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Items: 46

1.

Structure-based design, synthesis and biological evaluation of a novel series of isoquinolone and pyrazolo[4,3-c]pyridine inhibitors of fascin 1 as potential anti-metastatic agents.

Francis S, Croft D, Schüttelkopf AW, Parry C, Pugliese A, Cameron K, Claydon S, Drysdale M, Gardner C, Gohlke A, Goodwin G, Gray CH, Konczal J, McDonald L, Mezna M, Pannifer A, Paul NR, Machesky L, McKinnon H, Bower J.

Bioorg Med Chem Lett. 2019 Apr 15;29(8):1023-1029. doi: 10.1016/j.bmcl.2019.01.035. Epub 2019 Jan 30.

2.

A Novel Small-Molecule Inhibitor of MRCK Prevents Radiation-Driven Invasion in Glioblastoma.

Birch JL, Strathdee K, Gilmour L, Vallatos A, McDonald L, Kouzeli A, Vasan R, Qaisi AH, Croft DR, Crighton D, Gill K, Gray CH, Konczal J, Mezna M, McArthur D, Schüttelkopf AW, McConnell P, Sime M, Holmes WM, Bower J, McKinnon HJ, Drysdale M, Olson MF, Chalmers AJ.

Cancer Res. 2018 Nov 15;78(22):6509-6522. doi: 10.1158/0008-5472.CAN-18-1697. Epub 2018 Oct 2.

PMID:
30279244
3.

The Meisenheimer Complex as a Paradigm in Drug Discovery: Reversible Covalent Inhibition through C67 of the ATP Binding Site of PLK1.

Pearson RJ, Blake DG, Mezna M, Fischer PM, Westwood NJ, McInnes C.

Cell Chem Biol. 2018 Sep 20;25(9):1107-1116.e4. doi: 10.1016/j.chembiol.2018.06.001. Epub 2018 Jul 12.

PMID:
30017915
4.

Colorectal Tumors Require NUAK1 for Protection from Oxidative Stress.

Port J, Muthalagu N, Raja M, Ceteci F, Monteverde T, Kruspig B, Hedley A, Kalna G, Lilla S, Neilson L, Brucoli M, Gyuraszova K, Tait-Mulder J, Mezna M, Svambaryte S, Bryson A, Sumpton D, McVie A, Nixon C, Drysdale M, Esumi H, Murray GI, Sansom OJ, Zanivan SR, Murphy DJ.

Cancer Discov. 2018 May;8(5):632-647. doi: 10.1158/2159-8290.CD-17-0533. Epub 2018 Mar 2.

5.

Discovery of Potent and Selective MRCK Inhibitors with Therapeutic Effect on Skin Cancer.

Unbekandt M, Belshaw S, Bower J, Clarke M, Cordes J, Crighton D, Croft DR, Drysdale MJ, Garnett MJ, Gill K, Gray C, Greenhalgh DA, Hall JAM, Konczal J, Lilla S, McArthur D, McConnell P, McDonald L, McGarry L, McKinnon H, McMenemy C, Mezna M, Morrice NA, Munro J, Naylor G, Rath N, Schüttelkopf AW, Sime M, Olson MF.

Cancer Res. 2018 Apr 15;78(8):2096-2114. doi: 10.1158/0008-5472.CAN-17-2870. Epub 2018 Jan 30.

6.

A fully automated procedure for the parallel, multidimensional purification and nucleotide loading of the human GTPases KRas, Rac1 and RalB.

Gray CH, Konczal J, Mezna M, Ismail S, Bower J, Drysdale M.

Protein Expr Purif. 2017 Apr;132:75-84. doi: 10.1016/j.pep.2017.01.010. Epub 2017 Jan 28.

7.

A novel small-molecule MRCK inhibitor blocks cancer cell invasion.

Unbekandt M, Croft DR, Crighton D, Mezna M, McArthur D, McConnell P, Schüttelkopf AW, Belshaw S, Pannifer A, Sime M, Bower J, Drysdale M, Olson MF.

Cell Commun Signal. 2014 Oct 5;12:54. doi: 10.1186/s12964-014-0054-x.

8.

5-Deazaflavin derivatives as inhibitors of p53 ubiquitination by HDM2.

Dickens MP, Roxburgh P, Hock A, Mezna M, Kellam B, Vousden KH, Fischer PM.

Bioorg Med Chem. 2013 Nov 15;21(22):6868-77. doi: 10.1016/j.bmc.2013.09.038. Epub 2013 Sep 25.

9.

Small molecules that bind the Mdm2 RING stabilize and activate p53.

Roxburgh P, Hock AK, Dickens MP, Mezna M, Fischer PM, Vousden KH.

Carcinogenesis. 2012 Apr;33(4):791-8. doi: 10.1093/carcin/bgs092. Epub 2012 Feb 2.

PMID:
22301280
10.

Development of a high-throughput screening method for LIM kinase 1 using a luciferase-based assay of ATP consumption.

Mezna M, Wong AC, Ainger M, Scott RW, Hammonds T, Olson MF.

J Biomol Screen. 2012 Apr;17(4):460-8. doi: 10.1177/1087057111430529. Epub 2011 Dec 7.

11.

Co-crystal structures of inhibitors with MRCKβ, a key regulator of tumor cell invasion.

Heikkila T, Wheatley E, Crighton D, Schroder E, Boakes A, Kaye SJ, Mezna M, Pang L, Rushbrooke M, Turnbull A, Olson MF.

PLoS One. 2011;6(9):e24825. doi: 10.1371/journal.pone.0024825. Epub 2011 Sep 20.

12.

Discovery and characterization of 2-anilino-4- (thiazol-5-yl)pyrimidine transcriptional CDK inhibitors as anticancer agents.

Wang S, Griffiths G, Midgley CA, Barnett AL, Cooper M, Grabarek J, Ingram L, Jackson W, Kontopidis G, McClue SJ, McInnes C, McLachlan J, Meades C, Mezna M, Stuart I, Thomas MP, Zheleva DI, Lane DP, Jackson RC, Glover DM, Blake DG, Fischer PM.

Chem Biol. 2010 Oct 29;17(10):1111-21. doi: 10.1016/j.chembiol.2010.07.016.

13.

Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.

Wang S, Midgley CA, Scaërou F, Grabarek JB, Griffiths G, Jackson W, Kontopidis G, McClue SJ, McInnes C, Meades C, Mezna M, Plater A, Stuart I, Thomas MP, Wood G, Clarke RG, Blake DG, Zheleva DI, Lane DP, Jackson RC, Glover DM, Fischer PM.

J Med Chem. 2010 Jun 10;53(11):4367-78. doi: 10.1021/jm901913s.

PMID:
20462263
14.

Activating ROCK1 somatic mutations in human cancer.

Lochhead PA, Wickman G, Mezna M, Olson MF.

Oncogene. 2010 Apr 29;29(17):2591-8. doi: 10.1038/onc.2010.3. Epub 2010 Feb 8.

PMID:
20140017
15.

Inhibitors of Polo-like kinase reveal roles in spindle-pole maintenance.

McInnes C, Mazumdar A, Mezna M, Meades C, Midgley C, Scaerou F, Carpenter L, Mackenzie M, Taylor P, Walkinshaw M, Fischer PM, Glover D.

Nat Chem Biol. 2006 Nov;2(11):608-17. Epub 2006 Oct 8.

PMID:
17028581
16.

Catch the kinase conformer.

McInnes C, Mezna M, Kontopidis G.

Chem Biol. 2006 Jul;13(7):693-4.

17.

Differential binding of inhibitors to active and inactive CDK2 provides insights for drug design.

Kontopidis G, McInnes C, Pandalaneni SR, McNae I, Gibson D, Mezna M, Thomas M, Wood G, Wang S, Walkinshaw MD, Fischer PM.

Chem Biol. 2006 Feb;13(2):201-11.

18.

Progress in the discovery of polo-like kinase inhibitors.

McInnes C, Mezna M, Fischer PM.

Curr Top Med Chem. 2005;5(2):181-97. Review.

PMID:
15853646
19.

Synthesis and biological activity of 2-anilino-4-(1H-pyrrol-3-yl) pyrimidine CDK inhibitors.

Wang S, Wood G, Meades C, Griffiths G, Midgley C, McNae I, McInnes C, Anderson S, Jackson W, Mezna M, Yuill R, Walkinshaw M, Fischer PM.

Bioorg Med Chem Lett. 2004 Aug 16;14(16):4237-40.

PMID:
15261277
20.

Structural determinants of CDK4 inhibition and design of selective ATP competitive inhibitors.

McInnes C, Wang S, Anderson S, O'Boyle J, Jackson W, Kontopidis G, Meades C, Mezna M, Thomas M, Wood G, Lane DP, Fischer PM.

Chem Biol. 2004 Apr;11(4):525-34.

21.

2-Anilino-4-(thiazol-5-yl)pyrimidine CDK inhibitors: synthesis, SAR analysis, X-ray crystallography, and biological activity.

Wang S, Meades C, Wood G, Osnowski A, Anderson S, Yuill R, Thomas M, Mezna M, Jackson W, Midgley C, Griffiths G, Fleming I, Green S, McNae I, Wu SY, McInnes C, Zheleva D, Walkinshaw MD, Fischer PM.

J Med Chem. 2004 Mar 25;47(7):1662-75.

PMID:
15027857
22.

Subtype identification and functional properties of inositol 1,4, 5-trisphosphate receptors in heart and aorta.

Tovey SC, Dyer JL, Godfrey RE, Khan SZ, Bilmen JG, Mezna M, Michelangeli F.

Pharmacol Res. 2000 Dec;42(6):581-90.

PMID:
11058412
23.

The mechanism of inhibition of the Ca2+-ATPase by mastoparan. Mastoparan abolishes cooperative ca2+ binding.

Longland CL, Mezna M, Michelangeli F.

J Biol Chem. 1999 May 21;274(21):14799-805.

24.

Biochemical mechanisms of calcium mobilisation induced by mastoparan and chimeric hormone-mastoparan constructs.

Longland CL, Mezna M, Langel U, Hällbrink M, Soomets U, Wheatley M, Michelangeli F, Howl J.

Cell Calcium. 1998 Jul;24(1):27-34.

PMID:
9793686
25.

The effects of thimerosal on the purified InsP3 receptor.

Mezna M, Longland CL, Michelangeli F.

Biochem Soc Trans. 1998 Aug;26(3):S290. No abstract available.

PMID:
9766009
26.

2-Hydroxycarbazole induces Ca2+ release from sarcoplasmic reticulum by activating the ryanodine receptor.

Tovey SC, Longland CL, Mezna M, Michelangeli F.

Eur J Pharmacol. 1998 Aug 7;354(2-3):245-51.

PMID:
9754926
28.

The effect of phosphate transporter inhibitors on the InsP3-induced Ca2+ release.

Mezna M, Michelangeli F.

Biochem Soc Trans. 1997 Aug;25(3):451S. No abstract available.

PMID:
9388675
29.

Calcium-mobilizing actions of chimeric hormone-mastoparan peptides.

Mezna M, Langel U, Hällbrink M, Wheatley M, Michelangeli F, Howl J.

Biochem Soc Trans. 1997 Aug;25(3):450S. No abstract available.

PMID:
9388674
30.

Pharmacological properties of the Ca2+-release mechanism sensitive to NAADP in the sea urchin egg.

Genazzani AA, Mezna M, Dickey DM, Michelangeli F, Walseth TF, Galione A.

Br J Pharmacol. 1997 Aug;121(7):1489-95.

32.

Identification and characterization of inositol 1,4,5-trisphosphate receptors in rat testis.

Tovey SC, Godfrey RE, Hughes PJ, Mezna M, Minchin SD, Mikoshiba K, Michelangeli F.

Cell Calcium. 1997 Apr;21(4):311-9.

PMID:
9160167
33.

Kinetic properties of nicotinic acid adenine dinucleotide phosphate-induced Ca2+ release.

Genazzani AA, Mezna M, Summerhill RJ, Galione A, Michelangeli F.

J Biol Chem. 1997 Mar 21;272(12):7669-75.

35.

Conformational changes associated with activation of bee venom phospholipase A2.

Ahmed T, Kelly SM, Lawrence AJ, Mezna M, Price NC.

J Biochem. 1996 Dec;120(6):1224-31.

36.

Can phenolic plasticising agents affect testicular development by disturbing intracellular calcium homeostasis?

Michelangeli F, Tovey S, Lowes DA, Tien RF, Mezna M, McLellan H, Hughes P.

Biochem Soc Trans. 1996 May;24(2):293S. No abstract available.

PMID:
8736951
37.

Effects of aliphatic alcohols on the ER calcium pumps and InsP3 receptors from porcine cerebellum.

Mezna M, Patchick T, Tovey S, Michelangeli F.

Biochem Soc Trans. 1996 May;24(2):292S. No abstract available.

PMID:
8736950
38.
39.
40.

Pharmacological modulators of the inositol 1,4,5-trisphosphate receptor.

Michelangeli F, Mezna M, Tovey S, Sayers LG.

Neuropharmacology. 1995 Sep;34(9):1111-22. Review.

PMID:
8532181
41.
42.

Modulation of the inositol 1,4,5-trisphosphate-sensitive calcium channel from rat cerebellum by alkali metal ions.

Mezna M, Michelangeli F.

Biochem Soc Trans. 1995 Aug;23(3):428S. No abstract available.

PMID:
8566316
43.

Opening up Ca2+ stores with InsP3.

Mezna M, Michelangeli F.

Nature. 1995 Jul 27;376(6538):300-1. No abstract available.

PMID:
7630394
45.

Zinc and barium inhibit the phospholipase A2 from Naja naja atra by different mechanisms.

Mezna M, Ahmad T, Chettibi S, Drainas D, Lawrence AJ.

Biochem J. 1994 Jul 15;301 ( Pt 2):503-8.

46.

Conductimetric assays for the hydrolase and transferase activities of phospholipase D enzymes.

Mezna M, Lawrence AJ.

Anal Biochem. 1994 May 1;218(2):370-6.

PMID:
8074295

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