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Akademický článek

Dual TTK/PLK1 inhibition has potent anticancer activity in TNBC as monotherapy and in combination

Autor: Elisa Zanini, Nicole Forster-Gross, Felix Bachmann, Adrian Brüngger, Paul McSheehy, Karine Litherland, Karin Burger, Anna C. Groner, Mila Roceri, Luc Bury, Martin Stieger, Nicole Willemsen-Seegers, Jos de Man, Diep Vu-Pham, Helma W. E. van Riel, Guido J. R. Zaman, Rogier C. Buijsman, Laurenz Kellenberger, Heidi A. Lane

Publikováno v: Frontiers in Oncology, Vol 14 (2024)

BackgroundThreonine tyrosine kinase (TTK) and polo-like kinase 1 (PLK1) are common essential kinases that collaborate in activating the spindle assembly checkpoint (SAC) at the kinetochore, ensuring appropriate chromosome alignment and segregation pr

Externí odkaz: https://doaj.org/article/cf9a84a3e06f4b3a99f2975a86de17db

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Akademický článek

Targeting Indoleamine 2,3-Dioxygenase in Cancer Models Using the Novel Small Molecule Inhibitor NTRC 3883-0

Autor: Yvonne Grobben, Jos de Man, Antoon M. van Doornmalen, Michelle Muller, Nicole Willemsen-Seegers, Diep Vu-Pham, Winfried R. Mulder, Martine B. W. Prinsen, Joeri de Wit, Jan Gerard Sterrenburg, Freek van Cauter, Judith E. den Ouden, Anne M. van Altena, Leon F. Massuger, Joost C. M. Uitdehaag, Rogier C. Buijsman, Guido J. R. Zaman

Publikováno v: Frontiers in Immunology, Vol 11 (2021)

Indoleamine 2,3-dioxygenase (IDO1) is a key regulator of immune suppression by catalyzing the oxidation of L-tryptophan. IDO1 expression has been related to poor prognosis in several cancers and to resistance to checkpoint immunotherapies. We describ

Externí odkaz: https://doaj.org/article/67d223be9e3a4daabf3fe18bdc0d30fd

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Akademický článek

Structural insights into human Arginase-1 pH dependence and its inhibition by the small molecule inhibitor CB-1158

Autor: Yvonne Grobben, Joost C.M. Uitdehaag, Nicole Willemsen-Seegers, Werner W.A. Tabak, Jos de Man, Rogier C. Buijsman, Guido J.R. Zaman

Publikováno v: Journal of Structural Biology: X, Vol 4, Iss , Pp 100014- (2020)

Arginase-1 is a manganese-dependent metalloenzyme that catalyzes the hydrolysis of L-arginine into L-ornithine and urea. Arginase-1 is abundantly expressed by tumor-infiltrating myeloid cells that promote tumor immunosuppression, which is relieved by

Externí odkaz: https://doaj.org/article/69e071817d594ce39d3c3d4b2449e42f

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Akademický článek

Selective Targeting of CTNBB1-, KRAS- or MYC-Driven Cell Growth by Combinations of Existing Drugs.

Autor: Joost C M Uitdehaag, Jeroen A D M de Roos, Antoon M van Doornmalen, Martine B W Prinsen, Jill A P Spijkers-Hagelstein, Judith R F de Vetter, Jos de Man, Rogier C Buijsman, Guido J R Zaman

Publikováno v: PLoS ONE, Vol 10, Iss 5, p e0125021 (2015)

The aim of combination drug treatment in cancer therapy is to improve response rate and to decrease the probability of the development of drug resistance. Preferably, drug combinations are synergistic rather than additive, and, ideally, drug combinat

Externí odkaz: https://doaj.org/article/ef8b227b2f6d4dc1b37d97ccc9facfc1

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Akademický článek

Comparison of the cancer gene targeting and biochemical selectivities of all targeted kinase inhibitors approved for clinical use.

Autor: Joost C M Uitdehaag, Jeroen A D M de Roos, Antoon M van Doornmalen, Martine B W Prinsen, Jos de Man, Yoshinori Tanizawa, Yusuke Kawase, Kohichiro Yoshino, Rogier C Buijsman, Guido J R Zaman

Publikováno v: PLoS ONE, Vol 9, Iss 3, p e92146 (2014)

The anti-proliferative activities of all twenty-five targeted kinase inhibitor drugs that are in clinical use were measured in two large assay panels: (1) a panel of proliferation assays of forty-four human cancer cell lines from diverse tumour tissu

Externí odkaz: https://doaj.org/article/f0dfe06ae41c471a84f2bb2bd66742e5

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Data from TTK Inhibitors as a Targeted Therapy for CTNNB1 (β-catenin) Mutant Cancers

Autor: Joost C.M. Uitdehaag, Rogier C. Buijsman, Jos de Man, Martine B.W. Prinsen, Marion A.A. Libouban, Jeroen A.D.M. de Roos, Guido J.R. Zaman

The spindle assembly checkpoint kinase TTK (Mps1) is a key regulator of chromosome segregation and is the subject of novel targeted therapy approaches by small-molecule inhibitors. Although the first TTK inhibitors have entered phase I dose escalatin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::45622369852106526e9379507da3c52a
https://doi.org/10.1158/1535-7163.c.6538819.v1

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