Key in our rational, mechanism-based approach is our Triple E platform,
as published in Nature Chemical Biology (May 2016).

MB231 cells with SUMO2 in red and DAPI (nuclei) in blue. courtesy of Jim D. Sutherland (CIC bioGUNE).


A cascading activity-based probe sequentially targets E1-E2-E3 ubiquitin enzymes.

Monique P C Mulder, Katharina Witting, Ilana Berlin, Jonathan N Pruneda, Kuen-Phon Wu, Jer-Gung Chang, Remco Merkx, Johanna Bialas, Marcus Groettrup, Alfred C O Vertegaal, Brenda A Schulman, David Komander, Jacques Neefjes, Farid El Oualid* & Huib Ovaa*
* Corresponding authors

Nat Chem Biol 2016, 12: 523–530.


Myc-induced SUMOylation is a therapeutic vulnerability for B-cell lymphoma.

Alexander Hoellein, Mohammad Fallahi, Stephanie Schoeffmann, Sabine Steidle, Franz X. Schaub, Martina Rudelius, Iina Laitinen, Lisa Nilsson, Andrei Goga, Christian Peschel, Jonas A. Nilsson, John L. Cleveland, and Ulrich Keller

Blood 2014, 124: 2081–2090.


A SUMOylation-dependent transcriptional subprogram is required for Myc-driven tumorigenesis.

Kessler JD, Kahle KT, Sun T, Meerbrey KL, Schlabach MR, et al.

Science 2012, 335: 348–353. doi:10.1126/science.1212728.

Pharmacological treats for SUMO addicts.

Licciardello MP, Kubicek S

Pharmacol Res 2016, 107: 390–397. doi:10.1016/j.phrs.2016.01.004.

NOTCH1 activation in breast cancer confers sensitivity to inhibition of SUMOylation.

Licciardello MP, Müllner MK, Dürnberger G, Kerzendorfer C, Boidol B, et al.

Oncogene 2015, 34: 3780–3790.


Oncogenesis driven by the Ras/Raf pathway requires the SUMO E2 ligase Ubc9.

Yu B, Swatkoski S, Holly A, Lee LC, Giroux V, et al.

Proc Natl Acad Sci U S A 2015, 112: E1724-33.


Probing the roles of SUMOylation in cancer cell biology by using a selective SAE inhibitor.

He X, Riceberg J, Soucy T, Koenig E, Minissale J, et al.

Nat Chem Biol. 2017


Characterization of the loss of SUMO pathway function on cancer cells and tumor proliferation.

He X, Riceberg J, Pulukuri SM, Grossman S, Shinde V, et al.

PLoS ONE 2015, 10: e0123882.


SUMO and the robustness of cancer.

Seeler J-S, Dejean A

Nat Rev Cancer 2017, 17: 184–197.


Sumoylation: a regulatory protein modification in health and disease.

Flotho A, Melchior F

Annu Rev Biochem 2013, 82: 357–385.