Ausgewählte Publikationen

Alcohol-abuse drug disulfiram targets cancer via p97 segregase adapter NPL4.
Skrott Z, Mistrik M, Andersen KK, Friis S, Majera D, Gursky J, Ozdian T, Bartkova J, Turi Z,  Moudry P, Kraus M, Michalova M, Vaclavkova J, Dzubak P, Vrobel I, Pouckova P, Sedlacek J, Miklovicova A, Kutt A, Li J, Mattova J, Driessen C, Dou PQ, Olsen J, Hajduch M, Cvek B, Deshaies RJ, Bartek J.
Nature 2017 Dec 14;552(7684):194-199. doi: 10.1038

Improving the efficacy of proteasome inhibitors in the treatment of renal cell carcinoma by combination with the HIV-protease inhibitors lopinavir or nelfinavir.
Abt D, Besse A, Sedlarikova L, Kraus M, Bader J, Silzle T, Vodinska M, Slaby O, Schmid HP, Engeler DS, Driessen C, Besse L.  British J Urology 2017, doi: 10.1111

Bendamustine, lenalidomide and dexamethasone (BRd) has high activity as 2nd -line therapy for relapsed and refractory multiple myeloma - a phase II trial.
Mey UJ, Brugger W, Schwarb H, Pederiva S, Schwarzer A, Dechow T, Jehner P, Rauh J, Taverna CJ, Schmid M, Schmidt-Hieber M, Doerfel S, Fischer N, Ruefer A, Ziske C, Knauf W, Cathomas R, von Moos R, Hitz F, Sauter R, Hiendlmeyer E, Cantoni N, Bargetzi M, Driessen C.
Br J Haematol. 2017 Mar;176(5):770-782. doi: 10.1111

Carfilzomib resistance due to ABCB1/MDR1 overexpression is overcome by nelfinavir and lopinavir in multiple myeloma.
Besse A, Stolze SC, Rasche L, Weinhold N, Morgan GJ, Kraus M, Bader J, Overkleeft HS, Besse L, Driessen C. : Leukemia 2017, 1-11

The first-in-class alkylating HDAC inhibitor EDO-S101 is highly synergistic with proteasome inhibition against multiple myeloma through activation of multiple pathways.
Besse L, Kraus M, Besse A, Bader J, Silzle T, Mehrling T, Driessen C. : Blood Cancer Journal 2017(7)doi:10.1038

The p97 inhibitor CB-5083 is a unique disrupter of protein homeostasis in models of Multiple Myeloma.
Le Moigne R, Aftab BT, Djakovic S, Dhimolea E, Valle E, Murnane M, King EM, Soriano F, Menon M-K, Wu ZY, Wong ST, Lee GJ, Yao B, Wiita AP, Lam C, Rice J, Wang J, Chesi M, Bergsagel PL, Kraus M, Driessen C, Kiss von Soly S, Yakes FM, Wustrow D, Shawver L, Zhou H-J, III TGM, Wolf JL, Mitsiades CS, Anderson DJ, Rolfe M.  : Mol.Cancer Ther. 2017(16(11)):2375-2386, doi: 10.1158/1535-7163.

Structure-Based Design of β5c Selective Inhibitors of Human Constitutive Proteasomes.

Xin BT, de Bruin G, Huber EM, Besse A, Florea BI, Filippov DV, van der Marel GA, Kisselev AF, van der Stelt M, Driessen C, Groll M, Overkleeft HS.
J Med Chem. 2016 Aug 11;59(15):7177-87. doi: 10.1021

Proteasome inhibitor-adapted myeloma cells are largely independent from proteasome activity and show complex proteomic changes, in particular in redox and energy metabolism.
Soriano GP, Besse L, Li N, Kraus M, Besse A, Meeuwenoord N, Bader J, Everts B, den Dulk H, Overkleeft HS, Florea BI, Driessen C. : Leukemia 2016, 1-10

Treatment with the HIV protease inhibitor Nelfinavir triggers the unfolded protein response and may overcome proteasome inhibitor resistance of multiple myeloma in combination with bortezomib: a phase I trial (SAKK 65/08).
Driessen C, Kraus M, Joerger M, Rosing H, Bader J, Hitz F, Berset C, Xyrafas A, Hawle H, Berthod G, Overkleeft HS, Sessa C, Huitema A, Pabst T, von Moos R, Hess D, Mey UJ.
Haematologica. 2015 Dec 11. pii: haematol.2015.135780. [Epub ahead of print]

A Set of Activity-Based Probes to Visualize Human (Immuno)proteasome Activities.
de Bruin G, Xin BT, Kraus M, van der Stelt M, van der Marel GA, Kisselev AF, Driessen C, Florea BI, Overkleeft HS.
Angew Chem Int Ed Engl. 2015 Oct 29. doi: 10.1002/anie.201509092. [Epub ahead of print]

The novel β2-selective proteasome inhibitor LU-102 decreases phosphorylation of I kappa B and induces highly synergistic cytotoxicity in combination with ibrutinib in multiple myeloma cells.
Kraus J, Kraus M, Liu N, Besse L, Bader J, Geurink PP, de Bruin G, Kisselev AF, Overkleeft H, Driessen C.
Cancer Chemother Pharmacol. 2015 Aug;76(2):383-96. doi: 10.1007/s00280-015-2801-0. Epub 2015 Jun 23.

The novel β2-selective proteasome inhibitor LU-102 synergizes with bortezomib and carfilzomib to overcome proteasome inhibitor resistance of myeloma cells.
Kraus M, Bader J, Geurink PP, Weyburne ES, Mirabella AC, Silzle T, Shabaneh TB, van der Linden WA, de Bruin G, Haile SR, van Rooden E, Appenzeller C, Li N, Kisselev AF, Overkleeft H, Driessen C.
Haematologica. 2015 Oct;100(10):1350-60. doi: 10.3324/haematol.2014.109421. Epub 2015 Jun 11.

Improved survival of older patients with multiple myeloma in the era of novel agents.
Mey UJ, Leitner C, Driessen C, Cathomas R, Klingbiel D, Hitz F.
Hematol Oncol. 2015 Apr 21. doi: 10.1002/hon.2205. [Epub ahead of print]

Direct and two-step bioorthogonal probes for Bruton's tyrosine kinase based on ibrutinib: a comparative study.
Liu N, Hoogendoorn S, van de Kar B, Kaptein A, Barf T, Driessen C, Filippov DV, van der Marel GA, van der Stelt M, Overkleeft HS.
Org Biomol Chem. 2015 May 14;13(18):5147-57. doi: 10.1039/c5ob00474h.

Cancer-selective targeting of the NF-κB survival pathway with GADD45β/MKK7 inhibitors.
Tornatore L, Sandomenico A, Raimondo D, Low C, Rocci A, Tralau-Stewart C, Capece D, D'Andrea D, Bua M, Boyle E, van Duin M, Zoppoli P, Jaxa-Chamiec A, Thotakura AK, Dyson J, Walker BA, Leonardi A, Chambery A, Driessen C, Sonneveld P, Morgan G, Palumbo A, Tramontano A, Rahemtulla A, Ruvo M, Franzoso G.
Cancer Cell. 2014 Oct 13;26(4):495-508. doi: 10.1016/j.ccr.2014.07.027. Erratum in: Cancer Cell. 2014 Dec 8;26(6):938.

Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes.
de Bruin G, Huber EM, Xin BT, van Rooden EJ, Al-Ayed K, Kim KB, Kisselev AF, Driessen C, van der Stelt M, van der Marel GA, Groll M, Overkleeft HS.
J Med Chem. 2014 Jul 24;57(14):6197-209. doi: 10.1021/jm500716s. Epub 2014 Jul 15.

Ritonavir, nelfinavir, saquinavir and lopinavir induce proteotoxic stress in acute myeloid leukemia cells and sensitize them for proteasome inhibitor treatment at low micromolar drug concentrations.
Kraus M, Müller-Ide H, Rückrich T, Bader J, Overkleeft H, Driessen C.
Leuk Res. 2014 Mar;38(3):383-92. doi: 10.1016/j.leukres.2013.12.017. Epub 2013 Dec 25.

Combined inhibition of p97 and the proteasome causes lethal disruption of the secretory apparatus in multiple myeloma cells.
Auner HW, Moody AM, Ward TH, Kraus M, Milan E, May P, Chaidos A, Driessen C, Cenci S, Dazzi F, Rahemtulla A, Apperley JF, Karadimitris A, Dillon N.
PLoS One. 2013 Sep 17;8(9):e74415. doi: 10.1371/journal.pone.0074415. eCollection 2013.

Incorporation of non-natural amino acids improves cell permeability and potency of specific inhibitors of proteasome trypsin-like sites.
Geurink PP, van der Linden WA, Mirabella AC, Gallastegui N, de Bruin G, Blom AE, Voges MJ, Mock ED, Florea BI, van der Marel GA, Driessen C, van der Stelt M, Groll M, Overkleeft HS, Kisselev AF.
J Med Chem. 2013 Feb 14;56(3):1262-75. doi: 10.1021/jm3016987. Epub 2013 Jan 28.

Imatinib mesylate and nilotinib affect MHC-class I presentation by modulating the proteasomal processing of antigenic peptides.
Held SA, Duchardt KM, Tenzer S, Rückrich T, von Schwarzenberg K, Bringmann A, Kurts C, Schild H, Driessen C, Brossart P, Heine A.
Cancer Immunol Immunother. 2013 Apr;62(4):715-26. doi: 10.1007/s00262-012-1373-7. Epub 2012 Nov 25.

Cathepsin S dominates autoantigen processing in human thymic dendritic cells.
Stoeckle C, Quecke P, Rückrich T, Burster T, Reich M, Weber E, Kalbacher H, Driessen C, Melms A, Tolosa E.
J Autoimmun. 2012 Jun;38(4):332-43. doi: 10.1016/j.jaut.2012.02.003. Epub 2012 Mar 16.

Nonproteasomal Targets of the Proteasome Inhibitors Bortezomib and Carfilzomib: a Link to Clinical Adverse Events.
Arastu-Kapur S, Anderl JL, Kraus M, Parlati F, Shenk KD, Lee SJ, Muchamuel T, Bennett MK, Driessen C, Ball AJ, Kirk CJ. Clin Cancer Res. 2011 Apr 19.

Harman A.N.; Kraus M.; Bye Ch.R.; Byth K.; Turville S.G.; Tang O.; Mercier S.K.; Stern J.L.; Driessen C., Slobedman B, Cunningham A.L., HIV-1 Infected Dendritic Cells Show Two Phases of Gene Expression Changes With Lysosomal Enzyme Activity Decreased During the Second Phase. Blood 2009, 114(1):85-94

Hillaert U, Verdoes M, Florea BI, Saragliadis A, Habets KL, Kuiper J, Van Calenbergh S, Ossendorp F, van der Marel GA, Driessen C, Overkleeft HS. Receptor-mediated targeting of cathepsins in professional antigen presenting cells. Angew Chem Int Ed Engl. 2009;48(9):1629-32

Clerc J, Florea BI, Kraus M, Groll M, Huber R, Bachmann AS, Dudler R, Driessen C, Overkleeft HS, Kaiser M. Syringolin A selectively labels the 20 S proteasome in murine EL4 and wild-type and bortezomib-adapted leukaemic cell lines. Chembiochem. 2009 10(16):2638-43.

Rückrich T, Kraus M, Gogel J, Beck A, Ovaa H, Verdoes M, Overkleeft HS, Kalbacher H, Driessen C. Characterization of the ubiquitin-proteasome system in bortezomib-adapted cells. Leukemia. 2009 23(6):1098-105

Kessler T, Reich M, Jahn G, Tolosa E, Beck A, Kalbacher H, Overkleeft H, Schempp S, Driessen C, Human cytomegalovirus infection interferes with major histocompatibility complex type II maturation and endocytic proteases in dendritic cells at multiple levels. J Gen Virol. 2008 Oct; 89:2427-36. 

Stoeckle C, Sommandas V, Adamopoulou E, Belisle K, Schiekofer S, Melms A, Weber E, Driessen C, Boehm BO, Tolosa E, Burster T .Cathepsin G is differentially expressed in primary human antigen-presenting cells. Cell Immunol. 2009;255(1-2):41-5.

Kraus, M., Malenke, E., Gogel, J., Müller, H., Rückrich, T., Overkleeft, H., Ovaa, H., Koscielniak E., Hartmann, J., Driessen, C. Ritonavir induces ER-stress and sensitizes sarcoma cells towards bortezomib-induced apoptosis. Molecular Cancer Therapeutics 2008 Jul;7(7):1940-8

Fissolo, N., Kraus, M., Reich, M., Ayturan, M., Overkleeft, H., Driessen, C., Weissert, R. Experimental Dual inhibition of lysosomal and proteasomal proteolysis ameliorates a model of multiple sclerosis
Eur J Immunol, 2008, Sept.; 38(9)2401-11.

Busse, A., Kraus, M., Il-Kang, N., Rietz, A., Scheibenbogen, C., Driessen, C., Blau, I., Thiel, E., Keilholz, U. Sensitivity of tumor cells to proteasome inhibitors is associated with expression level and composition of proteasome subunits. Cancer, 2008 Feb 1; 112(3): 659-70

Horger, M., Pereira, P., Claussen, C., Kanz, L., Vonthein, R., Denecke, B., Driessen, C. Incidence and significance of hyperattenuating bone marrow abnormalities in myeloma patients referred for staging using whole-body nonenhanced low-dose MDCT and correlation with hematologic parameters: initial results. British J. of Radiology, 2008 May; 81(965): 386-96

Kraus M., Malenke E, Gogel J, Müller H, Rückrich T, Overkleeft H, Ovaa H, Koscielniak E. Hartmann JT, Driessen C. Ritonavir induces endoplasmic reticulum stress and sensitizes sarcoma cells toward bortezomib-induced apoptosis. Molecular cancer therapeutics 2008, 7: 1940-8