Hormone Dependent Cancer

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.

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.

Roatsch, M., Hoffmann, I., Abboud, M., Hancock, R., Tarhonskaya, H., Hsu, K-F., Wilkins, S., Yeh, T-L., Lippl, K., Serrer, K., Moneke, I., Ahrens, T., Robaa, D., Wenzler, S., Barthes, N., Franz, H., Sippl, W., Lassmann, S., Diederichs, S., Schleicher, E., Schofield, C., Kawamura, A., Schüle, R. and Jung, M. (2019). The Clinically Used Iron Chelator Deferasirox is an Inhibitor of Epigenetic JumonjiC Domain-Containing Histone Demethylases. ACS Chemical Biology, doi:10.1021/acschembio.9b00289.

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.

Michel, N.A., Colberg, C., Buscher, K., Sommer, B., Pramod, A.B., Ehinger, Dufner, E.B., Hoppe, N., Pfeiffer, K., Marchini, T., Willecke, F., Stachon, P., Hilgendorf, I., Heidt, T., von zu Mühlen, C., von Elverfeldt, D., Pfeifer, D., Schüle, R., Kintscher, U., Brachs, S., Ley, K., Bode, C., Zirlik. A and Wolf, W. (2018). Inflammatory pathways regulated by tumor-necrosis receptor associated factor 1 protect from metabolic consequences in diet-induced obesity. Circ. Res. 122, 693-700.

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.

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.

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.

Moreno-Juan V., Filipchuk A., Antón-Bolaños N., Mezzera C., Gezelius H., Andrés B., Rodríguez-Malmierca L., Susín R., Schaad O., Iwasato T., Schüle R., Rutlin M., Nelson S., Ducret S., Valdeolmillos M., Rijli F.M., López-Bendito G. Prenatal thalamic waves regulate cortical area size prior to sensory processing (2017). Nat Commun. 8:14172.

Duteil, D., Tosic, M., Lausecker, F., L, Nenseth, H. Z., Müller, J. M., 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.

Robaa D., Wagner T., Luise C., Carlino L., McMillan J., Flaig R., Schüle R., Jung M., Sippl W. (2016). Identification and Structure-Activity Relationship Studies of Small-Molecule Inhibitors of the Methyllysine Reader Protein Spindlin1. ChemMedChem. [Epub ahead of print]

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.

Morera L., Roatsch M., Fürst M.C., Hoffmann I., Senger J., Hau M., Franz H., Schüle R., Heinrich M.R., Jung M. (2016). 4-Biphenylalanine- and 3-Phenyltyrosine-Derived Hydroxamic Acids as Inhibitors of the JumonjiC-Domain-Containing Histone Demethylase KDM4A. ChemMedChem. 11(18):2063-2083.

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.

Wu X., Schneider N., Platen A., Mitra I., Blazek M., Zengerle R., Schüle R., Meier M. (2016). In situ characterization of the mTORC1 during adipogenesis of human adult stem cells on chip. Proc. Natl. Acad. Sci. USA. 113(29):E4143-4150.

Hügle M., Lucas X., Weitzel G., Ostrovskyi D., Breit B., Gerhardt S., Schmidtkunz K., Jung M., Schüle R., Einsle O., Günther S., Wohlwend D. (2016). Preparation data of the bromodomains BRD3(1), BRD3(2), BRD4(1), and BRPF1B and crystallization of BRD4(1)-inhibitor complexes. Data Brief. 7:1370-1374.

Roatsch M., Robaa D., Pippel M., Nettleship J.E., Reddivari Y., Bird L.E., Hoffmann I., Franz H., Owens R.J., Schüle R., Flaig R., Sippl W., Jung M. (2016). Substituted 2-(2-aminopyrimidin-4-yl)pyridine-4-carboxylates as potent inhibitors of JumonjiC domain-containing histone demethylases. Future Med Chem. 8(13):1553-1571.

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.    

Al-Nomani L, Friedrichs J, Schüle R, Büttner R, Friedrichs N. (2015). Tumoral expression of nuclear cofactor FHL2 is associated with lymphatic metastasis in sporadic but not in HNPCC-associated colorectal cancer. (2015). Pathol. Res. Pract. 211 (2), 171-174.

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. 

Krönig M., Walter M., Drendel V., Werner M., Jilg C.A., Richter A.S., Backofen R., McGarry D., Follo M., Schultze-Seemann W., Schule R. (2015). Cell type specific gene expression analysis of prostate needle biopsies resolves tumor tissue heterogeneity. Oncotarget. 6 (2), 1302-1314.

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.

Ruger N., Roatsch M., Emmrich T., Franz H., Schüle R., Jung M., Link A. (2015). Tetrazolylhydrazides as Selective Fragment-Like Inhibitors of the JumonjiC-Domain-Containing Histone Demethylase KDM4A. Chemmedchem. 10 (11), 1875-1883.

Westphal P., Mauch C., Florin A., Czerwitzki J., Olligschlager N., Wodtke C., Schule R., Buttner R., Friedrichs N. (2015). Enhanced FHL2 and TGF-beta1 Expression Is Associated With Invasive Growth and Poor Survival in Malignant Melanomas. Am. J. Clin. Pathol. 143 (2), 248-56.

Friedrichs J., Fink D., Mauch C., Kindler D., Hartmann W., Schüle R., Buettner R., Friedrichs N. (2015). TGF-β1-dependent induction and nuclear translocation of FHL2 promotes keratin expression in pilomatricoma. Virchows Arch.  466 (2), 199-208.

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.

Heyne K., Förster J., Schüle R., Roemer K. (2014). Transcriptional repressor NIR interacts with the p53-inhibiting ubiquitin ligase MDM2. Nucleic Acids Res. 42 (6), 3565-3579.

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.

Nam, H.J., Boo, K., Kim, D.H., Choe, H.K., Kim, C.R., Sun, W., Kim, H., Kim, K., Lee, H., Schüle, R., Yoo, S-H., Takahashi, J.S., Cho, S., Son, G.H. and Baek, S.H. (2014). Phosphorylation of LSD1 by PKCa Is Crucial for Circadian Rhythmicity and Phase Resetting. Mol. Cell 53, 791-805.  

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.  

Heyne, K., Förster, J., Schüle, R. and Roemer. K. (2014). Transcriptional repressor NIR interacts with the p53-inhibiting ubiquitin ligase MDM2. Nucleic Acids Res. 42, 3565-79.  

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.

Lucas, X., Wohlwend, D., Hügle, M., Schmidtkunz, K., Gerhardt, S., Schüle, R., Jung, M., Einsle, O. and Günther, S. (2013). 4-acyl pyrroles: Mimicking acetylated lysines in histone code reading. Angew Chem Int Ed Engl. 52, 14055-14059.  

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.  

Brun, J., Dieudonné, F.X., Marty, C., Müller, J., Schüle, R., Patiño-García, A., Lecanda, F., Fromigué, O. and Marie, P.J. (2013). FHL2 silencing reduces Wnt signaling and osteosarcoma tumorigenesis in vitro and in vivo. PLoS One 8(1):e55034. Epub 2013 Jan 28.  

Sprüssel, A., Schulte, J.H., Weber, S., Necke, M., Händschke, K., Thor, T., Pajtler, K.W., Schramm, A., König, K., Diehl, L., Mestdagh, P., Vandesompele, J., Speleman, F., Jastrow, H., Heukamp, L.C., Schüle, R., Dührsen, U., Buettner, R., Eggert, A. and Göthert, J.R. (2012). Lysine-specific demethylase 1 restricts hematopoietic progenitor proliferation and is essential for terminal differentiation. Leukemia 26, 2039-2051.

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.

Ibrahim, S.A, Yip, G.W., Stock, C., Pan, J.W., Neubauer, C., Poeter, M., Pupjalis, D., Koo, C.Y., Kelsch, R, Schüle, R., Rescher, U., Kiesel, L. and Götte, M. (2012). Targeting of syndecan-1 by microRNA miR-10b promotes breast cancer cell motility and invasiveness via a Rho-GTPase- and E-cadherin-dependent mechanism. Int. J. Cancer 131, 884-896.  

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.

Gullotti, L., Czerwitzki, J., Kirfel, J., Propping, P., Rahner, N., Steinke, V., Kahl, P., Engel, C., Schule, R., Buettner, R., et al. (2011). FHL2 expression in peritumoural fibroblasts correlates with lymphatic metastasis in sporadic but not in HNPCC-associated colon cancer. Lab Invest 91, 1695-705.

Rafael, M.S., Laize, V., Bensimon-Brito, A., Leite, R.B., Schule, R., and Cancela, M.L. (2012). Four-and-a-half LIM domains protein 2 (FHL2) is associated with the development of craniofacial musculature in the teleost fish Sparus aurata. Cell Mol Life Sci. 69, 423-34.

Schildhaus, H.U., Riegel, R., Hartmann, W., Steiner, S., Wardelmann, E., Merkelbach-Bruse, S., Tanaka, S., Sonobe, H., Schule, R., Buettner, R., et al. (2011). Lysine-specific demethylase 1 is highly expressed in solitary fibrous tumors, synovial sarcomas, rhabdomyosarcomas, desmoplastic small round cell tumors, and malignant peripheral nerve sheath tumors. Hum Pathol 42, 1667-1675.

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.

Heyne K, Willnecker V, Schneider J, Conrad M, Raulf N, Schüle R, Roemer K (2010). NIR, an inhibitor of histone acetyltransferases, regulates transcription factor TAp63 and is controlled by the cell cycle. Nucleic Acids Res.

Lim S, Janzer A, Becker A, Zimmer A, Schüle R, Buettner R, Kirfel J (2010). Lysine-specific demethylase 1 (LSD1) is highly expressed in ER-negative breast cancers and a biomarker predicting aggressive biology. Carcinogenesis 31, 512-20.

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, Machmur R, Heinke R, Trojer P, Bauer I, Brosch G, Schule R, Hanefeld W, Sippl W, Jung M. (2007). A novel arginine methyltransferase inhibitor with cellular activity. Bioorg Med Chem Lett. 17, 4150-3.

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, J.M., 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, J.M., 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, J.M., 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.

Conceicao, N., Henriques, N.M. , Marc C.P., Ohresser, M.C.P., Hublitz, P., Schuele, R. and Cancela, L.M. (2002). Molecular cloning of the MGP gene from Xenopus laevis: functional analysis of the promoter identifies a calcium sensitive region required for basal activity. Eur. J. Biochem. 269, 1947-1956.

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.

Stehlin C, Wurtz JM, Steinmetz A, Greiner E, Schuele R., Moras D, Renaud JP. (2001). X-ray structure of the orphan nuclear receptor RORbeta ligand-binding domain in the active conformation. EMBO J. 20, 5822-5831.

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.

Dörflinger, U., Pscherer, A., Moser, M., Ruemmele, P., Schuele, R. and Buettner, R. (1999) Activation of somatostatin receptor II expression by transcription factors MIBP1 and SEF-2 in the murine brain. Mol. Cell. Biol. 19, 3736-3747.

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.

Pfitzner, E., Kirfel, J., Becker, P., Rolke, A. and Schuele, R. (1998) Physical interaction between retinoic acid receptor and the oncoprotein Myb inbhibits retinoic acid dependent transactivation. Proc. Natl. Acad. Sci. USA 95, 5539-5544.

Kirfel, J., Kelter, M., Cancela, L.M., Price, P. and Schuele, R. (1997) Identification of a novel negative retinoic acid receptor response element in the promotor of the human matrix Gla protein gene. Proc. Natl. Acad. Sci. USA 94, 2227-2232.

Pscherer, A., Dörflinger, U., Kirfel, J., Gawlas, K., Rueschoff, J., Buettner, R. and Schuele, R. (1996) The helix-loop-helix transcription factor SEF-2 regulates the activity of a novel initiator element in the promoter of the human somatostatin receptor II gene. EMBO J. 15, 6680-6690.     

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.

Pfitzner, E., Becker, P., Rolke, A. and Schuele, R. (1995) Functional antagonism between the retinoic acid receptor and the viral transactivator BZLF1 is mediated by protein-protein interactions. Proc. Natl. Acad. Sci. USA 92, 12265-12269.

Moser, M., Imhof, A., Pscherer, A., Bauer, R., Amselgruber, W., Sinowatz, F., Hofstädter, F., Schuele, R. and Buettner, R. (1995) Cloning and characterization of a second AP-2 transcription factor: AP-2b. Development 121, 2779-2788.

Rohrer, R., Raulf, F., Bruns, Ch., Hofstädter, F, Buettner, R. and Schuele, R. (1993) Cloning and characterization of a fourth human somatostatin receptor. Proc. Natl. Acad. Sci. USA 90, 4196-4200.

Schuele, R., Pundi, R., Yang, N., Kliewer, S., Bolado, J., Verma, I.M. and Evans, R.M. (1991) Retinoic acid is a negative regulator of AP-1 responsive genes. Proc. Natl. Acad. Sci. USA 88, 6092-6096.     

Yang, N., Schuele, R., Mangelsdorf, D.J. and Evans, R.M. (1991) Characterization of DNA binding and retinoic acid binding properties of retinoic acid receptor. Proc. Natl. Acad. Sci. USA 88, 3559-3563.     

Schuele, R., Pundi, R., Kliewer, S., Ransone, L.J., Bolado, J., Yang, N., Verma, I.M. and Evans, R.M. (1990) Functional antagonism between oncoprotein c-Jun and the glucocorticoid receptor. Cell 62, 1217-1226.     

Schuele, R., Umesono, K., Mangelsdorf, D., Bolado, J., Pike, W.J. and Evans, R.M. (1990). Jun/Fos and receptors for vitamin A and D recognize a common response element in the human osteocalcin gene. Cell 61, 497-504.     Schuele, R. (1988) Hormonal regulation of the rat tryptophan oxygenase gene. Intemann Press, Muenchen.     Schuele, R., Muller, M., Kaltschmidt, Ch. and Renkawitz, R. (1988) Many transcription factors interact synergistically with steroid receptors. Science 242, 1418-1420.     

Schuele, R., Muller, M., Otzuka-Murakami, H. and Renkawitz, R. (1988) Cooperativity of the glucocorticoid receptor and the CACCC-box binding factor. Nature 322, 87-90.     Danesch, U., Gloss, B., Schmid, W., Schuetz, G., Schuele, R. and Renkawitz, R. (1987) Glucocorticoid induction of the rat tryptophan oxygenase gene is mediated by two widely separated glucocorticoid responsive elements. EMBO J. 6, 625-630.