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Items: 44

1.

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.

PMID:
30091600
2.

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.

PMID:
29775310
3.

ASTX660, a Novel Non-peptidomimetic Antagonist of cIAP1/2 and XIAP, Potently Induces TNFα-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.

4.

Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor.

Perera TPS, Jovcheva E, Mevellec L, Vialard J, De Lange D, Verhulst T, Paulussen C, Van De Ven K, King P, Freyne E, Rees DC, Squires M, Saxty G, Page M, Murray CW, Gilissen R, Ward G, Thompson NT, Newell DR, Cheng N, Xie L, Yang J, Platero SJ, Karkera JD, Moy C, Angibaud P, Laquerre S, Lorenzi MV.

Mol Cancer Ther. 2017 Jun;16(6):1010-1020. doi: 10.1158/1535-7163.MCT-16-0589. Epub 2017 Mar 24.

5.

Emergence of resistance to tyrosine kinase inhibitors in non-small-cell lung cancer can be delayed by an upfront combination with the HSP90 inhibitor onalespib.

Courtin A, Smyth T, Hearn K, Saini HK, Thompson NT, Lyons JF, Wallis NG.

Br J Cancer. 2016 Oct 25;115(9):1069-1077. doi: 10.1038/bjc.2016.294. Epub 2016 Sep 27.

6.

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.

7.

AT13148 is a novel, oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity.

Yap TA, Walton MI, Grimshaw KM, Te Poele RH, Eve PD, Valenti MR, de Haven Brandon AK, Martins V, Zetterlund A, Heaton SP, Heinzmann K, Jones PS, Feltell RE, Reule M, Woodhead SJ, Davies TG, Lyons JF, Raynaud FI, Eccles SA, Workman P, Thompson NT, Garrett MD.

Clin Cancer Res. 2012 Jul 15;18(14):3912-23. doi: 10.1158/1078-0432.CCR-11-3313. Epub 2012 Jul 10.

8.

The HSP90 inhibitor, AT13387, is effective against imatinib-sensitive and -resistant gastrointestinal stromal tumor models.

Smyth T, Van Looy T, Curry JE, Rodriguez-Lopez AM, Wozniak A, Zhu M, Donsky R, Morgan JG, Mayeda M, Fletcher JA, Schöffski P, Lyons J, Thompson NT, Wallis NG.

Mol Cancer Ther. 2012 Aug;11(8):1799-808. doi: 10.1158/1535-7163.MCT-11-1046. Epub 2012 Jun 19.

9.

The heat shock protein 90 inhibitor, AT13387, displays a long duration of action in vitro and in vivo in non-small cell lung cancer.

Graham B, Curry J, Smyth T, Fazal L, Feltell R, Harada I, Coyle J, Williams B, Reule M, Angove H, Cross DM, Lyons J, Wallis NG, Thompson NT.

Cancer Sci. 2012 Mar;103(3):522-7. doi: 10.1111/j.1349-7006.2011.02191.x. Epub 2012 Feb 9.

10.

Potent, selective inhibitors of fibroblast growth factor receptor define fibroblast growth factor dependence in preclinical cancer models.

Squires M, Ward G, Saxty G, Berdini V, Cleasby A, King P, Angibaud P, Perera T, Fazal L, Ross D, Jones CG, Madin A, Benning RK, Vickerstaffe E, O'Brien A, Frederickson M, Reader M, Hamlett C, Batey MA, Rich S, Carr M, Miller D, Feltell R, Thiru A, Bethell S, Devine LA, Graham BL, Pike A, Cosme J, Lewis EJ, Freyne E, Lyons J, Irving J, Murray C, Newell DR, Thompson NT.

Mol Cancer Ther. 2011 Sep;10(9):1542-52. doi: 10.1158/1535-7163.MCT-11-0426. Epub 2011 Jul 15.

11.

Preclinical pharmacology, antitumor activity, and development of pharmacodynamic markers for the novel, potent AKT inhibitor CCT128930.

Yap TA, Walton MI, Hunter LJ, Valenti M, de Haven Brandon A, Eve PD, Ruddle R, Heaton SP, Henley A, Pickard L, Vijayaraghavan G, Caldwell JJ, Thompson NT, Aherne W, Raynaud FI, Eccles SA, Workman P, Collins I, Garrett MD.

Mol Cancer Ther. 2011 Feb;10(2):360-71. doi: 10.1158/1535-7163.MCT-10-0760. Epub 2010 Dec 29.

12.

Activity of the multitargeted kinase inhibitor, AT9283, in imatinib-resistant BCR-ABL-positive leukemic cells.

Tanaka R, Squires MS, Kimura S, Yokota A, Nagao R, Yamauchi T, Takeuchi M, Yao H, Reule M, Smyth T, Lyons JF, Thompson NT, Ashihara E, Ottmann OG, Maekawa T.

Blood. 2010 Sep 23;116(12):2089-95. doi: 10.1182/blood-2009-03-211466. Epub 2010 Jun 14.

PMID:
20548094
13.

AT9283, a potent inhibitor of the Aurora kinases and Jak2, has therapeutic potential in myeloproliferative disorders.

Dawson MA, Curry JE, Barber K, Beer PA, Graham B, Lyons JF, Richardson CJ, Scott MA, Smyth T, Squires MS, Thompson NT, Green AR, Wallis NG.

Br J Haematol. 2010 Jul;150(1):46-57. doi: 10.1111/j.1365-2141.2010.08175.x. Epub 2010 May 7.

PMID:
20507304
14.

AT7867 is a potent and oral inhibitor of AKT and p70 S6 kinase that induces pharmacodynamic changes and inhibits human tumor xenograft growth.

Grimshaw KM, Hunter LJ, Yap TA, Heaton SP, Walton MI, Woodhead SJ, Fazal L, Reule M, Davies TG, Seavers LC, Lock V, Lyons JF, Thompson NT, Workman P, Garrett MD.

Mol Cancer Ther. 2010 May;9(5):1100-10. doi: 10.1158/1535-7163.MCT-09-0986. Epub 2010 Apr 27.

15.

AT7519, a cyclin-dependent kinase inhibitor, exerts its effects by transcriptional inhibition in leukemia cell lines and patient samples.

Squires MS, Cooke L, Lock V, Qi W, Lewis EJ, Thompson NT, Lyons JF, Mahadevan D.

Mol Cancer Ther. 2010 Apr;9(4):920-8. doi: 10.1158/1535-7163.MCT-09-1071. Epub 2010 Mar 30.

16.

Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines.

Squires MS, Feltell RE, Wallis NG, Lewis EJ, Smith DM, Cross DM, Lyons JF, Thompson NT.

Mol Cancer Ther. 2009 Feb;8(2):324-32. doi: 10.1158/1535-7163.MCT-08-0890. Epub 2009 Jan 27.

17.

The p85 subunit of phosphoinositide 3-kinase is associated with beta-catenin in the cadherin-based adhesion complex.

Woodfield RJ, Hodgkin MN, Akhtar N, Morse MA, Fuller KJ, Saqib K, Thompson NT, Wakelam MJ.

Biochem J. 2001 Dec 1;360(Pt 2):335-44.

18.

Phosphatidylinositol 3-kinase and focal adhesion kinase are early signals in the growth factor-like responses to thrombospondin-1 seen in human vascular smooth muscle.

Lymn JS, Rao SJ, Clunn GF, Gallagher KL, O'Neil C, Thompson NT, Hughes AD.

Arterioscler Thromb Vasc Biol. 1999 Sep;19(9):2133-40.

PMID:
10479655
19.

CD4+ CD45RA+ and CD4+ CD45RO+ T cells differ in their TCR-associated signaling responses.

Hall SR, Heffernan BM, Thompson NT, Rowan WC.

Eur J Immunol. 1999 Jul;29(7):2098-106.

20.

Phospholipase D1 localises to secretory granules and lysosomes and is plasma-membrane translocated on cellular stimulation.

Brown FD, Thompson N, Saqib KM, Clark JM, Powner D, Thompson NT, Solari R, Wakelam MJ.

Curr Biol. 1998 Jul 2;8(14):835-8.

21.

Convergence of Schiff base costimulatory signaling and TCR signaling at the level of mitogen-activated protein kinase ERK2.

Chen H, Hall S, Heffernan B, Thompson NT, Rogers MV, Rhodes J.

J Immunol. 1997 Sep 1;159(5):2274-81.

PMID:
9278316
22.

Role of c-lyn in the functional effects of GM-CSF on human neutrophils.

Thompson NT, Randall RW, Garland LG.

Biochem Soc Trans. 1995 May;23(2):196S. No abstract available.

PMID:
7672217
23.

Phospholipase D: regulation and functional significance.

Thompson NT, Garland LG, Bonser RW.

Adv Pharmacol. 1993;24:199-238. Review.

PMID:
8389186
24.

Tyrosine phosphorylation is involved in receptor coupling to phospholipase D but not phospholipase C in the human neutrophil.

Uings IJ, Thompson NT, Randall RW, Spacey GD, Bonser RW, Hudson AT, Garland LG.

Biochem J. 1992 Feb 1;281 ( Pt 3):597-600. Erratum in: Biochem J 1992 May 1;283(Pt 3):919.

25.

Receptor-coupled phospholipase D and its inhibition.

Thompson NT, Bonser RW, Garland LG.

Trends Pharmacol Sci. 1991 Nov;12(11):404-8. Review. No abstract available.

PMID:
1665608
26.

A quantitative investigation into the dependence of Ca2+ mobilisation on changes in inositol 1,4,5-trisphosphate levels in the stimulated neutrophil.

Thompson NT, Bonser RW, Tateson JE, Spacey GD, Randall RW, Hodson HF, Garland LG.

Br J Pharmacol. 1991 Jun;103(2):1592-6.

27.

Demethoxyviridin and wortmannin block phospholipase C and D activation in the human neutrophil.

Bonser RW, Thompson NT, Randall RW, Tateson JE, Spacey GD, Hodson HF, Garland LG.

Br J Pharmacol. 1991 May;103(1):1237-41.

28.

The temporal relationship between phospholipase activation, diradylglycerol formation and superoxide production in the human neutrophil.

Thompson NT, Tateson JE, Randall RW, Spacey GD, Bonser RW, Garland LG.

Biochem J. 1990 Oct 1;271(1):209-13.

29.

A novel and sensitive assay for phospholipase D in intact cells.

Randall RW, Bonser RW, Thompson NT, Garland LG.

FEBS Lett. 1990 May 7;264(1):87-90.

30.

Phospholipase D activation is functionally linked to superoxide generation in the human neutrophil.

Bonser RW, Thompson NT, Randall RW, Garland LG.

Biochem J. 1989 Dec 1;264(2):617-20. Erratum in: Biochem J 1990 Feb 1;265(3):932.

31.
32.

Evidence that a second stereochemical centre in diacylglycerols defines interaction at the recognition site on protein kinase C.

Bonser RW, Thompson NT, Hodson HF, Beams RM, Garland LG.

FEBS Lett. 1988 Jul 18;234(2):341-4.

33.

Decrease of cellular ATP by dihexanoylglycerol may limit responses to protein kinase C activation.

Dawson J, Thompson NT, Bonser RW, Hodson HF, Garland LG.

FEBS Lett. 1987 Apr 6;214(1):171-5.

34.
35.

Inhibition of phorbol ester stimulated superoxide production by 1-oleoyl-2-acetyl-sn-glycerol (OAG); fact or artefact?

Bonser RW, Dawson J, Thompson NT, Hodson HF, Garland LG.

FEBS Lett. 1986 Dec 1;209(1):134-8.

37.

The use of the platelet aggregometer to monitor thrombin-induced conversion of fibrinogen to fibrin.

Ruda EM, Thompson NT, Scrutton MC.

Thromb Res. 1985 Dec 1;40(5):703-9. No abstract available.

PMID:
4089835
38.
39.

Intracellular calcium fluxes in human platelets.

Thompson NT, Scrutton MC.

Eur J Biochem. 1985 Mar 1;147(2):421-7.

40.

The role of cytoplasmic free calcium in the responses of quin2-loaded human platelets to vasopressin.

Hallam TJ, Thompson NT, Scrutton MC, Rink TJ.

Biochem J. 1984 Aug 1;221(3):897-901.

42.

Variability of dermal elastin visualized ultrastructurally with iron hematoxylin.

Spicer SS, Brissie RM, Thompson NT.

Am J Pathol. 1975 Jun;79(3):481-98.

43.

The variable fine structure of elastin visualized with Verhoeff's iron hematoxylin.

Brissie RM, Spicer SS, Thompson NT.

Anat Rec. 1975 Jan;181(1):83-94.

PMID:
45879
44.

Ultrastructural staining of thin sections with iron hematoxylin.

Brissie RM, Spicer SS, Hall BJ, Thompson NT.

J Histochem Cytochem. 1974 Sep;22(9):895-907. No abstract available.

PMID:
4138032

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