Gerjan de Bruin
Structure-Based Design of Inhibitors Selective for Human Proteasome β2c or β2i Subunits
Xin B, Groll M, van der Marel G, Driessen C, Florea B, Kisselev A, Weyburne E, Janssens M, Du Y, Espinal C, Maurits E, Heinemeyer W, de Bruin G, Huber E, Overkleeft H. Structure-Based Design of Inhibitors Selective for Human Proteasome β2c or β2i Subunits. J Med Chem 2019; 62:1626-1642.
05.02.2019Structure-Based Design of Inhibitors Selective for Human Proteasome β2c or β2i Subunits
05.02.2019J Med Chem 2019; 62:1626-1642
Xin Bo-Tao, Groll Michael, van der Marel Gijsbert A, Driessen Christoph, Florea Bogdan I, Kisselev Alexei F, Weyburne Emily S, Janssens Marissa, Du Yimeng, Espinal Christofer, Maurits Elmer, Heinemeyer Wolfgang, de Bruin Gerjan, Huber Eva M, Overkleeft Herman S
Structure-Based Design of β5c Selective Inhibitors of Human Constitutive Proteasomes
Xin B, Groll M, Driessen C, van der Stelt M, Kisselev A, van der Marel G, Filippov D, Florea B, Besse A, Huber E, de Bruin G, Overkleeft H. Structure-Based Design of β5c Selective Inhibitors of Human Constitutive Proteasomes. J Med Chem 2016; 59:7177-87.
01.08.2016Structure-Based Design of β5c Selective Inhibitors of Human Constitutive Proteasomes
01.08.2016J Med Chem 2016; 59:7177-87
Xin Bo-Tao, Groll Michael, Driessen Christoph, van der Stelt Mario, Kisselev Alexei F, van der Marel Gijsbert A, Filippov Dmitri V, Florea Bogdan I, Besse Andrej, Huber Eva M, de Bruin Gerjan, Overkleeft Herman S
A Set of Activity-Based Probes to Visualize Human (Immuno)proteasome Activities
de Bruin G, Xin B, Kraus M, van der Stelt M, van der Marel G, Kisselev A, Driessen C, Florea B, Overkleeft H. A Set of Activity-Based Probes to Visualize Human (Immuno)proteasome Activities. Angew Chem Int Ed Engl 2015; 55:4199-203.
29.10.2015A Set of Activity-Based Probes to Visualize Human (Immuno)proteasome Activities
29.10.2015Angew Chem Int Ed Engl 2015; 55:4199-203
de Bruin Gerjan, Xin Bo Tao, Kraus Marianne, van der Stelt Mario, van der Marel Gijsbert A, Kisselev Alexei F, Driessen Christoph, Florea Bogdan I, Overkleeft Herman S
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 P, de Bruin G, Kisselev A, Overkleeft H, Driessen C. 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. Cancer Chemother Pharmacol 2015; 76:383-96.
23.06.2015The 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.
23.06.2015Cancer Chemother Pharmacol 2015; 76:383-96
Kraus Johannes, Kraus Marianne, Liu Nora, Besse Lenka, Bader Jürgen, Geurink Paul P, de Bruin Gerjan, Kisselev Alexei F, Overkleeft Herman, Driessen Christoph
The novel β2-selective proteasome inhibitor LU-102 synergizes with bortezomib and carfilzomib to overcome proteasome inhibitor resistance of myeloma cells
Kraus M, Overkleeft H, Kisselev A, Li N, Appenzeller C, van Rooden E, Haile S, de Bruin G, van der Linden W, Shabaneh T, Silzle T, Mirabella A, Weyburne E, Geurink P, Bader J, Driessen C. The novel β2-selective proteasome inhibitor LU-102 synergizes with bortezomib and carfilzomib to overcome proteasome inhibitor resistance of myeloma cells. Haematologica 2015; 100:1350-60.
11.06.2015The novel β2-selective proteasome inhibitor LU-102 synergizes with bortezomib and carfilzomib to overcome proteasome inhibitor resistance of myeloma cells
11.06.2015Haematologica 2015; 100:1350-60
Kraus Marianne, Overkleeft Herman, Kisselev Alexei F, Li Nan, Appenzeller Christina, van Rooden Eva, Haile Sarah, de Bruin Gerjan, van der Linden Wouter A, Shabaneh Tamer B, Silzle Tobias, Mirabella Anne C, Weyburne Emily S, Geurink Paul P, Bader Juergen, Driessen Christoph
Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes
de Bruin G, Groll M, van der Marel G, van der Stelt M, Driessen C, Kisselev A, Kim K, Al-Ayed K, van Rooden E, Xin B, Huber E, Overkleeft H. Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. J Med Chem 2014; 57:6197-209.
15.07.2014Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes
15.07.2014J Med Chem 2014; 57:6197-209
de Bruin Gerjan, Groll Michael, van der Marel Gijsbert A, van der Stelt Mario, Driessen Christoph, Kisselev Alexei F, Kim Kyung-Bo, Al-Ayed Karol, van Rooden Eva J, Xin Bo-Tao, Huber Eva M, Overkleeft Herman S
Incorporation of non-natural amino acids improves cell permeability and potency of specific inhibitors of proteasome trypsin-like sites
Geurink P, Overkleeft H, Groll M, van der Stelt M, Driessen C, van der Marel G, Florea B, Mock E, Voges M, Blom A, de Bruin G, Gallastegui N, Mirabella A, van der Linden W, Kisselev A. Incorporation of non-natural amino acids improves cell permeability and potency of specific inhibitors of proteasome trypsin-like sites. J Med Chem 2013; 56:1262-75.
28.01.2013Incorporation of non-natural amino acids improves cell permeability and potency of specific inhibitors of proteasome trypsin-like sites
28.01.2013J Med Chem 2013; 56:1262-75
Geurink Paul P, Overkleeft Herman S, Groll Michael, van der Stelt Mario, Driessen Christoph, van der Marel Gijs A, Florea Bogdan I, Mock Elliot D, Voges Mathias J, Blom Annet E M, de Bruin Gerjan, Gallastegui Nerea, Mirabella Anne C, van der Linden Wouter A, Kisselev Alexei F