymes but also identify histone demethylation as a secondary target of Histone deacetylase (HDAC) inhibitors. GeneRIF 23028

A highly specific mechanism of histone H3-K4 recognition by histone demethylase LSD1.

Forneris F., Binda C., Dall'Aglio A., Fraaije M.W., Battaglioli E., Mattevi A.

J. Biol. Chem. 281:35289-35295(2006) GeneRIF 23028 · Mapped (2)
Epigenetic modifications on histone H3 need to be removed before Lys4 demethylation can efficiently occur. GeneRIF 23028

Androgen receptor coactivators lysine-specific histone demethylase 1 and four and a half LIM domain protein 2 predict risk of prostate cancer recurrence.

Kahl P., Gullotti L., Heukamp L.C., Wolf S., Friedrichs N., Vorreuther R., Solleder G., Bastian P.J., Ellinger J., Metzger E. et al.

Cancer Res. 66:11341-11347(2006) GeneRIF 23028 · Mapped (2)
Data suggest that LSD1 may serve as novel biomarker predictive for prostate cancer with aggressive biology and point to a role of LSD1 in constitutive activation of AR-mediated growth signals. GeneRIF 23028

Cooperative demethylation by JMJD2C and LSD1 promotes androgen receptor-dependent gene expression.

Wissmann M., Yin N., Muller J.M., Greschik H., Fodor B.D., Jenuwein T., Vogler C., Schneider R., Gunther T., Buettner R. et al.

Nat. Cell Biol. 9:347-353(2007) GeneRIF 23028 · Mapped (17)
JMJD2C and LSD1 interact and both demethylases cooperatively stimulate androgen receptor-dependent gene transcription. GeneRIF 23028

trans-2-Phenylcyclopropylamine is a mechanism-based inactivator of the histone demethylase LSD1.

Schmidt D.M., McCafferty D.G.

Biochemistry 46:4408-4416(2007) GeneRIF 23028 · Mapped (2)
Tranylcypromine is a mechanism-based inactivator of LSD1. GeneRIF 23028

The lysine-specific demethylase 1 is required for cell proliferation in both p53-dependent and -independent manners.

Scoumanne A., Chen X.

J. Biol. Chem. 282:15471-15475(2007) GeneRIF 23028 · Mapped (34)
LSD1 has a pro-oncogenic function by modulating pro-survival gene expression and p53 transcriptional activity GeneRIF 23028

Lysine-specific demethylase 1 as a potential therapeutic target.

Stavropoulos P., Hoelz A.

Expert Opin. Ther. Targets 11:809-820(2007) GeneRIF 23028 · Mapped (2)
This review underscores the involvement of the first histone demethylase lysine-specific demethylase-1 in transcriptional regulation and describes a dynamic view of histone methylation by an array of other antagonizing histone-modifying enzymes. GeneRIF 23028

Mechanistic analysis of a suicide inactivator of histone demethylase LSD1.

Szewczuk L.M., Culhane J.C., Yang M., Majumdar A., Yu H., Cole P.A.

Biochemistry 46:6892-6902(2007) GeneRIF 23028 · Mapped (2)
Pull down of spiked and endogenous LSD1 from HeLa cell nuclear extracts set the stage for activity-based demethylase proteomics. GeneRIF 23028

Structural basis of histone demethylation by LSD1 revealed by suicide inactivation.

Yang M., Culhane J.C., Szewczuk L.M., Gocke C.B., Brautigam C.A., Tomchick D.R., Machius M., Cole P.A., Yu H.

Nat. Struct. Mol. Biol. 14:535-539(2007) GeneRIF 23028 PDB 2UXN · Mapped (4)
The LSD1 active site cannot productively accommodate more than three residues on the N-terminal side of the methyllysine explaining its histone H3-K4 specificity. GeneRIF 23028

Recognition of unmethylated histone H3 lysine 4 links BHC80 to LSD1-mediated gene repression.

Lan F., Collins R.E., De Cegli R., Alpatov R., Horton J.R., Shi X., Gozani O., Cheng X., Shi Y.

Nature 448:718-722(2007) GeneRIF 23028 · Mapped (3)
findings couple the function of BHC80 to that of LSD1 and indicate that unmodified H3K4 is part of the 'histone code' GeneRIF 23028

Lysine-specific demethylase 1 (LSD1) Is required for the transcriptional repression of the telomerase reverse transcriptase (hTERT) gene.

Zhu Q., Liu C., Ge Z., Fang X., Zhang X., Straat K., Bjorkholm M., Xu D.

PLoS ONE 3:e1446-e1446(2008) GeneRIF 23028 · Mapped (2)
represses hTERT transcription via demethylating H3-K4 in normal and cancerous cells and together with HDACs participates in the establishment of a stable repression state of the hTERT gene in normal or differentiated malignant cells GeneRIF 23028

Cell cycle association of the retinoblastoma protein Rb and the histone demethylase LSD1 with the Epstein-Barr virus latency promoter Cp.

Chau C.M., Deng Z., Kang H., Lieberman P.M.

J. Virol. 82:3428-3437(2008) GeneRIF 23028 · Mapped (20)
These findings indicate that Epstein-Barr virus C promoter (Cp) is a cell cycle-regulated promoter that is under the control of Rb and the histone demethylase LSD1 in multiple latency types. GeneRIF 23028

Transrepressive function of TLX requires the histone demethylase LSD1.

Yokoyama A., Takezawa S., Schule R., Kitagawa H., Kato S.

Mol. Cell. Biol. 28:3995-4003(2008) GeneRIF 23028 · Mapped (6)
LSD1 is a histone demethylase that is the prime corepressor for TLX GeneRIF 23028

ZNF198 stabilizes the LSD1-CoREST-HDAC1 complex on chromatin through its MYM-type zinc fingers.

Gocke C.B., Yu H.

PLoS ONE 3:e3255-e3255(2008) GeneRIF 23028 · Mapped (15)
ZNF198 through its multiple protein-protein interaction interfaces helps to maintain the intact LSD1-CoREST-HDAC1 complex on specific non-REST-responsive promoters and may also prevent SUMO-dependent dissociation of HDAC1 GeneRIF 23028

Enhancing nuclear receptor-induced transcription requires nuclear motor and LSD1-dependent gene networking in interchromatin granules.

Hu Q., Kwon Y.S., Nunez E., Cardamone M.D., Hutt K.R., Ohgi K.A., Garcia-Bassets I., Rose D.W., Glass C.K., Rosenfeld M.G. et al.

Proc. Natl. Acad. Sci. U.S.A. 105:19199-19204(2008) GeneRIF 23028 · Mapped (2)
The histone lysine demethylase LSD1 is required for these ligand-induced interactive loci to associate with distinct interchromatin granules long thought to serve as "storage" sites for the splicing machinery GeneRIF 23028

Involvement of histone demethylase LSD1 in Blimp-1-mediated gene repression during plasma cell differentiation.

Su S.T., Ying H.Y., Chiu Y.K., Lin F.R., Chen M.Y., Lin K.I.

Mol. Cell. Biol. 29:1421-1431(2009) GeneRIF 23028 · Mapped (16)
Blimp-1 binding to its target sites is accompanied by LSD1 binding to those same sites and LSD1 binding correlates with histone modifications of accessible chromatin. GeneRIF 23028

Lysine-specific demethylase 1 is strongly expressed in poorly differentiated neuroblastoma: implications for therapy.

Schulte J.H., Lim S., Schramm A., Friedrichs N., Koster J., Versteeg R., Ora I., Pajtler K., Klein-Hitpass L., Kuhfittig-Kulle S. et al.

Cancer Res. 69:2065-2071(2009) GeneRIF 23028 · Mapped (2)
inhibition of LSD1 reprograms the transcriptome of neuroblastoma cells and inhibits neuroblastoma xenograft growth. GeneRIF 23028

LSD1-mediated epigenetic modification is required for TAL1 function and hematopoiesis.

Hu X., Li X., Valverde K., Fu X., Noguchi C., Qiu Y., Huang S.

Proc. Natl. Acad. Sci. U.S.A. 106:10141-10146(2009) GeneRIF 23028 · Mapped (14)
LSD1 may negatively regulate TAL1-mediated transcription and suggest that the dynamic regulation of TAL1-associated LSD1/HDAC1 complex may determine the onset of erythroid differentiation programs. GeneRIF 23028

Gfi-1B promoter remains associated with active chromatin marks throughout erythroid differentiation of human primary progenitor cells.

Laurent B., Randrianarison-Huetz V., Kadri Z., Romeo P.H., Porteu F., Dumenil D.

Stem Cells 27:2153-2162(2009) GeneRIF 23028 · Mapped (8)
Analysis of chromatin modification patterns shows that LSD1 are recruited to the c-myc promoter leading to appearance of repressive chromatin marks. GeneRIF 23028

LSD1 is a subunit of the NuRD complex and targets the metastasis programs in breast cancer.

Wang Y., Zhang H., Chen Y., Sun Y., Yang F., Yu W., Liang J., Sun L., Yang X., Shi L. et al.

Cell 138:660-672(2009) GeneRIF 23028 · Mapped (2)
Study reports that LSD1 is an integral component of the Mi-2/nucleosome remodeling and deacetylase (NuRD) complex and demonstrated that LSD1 inhibits the invasion of breast cancer cells in vitro. GeneRIF 23028

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.

Magerl C., Ellinger J., Braunschweig T., Kremmer E., Koch L.K., Holler T., Buttner R., Luscher B., Gutgemann I.

Hum. Pathol. 41:181-189(2010) GeneRIF 23028 · Mapped (6)
high dimethylation of histone H3 at lysine 4 expression is rare in hepatocellular carcinoma compared with other carcinomas possibly due to complex epigenetic regulation involving LSD1 GeneRIF 23028

Novel oligoamine analogues inhibit lysine-specific demethylase 1 and induce reexpression of epigenetically silenced genes.

Huang Y., Stewart T.M., Wu Y., Baylin S.B., Marton L.J., Perkins B., Jones R.J., Woster P.M., Casero R.A. Jr.

Clin. Cancer Res. 15:7217-7228(2009) GeneRIF 23028 · Mapped (3)
when LSD1 is inhibited by oligoamine analogues aberrantly silenced genes are reexpressed GeneRIF 23028

Lysine-specific demethylase 1 (LSD1) is highly expressed in ER-negative breast cancers and a biomarker predicting aggressive biology.

Lim S., Janzer A., Becker A., Zimmer A., Schule R., Buettner R., Kirfel J.

Carcinogenesis 31:512-520(2010) GeneRIF 23028 · Mapped (2)
Very high LSD1 levels oocur in estrogen receptor (ER)-negative breast tumors. LSD1 is recruited to the promoters of proliferation-associated genes like p21 ERBB2 and CCNA2. GeneRIF 23028

Genetic alterations and changes in expression of histone demethylases in prostate cancer.

Suikki H.E., Kujala P.M., Tammela T.L., van Weerden W.M., Vessella R.L., Visakorpi T.

Prostate 70:889-898(2010) GeneRIF 23028 · Mapped (10)
identification of genetic alterations & expression changes of LSD1 JHDM2A & GASC1 in prostate cancer (PC); as no genetic alterations & only modest expression changes were found it is unlikely they play a major role in progression of PC GeneRIF 23028

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