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Optimized Target Residence Time: Type I1/2 Inhibitors for p38α MAP Kinase with Improved Binding Kinetics through Direct Interaction with the R-Spine.
Wentsch HK, Walter NM, Bührmann M, Mayer-Wrangowski S, Rauh D, Zaman GJR, Willemsen-Seegers N, Buijsman RC, Henning M, Dauch D, Zender L, Laufer S. Wentsch HK, et al. Angew Chem Int Ed Engl. 2017 May 2;56(19):5363-5367. doi: 10.1002/anie.201701185. Epub 2017 Apr 11. Angew Chem Int Ed Engl. 2017. PMID: 28397331
Design, Synthesis, and Biological Evaluation of Novel Type I1/2 p38α MAP Kinase Inhibitors with Excellent Selectivity, High Potency, and Prolonged Target Residence Time by Interfering with the R-Spine.
Walter NM, Wentsch HK, Bührmann M, Bauer SM, Döring E, Mayer-Wrangowski S, Sievers-Engler A, Willemsen-Seegers N, Zaman G, Buijsman R, Lämmerhofer M, Rauh D, Laufer SA. Walter NM, et al. Among authors: willemsen seegers n. J Med Chem. 2017 Oct 12;60(19):8027-8054. doi: 10.1021/acs.jmedchem.7b00745. Epub 2017 Sep 7. J Med Chem. 2017. PMID: 28834431
Cell Panel Profiling Reveals Conserved Therapeutic Clusters and Differentiates the Mechanism of Action of Different PI3K/mTOR, Aurora Kinase and EZH2 Inhibitors.
Uitdehaag JC, de Roos JA, Prinsen MB, Willemsen-Seegers N, de Vetter JR, Dylus J, van Doornmalen AM, Kooijman J, Sawa M, van Gerwen SJ, de Man J, Buijsman RC, Zaman GJ. Uitdehaag JC, et al. Mol Cancer Ther. 2016 Dec;15(12):3097-3109. doi: 10.1158/1535-7163.MCT-16-0403. Epub 2016 Sep 1. Mol Cancer Ther. 2016. PMID: 27587489
Combined Cellular and Biochemical Profiling to Identify Predictive Drug Response Biomarkers for Kinase Inhibitors Approved for Clinical Use between 2013 and 2017.
Uitdehaag JCM, Kooijman JJ, de Roos JADM, Prinsen MBW, Dylus J, Willemsen-Seegers N, Kawase Y, Sawa M, de Man J, van Gerwen SJC, Buijsman RC, Zaman GJR. Uitdehaag JCM, et al. Among authors: willemsen seegers n. Mol Cancer Ther. 2019 Feb;18(2):470-481. doi: 10.1158/1535-7163.MCT-18-0877. Epub 2018 Oct 31. Mol Cancer Ther. 2019. PMID: 30381447
High-Throughput Fluorescence-Based Activity Assay for Arginase-1.
Grobben Y, Willemsen-Seegers N, Uitdehaag JCM, de Man J, van Groningen J, Friesen J, van den Hurk H, Buijsman RC, Zaman GJR. Grobben Y, et al. Among authors: willemsen seegers n. SLAS Discov. 2020 Oct;25(9):1018-1025. doi: 10.1177/2472555220919340. Epub 2020 May 16. SLAS Discov. 2020. PMID: 32418491 Free article.
Pharmacological validation of TDO as a target for Parkinson's disease.
Perez-Pardo P, Grobben Y, Willemsen-Seegers N, Hartog M, Tutone M, Muller M, Adolfs Y, Pasterkamp RJ, Vu-Pham D, van Doornmalen AM, van Cauter F, de Wit J, Gerard Sterrenburg J, Uitdehaag JCM, de Man J, Buijsman RC, Zaman GJR, Kraneveld AD. Perez-Pardo P, et al. Among authors: willemsen seegers n. FEBS J. 2021 Jul;288(14):4311-4331. doi: 10.1111/febs.15721. Epub 2021 Feb 18. FEBS J. 2021. PMID: 33471408 Free PMC article.
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