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Optimisation of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors.
Ray P, Wright J, Adam J, Boucharens S, Black D, Brown AR, Epemolu O, Fletcher D, Huggett M, Jones P, Laats S, Lyons A, de Man J, Morphy R, Sherborne B, Sherry L, Straten Nv, Westwood P, York M. Ray P, et al. Among authors: de man j. Bioorg Med Chem Lett. 2011 Feb 15;21(4):1084-8. doi: 10.1016/j.bmcl.2010.12.104. Epub 2010 Dec 28. Bioorg Med Chem Lett. 2011. PMID: 21251828
Fragment-based discovery of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors.
Ray P, Wright J, Adam J, Bennett J, Boucharens S, Black D, Cook A, Brown AR, Epemolu O, Fletcher D, Haunso A, Huggett M, Jones P, Laats S, Lyons A, Mestres J, de Man J, Morphy R, Rankovic Z, Sherborne B, Sherry L, van Straten N, Westwood P, Zaman GZ. Ray P, et al. Among authors: de man j. Bioorg Med Chem Lett. 2011 Jan 1;21(1):97-101. doi: 10.1016/j.bmcl.2010.11.060. Epub 2010 Nov 19. Bioorg Med Chem Lett. 2011. PMID: 21145740
Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis.
Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Boga SB, Alhassan AB, Yu Y, Vaccaro H, Liu S, Yang C, Wu H, Cooper A, de Man J, Kaptein A, Maloney K, Hornak V, Gao YD, Fischmann TO, Raaijmakers H, Vu-Pham D, Presland J, Mansueto M, Xu Z, Leccese E, Zhang-Hoover J, Knemeyer I, Garlisi CG, Bays N, Stivers P, Brandish PE, Hicks A, Kim R, Kozlowski JA. Liu J, et al. Among authors: de man j. ACS Med Chem Lett. 2015 Dec 19;7(2):198-203. doi: 10.1021/acsmedchemlett.5b00463. eCollection 2016 Feb 11. ACS Med Chem Lett. 2015. PMID: 26985298 Free PMC 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: de man j, de wit j. 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.
Targeting Indoleamine 2,3-Dioxygenase in Cancer Models Using the Novel Small Molecule Inhibitor NTRC 3883-0.
Grobben Y, de Man J, van Doornmalen AM, Muller M, Willemsen-Seegers N, Vu-Pham D, Mulder WR, Prinsen MBW, de Wit J, Sterrenburg JG, van Cauter F, den Ouden JE, van Altena AM, Massuger LF, Uitdehaag JCM, Buijsman RC, Zaman GJR. Grobben Y, et al. Among authors: de man j, de wit j. Front Immunol. 2021 Jan 28;11:609490. doi: 10.3389/fimmu.2020.609490. eCollection 2020. Front Immunol. 2021. PMID: 33584686 Free PMC article.
Inhibition of the spindle assembly checkpoint kinase TTK enhances the efficacy of docetaxel in a triple-negative breast cancer model.
Maia AR, de Man J, Boon U, Janssen A, Song JY, Omerzu M, Sterrenburg JG, Prinsen MB, Willemsen-Seegers N, de Roos JA, van Doornmalen AM, Uitdehaag JC, Kops GJ, Jonkers J, Buijsman RC, Zaman GJ, Medema RH. Maia AR, et al. Among authors: de roos ja, de man j. Ann Oncol. 2015 Oct;26(10):2180-92. doi: 10.1093/annonc/mdv293. Epub 2015 Jul 7. Ann Oncol. 2015. PMID: 26153498 Free article.
Target Residence Time-Guided Optimization on TTK Kinase Results in Inhibitors with Potent Anti-Proliferative Activity.
Uitdehaag JCM, de Man J, Willemsen-Seegers N, Prinsen MBW, Libouban MAA, Sterrenburg JG, de Wit JJP, de Vetter JRF, de Roos JADM, Buijsman RC, Zaman GJR. Uitdehaag JCM, et al. Among authors: de man j, de wit jjp, de vetter jrf, de roos jadm. J Mol Biol. 2017 Jul 7;429(14):2211-2230. doi: 10.1016/j.jmb.2017.05.014. Epub 2017 May 21. J Mol Biol. 2017. PMID: 28539250
218 results