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Items: 43

1.

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.

Mol Cancer Ther. 2019 Feb;18(2):470-481. doi: 10.1158/1535-7163.MCT-18-0877. Epub 2018 Oct 31.

PMID:
30381447
2.

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

Zaman GJR, de Roos JADM, Libouban MAA, Prinsen MBW, de Man J, Buijsman RC, Uitdehaag JCM.

Mol Cancer Ther. 2017 Nov;16(11):2609-2617. doi: 10.1158/1535-7163.MCT-17-0342. Epub 2017 Jul 27.

3.

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.

J Mol Biol. 2017 Jul 7;429(14):2211-2230. doi: 10.1016/j.jmb.2017.05.014. Epub 2017 May 21.

PMID:
28539250
4.

Stable aneuploid tumors cells are more sensitive to TTK inhibition than chromosomally unstable cell lines.

Libouban MAA, de Roos JADM, Uitdehaag JCM, Willemsen-Seegers N, Mainardi S, Dylus J, de Man J, Tops B, Meijerink JPP, Storchová Z, Buijsman RC, Medema RH, Zaman GJR.

Oncotarget. 2017 Jun 13;8(24):38309-38325. doi: 10.18632/oncotarget.16213.

5.

Compound Selectivity and Target Residence Time of Kinase Inhibitors Studied with Surface Plasmon Resonance.

Willemsen-Seegers N, Uitdehaag JCM, Prinsen MBW, de Vetter JRF, de Man J, Sawa M, Kawase Y, Buijsman RC, Zaman GJR.

J Mol Biol. 2017 Feb 17;429(4):574-586. doi: 10.1016/j.jmb.2016.12.019. Epub 2016 Dec 30.

PMID:
28043854
6.

Identification of an evolutionary conserved structural loop that is required for the enzymatic and biological function of tryptophan 2,3-dioxygenase.

Michels H, Seinstra RI, Uitdehaag JC, Koopman M, van Faassen M, Martineau CN, Kema IP, Buijsman R, Nollen EA.

Sci Rep. 2016 Dec 20;6:39199. doi: 10.1038/srep39199.

7.

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.

Mol Cancer Ther. 2016 Dec;15(12):3097-3109. Epub 2016 Sep 1.

8.

MEK and PI3K-AKT inhibitors synergistically block activated IL7 receptor signaling in T-cell acute lymphoblastic leukemia.

Canté-Barrett K, Spijkers-Hagelstein JA, Buijs-Gladdines JG, Uitdehaag JC, Smits WK, van der Zwet J, Buijsman RC, Zaman GJ, Pieters R, Meijerink JP.

Leukemia. 2016 Sep;30(9):1832-43. doi: 10.1038/leu.2016.83. Epub 2016 Apr 22.

9.

Structural modeling of JAK1 mutations in T-cell acute lymphoblastic leukemia reveals a second contact site between pseudokinase and kinase domains.

Canté-Barrett K, Uitdehaag JC, Meijerink JP.

Haematologica. 2016 May;101(5):e189-91. doi: 10.3324/haematol.2015.138248. Epub 2016 Jan 27. No abstract available.

10.

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.

Ann Oncol. 2015 Oct;26(10):2180-92. doi: 10.1093/annonc/mdv293. Epub 2015 Jul 7.

PMID:
26153498
11.

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

Uitdehaag JC, de Roos JA, van Doornmalen AM, Prinsen MB, Spijkers-Hagelstein JA, de Vetter JR, de Man J, Buijsman RC, Zaman GJ.

PLoS One. 2015 May 27;10(5):e0125021. doi: 10.1371/journal.pone.0125021. eCollection 2015. Erratum in: PLoS One. 2015;10(6):e0132230.

12.

High-throughput fluorescence-based screening assays for tryptophan-catabolizing enzymes.

Seegers N, van Doornmalen AM, Uitdehaag JC, de Man J, Buijsman RC, Zaman GJ.

J Biomol Screen. 2014 Oct;19(9):1266-74. doi: 10.1177/1087057114536616. Epub 2014 May 27.

PMID:
24870017
13.

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

Uitdehaag JC, de Roos JA, van Doornmalen AM, Prinsen MB, de Man J, Tanizawa Y, Kawase Y, Yoshino K, Buijsman RC, Zaman GJ.

PLoS One. 2014 Mar 20;9(3):e92146. doi: 10.1371/journal.pone.0092146. eCollection 2014.

14.

A guide to picking the most selective kinase inhibitor tool compounds for pharmacological validation of drug targets.

Uitdehaag JC, Verkaar F, Alwan H, de Man J, Buijsman RC, Zaman GJ.

Br J Pharmacol. 2012 Jun;166(3):858-76. doi: 10.1111/j.1476-5381.2012.01859.x. Review.

15.

Multidimensional profiling of CSF1R screening hits and inhibitors: assessing cellular activity, target residence time, and selectivity in a higher throughput way.

Uitdehaag JC, Sünnen CM, van Doornmalen AM, de Rouw N, Oubrie A, Azevedo R, Ziebell M, Nickbarg E, Karstens WJ, Ruygrok S.

J Biomol Screen. 2011 Oct;16(9):1007-17. doi: 10.1177/1087057111418113. Epub 2011 Aug 26.

PMID:
21873591
16.

Bet hedging based cooperation can limit kin selection and form a basis for mutualism.

Uitdehaag JC.

J Theor Biol. 2011 Jul 7;280(1):76-87. doi: 10.1016/j.jtbi.2011.04.002. Epub 2011 Apr 15.

PMID:
21510961
17.

A theoretical entropy score as a single value to express inhibitor selectivity.

Uitdehaag JC, Zaman GJ.

BMC Bioinformatics. 2011 Apr 12;12:94. doi: 10.1186/1471-2105-12-94.

18.

The seven types of drug discovery waste: toward a new lean for the drug industry.

Uitdehaag JC.

Drug Discov Today. 2011 May;16(9-10):369-71. doi: 10.1016/j.drudis.2011.02.013. Epub 2011 Feb 25. No abstract available.

PMID:
21354473
19.

Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors.

Cai J, Robinson J, Belshaw S, Everett K, Fradera X, van Zeeland M, van Berkom L, van Rijnsbergen P, Popplestone L, Baugh M, Dempster M, Bruin J, Hamilton W, Kinghorn E, Westwood P, Kerr J, Rankovic Z, Arbuckle W, Bennett DJ, Jones PS, Long C, Martin I, Uitdehaag JC, Meulemans T.

Bioorg Med Chem Lett. 2010 Dec 1;20(23):6890-4. doi: 10.1016/j.bmcl.2010.10.012. Epub 2010 Oct 26.

PMID:
21030256
20.

Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: improving selectivity over hERG.

Rankovic Z, Cai J, Kerr J, Fradera X, Robinson J, Mistry A, Finlay W, McGarry G, Andrews F, Caulfield W, Cumming I, Dempster M, Waller J, Arbuckle W, Anderson M, Martin I, Mitchell A, Long C, Baugh M, Westwood P, Kinghorn E, Jones P, Uitdehaag JC, van Zeeland M, Potin D, Saniere L, Fouquet A, Chevallier F, Deronzier H, Dorleans C, Nicolai E.

Bioorg Med Chem Lett. 2010 Nov 1;20(21):6237-41. doi: 10.1016/j.bmcl.2010.08.101. Epub 2010 Aug 24.

PMID:
20843687
21.

6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors.

Cai J, Baugh M, Black D, Long C, Jonathan Bennett D, Dempster M, Fradera X, Gillespie J, Andrews F, Boucharens S, Bruin J, Cameron KS, Cumming I, Hamilton W, Jones PS, Kaptein A, Kinghorn E, Maidment M, Martin I, Mitchell A, Rankovic Z, Robinson J, Scullion P, Uitdehaag JC, Vink P, Westwood P, van Zeeland M, van Berkom L, Bastiani M, Meulemans T.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4350-4. doi: 10.1016/j.bmcl.2010.06.072. Epub 2010 Jun 17.

PMID:
20598883
22.

2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors.

Cai J, Bennett DJ, Rankovic Z, Dempster M, Fradera X, Gillespie J, Cumming I, Finlay W, Baugh M, Boucharens S, Bruin J, Cameron KS, Hamilton W, Kerr J, Kinghorn E, McGarry G, Robinson J, Scullion P, Uitdehaag JC, van Zeeland M, Potin D, Saniere L, Fouquet A, Chevallier F, Deronzier H, Dorleans C, Nicolai E.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4447-50. doi: 10.1016/j.bmcl.2010.06.049. Epub 2010 Jun 15.

PMID:
20594841
23.

4-(3-Trifluoromethylphenyl)-pyrimidine-2-carbonitrile as cathepsin S inhibitors: N3, not N1 is critically important.

Cai J, Fradera X, van Zeeland M, Dempster M, Cameron KS, Bennett DJ, Robinson J, Popplestone L, Baugh M, Westwood P, Bruin J, Hamilton W, Kinghorn E, Long C, Uitdehaag JC.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4507-10. doi: 10.1016/j.bmcl.2010.06.043. Epub 2010 Jun 10.

PMID:
20580231
24.

X-ray structures of the LXRalpha LBD in its homodimeric form and implications for heterodimer signaling.

Fradera X, Vu D, Nimz O, Skene R, Hosfield D, Wynands R, Cooke AJ, Haunsø A, King A, Bennett DJ, McGuire R, Uitdehaag JC.

J Mol Biol. 2010 May 28;399(1):120-32. doi: 10.1016/j.jmb.2010.04.005. Epub 2010 Apr 9.

PMID:
20382159
25.

The dependency game: multiperson reciprocal sharing leads to stable cooperation which can evolve into group formation.

Uitdehaag JC.

J Theor Biol. 2009 Sep 21;260(2):253-60. doi: 10.1016/j.jtbi.2009.06.009. Epub 2009 Jun 13.

PMID:
19527733
26.

The X-ray structure of RU486 bound to the progesterone receptor in a destabilized agonistic conformation.

Raaijmakers HC, Versteegh JE, Uitdehaag JC.

J Biol Chem. 2009 Jul 17;284(29):19572-9. doi: 10.1074/jbc.M109.007872. Epub 2009 Apr 16.

27.

Identification of acceptor substrate binding subsites +2 and +3 in the amylomaltase from Thermus thermophilus HB8.

Kaper T, Leemhuis H, Uitdehaag JC, van der Veen BA, Dijkstra BW, van der Maarel MJ, Dijkhuizen L.

Biochemistry. 2007 May 1;46(17):5261-9. Epub 2007 Apr 4.

PMID:
17407266
28.

Where is the optimism? Warrior teachings to regain the drug discovery spirit.

Uitdehaag JC.

Drug Discov Today. 2007 Feb;12(3-4):105-7. Epub 2006 Dec 15. No abstract available.

PMID:
17275729
29.

Crystal structure of the CUB1-EGF-CUB2 region of mannose-binding protein associated serine protease-2.

Feinberg H, Uitdehaag JC, Davies JM, Wallis R, Drickamer K, Weis WI.

EMBO J. 2003 May 15;22(10):2348-59.

30.

Properties and applications of starch-converting enzymes of the alpha-amylase family.

van der Maarel MJ, van der Veen B, Uitdehaag JC, Leemhuis H, Dijkhuizen L.

J Biotechnol. 2002 Mar 28;94(2):137-55. Review.

PMID:
11796168
31.

The remote substrate binding subsite -6 in cyclodextrin-glycosyltransferase controls the transferase activity of the enzyme via an induced-fit mechanism.

Leemhuis H, Uitdehaag JC, Rozeboom HJ, Dijkstra BW, Dijkhuizen L.

J Biol Chem. 2002 Jan 11;277(2):1113-9. Epub 2001 Nov 5.

32.

Hydrophobic amino acid residues in the acceptor binding site are main determinants for reaction mechanism and specificity of cyclodextrin-glycosyltransferase.

van der Veen BA, Leemhuis H, Kralj S, Uitdehaag JC, Dijkstra BW, Dijkhuizen L.

J Biol Chem. 2001 Nov 30;276(48):44557-62. Epub 2001 Sep 12.

33.

Enzymatic circularization of a malto-octaose linear chain studied by stochastic reaction path calculations on cyclodextrin glycosyltransferase.

Uitdehaag JC, van der Veen BA, Dijkhuizen L, Elber R, Dijkstra BW.

Proteins. 2001 May 15;43(3):327-35.

PMID:
11288183
34.

Engineering of cyclodextrin glycosyltransferase reaction and product specificity.

van der Veen BA, Uitdehaag JC, Dijkstra BW, Dijkhuizen L.

Biochim Biophys Acta. 2000 Dec 29;1543(2):336-360. Review. No abstract available.

PMID:
11150613
35.
37.

Rational design of cyclodextrin glycosyltransferase from Bacillus circulans strain 251 to increase alpha-cyclodextrin production.

van der Veen BA, Uitdehaag JC, Penninga D, van Alebeek GJ, Smith LM, Dijkstra BW, Dijkhuizen L.

J Mol Biol. 2000 Mar 3;296(4):1027-38.

PMID:
10686101
38.
39.

The cyclization mechanism of cyclodextrin glycosyltransferase (CGTase) as revealed by a gamma-cyclodextrin-CGTase complex at 1.8-A resolution.

Uitdehaag JC, Kalk KH, van Der Veen BA, Dijkhuizen L, Dijkstra BW.

J Biol Chem. 1999 Dec 3;274(49):34868-76.

40.

X-ray structures along the reaction pathway of cyclodextrin glycosyltransferase elucidate catalysis in the alpha-amylase family.

Uitdehaag JC, Mosi R, Kalk KH, van der Veen BA, Dijkhuizen L, Withers SG, Dijkstra BW.

Nat Struct Biol. 1999 May;6(5):432-6.

PMID:
10331869
41.

Reassessment of acarbose as a transition state analogue inhibitor of cyclodextrin glycosyltransferase.

Mosi R, Sham H, Uitdehaag JC, Ruiterkamp R, Dijkstra BW, Withers SG.

Biochemistry. 1998 Dec 8;37(49):17192-8.

PMID:
9860832
42.
43.

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