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Items: 12


Dual-mechanism ERK1/2 inhibitors exploit a distinct binding mode to block phosphorylation and nuclear accumulation of ERK1/2.

Kidger AM, Munck JM, Saini HK, Balmanno K, Minihane E, Courtin A, Graham B, O'Reilly M, Odle R, Cook SJ.

Mol Cancer Ther. 2019 Nov 20. pii: molcanther.0505.2019. doi: 10.1158/1535-7163.MCT-19-0505. [Epub ahead of print]


Selective DNA-PKcs inhibition extends the therapeutic index of localized radiotherapy and chemotherapy.

Willoughby CE, Jiang Y, Thomas HD, Willmore E, Kyle S, Wittner A, Phillips N, Zhao Y, Tudhope SJ, Prendergast L, Junge G, Lourenco LM, Finlay MRV, Turner P, Munck JM, Griffin RJ, Rennison T, Pickles J, Cano C, Newell DR, Reeves HL, Ryan AJ, Wedge SR.

J Clin Invest. 2019 Nov 25. pii: 127483. doi: 10.1172/JCI127483. [Epub ahead of print]


A Fragment-Derived Clinical Candidate for Antagonism of X-Linked and Cellular Inhibitor of Apoptosis Proteins: 1-(6-[(4-Fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-1 H,2 H,3 H-pyrrolo[3,2- b]pyridin-1-yl)-2-[(2 R,5 R)-5-methyl-2-([(3R)-3-methylmorpholin-4-yl]methyl)piperazin-1-yl]ethan-1-one (ASTX660).

Johnson CN, Ahn JS, Buck IM, Chiarparin E, Day JEH, Hopkins A, Howard S, Lewis EJ, Martins V, Millemaggi A, Munck JM, Page LW, Peakman T, Reader M, Rich SJ, Saxty G, Smyth T, Thompson NT, Ward GA, Williams PA, Wilsher NE, Chessari G.

J Med Chem. 2018 Aug 23;61(16):7314-7329. doi: 10.1021/acs.jmedchem.8b00900. Epub 2018 Aug 9.


Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2.

Heightman TD, Berdini V, Braithwaite H, Buck IM, Cassidy M, Castro J, Courtin A, Day JEH, East C, Fazal L, Graham B, Griffiths-Jones CM, Lyons JF, Martins V, Muench S, Munck JM, Norton D, O'Reilly M, Palmer N, Pathuri P, Reader M, Rees DC, Rich SJ, Richardson C, Saini H, Thompson NT, Wallis NG, Walton H, Wilsher NE, Woolford AJ, Cooke M, Cousin D, Onions S, Shannon J, Watts J, Murray CW.

J Med Chem. 2018 Jun 14;61(11):4978-4992. doi: 10.1021/acs.jmedchem.8b00421. Epub 2018 May 31.


ASTX660, a Novel Non-peptidomimetic Antagonist of cIAP1/2 and XIAP, Potently Induces TNF╬▒-Dependent Apoptosis in Cancer Cell Lines and Inhibits Tumor Growth.

Ward GA, Lewis EJ, Ahn JS, Johnson CN, Lyons JF, Martins V, Munck JM, Rich SJ, Smyth T, Thompson NT, Williams PA, Wilsher NE, Wallis NG, Chessari G.

Mol Cancer Ther. 2018 Jul;17(7):1381-1391. doi: 10.1158/1535-7163.MCT-17-0848. Epub 2018 Apr 25.


Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors.

Murray CW, Berdini V, Buck IM, Carr ME, Cleasby A, Coyle JE, Curry JE, Day JE, Day PJ, Hearn K, Iqbal A, Lee LY, Martins V, Mortenson PN, Munck JM, Page LW, Patel S, Roomans S, Smith K, Tamanini E, Saxty G.

ACS Med Chem Lett. 2015 Jun 4;6(7):798-803. doi: 10.1021/acsmedchemlett.5b00143. eCollection 2015 Jul 9.


DNA-PK-A candidate driver of hepatocarcinogenesis and tissue biomarker that predicts response to treatment and survival.

Cornell L, Munck JM, Alsinet C, Villanueva A, Ogle L, Willoughby CE, Televantou D, Thomas HD, Jackson J, Burt AD, Newell D, Rose J, Manas DM, Shapiro GI, Curtin NJ, Reeves HL.

Clin Cancer Res. 2015 Feb 15;21(4):925-33. doi: 10.1158/1078-0432.CCR-14-0842. Epub 2014 Dec 5.


Inhibition of HSP90 by AT13387 delays the emergence of resistance to BRAF inhibitors and overcomes resistance to dual BRAF and MEK inhibition in melanoma models.

Smyth T, Paraiso KHT, Hearn K, Rodriguez-Lopez AM, Munck JM, Haarberg HE, Sondak VK, Thompson NT, Azab M, Lyons JF, Smalley KSM, Wallis NG.

Mol Cancer Ther. 2014 Dec;13(12):2793-2804. doi: 10.1158/1535-7163.MCT-14-0452. Epub 2014 Oct 27.


Intra-ER sorting of the peroxisomal membrane protein Pex3 relies on its luminal domain.

Fakieh MH, Drake PJ, Lacey J, Munck JM, Motley AM, Hettema EH.

Biol Open. 2013 Jun 25;2(8):829-37. doi: 10.1242/bio.20134788. eCollection 2013 Aug 15.


Chemosensitization of cancer cells by KU-0060648, a dual inhibitor of DNA-PK and PI-3K.

Munck JM, Batey MA, Zhao Y, Jenkins H, Richardson CJ, Cano C, Tavecchio M, Barbeau J, Bardos J, Cornell L, Griffin RJ, Menear K, Slade A, Thommes P, Martin NM, Newell DR, Smith GC, Curtin NJ.

Mol Cancer Ther. 2012 Aug;11(8):1789-98. doi: 10.1158/1535-7163.MCT-11-0535. Epub 2012 May 10.


Further characterisation of the cellular activity of the DNA-PK inhibitor, NU7441, reveals potential cross-talk with homologous recombination.

Tavecchio M, Munck JM, Cano C, Newell DR, Curtin NJ.

Cancer Chemother Pharmacol. 2012 Jan;69(1):155-64. doi: 10.1007/s00280-011-1662-4. Epub 2011 Jun 1.


A dual function for Pex3p in peroxisome formation and inheritance.

Munck JM, Motley AM, Nuttall JM, Hettema EH.

J Cell Biol. 2009 Nov 16;187(4):463-71. doi: 10.1083/jcb.200906161. Epub 2009 Nov 9.

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