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Items: 48

1.

Identification of Atuveciclib (BAY 1143572), the First Highly Selective, Clinical PTEFb/CDK9 Inhibitor for the Treatment of Cancer.

Lücking U, Scholz A, Lienau P, Siemeister G, Kosemund D, Bohlmann R, Briem H, Terebesi I, Meyer K, Prelle K, Denner K, Bömer U, Schäfer M, Eis K, Valencia R, Ince S, von Nussbaum F, Mumberg D, Ziegelbauer K, Klebl B, Choidas A, Nussbaumer P, Baumann M, Schultz-Fademrecht C, Rühter G, Eickhoff J, Brands M.

ChemMedChem. 2017 Nov 8;12(21):1776-1793. doi: 10.1002/cmdc.201700447. Epub 2017 Oct 16.

2.

Conformational Adaption May Explain the Slow Dissociation Kinetics of Roniciclib (BAY 1000394), a Type I CDK Inhibitor with Kinetic Selectivity for CDK2 and CDK9.

Ayaz P, Andres D, Kwiatkowski DA, Kolbe CC, Lienau P, Siemeister G, Lücking U, Stegmann CM.

ACS Chem Biol. 2016 Jun 17;11(6):1710-9. doi: 10.1021/acschembio.6b00074. Epub 2016 Apr 19.

3.

Probing the catalytic functions of Bub1 kinase using the small molecule inhibitors BAY-320 and BAY-524.

Baron AP, von Schubert C, Cubizolles F, Siemeister G, Hitchcock M, Mengel A, Schröder J, Fernández-Montalván A, von Nussbaum F, Mumberg D, Nigg EA.

Elife. 2016 Feb 17;5. pii: e12187. doi: 10.7554/eLife.12187.

4.

Novel Mps1 Kinase Inhibitors with Potent Antitumor Activity.

Wengner AM, Siemeister G, Koppitz M, Schulze V, Kosemund D, Klar U, Stoeckigt D, Neuhaus R, Lienau P, Bader B, Prechtl S, Raschke M, Frisk AL, von Ahsen O, Michels M, Kreft B, von Nussbaum F, Brands M, Mumberg D, Ziegelbauer K.

Mol Cancer Ther. 2016 Apr;15(4):583-92. doi: 10.1158/1535-7163.MCT-15-0500. Epub 2016 Feb 1.

5.

Optimization of allosteric MEK inhibitors. Part 2: Taming the sulfamide group balances compound distribution properties.

Hartung IV, Hammer S, Hitchcock M, Neuhaus R, Scholz A, Siemeister G, Bohlmann R, Hillig RC, Pühler F.

Bioorg Med Chem Lett. 2016 Jan 1;26(1):186-93. doi: 10.1016/j.bmcl.2015.11.004. Epub 2015 Nov 3.

PMID:
26611920
6.

Modular Assembly of Allosteric MEK Inhibitor Structural Elements Unravels Potency and Feedback-Modulation Handles.

Hartung IV, Pühler F, Neuhaus R, Scholz A, Siemeister G, Geisler J, Hillig RC, von Ahsen O, Hitchcock M.

ChemMedChem. 2015 Dec;10(12):2004-13. doi: 10.1002/cmdc.201500442. Epub 2015 Nov 6.

PMID:
26541480
7.

Characterization of novel MPS1 inhibitors with preclinical anticancer activity.

Jemaà M, Galluzzi L, Kepp O, Senovilla L, Brands M, Boemer U, Koppitz M, Lienau P, Prechtl S, Schulze V, Siemeister G, Wengner AM, Mumberg D, Ziegelbauer K, Abrieu A, Castedo M, Vitale I, Kroemer G.

Cell Death Differ. 2013 Nov;20(11):1532-45. doi: 10.1038/cdd.2013.105. Epub 2013 Aug 9.

8.

The lab oddity prevails: discovery of pan-CDK inhibitor (R)-S-cyclopropyl-S-(4-{[4-{[(1R,2R)-2-hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)sulfoximide (BAY 1000394) for the treatment of cancer.

Lücking U, Jautelat R, Krüger M, Brumby T, Lienau P, Schäfer M, Briem H, Schulze J, Hillisch A, Reichel A, Wengner AM, Siemeister G.

ChemMedChem. 2013 Jul;8(7):1067-85. doi: 10.1002/cmdc.201300096. Epub 2013 May 13.

PMID:
23671017
9.

Optimization of allosteric MEK inhibitors. Part 1: Venturing into underexplored SAR territories.

Hartung IV, Hitchcock M, Pühler F, Neuhaus R, Scholz A, Hammer S, Petersen K, Siemeister G, Brittain D, Hillig RC.

Bioorg Med Chem Lett. 2013 Apr 15;23(8):2384-90. doi: 10.1016/j.bmcl.2013.02.028. Epub 2013 Feb 14.

PMID:
23474388
10.

BAY 1000394, a novel cyclin-dependent kinase inhibitor, with potent antitumor activity in mono- and in combination treatment upon oral application.

Siemeister G, Lücking U, Wengner AM, Lienau P, Steinke W, Schatz C, Mumberg D, Ziegelbauer K.

Mol Cancer Ther. 2012 Oct;11(10):2265-73. doi: 10.1158/1535-7163.MCT-12-0286. Epub 2012 Jul 19.

11.

Evaluation of activity and combination strategies with the microtubule-targeting drug sagopilone in breast cancer cell lines.

Eschenbrenner J, Winsel S, Hammer S, Sommer A, Mittelstaedt K, Drosch M, Klar U, Sachse C, Hannus M, Seidel M, Weiss B, Merz C, Siemeister G, Hoffmann J.

Front Oncol. 2011 Nov 16;1:44. doi: 10.3389/fonc.2011.00044. eCollection 2011.

12.

Off-target decoding of a multitarget kinase inhibitor by chemical proteomics.

Missner E, Bahr I, Badock V, Lücking U, Siemeister G, Donner P.

Chembiochem. 2009 May 4;10(7):1163-74. doi: 10.1002/cbic.200800796.

PMID:
19350611
13.

The oral multitarget tumour growth inhibitor, ZK 304709, inhibits growth of pancreatic neuroendocrine tumours in an orthotopic mouse model.

Scholz A, Wagner K, Welzel M, Remlinger F, Wiedenmann B, Siemeister G, Rosewicz S, Detjen KM.

Gut. 2009 Feb;58(2):261-70. doi: 10.1136/gut.2007.146415. Epub 2008 Oct 1.

PMID:
18829975
14.

Tomoregulin internalization confers selective cytotoxicity of immunotoxins on prostate cancer cells.

Zhao XY, Liu HL, Liu B, Willuda J, Siemeister G, Mahmoudi M, Dinter H.

Transl Oncol. 2008 Jul;1(2):102-9.

15.

Improved cellular pharmacokinetics and pharmacodynamics underlie the wide anticancer activity of sagopilone.

Hoffmann J, Vitale I, Buchmann B, Galluzzi L, Schwede W, Senovilla L, Skuballa W, Vivet S, Lichtner RB, Vicencio JM, Panaretakis T, Siemeister G, Lage H, Nanty L, Hammer S, Mittelstaedt K, Winsel S, Eschenbrenner J, Castedo M, Demarche C, Klar U, Kroemer G.

Cancer Res. 2008 Jul 1;68(13):5301-8. doi: 10.1158/0008-5472.CAN-08-0237.

16.

Use of the novel Plk1 inhibitor ZK-thiazolidinone to elucidate functions of Plk1 in early and late stages of mitosis.

Santamaria A, Neef R, Eberspächer U, Eis K, Husemann M, Mumberg D, Prechtl S, Schulze V, Siemeister G, Wortmann L, Barr FA, Nigg EA.

Mol Biol Cell. 2007 Oct;18(10):4024-36. Epub 2007 Aug 1.

17.

Macrocyclic aminopyrimidines as multitarget CDK and VEGF-R inhibitors with potent antiproliferative activities.

Lücking U, Siemeister G, Schäfer M, Briem H, Krüger M, Lienau P, Jautelat R.

ChemMedChem. 2007 Jan;2(1):63-77.

PMID:
17131463
18.

Molecular and pharmacodynamic characteristics of the novel multi-target tumor growth inhibitor ZK 304709.

Siemeister G, Luecking U, Wagner C, Detjen K, Mc Coy C, Bosslet K.

Biomed Pharmacother. 2006 Jul;60(6):269-72. Epub 2006 Jun 23.

PMID:
16887322
19.

From the insoluble dye indirubin towards highly active, soluble CDK2-inhibitors.

Jautelat R, Brumby T, Schäfer M, Briem H, Eisenbrand G, Schwahn S, Krüger M, Lücking U, Prien O, Siemeister G.

Chembiochem. 2005 Mar;6(3):531-40. No abstract available.

PMID:
15742375
20.

Differential regulation of in vivo angiogenesis by angiotensin II receptors.

Walther T, Menrad A, Orzechowski HD, Siemeister G, Paul M, Schirner M.

FASEB J. 2003 Nov;17(14):2061-7.

PMID:
14597675
21.

Cell transformation by the v-myc oncogene abrogates c-Myc/Max-mediated suppression of a C/EBP beta-dependent lipocalin gene.

Hartl M, Matt T, Schüler W, Siemeister G, Kontaxis G, Kloiber K, Konrat R, Bister K.

J Mol Biol. 2003 Oct 10;333(1):33-46.

PMID:
14516741
22.

Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.

Manley PW, Furet P, Bold G, Brüggen J, Mestan J, Meyer T, Schnell CR, Wood J, Haberey M, Huth A, Krüger M, Menrad A, Ottow E, Seidelmann D, Siemeister G, Thierauch KH.

J Med Chem. 2002 Dec 19;45(26):5687-93.

PMID:
12477352
23.

Identification of a soluble form of the angiopoietin receptor TIE-2 released from endothelial cells and present in human blood.

Reusch P, Barleon B, Weindel K, Martiny-Baron G, Gödde A, Siemeister G, Marmé D.

Angiogenesis. 2001;4(2):123-31.

PMID:
11806244
24.

Active interaction of human A375 melanoma cells with the lymphatics in vivo.

Papoutsi M, Siemeister G, Weindel K, Tomarev SI, Kurz H, Schächtele C, Martiny-Baron G, Christ B, Marmé D, Wilting J.

Histochem Cell Biol. 2000 Nov;114(5):373-85.

PMID:
11151407
25.

Targeting of endothelial KDR receptors with 3G2 immunoliposomes in vitro.

Benzinger P, Martiny-Baron G, Reusch P, Siemeister G, Kley JT, Marmé D, Unger C, Massing U.

Biochim Biophys Acta. 2000 Jun 1;1466(1-2):71-8.

26.

PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration.

Wood JM, Bold G, Buchdunger E, Cozens R, Ferrari S, Frei J, Hofmann F, Mestan J, Mett H, O'Reilly T, Persohn E, Rösel J, Schnell C, Stover D, Theuer A, Towbin H, Wenger F, Woods-Cook K, Menrad A, Siemeister G, Schirner M, Thierauch KH, Schneider MR, Drevs J, Martiny-Baron G, Totzke F.

Cancer Res. 2000 Apr 15;60(8):2178-89.

27.
28.

Characterization of a new potent, in vivo neutralizing monoclonal antibody to human vascular endothelial growth factor.

Schlaeppi JM, Siemeister G, Weindel K, Schnell C, Wood J.

J Cancer Res Clin Oncol. 1999;125(6):336-42.

PMID:
10363565
29.

The pivotal role of VEGF in tumor angiogenesis: molecular facts and therapeutic opportunities.

Siemeister G, Martiny-Baron G, Marmé D.

Cancer Metastasis Rev. 1998 Jun;17(2):241-8. Review. No abstract available.

PMID:
9770121
30.
31.

An antagonistic vascular endothelial growth factor (VEGF) variant inhibits VEGF-stimulated receptor autophosphorylation and proliferation of human endothelial cells.

Siemeister G, Schirner M, Reusch P, Barleon B, Marmé D, Martiny-Baron G.

Proc Natl Acad Sci U S A. 1998 Apr 14;95(8):4625-9.

32.
33.

Novel antibodies directed against the extracellular domain of the human VEGF-receptor type II.

Menrad A, Thierauch KH, Martiny-Baron G, Siemeister G, Schirner M, Schneider MR.

Hybridoma. 1997 Oct;16(5):465-71.

PMID:
9388030
35.

Defects of insulin and IGF-1 action at receptor and postreceptor level in a patient with type A syndrome of insulin resistance.

Knebel B, Kellner S, Kotzka J, Siemeister G, Dreyer M, Streicher R, Schiller M, Rüdiger HW, Seemanova E, Krone W, Müller-Wieland D.

Biochem Biophys Res Commun. 1997 May 29;234(3):626-30.

PMID:
9175764
36.

Mapping of the sites for ligand binding and receptor dimerization at the extracellular domain of the vascular endothelial growth factor receptor FLT-1.

Barleon B, Totzke F, Herzog C, Blanke S, Kremmer E, Siemeister G, Marmé D, Martiny-Baron G.

J Biol Chem. 1997 Apr 18;272(16):10382-8.

37.

Structure of the human apolipoprotein C-II gene promoter.

Streicher R, Avci H, Munck M, Siemeister G, Geisel J, Weisshaar C, Müller-Wieland D, Krone W.

Z Gastroenterol. 1996 Jun;34 Suppl 3:49-50.

PMID:
8767460
38.

Expression of biologically active isoforms of the tumor angiogenesis factor VEGF in Escherichia coli.

Siemeister G, Schnurr B, Mohrs K, Schächtele C, Marmé D, Martiny-Baron G.

Biochem Biophys Res Commun. 1996 May 15;222(2):249-55.

PMID:
8670191
39.

Reversion of deregulated expression of vascular endothelial growth factor in human renal carcinoma cells by von Hippel-Lindau tumor suppressor protein.

Siemeister G, Weindel K, Mohrs K, Barleon B, Martiny-Baron G, Marmé D.

Cancer Res. 1996 May 15;56(10):2299-301.

40.

SREBP-1 mediates activation of the low density lipoprotein receptor promoter by insulin and insulin-like growth factor-I.

Streicher R, Kotzka J, Müller-Wieland D, Siemeister G, Munck M, Avci H, Krone W.

J Biol Chem. 1996 Mar 22;271(12):7128-33.

41.

Recombinant human insulin receptor substrate-1 protein. Tyrosine phosphorylation and in vitro binding of insulin receptor kinase.

Siemeister G, al-Hasani H, Klein HW, Kellner S, Streicher R, Krone W, Müller-Wieland D.

J Biol Chem. 1995 Mar 3;270(9):4870-4.

42.

Sequence and expression of a glyceraldehyde-3-phosphate dehydrogenase-encoding gene from quail embryo fibroblasts.

Weiskirchen R, Siemeister G, Hartl M, Bister K.

Gene. 1993 Jun 30;128(2):269-72.

PMID:
8514192
43.

Molecular biology of insulin resistance.

Müller-Wieland D, Streicher R, Siemeister G, Krone W.

Exp Clin Endocrinol. 1993;101(1):17-29. Review.

PMID:
8477820
44.
48.

cDNA clones of the auxin-binding protein from corn coleoptiles (Zea mays L.): isolation and characterization by immunological methods.

Tillmann U, Viola G, Kayser B, Siemeister G, Hesse T, Palme K, Löbler M, Klämbt D.

EMBO J. 1989 Sep;8(9):2463-7.

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