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Items: 1 to 20 of 131

1.

Novel Mps1 Kinase Inhibitors with Potent Antitumor Activity.

Wengner AM, Siemeister G, Koppitz M, Schulze V, Kosemund D, Klar U, Stoeckigt D, Neuhaus R, Lienau P, Bader B, Prechtl S, Raschke M, Frisk AL, von Ahsen O, Michels M, Kreft B, von Nussbaum F, Brands M, Mumberg D, Ziegelbauer K.

Mol Cancer Ther. 2016 Apr;15(4):583-92. doi: 10.1158/1535-7163.MCT-15-0500. Epub 2016 Feb 1.

2.

Characterization of novel MPS1 inhibitors with preclinical anticancer activity.

Jemaà M, Galluzzi L, Kepp O, Senovilla L, Brands M, Boemer U, Koppitz M, Lienau P, Prechtl S, Schulze V, Siemeister G, Wengner AM, Mumberg D, Ziegelbauer K, Abrieu A, Castedo M, Vitale I, Kroemer G.

Cell Death Differ. 2013 Nov;20(11):1532-45. doi: 10.1038/cdd.2013.105. Epub 2013 Aug 9.

3.

Functional characterization of CFI-402257, a potent and selective Mps1/TTK kinase inhibitor, for the treatment of cancer.

Mason JM, Wei X, Fletcher GC, Kiarash R, Brokx R, Hodgson R, Beletskaya I, Bray MR, Mak TW.

Proc Natl Acad Sci U S A. 2017 Mar 21;114(12):3127-3132. doi: 10.1073/pnas.1700234114. Epub 2017 Mar 7.

4.

Effects of the selective MPS1 inhibitor MPS1-IN-3 on glioblastoma sensitivity to antimitotic drugs.

Tannous BA, Kerami M, Van der Stoop PM, Kwiatkowski N, Wang J, Zhou W, Kessler AF, Lewandrowski G, Hiddingh L, Sol N, Lagerweij T, Wedekind L, Niers JM, Barazas M, Nilsson RJ, Geerts D, De Witt Hamer PC, Hagemann C, Vandertop WP, Van Tellingen O, Noske DP, Gray NS, Würdinger T.

J Natl Cancer Inst. 2013 Sep 4;105(17):1322-31. doi: 10.1093/jnci/djt168. Epub 2013 Aug 12.

5.

Discovery of 4-(4-aminopyrazolo[1,5-a][1,3,5]triazin-8-yl)benzamides as novel, highly potent and selective, orally bioavailable inhibitors of Tyrosine Threonine Kinase, TTK.

Laufer R, Li SW, Liu Y, Ng G, Lang Y, Feher M, Brokx R, Beletskaya I, Hodgson R, Mao G, Plotnikova O, Awrey DE, Mason JM, Wei X, Lin DC, Che Y, Kiarash R, Madeira B, Fletcher GC, Mak TW, Bray MR, Pauls HW.

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3562-6. doi: 10.1016/j.bmcl.2016.06.021. Epub 2016 Jun 9.

PMID:
27335255
6.

TC Mps1 12, a novel Mps1 inhibitor, suppresses the growth of hepatocellular carcinoma cells via the accumulation of chromosomal instability.

Choi M, Min YH, Pyo J, Lee CW, Jang CY, Kim JE.

Br J Pharmacol. 2017 Jun;174(12):1810-1825. doi: 10.1111/bph.13782. Epub 2017 Apr 22.

7.

Mitotic Checkpoint Kinase Mps1 Has a Role in Normal Physiology which Impacts Clinical Utility.

Martinez R, Blasina A, Hallin JF, Hu W, Rymer I, Fan J, Hoffman RL, Murphy S, Marx M, Yanochko G, Trajkovic D, Dinh D, Timofeevski S, Zhu Z, Sun P, Lappin PB, Murray BW.

PLoS One. 2015 Sep 23;10(9):e0138616. doi: 10.1371/journal.pone.0138616. eCollection 2015.

8.

Discovery of imidazo[1,2-b]pyridazine derivatives: selective and orally available Mps1 (TTK) kinase inhibitors exhibiting remarkable antiproliferative activity.

Kusakabe K, Ide N, Daigo Y, Itoh T, Yamamoto T, Hashizume H, Nozu K, Yoshida H, Tadano G, Tagashira S, Higashino K, Okano Y, Sato Y, Inoue M, Iguchi M, Kanazawa T, Ishioka Y, Dohi K, Kido Y, Sakamoto S, Ando S, Maeda M, Higaki M, Baba Y, Nakamura Y.

J Med Chem. 2015 Feb 26;58(4):1760-75. doi: 10.1021/jm501599u. Epub 2015 Feb 10.

PMID:
25625617
9.

Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase.

Colombo R, Caldarelli M, Mennecozzi M, Giorgini ML, Sola F, Cappella P, Perrera C, Depaolini SR, Rusconi L, Cucchi U, Avanzi N, Bertrand JA, Bossi RT, Pesenti E, Galvani A, Isacchi A, Colotta F, Donati D, Moll J.

Cancer Res. 2010 Dec 15;70(24):10255-64. doi: 10.1158/0008-5472.CAN-10-2101.

10.

Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach.

Innocenti P, Woodward HL, Solanki S, Naud S, Westwood IM, Cronin N, Hayes A, Roberts J, Henley AT, Baker R, Faisal A, Mak GW, Box G, Valenti M, De Haven Brandon A, O'Fee L, Saville H, Schmitt J, Matijssen B, Burke R, van Montfort RL, Raynaud FI, Eccles SA, Linardopoulos S, Blagg J, Hoelder S.

J Med Chem. 2016 Apr 28;59(8):3671-88. doi: 10.1021/acs.jmedchem.5b01811. Epub 2016 Apr 7.

11.

Whole-genome duplication increases tumor cell sensitivity to MPS1 inhibition.

Jemaà M, Manic G, Lledo G, Lissa D, Reynes C, Morin N, Chibon F, Sistigu A, Castedo M, Vitale I, Kroemer G, Abrieu A.

Oncotarget. 2016 Jan 5;7(1):885-901. doi: 10.18632/oncotarget.6432.

12.

A unique hinge binder of extremely selective aminopyridine-based Mps1 (TTK) kinase inhibitors with cellular activity.

Kusakabe K, Ide N, Daigo Y, Itoh T, Yamamoto T, Kojima E, Mitsuoka Y, Tadano G, Tagashira S, Higashino K, Okano Y, Sato Y, Inoue M, Iguchi M, Kanazawa T, Ishioka Y, Dohi K, Kido Y, Sakamoto S, Ando S, Maeda M, Higaki M, Yoshizawa H, Murai H, Nakamura Y.

Bioorg Med Chem. 2015 May 1;23(9):2247-60. doi: 10.1016/j.bmc.2015.02.042. Epub 2015 Mar 4.

PMID:
25801152
13.

Characterisation of CCT271850, a selective, oral and potent MPS1 inhibitor, used to directly measure in vivo MPS1 inhibition vs therapeutic efficacy.

Faisal A, Mak GWY, Gurden MD, Xavier CPR, Anderhub SJ, Innocenti P, Westwood IM, Naud S, Hayes A, Box G, Valenti MR, De Haven Brandon AK, O'Fee L, Schmitt J, Woodward HL, Burke R, vanMontfort RLM, Blagg J, Raynaud FI, Eccles SA, Hoelder S, Linardopoulos S.

Br J Cancer. 2017 Apr 25;116(9):1166-1176. doi: 10.1038/bjc.2017.75. Epub 2017 Mar 23.

14.

Understanding inhibitor resistance in Mps1 kinase through novel biophysical assays and structures.

Hiruma Y, Koch A, Hazraty N, Tsakou F, Medema RH, Joosten RP, Perrakis A.

J Biol Chem. 2017 Sep 1;292(35):14496-14504. doi: 10.1074/jbc.M117.783555. Epub 2017 Jul 18.

15.

Preclinical evaluation of the WEE1 inhibitor MK-1775 as single-agent anticancer therapy.

Guertin AD, Li J, Liu Y, Hurd MS, Schuller AG, Long B, Hirsch HA, Feldman I, Benita Y, Toniatti C, Zawel L, Fawell SE, Gilliland DG, Shumway SD.

Mol Cancer Ther. 2013 Aug;12(8):1442-52. doi: 10.1158/1535-7163.MCT-13-0025. Epub 2013 May 22.

16.

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
17.

Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1).

Naud S, Westwood IM, Faisal A, Sheldrake P, Bavetsias V, Atrash B, Cheung KM, Liu M, Hayes A, Schmitt J, Wood A, Choi V, Boxall K, Mak G, Gurden M, Valenti M, de Haven Brandon A, Henley A, Baker R, McAndrew C, Matijssen B, Burke R, Hoelder S, Eccles SA, Raynaud FI, Linardopoulos S, van Montfort RL, Blagg J.

J Med Chem. 2013 Dec 27;56(24):10045-65. doi: 10.1021/jm401395s. Epub 2013 Dec 2.

18.

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
19.

Characterization of the cellular and antitumor effects of MPI-0479605, a small-molecule inhibitor of the mitotic kinase Mps1.

Tardif KD, Rogers A, Cassiano J, Roth BL, Cimbora DM, McKinnon R, Peterson A, Douce TB, Robinson R, Dorweiler I, Davis T, Hess MA, Ostanin K, Papac DI, Baichwal V, McAlexander I, Willardsen JA, Saunders M, Christophe H, Kumar DV, Wettstein DA, Carlson RO, Williams BL.

Mol Cancer Ther. 2011 Dec;10(12):2267-75. doi: 10.1158/1535-7163.MCT-11-0453. Epub 2011 Oct 6.

20.

Selective inhibition of pancreatic ductal adenocarcinoma cell growth by the mitotic MPS1 kinase inhibitor NMS-P715.

Slee RB, Grimes BR, Bansal R, Gore J, Blackburn C, Brown L, Gasaway R, Jeong J, Victorino J, March KL, Colombo R, Herbert BS, Korc M.

Mol Cancer Ther. 2014 Feb;13(2):307-315. doi: 10.1158/1535-7163.MCT-13-0324. Epub 2013 Nov 26.

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