NTRC Publications:
- Grobben et al. (2021) Targeting indoleamine 2,3-dioxygenase in cancer models using the novel small molecule inhibitor NTRC 3883-0, Frontiers in Immunology, section Cancer Immunity and Immunotherapy, online first, January 28, 2021. (collaboration with Radboud University Medical Center)
https://www.frontiersin.org/articles/10.3389/fimmu.2020.609490/full
- Conlon et al. (2021) Comparative analysis of drug response and gene profiling of the HER2-targeted tyrosine kinase inhibitors, British Journal of Cancer, online first, January 21, 2021. (collaboration with Dublin City University and Puma Biotechnology, Inc.)
https://www.nature.com/articles/s41416-020-01257-x.
- Perez-Pardo et al. (2021) Pharmacological validation of TDO as a target for Parkinson’s disease, The FEBS Journal, online first, January 20, 2021. (collaboration with Utrecht University)
- den Ouden et al. (2020) Chemotherapy sensitivity testing on ovarian cancer cells isolated from malignant ascites, Oncotarget, 11:4570-4581. (collaboration with Radboud University Medical Center)
https://www.oncotarget.com/article/27827/
- Grobben et al. (2020) High-Throughput Fluorescence-Based Activity Assay for Arginase-1. SLAS Discovery, 25 (9):1018-1025.
https://journals.sagepub.com/doi/10.1177/2472555220919340.
- Grobben et al. (2020) Structural insights into human Arginase-1 pH dependence and its inhibition by the small molecule inhibitor CB-1158. Journal of Structural Biology: X, 4:100014.
https://doi.org/10.1016/j.yjsbx.2019.100014
- Uitdehaag et al. (2019) Combined cellular and biochemical profiling to identify predictive drug response biomarkers for kinase inhibitors approved for clinical use between 2013 and 2017, Molecular Cancer Therapeutics, 18 (2):470-481.
http://mct.aacrjournals.org/content/early/2018/10/31/1535-7163.MCT-18-0877
- Zaman et al. (2017) TTK inhibitors as a targeted therapy for CTNNB1 (β-catenin) mutant cancers, Molecular Cancer Therapeutics, 16 (11):2609-2617.
http://mct.aacrjournals.org/content/early/2017/07/27/1535-7163.MCT-17-0342
- Uitdehaag et al. (2017) Target Residence Time-Guided Optimization on TTK Kinase Results in Inhibitors with Potent Anti-Proliferative Activity, Journal of Molecular Biology, 429:2211-2230.
https://www.sciencedirect.com/science/article/pii/S0022283617302437
- Libouban et al. (2017) Stable aneuploid tumors cells are more sensitive to TTK inhibition than chromosomally unstable cell lines, Oncotarget, 8 (24):38309–38325. (collaboration with Netherlands Cancer Institute)
https://doi.org/10.18632/oncotarget.16213
- Willemsen-Seegers et al. (2017) Compound Selectivity and Target Residence Time of Kinase Inhibitors Studied with Surface Plasmon Resonance, Journal of Molecular Biology, 429:574-586.
https://www.sciencedirect.com/science/article/pii/S002228361
- Uitdehaag et al. (2016) Cell Panel Profiling Reveals Conserved Therapeutic Clusters and Differentiates the Mechanism of Action of Different PI3K/mTOR, Aurora Kinase and EZH2 Inhibitors, Molecular Cancer Therapeutics, 15 (12):3097-3109.
http://mct.aacrjournals.org/content/early/2016/09/01/1535-7163.MCT-16-0403
- Uitdehaag et al. (2015) Selective Targeting of CTNNB1-, KRAS- or MYC-Driven Cell Growth by Combinations of Existing Drugs, PLoS ONE, 10 (5):e0125021. http://dx.plos.org/10.1371/journal.pone.0125021
- Uitdehaag et al. (2014) Comparison of the Cancer Gene Targeting and Biochemical Selectivities of All Targeted Kinase Inhibitors Approved for Clinical Use, PLoS ONE, 9 (3):e92146.
http://www.plosone.org/article/info%3Adoi%2F10.1371%2Fjournal.pone.0092146
- Seegers et al. (2014) High-throughput fluorescence-based screening assays for tryptophan-catabolizing enzymes, Journal of Biomolecular Screening, 19 (9):1266-1274.
https://www.ncbi.nlm.nih.gov/pubmed/24870017
References to the assay technologies Arginase Gold™ and NFK Green™:
- Pei, Z. et al. (2019) TDO2 and IDO1 inhibitors, International Patent Application WO 2019/005559. (Affiliation: Genentech, Inc.)
https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2019005559.
- Pei, Z. et al. (2019) TDO2 and IDO1 inhibitors, International Patent Application WO 2019/006047. (Affiliation: Genentech, Inc.)
https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2019006047
- Liu, S. et al. (2019) Crystal of tricyclic acid, International Patent Application WO 2019/034139. (Affiliation: Chia Tai Tianqing Pharmaceutical Group Co., Ltd.)
https://patentscope.wipo.int/search/fr/detail.jsf?docId=WO2019034139
- Garapaty et al. (2017) Small molecule modulators to understand the role of IDO1 and TDO2 in cancer, Cancer Research, 77 (13 Supplement):5578-5578. (Affiliation: Jubilant Biosys Ltd.)
http://cancerres.aacrjournals.org/content/77/13_Supplement/5578
- More information on the assay technologies Arginase Gold™ and NFK Green™ can be found at www.residencetimer.com
References to NTRC Science Platforms:
- Beauchamp et al. (2020) Targeting N-myristoylation for therapy of B-cell lymphomas, Nature Communications, 11:5348. (Affiliations: University of Alberta, Pacylex Pharmaceuticals)
https://www.nature.com/articles/s41467-020-18998-1#Ack1
- van der Zwet et al. (2020) The central role of MAPK-ERK signalling in IL7-dependent and IL7-independent steroid resistance reveals a broad application of MEK-inhibitors compared to JAK1/2-inhibition in T-ALL, Oral presentation, ASH Annual Meeting 2020 (Affiliation: Prinses Máxima Center for Pediatric Oncology)
- Cordo et al. (2020) Phospho-proteomic profiling of T-Cell Acute Lymphoblastic Leukemia identifies targetable kinase activities and novel treatment combination strategies, Oral presentation, ASH Annual Meeting 2020 (Affiliation: Prinses Máxima Center for Pediatric Oncology)
- Borsari et al. (2019) Preclinical Development of PQR514, a Highly Potent PI3K Inhibitor Bearing a Difluoromethyl−Pyrimidine Moiety, ACS Medicinal Chemistry Letters, 10:1473-1479. (Affilitations: University of Basel, PIQUR Therapeutics AG)
https://pubs.acs.org/doi/full/10.1021/acsmedchemlett.9b00333
- Rageot et al. (2019) (S)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530), a Potent, Orally Bioavailable, and Brain-Penetrable Dual Inhibitor of Class I PI3K and mTOR Kinase, Journal of Medicinal Chemistry, 62 (13):6241-6261. (Affiliations: University of Basel, PIQUR Therapeutics AG)
https://doi.org/10.1021/acs.jmedchem.9b00525
- Grünewald et al. (2019) Rogaratinib: A potent and selective pan‐FGFR inhibitor with broad antitumor activity in FGFR‐overexpressing preclinical cancer models, International Journal of Cancer, 145 (5): 346-1357. (Affiliation: Bayer AG)
https://doi.org/10.1002/ijc.32224
- Gentile et al. (2018) A Novel Interaction Between the TLR7 and a Colchicine Derivative Revealed Through a Computational and Experimental Study, Pharmaceuticals, 11 (1):22. (Affiliation: University of Alberta)
https://doi.org/10.3390/ph11010022
- Bohnacker et al. (2017) Deconvolution of Buparlisib’s mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention, Nature Communications, 8:14683. (Affiliation: University of Basel)
https://www.nature.com/articles/ncomms14683
- Politz et al. (2017) Preclinical activity of the FGFR inhibitor rogaratinib (BAY 1163877) alone or in combination with antihormonal therapy in breast cancer, Cancer Research, 77 (13 Supplement):1079-1079. (Affiliation: Bayer AG)
http://cancerres.aacrjournals.org/content/77/13_Supplement/1079
- Wentsch et al. (2017) Optimized Target Residence Time: Type 1½Inhibitors for p38a MAP Kinase with Improved Binding Kinetics through Direct Interaction with the R-Spine, Angewandte Chemie International Edition, 56 (19):5363-5367. (Affiliation: Universität Tübingen)
https://doi.org/10.1002/anie.201701185
- Li et al. (2016) IL-7 Receptor Mutations and Steroid Resistance in Pediatric T cell Acute Lymphoblastic Leukemia: A Genome Sequencing Study, PLoS Med, 13 (12):e1002200. (Affiliations: Erasmus MC, NTRC)
https://journals.plos.org/plosmedicine/article?id=10.1371/journal.pmed.1002200
- Canté-Barrett et al. (2016) MEK and PI3K-AKT inhibitors synergistically block activated IL7 receptor signaling in T-cell acute lymphoblastic leukemia, Leukemia, 30:1832-1843. (Affiliations: Erasmus MC, NTRC)
https://www.nature.com/articles/leu201683
- Maia et al. (2015) Inhibition of the spindle assembly checkpoint kinase TTK enhances the efficacy of docetaxel in a triple-negative breast cancer model, Annals of Oncology, 26 (10):2180-2192. (Affiliations: Netherlands Cancer Institute, NTRC)
https://doi.org/10.1093/annonc/mdv293
- Cmiljanovic et al. (2015) PQR309: Structure-based design, synthesis and biological evaluation of a novel, selective, dual pan-PI3K/mTOR inhibitor, Cancer Research, 75 (15 Supplement): 2664-2664. (Affiliation: PIQUR Therapeutics AG)
https://cancerres.aacrjournals.org/content/75/15_Supplement/2664
- Hudlebusch et al. (2014) The development of therapeutic inhibitors of the KDM5 histone demethylases, Cancer Research, 74 (19 Supplement): 5161-5161. (Affiliation: EpiTherapeutics)
https://cancerres.aacrjournals.org/content/74/19_Supplement/5161