Publications

Peñarando J., Willmann D., Sum M., Jia Y., Berlin C., Braun L.M., Chen Z., Urban S., Jung M., Duteil D., Metzger D., Gratzke C., Zeiser R., Greschik H,. Schüle R., Metzger E. (2026). KMT9 drives T cell exclusion and dysfunction by promoting PMN-MDSCs infiltration and ARG1 expression in prostate cancer. Mol Cancer 25(1):223. doi: 10.1186/s12943-026-02801-8.

Greschik H, Friedrich F, Seifert L, Mousavizadeh F, Fiorentino F, Walz J, Zhang L, Li J, Fabbrizi E, Tomassi S, Panahi F, Papenkordt N, Wurnig SL, Osterroth J, Strasser AM, Ruprecht J, Moumbock AFA, Hügle M, Sum M, Peng L, Wang S, Baniahmad AA, Pulido-Cortés L, Timmers HTM, Flaig R, Metzger E, Breit B, Einsle O, Günther S, Rotili D, Mai A, Schüle R, Jung M.  (2026) . Development of High-Affinity CHD1 Chromodomain Inhibitors. J Med Chem. 69(10):12020-12047. doi: 10.1021/acs.jmedchem.5c03690.

Mak C. S. L., Zhu M, Fu J., Liang X., Wang X., Yuan F., Wang F., Hoang A. G., Song X., Shepherd P,. Liang D., Suh J., Contreras J., Dang T., Yan C., Figueroa B., Mazzocco M., Luo A., Pradhan B., Park J., Bashir M., Zhang M., Metzger E., Schüle R., Jain A. K., Karasik E., Frigo D., Foster B. A., Lee M. G., Corn P., Logothetis C. J., Aparicio A., Navone N., Troncoso P., Tan Z., Zhang J., Lin S. H., Wang G (2025). KDM4A promotes NEPC progression through regulation of MYC expression. Cancer Lett. 638:218184. doi: 10.1016/j.canlet.2025.218184.

Fetsch V., Schwöbel L.F., Ozyerli-Goknar E., Stell A.V., Punta M., Plenge T., Klaus T., Gupta M.K., Andrieux G., Shoumariyeh K., Pfeiffer S., Corrales E., Schlenke L., Baniadam H., Brandl S.M., Andreis M., Remen M., Hartmann A., Grueter K., Zwick M., Köhler N., Kuban M., Metzger E., Rummelt C., Duyster J. Börries M., Hofmann M., Färber J., Braun L.M., Zähringer A., Lübbert M., Toffalori C., Vago L., Heidel F.H., Minguet S., Apostolova P., Feuchtinger T., Maas-Bauer K., Blaeschke F,. Kühn M.W.M., Timmers M., Wertheimer T., Perner F., Zeiser R.  (2025). Menin inhibition enhances graft-versus-leukemia effects by T-cell activation and endogenous retrovirus induction in AML. Blood. doi: 10.1182/blood.2025029712.

Pulido-Cortés L., Gielingh H., Thijssen V., Liu M., Yoshisada R., Romão Soares L., Nizamuddin S., Friedrich F., Greschik H., Peng L. Vargas Honorato R., Jung M., Bonvin A.M.J.J., Biniossek M.L., Schüle R., Jongkees S., van Ingen H., Timmers H.T.M. (2025). Molecular determinants for recognition of serotonylated chromatin. Nucleic Acids Res. 53(13):gkaf612. doi: 10.1093/nar/gkaf612. 

Staehle H.F., Koellerer C., Staehle A.M., Schulze J., Eble P., Müller A., Zell F., Müller J.M., Perner F., Attia A., Mallm J.P., Pozdnyakova O., Rippe K., Brors B., Feuerbach L., Imbusch C.D., Metzger E., Schüle R., Pahl H.L., Jutzi J.S. (2025). Lysine-specific demethylase 1 regulates hematopoietic stem cell expansion and myeloid cell differentiation. Cell Death Dis. 16(1):619. doi: 10.1038/s41419-025-07951-z.

Kruszewski M., Schmoor C., Berg T., Rehman U.U., Schittenhelm M., Götze K., Kündgen A., Pabst C., Ma T., Frey A., Stomper J., Pfeifer D., Metzger E., Jung J., Moschallski K., Thomas J., Bug G., Duyster J., Jung M., Schüle R., Wäsch R., Grishina O., Lübbert M. (2025). Sensitization of Non-M3 Acute Myeloid Leukemia Blasts to All-Trans Retinoic Acid by the LSD1 Inhibitor Tranylcypromine: TRANSATRA Phase I Study. Eur J Haematol. 115(3):266-277. doi: 10.1111/ejh.14426.

Kinzler M.N., Metzger E., Schulz R., Bankov K., Ramos-Triguero A., Schulze F., Gretser S., Abedin N., Wiegering A., Zeuzem S., Walter D., Reis H., Schüle R., Wild P.J. (2025). Overexpression of KMT9α is associated with poor outcome in cholangiocarcinoma patients. J Cancer Res Clin Oncol. 151(5):161. doi: 10.1007/s00432-025-06214-w.

Schmidt S.K., Fischer S., El Ahmad Z., Schmid R., Metzger E., Schüle R., Hellerbrand C., Arkudas A., Kengelbach-Weigand A., Kappelmann-Fenzl M., Bosserhoff A.K. (2025). Modeling a mesenchymal cell state by bioprinting for the molecular analysis of dormancy in melanoma. Mater Today Bio.  doi: 10.1016/j.mtbio.2025.101674.

Wang S., Barthes N.P.F., Urban S., Hazai V.I., Klein S.O., Pappert T., Kümmel P., Heller N., Bacher J., Staudt M., Ruprecht J., Peng L., Sum M., Berlin C., Sarraf D., Regenass P., Warstat R., Walz J,. Mishra P., Zhang L., Einsle O., Günther S., Breit B., Metzger E., Jung M., Schüle R. (2025). Structure-Guided Design of a KMT9 Inhibitor Prodrug with Cellular Activity. J Med Chem. doi: 10.1021/acs.jmedchem.4c02953.

Jia Y., Wang S., Urban S., Müller J.M., Sum M., Wang Q., Bauer H., Schulte U., Rampelt H., Pfanner N., Schüle K.M., Imhof A,. Forné I., Berlin C., Sigle A., Gratzke C., Greschik H., Metzger E., Schüle R. (2025). Mitochondrial KMT9 methylates DLAT to control pyruvate dehydrogenase activity and prostate cancer growth. Nat Commun. 16(1):1191. doi: 10.1038/s41467-025-56492-8.

Colcerasa A., Friedrich F., Melesina J., Moser P., Vogelmann A., Tzortzoglou P., Neuwirt E., Sum M., Robaa D., Zhang L., Ramos-Morales E., Romier C., Einsle O., Metzger E., Schüle R., Groß O. Sippl W., Jung M. (2024). Structure-Activity Studies of 1,2,4-Oxadiazoles for the Inhibition of the NAD⁺-Dependent Lysine Deacylase Sirtuin 2.  J Med Chem. 67(12):10076-10095. doi: 10.1021/acs.jmedchem.4c00229.

Cai Q., Sahu R., Ueberschlag-Pitiot V., Souali-Crespo S., Charvet C., Silem I., Cottard F., Ye T., Taleb F., Metzger E., Schüle R., Billas IML., Laverny G., Metzger, D., Duteil D. (2024). LSD1 inhibition circumvents glucocorticoid-induced muscle wasting of male mice. Nat Commun. 15(1):3563. doi:10.1038/s41467-024-47846-9.

Seitz J., Auth M., Prinz T., Hau M., Tzortzoglou P., Schulz-Fincke J., Schmidtkunz K., Baniahmad AA., Willmann D., Metzger E., Hein L., Preissl S., Schüle R., Jung M. (2024). Soft drug inhibitors for the epigenetic targets lysine-specific demethylase 1 and histone deacetylases. Arch Pharm (Weinheim) e2400450. doi: 10.1002/ardp.202400450.

Totonji S., Ramos-Triguero A., Willmann D., Sum M., Urban S., Bauer H. Rieder A., Wang S., Greschik H., Metzger E., Schüle R. (2024). Lysine Methyltransferase 9 (KMT9) Is an Actionable Target in Muscle-Invasive Bladder Cancer. Cancers (Basel). 16(8):1532. doi: 10.3390/cancers16081532.

Wang S., Klein SO., Urban S., Staudt M., Barthes NPF., Willmann D., Bacher J., Sum M., Bauer H., Peng L., Rennar GA., Gratzke C., Schüle KM., Zhang L., Einsle O., Greschik H., MacLeod C., Thomson CG., Jung M., Metzger E., Schüle R. (2024). Structure-guided design of a selective inhibitor of the methyltransferase KMT9 with cellular activity. Nature Communications 15, Article number: 43. doi: 10.1038/s41467-023-44243-6.

Berlin C., Cottard F., Willmann D., Urban S., Tirier SM., Marx L., Rippe K., Schmitt M., Petrocelli V., Greten FR., Fichtner-Feigl S., Kesselring R., Metzger E., Schüle R. (2022). KMT9 Controls Stemness and Growth of Colorectal Cancer. Cancer Res. 15;82(2):210-220. doi: 10.1158/0008-5472.

Herrlinger EM., Hau M., Redhaber DM., Greve G., Willmann D., Steimle S., Müller M., Lübbert M., Miething CC., Schüle R., Jung M. (2020 ). Nitroreductase-Mediated Release of Inhibitors of Lysine-Specific Demethylase 1 (LSD1) from Prodrugs in Transfected Acute Myeloid Leukaemia Cells. Chembiochem. 21(16):2329-2347. doi: 10.1002/cbic.202000138.

Baumert H.M., Metzger E., Fahrner, M., George J., Thomas R.K., Schilling O. and Schüle R. (2020). Depletion of histone methyltransferase KMT9 inhibits lung cancer cell proliferation by inducing non-apoptotic cell death. Cancer Cell International 20,  doi: 10.1186/s12935-020-1141-2.

Haydn T., Kehr S., Willmann D., Metzger E., Schüle R., Fulda S. (2020). Next-generation sequencing reveals a novel role of lysine-specific demethylase 1 in adhesion of rhabdomyosarcoma cells. Int J Cancer. 146(12):3435-3449. doi: 10.1002/ijc.32806.

Xiong Y., Greschik H., Johansson C., Seifert L., Bacher J., Park KS., Babault N., Martini M., Fagan V., Li F., Chau I., Christott T., Dilworth D., Barsyte-Lovejoy D., Vedadi M., Arrowsmith CH., Brennan P., Fedorov O., Jung M., Farnie G., Liu J., Oppermann U., Schüle R., Jin J. (2019). Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1). J Med Chem.,  Epub Jul 24, doi: 10.1021/acs.jmedchem.9b00522.

Metzger, E., Wang, S., Urban, S., Willmann, D., Schmidt, A., Offermann, A., Allen, A., Sum, M., Obier, N., Cottard, F., Ulferts, S., Preca, B.-T., Hermann, B., Maurer, J., Greschik, H., Hornung, V., Einsle, O., Perne, S., Imhof, A., Jung, M. and Schüle R. (2019). KMT9 mono-methylates histone H4 Lysine 12 and controls proliferation of prostate cancer cells. Nat. Struct. Mol. Biol. 26, 361-371.

Yan, X., Greschik, H., Johansson, C., Seifert, L., Bacher, J., Park, K-s., Babault, N., Martini, M., Fagan, V., Li, F., Chau, I., Christott, T., Dilworth, D., Barsyte-Lovejoy, D., Vedadi, M., Arrowsmith, C., Brennan, P., Fedorov, O., Jung, M., Farnie, G., Liu, J., Oppermann, U., Schüle, R. and Jin, J. (2019). Discovery of a potent and selective fragment-like inhibitor of methyllysine reader protein Spindlin 1 (SPIN1). J. Med. Chem., doi: 10.1021/acs.jmedchem.9b00522.

Fagan, V., Johansson, C., Gileadi, C., Monteiro, O., Dunford, J., Nibhani, R., Philpott, M., Malzahn, J., Wells, G.,Farham, R., Cribbs, A., Halidi, N., Li, F.,Chau I., Greschik, H., Velupillai, S., Al-lali-Hassani, A., Bennett, J., Christott, T., Giroud, C., Lewis, A.M., Huber, K.VM, Athanasou, N., Bountra, C., Jung, M. Schüle, R., Vedadi, M., Arrowsmith, C., Xiong, Y.,Jin, J., Fedorov, O., Farnie, G., Brennan, P.E. and Oppermann, U. (2019). A chemical probe for Tudor domain protein SPIN1 to investigate chromatin function. ChemRxi, doi: 10.26434/chemrxiv.7673129.

Barth, J., Abou-El-Ardat, K., Dalic, D., Kurrle, N., Scheder, A-M., Mohr, S., Schütte, J., Vassen, L., Greve, G., Schulz-Fincke, J., Schmitt, M., Tosic, M., Metzger, E., Bug, G., Khandanpour, C., Wagner, S., Lübbert, M., Jung, M., Serve, H., Schüle, R. and Tobias Berg. (2019). LSD1 inhibition by tranylcypromine derivatives interferes with GFI1-mediated repression of PU.1 target genes and induces differentiation in AML. Leukemia. 33,1411-1426.

Tosic M., Allen A., Willmann D., Lepper C., Kim J., Duteil D., Schüle R. (2018). Lsd1 regulates skeletal muscle regeneration and directs the fate of satellite cells. Nat Commun. 9(1):366. doi: 10.1038/s41467-017-02740-5.

Duteil, D., Tourrette, Y., Eberlin, A., Willmann, D., Patel, D., Friedrichs, N., Müller, J.M. and Schüle, R. (2018). The histone acetyltransferase inhibitor Nir regulates epidermis development. Development 145, doi: 10.1242/dev.158543.

Greschik H., Duteil D., Messaddeq N., Willmann D., Arrigoni L., Sum M., Jung M., Metzger D., Manke T., Günther T., Schüle R. (2017). The histone code reader Spin1 controls skeletal muscle development. Cell Death Dis. 23;8(11):e3173. doi: 10.1038/cddis.2017.468.

Koch, S.C., Del Barrio, M.G., Dalet, A., Gatto, G., Günther, T., Zhang, J., Seidler, B., Saur, D., Schüle, R. and Goulding, M. (2017) RORbeta spinal interneurons gate sensory transmission during locomotion to secure a fluid walking gait. Neuron 96, 1-13.

Metzger E., Stepputtis S.S., Strietz J., Preca B.T., Urban S., Willmann D., Allen A., Zenk F., Iovino N., Bronsert P., Proske A., Follo M., Boerries M., Stickeler E., Xu J., Wallace M.B., Stafford J.A., Kanouni T., Maurer J., Schüle R. (2017. KDM4 Inhibition Targets Breast Cancer Stem-like Cells. Cancer Res. 77(21):5900-5912. doi: 10.1158/0008-5472

Duteil, D., Tosic, M., Willmann, D., Georgiadi, A., Kanouni, T. and Schüle, R. (2017). Lsd1 prevents age-programed loss of beige adipocytes. PNAS 114(20):5265-5270.

Schulz-Fincke, J., Hau, M., Barth, J., Robaa, D., Willmann, D., Kürner, A., Haas, J., Greve, G., Haydn, T., Fulda, S., Lübbert, M., Lüdeke, S., Berg, T., Sippl, W., Schüle, R. and Jung, M. (2017). 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.

Castex J., Willmann D., Kanouni T., Arrigoni L., Li Y., Friedrich M., Schleicher M., Wöhrle S., Pearson M., Kraut N., Méret M., Manke T., Metzger E., Schüle R., Günther T. (2017 ) Inactivation of Lsd1 triggers senescence in trophoblast stem cells by induction of Sirt4. Cell Death Dis. 8(2):e2631. doi: 10.1038/cddis.2017.48.

Scionti I., Hayashi S., Mouradian S., Girard E., Esteves de Lima J., Morel V., Simonet T., Wurmser M., Maire P., Ancelin K., Metzger E., Schüle R., Goillot E., Relaix F., Schaeffer L.  (2017). LSD1 Controls Timely MyoD Expression via MyoD Core Enhancer Transcription. Cell Rep. 18(8):1996-2006. doi: 10.1016/j.celrep.2017.01.078.

Haydn T., Metzger E., Schuele R., Fulda S. (2017). Concomitant epigenetic targeting of LSD1 and HDAC synergistically induces mitochondrial apoptosis in rhabdomyosarcoma cells. Cell Death Dis. 8(6):e2879. doi: 10.1038/cddis.2017.239.

Duteil, D., Tosic, M., Lausecker, F., L, Nenseth, H. Z., Müller, JM., Urban, S., Willmann, W., Petroll, K., Messaddeq, N., Arrigoni, L., Manke, T-, Kornfeld, J.-W., Brüning, J.C., Zagoriy, V., Meret, M., Dengjel, J., Kanouni, T. and Schüle, R. (2016). Lsd1 ablation triggers metabolic reprogramming of brown adipose tissue. Cell Rep. doi: 10.1016/j.celrep.2016.09.053

Rohde M., Sievers E., Janzer A., Willmann D., Egert A., Schorle H., Schüle R., Kirfel J. (2016). Overexpression of histone demethylase Fbxl10 leads to enhanced migration in mouse embryonic fibroblasts. Exp Cell Res. S0014-4827(16)30265-8.

Ostrovskyi D., Rumpf T., Eib J., Lumbroso A., Slynko I., Klaeger S., Heinzlmeir S., Forster M., Gehringer M., Pfaffenrot E., Bauer S.M., Schmidtkunz K., Wenzler S., Metzger E., Kuster B., Laufer S., Schüle R., Sippl W., Breit B., Jung M. (2016). Tofacitinib and analogs as inhibitors of the histone kinase PRK1 (PKN1). Future Med Chem. 8(13):1537-51..

Slynko I., Schmidtkunz K., Rumpf T., Klaeger S., Heinzlmeir S., Najar A., Metzger E., Kuster B., Schüle R., Jung M., Sippl W. (2016). Identification of Highly Potent Protein Kinase C-Related Kinase 1 Inhibitors by Virtual Screening, Binding Free Energy Rescoring, and in vitro Testing. ChemMedChem. 11(18):2084-2094.

Wagner T., Greschik H., Burgahn T., Schmidtkunz K., Schott A.K., McMillan J., Baranauskienė L., Xiong Y., Fedorov O., Jin J., Oppermann U., Matulis D., Schüle R., Jung M. (2016). Identification of a small-molecule ligand of the epigenetic reader protein Spindlin1 via a versatile screening platform. Nucleic Acids Res. 44(9):e88.

Ancelin K., Syx L., Borensztein M., Ranisavljevic N., Vassilev I., Briseño-Roa L., Liu T., Metzger E., Servant N., Barillot E., Chen C.J., Schüle R., Heard E. (2016). Maternal LSD1/KDM1A is an essential regulator of chromatin and transcription landscapes during zygotic genome activation. Elife  2: 5.

Metzger E., Willmann D., McMillan J., Forne I., Metzger P., Gerhardt S., Petroll K., von Maessenhausen A., Urban S., Schott A.K., Espejo A., Eberlin A., Wohlwend D., Schule K.M., Schleicher M., Perner S., Bedford M.T., Jung M., Dengjel J., Flaig R., Imhof A., Einsle O., Schüle R. (2016). Assembly of methylated KDM1A and CHD1 drives androgen receptor-dependent transcription and translocation. Nat. Struct. Mol. Biol. 23(2): 132-139.

Franz H., Greschik H., Willmann D., Ozretic L., Jilg C.A., Wardelmann E., Jung M., Buettner R., Schüle R. (2015). The histone code reader SPIN1 controls RET signaling in liposarcoma. Oncotarget 6 (7), 4773-4789.    

Fedorov O., Castex J., Tallant C., Owen D.R., Martin S., Aldeghi M., Monteiro O., Filippakopoulos P., Picaud S., Trzupek J.D., Gerstenberger B.S., Bountra C., Willmann D., Wells C., Philpott M., Rogers C., Biggin P.C., Brennan P.E., Bunnage M.E., Schüle R., Günther T., Knapp S., Muller S. (2015). Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance. Sci. Adv. 2015; 1 (10), e1500723-e1500723. 

Rönsch K., Jägle S., Rose K., Seidl M., Baumgartner F., Freihen V., Yousaf A., Metzger E., Lassmann S., Schüle R., Zeiser R., Michoel T., Hecht A. (2015). SNAIL1 combines competitive displacement of ASCL2 and epigenetic mechanisms to rapidly silence the EPHB3 tumor suppressor in colorectal cancer. Mol. Oncol. 9 (2), 335-354.

Jilg C.A., Ketscher A., Metzger E., Hummel B., Willmann D., Rüsseler V., Drendel V., Imhof A., Jung M., Franz H., Hölz S., Krönig M., Müller J.M., Schüle R. (2014). PRK1/PKN1 controls migration and metastasis of androgen-independent prostate cancer cells. Oncotarget.  5(24), 12646-64.

Ketscher A., Jilg C.A., Willmann D., Hummel B., Imhof A., Rüsseler V., Hölz S., Metzger E, Müller J.M., Schüle R. (2014). LSD1 controls metastasis of androgen-independent prostate cancer cells through PXN and LPAR6. Oncogenesis  3: e120.

Duteil D., Metzger E., Willmann D., Karagianni P., Friedrichs N., Greschik H., Günther T., Buettner R., Talianidis I., Metzger D., Schüle R. (2014). LSD1 promotes oxidative metabolism of white adipose tissue. Nat. Commun. 5:4093.

Cai C., He H.H., Gao S., Chen S., Yu Z., Gao Y., Chen S., Chen M.W., Zhang J., Ahmed M., Wang Y., Metzger E., Schüle R., Liu X.S., Brown M., Balk S.P. (2014). Lysine-specific demethylase 1 has dual functions as a major regulator of androgen receptor transcriptional activity. Cell Rep. 9(5), 1618-27.

Pohlkamp T., Steller L., May P., Günther T., Schüle R., Frotscher M., Herz J., Bock H.H. (2014). Generation and characterization of an Nse-CreERT2 transgenic line suitable for inducible gene manipulation in cerebellar granule cells. Plos One 9 (6), e100384-e100384.

Slynko I., Scharfe M., Rumpf T., Eib J., Metzger E., Schüle R., Jung M., Sippl W. (2014.) Virtual screening of PRK1 inhibitors: ensemble docking, rescoring using binding free energy calculation and QSAR model development. J. Chem. Inf. Model. 54 (1), 138-150.

Ray S.K., Li H.J., Metzger E., Schüle R., Leiter A.B. (2014). CtBP and Associated LSD1 are Required for Transcriptional Activation by NeuroD1 in Gastrointestinal Endocrine Cells. Mol Cell Biol. 34(12), 2308-17.

Schmitt, M.L., Ladwein, K.I., Carlino, L., Schulz-Fincke, J., Willmann, D., Metzger, E., Schilcher, P., Imhof, A., Schüle, R., Sippl, W. and Jung, M. (2014). Heterogeneous antibody based activity assay for lysine specific demethylase 1 (LSD1) on a histone peptide substrate. J. Biomol. Screen 19(6), 973-978.

Zhu, D., Hölz, S., Metzger, E., Pavlovic, M., Jandausch, A., Jilg, C., Galgoczy, P., Herz, C., Moser, M., Metzger, D., Günther, T., Arnold, S.J. and Schüle, R. (2014). Lsd1 regulates differentiation onset and migration of trophoblast stem cells Nat. Commun. 5, 3174-3184.  

Slynko, I., Scharfe, M., Rumpf, T., Eib, J., Metzger, E., Schüle, R., Jung, M. and  Sippl, W. (2014). Virtual Screening of PRK1 Inhibitors: Ensemble Docking, RescoringUsing Binding Free Energy Calculation and QSAR Model Development. J Chem Inf Model. 54, 138-50.

Schmitt, M.L., Hauser, A.T., Carlino, L., Pippel, M., Schulz-Fincke, J., Metzger, E., Willmann, D., Yiu, T., Barton, M., Schüle, R., Sippl, W. and Jung, M. (2013). Nonpeptidic propargy-lamines as inhibitors of lysine specific demethylase 1 (LSD1) with cellular activity. J Med Chem. 56, 7334-7342.  

Köhler, J., Erlenkamp, G., Eberlin, A., Rumpf, T., Slynko, I., Metzger, E., Schüle, R., Sippl, W. and Jung. M. (2012). Lestaurtinib inhibits histone phosphorylation and androgen-dependent gene expression in prostate cancer cells. PLoS One 7(4):e34973. Epub 2012 Apr 20.

Willmann, D., Lim, S., Wetzel, S., Metzger, E., Jandausch, A., Wilk, W., Jung, M., Forne, I., Imhof, A., Janzer, A., Kirfel, J., Waldmann, H., Schule, R., Buettner, R. (2012). Impairment of prostate cancer cell growth by a selective and reversible lysine-specific demethylase 1 inhibitor. Int J Cancer. 131, 2704-9.

Kaufmann, K.B., Gründer, A., Hadlich, T., Wehrle, J., Gothwal, M., Bogeska, R., Seeger, T.S., Kayser, S., Pham, K.B., Jutzi, J.S., Ganzenmüller, L., Steinemann, D., Schlegelberger, B., Wagner, J.M., Jung, M., Will, B., Steidl, U., Aumann, K., Werner, M., Günther, T., Schule, R., Rambaldi, A., Pahl, H.L. (2012). A novel murine model of myeloproliferative disorders generated by overexpression of the transcription factor NF-E2. J Exp Med. 209, 35-50.

Hauser A.T., Bissinger E.M., Metzger E., Repenning A., Bauer U.M., Mai A., Schule R., Jung M. Screening assays for epigenetic targets using native histones as substrates (2012). J Biomol Screen 17(1), 18-26.

Bissinger, E.M., Heinke, R., Spannhoff, A., Eberlin, A., Metzger, E., Cura, V., Hassenboehler, P., Cavarelli, J., Schule, R., Bedford, M.T., et al. (2011). Acyl derivatives of p-aminosulfonamides and dapsone as new inhibitors of the arginine methyltransferase hPRMT1. Bioorg Med Chem 19, 3717-3731.

Arampatzidou, M., Mayer, K., Iolyeva, M.E., Asrat, S.G., Ravichandran, M., Günther, T., Schüle, R., Reinheckel, T. and Brix, K. (2011). Studies of intestinal morphology and cathepsin B expression in a transgenic mouse aiming at intestine-specific expression of Cath B-EGFP. Biol. Chem. 392, 983-993.

Nair, S S, Nair, B C, Cortez, V, Chakravarty, D, Metzger, E, Schüle, R, Brann, D W, Tekmal, R R, Vadlamudi, R K (2010). PELP1 is a reader of histone H3 methylation that facilitates oestrogen receptor-alpha target gene activation by regulating lysine demethylase 1 specificity. EMBO reports 11, 438-44.

Metzger E, Imhof A, Patel D, Kahl P, Hoffmeyer K, Friedrichs N, Müller JM, Greschik H, Kirfel J, Ji S, Kunowska N, Beisenherz-Huss C, Günther T, Buettner R, Schüle R. (2010). Phosphorylation of histone H3T6 by PKCbeta(I) controls demethylation at histone H3K4. Nature 464, 792-6.

Schulte, EC, Slawik, H, Schüle, R, Gunther, T, Hüll, M (2009). Alterations in excitotoxicity and prostaglandin metabolism in a transgenic mouse model of Alzheimer's disease. Neurochem Int. 55, 689-96.

Schulte, JH, Lim, S, Schramm, A, Friedrichs, N, Koster, J, Versteeg, R, Ora, I, Pajtler, K, Klein-Hitpass, L, Kuhfittig-Kulle, S, Metzger, E, Schüle, R, Eggert, A, Buettner, R, Kirfel, J. (2009). Lysine-specific demethylase 1 is strongly expressed in poorly differentiated neuroblastoma: implications for therapy. Cancer Res. 69, 2065-71.

Zhao Y, Lang G, Ito S, Bonnet J, Metzger E, Sawatsubashi S, Suzuki E, Le Guezennec X, Stunnenberg HG, Krasnov A, Georgieva SG, Schüle R, Takeyama K, Kato S, Tora L, Devys D. (2008). A TFTC/STAGA module mediates histone H2A and H2B deubiquitination, coactivates nuclear receptors, and counteracts heterochromatin silencing. Molecular Cell. 29, 92-101.

Metzger E, Yin N, Wissmann M, Kunowska N, Fischer K, Friedrichs N, Patnaik D, Higgins JM, Potier N, Scheidtmann KH, Buettner R, Schüle R. (2008). Phosphorylation of histone H3 at threonine 11 establishes a novel chromatin mark for transcriptional regulation. Nat Cell Biol. 10, 53-60.

Spira D, Stypmann J, Tobin DJ, Petermann I, Mayer C, Haggemann S, Vasiljeva O, Gunther T, Schule R, Peters C, Reinheckel T. (2007). Cell type-specific functions of the lysosomal protease cathepsin L in the heart. J Biol Chem. J Biol Chem. 282, 37045-37052.

Spannhoff A, Heinke R, Bauer I, Trojer P, Metzger E, Gust R, Schule R, Brosch G, Sippl W, Jung M. (2007). Target-based approach to inhibitors of histone arginine methyltransferases. Bioorg J Med Chem. 50, 2319-25.

Nair SS, Guo Z, Mueller JM, Koochekpour S, Qiu Y, Tekmal RR, Schule R, Kung HJ, Kumar R, Vadlamudi RK. (2007). Proline-, glutamic acid-, and leucine-rich protein-1/modulator of nongenomic activity of estrogen receptor enhances androgen receptor functions through LIM-only coactivator, four-and-a-half LIM-only protein. Mol Endocrinol. 21, 613-24.

Wixler V, Hirner S, Muller JM, Gullotti L, Will C, Kirfel J, Gunther T, Schneider H, Bosserhoff A, Schorle H, Park J, Schule R, Buettner R. (2007). Deficiency in the LIM-only protein Fhl2 impairs skin wound healing. J Cell Biol. 177, 163-72.

Wissmann M, Yin N, Mueller JM, Greschik H, Fodor BD, Jenuwein T, Vogler C, Schneider R, Guenther T, Buettner R, Metzger E, Schuele R (2007). Co-operative demethylation by JMJD2C and LSD1 promotes androgen receptor-dependent gene expression. Nat Cell Biol. 9, 347-353.

Nair SS, Guo Z, Müller JM, Koochekapour S, Qiu Y, Tekmal RR, Schüle R, Kung HJ, Kumar R, Vadlamundi RK. (2007) PELP1/MNAR enhances androgen receptor functions through LIM-only coactivator FHL2. Mol Endocrinol. 21, 613-624.

Kahl P, Gullotti L, Heukamp LC, Wolf S, Friedrichs N, Vorreuther R, Solleder G, Bastian PJ, Ellinger J, Metzger E, Schuele R, Buettner R (2006). Androgen Receptor Coactivators Lysine-Specific Histone Demethylase 1 and Four and a Half LIM Domain Protein 2 Predict Risk of Prostate Cancer Recurrence. Cancer Res. 66, 11341-11347.

Bagheri-Fam S, Barrionuevo F, Dohrmann U, Gunther T, Schule R, Kemler R, Mallo M, Kanzler B, Scherer G. (2006). Long-range upstream and downstream enhancers control distinct subsets of the complex spatiotemporal Sox9 expression pattern. Dev. Biol. 291, 382-97.

Gabriel B, Fischer DC, Orlowska-Volk M, zur Hausen A, Schuele R, Muller JM and Hasenburg A (2006). Expression of the transcriptional coregulator FHL2 in human breast cancer: a clinicopathologic study. J. Soc. Gynecol. Investig. 13, 69-75.

Hublitz P, Kunowska N, Mayer UP, Muller JM, Heyne K, Yin N, Fritzsche C,Poli C, Miguet L, Schupp IW, van Grunsven LA, Potiers N, van Dorsselaer A,Metzger E, Roemer K, Schuele, R. (2005). NIR is a novel INHAT repressor that modulates the transcriptional activity of p53. Genes Dev. 19, 2912-24.

Metzger E, Wissmann M, Yin N, Muller JM, Schneider R, Peters AH, Gunther T, Buettner R, Schuele, R. (2005). LSD1 demethylates repressive histone marks to promote androgen-receptor-dependent transcription Nature. 437, 436-439.

Gunther T, Poli C, Muller JM, Catala-Lehnen P, Schinke T, Yin N, Vomstein S, Amling M, Schuele, R. (2005). Fhl2 deficiency results in osteopenia due to decreased activity of osteoblasts. EMBO J. 24, 3049-56.

Bai, S., Kitaura, H., Zhao, H., Chen, J., Muller, JM., Schuele, R., Darnay, B., Novack, D.V., Ross, F.P. and Teitelbaum. S.L. (2005). FHL2 inhibits the activated osteoclast in a TRAF6-dependent manner. J. Clin. Invest. 115, 2742-2751.

Purcell, N.H., Darwis, D., Bueno, O.F., Muller, JM., Schuele, R. and Molkentin, J.D. (2004). Extracellular signal-regulated kinase 2 (ERK2) interacts with and is negatively regulated by the LIM-only protein FHL2 in cardiomyocytes. Mol. Cell. Biol. 24, 1081-1095.

Gabriel B, Mildenberger S, Weisser CW, Metzger E, Gitsch G, Schuele, R , Mueller JM (2004). Focal adhesion kinase interacts with the transcriptional coactivator FHL2 and both are overexpressed in epithelial ovarian cancer. Anticancer Res. 24, 921-7.

Samson, T., Smyth, N., Janetzky, S., Wendler, O., Mueller, JM., Schuele, R., von der Mark, H., von der Mark, K. and Wixler, V. (2004). The LIM-only proteins FHL2 and FHL3 interact with alpha- and beta-subunits of the muscle alpha7beta1 integrin receptor. J. Biol. Chem. 279, 28641-28652.

Hagemann, S., Guenther, T., Dennemärker, J., Lohmueller, T., Brömme, D., Schuele, R., Peters, C. and Reinheckel,T. (2004). The human cysteine protease cathepsin V can compensate for murine cathepsin L in mouse epidermis and hair follicles. Eur. J. Cell. Biol. 83, 775-780.

Oehler, MK., Greschik, H., Fischer, DC., Tong, X., Schuele, R. and Kieback, DG. (2004). Functional characterization of somatic point mutations of the human estrogen receptor alpha in adenomyosis uteri. Mol. Hum. Reprod. 12, 853-860.

Philippar U, Schratt G, Dieterich C, Muller JM, Galgoczy P, Engel FB, Keating MT, Gertler F, Schuele, R., Vingron M, Nordheim A. (2004). The SRF Target Gene Fhl2 Antagonizes RhoA/MAL-Dependent Activation of SRF. Mol. Cell. 16, 867-80.

Stehlin-Gaon C, Willmann D, Zeyer D, Sanglier S, Van Dorsselaer A, Renaud JP, Moras D, Schule R. (2003). All-trans retinoic acid is a ligand for the orphan nuclear receptor ROR beta. Nat. Struct. Biol. 10, 820-825.

Metzger E, Muller JM, Ferrari S, Buettner R, Schuele, R. (2003). A novel inducible transactivation domain in the androgen receptor: implications for PRK in prostate cancer. EMBO J. 15, 270-280.

Du, X., Hublitz, P., Guenther, T., Wilhelm, D., Englert, C. and Schuele, R. (2002). The LIM-only coactivator FHL2 modulates WT1 transcriptional activity during gonadal differentiation. Biochimica et Biophysica Acta. 1577, 93-101.

Mueller, J.M., Metzger, E., Greschik, H., Bosserhoff, A-K., Mercep, L., Buettner, R. and Schuele, R. (2002). The transcriptional coactivator FHL2 transmits Rho signals from the cell membrane into the nucleus. EMBO J. 21, 736-748.

Greiner, E., Kirfel, J., Greschik, H., Huang, D., Becker, P., Kapfhammer, J.P. and Schuele, R. (2000). Differential ligand-dependent protein-protein interactions between nuclear receptors and a neuronal-specific cofactor. Proc. Natl. Acad. Sci. USA 97, 7160-7165.

Mueller, J.M., Isele, U., Metzger, E., Rempel, A., Moser, M., Pscherer, A., Breyer, T., Holubarsch, C., Buettner, R. and Schuele, R. (2000) FHL2, a novel tissue-specific coactivator of the androgen receptor. EMBO J. 19, 359-369.

Greschik, H., Wurtz, J.-M., Hublitz, P., Köhler, F., Moras, D. and Schuele, R. (1999) Characterization of the DNA-binding and dimerization properties of the nuclear orphan receptor GCNF. Mol. Cell. Biol. 19, 690-703.  

Greiner, E., Kirfel, J., Dörflinger, U., Greschik, H., Becker, P., Mercep, A. and Schuele, R. (1996) Functional analysis of retinoid Z receptor b, a brain-specific nuclear orphan receptor. Proc. Natl. Acad. Sci. USA 93, 10105-10110.