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Items: 9

1.

High Proliferation Rate and a Compromised Spindle Assembly Checkpoint Confers Sensitivity to the MPS1 Inhibitor BOS172722 in Triple-Negative Breast Cancers.

Anderhub SJ, Mak GW, Gurden MD, Faisal A, Drosopoulos K, Walsh K, Woodward HL, Innocenti P, Westwood IM, Naud S, Hayes A, Theofani E, Filosto S, Saville H, Burke R, van Montfort RLM, Raynaud FI, Blagg J, Hoelder S, Eccles SA, Linardopoulos S.

Mol Cancer Ther. 2019 Oct;18(10):1696-1707. doi: 10.1158/1535-7163.MCT-18-1203.

PMID:
31575759
2.

Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4- d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N2-(2-Ethoxy-4-(4-methyl-4 H-1,2,4-triazol-3-yl)phenyl)-6-methyl- N8-neopentylpyrido[3,4- d]pyrimidine-2,8-diamine (BOS172722).

Woodward HL, Innocenti P, Cheung KJ, Hayes A, Roberts J, Henley AT, Faisal A, Mak GW, Box G, Westwood IM, Cronin N, Carter M, Valenti M, De Haven Brandon A, O'Fee L, Saville H, Schmitt J, Burke R, Broccatelli F, van Montfort RLM, Raynaud FI, Eccles SA, Linardopoulos S, Blagg J, Hoelder S.

J Med Chem. 2018 Sep 27;61(18):8226-8240. doi: 10.1021/acs.jmedchem.8b00690. Epub 2018 Sep 10.

3.

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.

4.

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.

5.

CDK5RAP3 is a novel repressor of p14ARF in hepatocellular carcinoma cells.

Mak GW, Lai WL, Zhou Y, Li M, Ng IO, Ching YP.

PLoS One. 2012;7(7):e42210. doi: 10.1371/journal.pone.0042210. Epub 2012 Jul 31.

6.

The LIM-only protein FHL2 regulates interleukin-6 expression through p38 MAPK mediated NF-κB pathway in muscle cells.

Wong CH, Mak GW, Li MS, Tsui SK.

Cytokine. 2012 Aug;59(2):286-93. doi: 10.1016/j.cyto.2012.04.044. Epub 2012 May 24.

PMID:
22633286
7.

Overexpression of a novel activator of PAK4, the CDK5 kinase-associated protein CDK5RAP3, promotes hepatocellular carcinoma metastasis.

Mak GW, Chan MM, Leong VY, Lee JM, Yau TO, Ng IO, Ching YP.

Cancer Res. 2011 Apr 15;71(8):2949-58. doi: 10.1158/0008-5472.CAN-10-4046. Epub 2011 Mar 8.

8.

Impact of G₂ checkpoint defect on centromeric instability.

Deng W, Tsao SW, Mak GW, Tsang CM, Ching YP, Guan XY, Huen MS, Cheung AL.

Oncogene. 2011 Mar 17;30(11):1281-9. doi: 10.1038/onc.2010.508. Epub 2010 Nov 8.

PMID:
21057540
9.

Green fluorescent protein induces the secretion of inflammatory cytokine interleukin-6 in muscle cells.

Mak GW, Wong CH, Tsui SK.

Anal Biochem. 2007 Mar 15;362(2):296-8. Epub 2007 Jan 4. No abstract available.

PMID:
17258166

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