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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.


Correction to: Supporting Aboriginal and Torres Strait islander cultural educators and cultural mentors in Australian general practice education.

Reath J, Abbott P, Kurti L, Morgan R, Martin M, Parry A, Gordon E, Thomas J, Drysdale M.

BMC Med Educ. 2018 Nov 22;18(1):276. doi: 10.1186/s12909-018-1359-z.


Supporting aboriginal and Torres Strait islander cultural educators and cultural mentors in Australian general practice education.

Reath J, Abbott P, Kurti L, Morgan R, Martin M, Parry A, Gordon E, Thomas J, Drysdale M.

BMC Med Educ. 2018 Oct 11;18(1):236. doi: 10.1186/s12909-018-1340-x. Erratum in: BMC Med Educ. 2018 Nov 22;18(1):276.


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.


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.


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.


Accepting from the best donor; analysis of long-lifetime donor fluorescent protein pairings to optimise dynamic FLIM-based FRET experiments.

Martin KJ, McGhee EJ, Schwarz JP, Drysdale M, Brachmann SM, Stucke V, Sansom OJ, Anderson KI.

PLoS One. 2018 Jan 2;13(1):e0183585. doi: 10.1371/journal.pone.0183585. eCollection 2018.


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.


Obesity-Induced Structural and Neuronal Plasticity in the Lateral Orbitofrontal Cortex.

Thompson JL, Drysdale M, Baimel C, Kaur M, MacGowan T, Pitman KA, Borgland SL.

Neuropsychopharmacology. 2017 Jun;42(7):1480-1490. doi: 10.1038/npp.2016.284. Epub 2017 Jan 2.


Cultural desire need not improve with cultural knowledge: A cross-sectional study of student nurses.

Isaacs AN, Raymond A, Jacob E, Jones J, McGrail M, Drysdale M.

Nurse Educ Pract. 2016 Jul;19:91-6. doi: 10.1016/j.nepr.2016.05.009. Epub 2016 Jun 2.


Identification of a Selective G1-Phase Benzimidazolone Inhibitor by a Senescence-Targeted Virtual Screen Using Artificial Neural Networks.

Bilsland AE, Pugliese A, Liu Y, Revie J, Burns S, McCormick C, Cairney CJ, Bower J, Drysdale M, Narita M, Sadaie M, Keith WN.

Neoplasia. 2015 Sep;17(9):704-715. doi: 10.1016/j.neo.2015.08.009.


Identification of novel, in vivo active Chk1 inhibitors utilizing structure guided drug design.

Massey AJ, Stokes S, Browne H, Foloppe N, Fiumana A, Scrace S, Fallowfield M, Bedford S, Webb P, Baker L, Christie M, Drysdale MJ, Wood M.

Oncotarget. 2015 Nov 3;6(34):35797-812. doi: 10.18632/oncotarget.5929.


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.


Lethal factor, but not edema factor, is required to cause fatal anthrax in cynomolgus macaques after pulmonary spore challenge.

Hutt JA, Lovchik JA, Drysdale M, Sherwood RL, Brasel T, Lipscomb MF, Lyons CR.

Am J Pathol. 2014 Dec;184(12):3205-16. doi: 10.1016/j.ajpath.2014.08.008. Epub 2014 Oct 5.


Fragment-based hit identification: thinking in 3D.

Morley AD, Pugliese A, Birchall K, Bower J, Brennan P, Brown N, Chapman T, Drysdale M, Gilbert IH, Hoelder S, Jordan A, Ley SV, Merritt A, Miller D, Swarbrick ME, Wyatt PG.

Drug Discov Today. 2013 Dec;18(23-24):1221-7. doi: 10.1016/j.drudis.2013.07.011. Epub 2013 Jul 30. Review.


Targeting conserved water molecules: design of 4-aryl-5-cyanopyrrolo[2,3-d]pyrimidine Hsp90 inhibitors using fragment-based screening and structure-based optimization.

Davies NG, Browne H, Davis B, Drysdale MJ, Foloppe N, Geoffrey S, Gibbons B, Hart T, Hubbard R, Jensen MR, Mansell H, Massey A, Matassova N, Moore JD, Murray J, Pratt R, Ray S, Robertson A, Roughley SD, Schoepfer J, Scriven K, Simmonite H, Stokes S, Surgenor A, Webb P, Wood M, Wright L, Brough P.

Bioorg Med Chem. 2012 Nov 15;20(22):6770-89. doi: 10.1016/j.bmc.2012.08.050. Epub 2012 Sep 4.


Appropriate health promotion for Australian Aboriginal and Torres Strait Islander communities: crucial for closing the gap.

Demaio A, Drysdale M, de Courten M.

Glob Health Promot. 2012 Jun;19(2):58-62. doi: 10.1177/1757975912441230.


Expression of either lethal toxin or edema toxin by Bacillus anthracis is sufficient for virulence in a rabbit model of inhalational anthrax.

Lovchik JA, Drysdale M, Koehler TM, Hutt JA, Lyons CR.

Infect Immun. 2012 Jul;80(7):2414-25. doi: 10.1128/IAI.06340-11. Epub 2012 Apr 23.


Evaluating the respiratory bioaccessibility of nickel in soil through the use of a simulated lung fluid.

Drysdale M, Ljung Bjorklund K, Jamieson HE, Weinstein P, Cook A, Watkins RT.

Environ Geochem Health. 2012 Apr;34(2):279-88. doi: 10.1007/s10653-011-9435-x. Epub 2011 Oct 9.


Adenosine-derived inhibitors of 78 kDa glucose regulated protein (Grp78) ATPase: insights into isoform selectivity.

Macias AT, Williamson DS, Allen N, Borgognoni J, Clay A, Daniels Z, Dokurno P, Drysdale MJ, Francis GL, Graham CJ, Howes R, Matassova N, Murray JB, Parsons R, Shaw T, Surgenor AE, Terry L, Wang Y, Wood M, Massey AJ.

J Med Chem. 2011 Jun 23;54(12):4034-41. doi: 10.1021/jm101625x. Epub 2011 May 20.


Preclinical antitumor activity of the orally available heat shock protein 90 inhibitor NVP-BEP800.

Massey AJ, Schoepfer J, Brough PA, Brueggen J, Chène P, Drysdale MJ, Pfaar U, Radimerski T, Ruetz S, Schweitzer A, Wood M, Garcia-Echeverria C, Jensen MR.

Mol Cancer Ther. 2010 Apr;9(4):906-19. doi: 10.1158/1535-7163.MCT-10-0055. Epub 2010 Apr 6.


A novel, small molecule inhibitor of Hsc70/Hsp70 potentiates Hsp90 inhibitor induced apoptosis in HCT116 colon carcinoma cells.

Massey AJ, Williamson DS, Browne H, Murray JB, Dokurno P, Shaw T, Macias AT, Daniels Z, Geoffroy S, Dopson M, Lavan P, Matassova N, Francis GL, Graham CJ, Parsons R, Wang Y, Padfield A, Comer M, Drysdale MJ, Wood M.

Cancer Chemother Pharmacol. 2010 Aug;66(3):535-45. doi: 10.1007/s00280-009-1194-3. Epub 2009 Dec 13.


Combining hit identification strategies: fragment-based and in silico approaches to orally active 2-aminothieno[2,3-d]pyrimidine inhibitors of the Hsp90 molecular chaperone.

Brough PA, Barril X, Borgognoni J, Chene P, Davies NG, Davis B, Drysdale MJ, Dymock B, Eccles SA, Garcia-Echeverria C, Fromont C, Hayes A, Hubbard RE, Jordan AM, Jensen MR, Massey A, Merrett A, Padfield A, Parsons R, Radimerski T, Raynaud FI, Robertson A, Roughley SD, Schoepfer J, Simmonite H, Sharp SY, Surgenor A, Valenti M, Walls S, Webb P, Wood M, Workman P, Wright L.

J Med Chem. 2009 Aug 13;52(15):4794-809. doi: 10.1021/jm900357y.


Novel adenosine-derived inhibitors of 70 kDa heat shock protein, discovered through structure-based design.

Williamson DS, Borgognoni J, Clay A, Daniels Z, Dokurno P, Drysdale MJ, Foloppe N, Francis GL, Graham CJ, Howes R, Macias AT, Murray JB, Parsons R, Shaw T, Surgenor AE, Terry L, Wang Y, Wood M, Massey AJ.

J Med Chem. 2009 Mar 26;52(6):1510-3. doi: 10.1021/jm801627a.


Discriminating virulence mechanisms among Bacillus anthracis strains by using a murine subcutaneous infection model.

Chand HS, Drysdale M, Lovchik J, Koehler TM, Lipscomb MF, Lyons CR.

Infect Immun. 2009 Jan;77(1):429-35. doi: 10.1128/IAI.00647-08. Epub 2008 Nov 3.


Medicinal chemistry of Hsp90 inhibitors.

Drysdale MJ, Brough PA.

Curr Top Med Chem. 2008;8(10):859-68. Review.


NVP-AUY922: a small molecule HSP90 inhibitor with potent antitumor activity in preclinical breast cancer models.

Jensen MR, Schoepfer J, Radimerski T, Massey A, Guy CT, Brueggen J, Quadt C, Buckler A, Cozens R, Drysdale MJ, Garcia-Echeverria C, Chène P.

Breast Cancer Res. 2008;10(2):R33. doi: 10.1186/bcr1996. Epub 2008 Apr 22.


NVP-AUY922: a novel heat shock protein 90 inhibitor active against xenograft tumor growth, angiogenesis, and metastasis.

Eccles SA, Massey A, Raynaud FI, Sharp SY, Box G, Valenti M, Patterson L, de Haven Brandon A, Gowan S, Boxall F, Aherne W, Rowlands M, Hayes A, Martins V, Urban F, Boxall K, Prodromou C, Pearl L, James K, Matthews TP, Cheung KM, Kalusa A, Jones K, McDonald E, Barril X, Brough PA, Cansfield JE, Dymock B, Drysdale MJ, Finch H, Howes R, Hubbard RE, Surgenor A, Webb P, Wood M, Wright L, Workman P.

Cancer Res. 2008 Apr 15;68(8):2850-60. doi: 10.1158/0008-5472.CAN-07-5256.


Application of in vivo induced antigen technology (IVIAT) to Bacillus anthracis.

Rollins SM, Peppercorn A, Young JS, Drysdale M, Baresch A, Bikowski MV, Ashford DA, Quinn CP, Handfield M, Hillman JD, Lyons CR, Koehler TM, Calderwood SB, Ryan ET.

PLoS One. 2008 Mar 19;3(3):e1824. doi: 10.1371/journal.pone.0001824.


4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer.

Brough PA, Aherne W, Barril X, Borgognoni J, Boxall K, Cansfield JE, Cheung KM, Collins I, Davies NG, Drysdale MJ, Dymock B, Eccles SA, Finch H, Fink A, Hayes A, Howes R, Hubbard RE, James K, Jordan AM, Lockie A, Martins V, Massey A, Matthews TP, McDonald E, Northfield CJ, Pearl LH, Prodromou C, Ray S, Raynaud FI, Roughley SD, Sharp SY, Surgenor A, Walmsley DL, Webb P, Wood M, Workman P, Wright L.

J Med Chem. 2008 Jan 24;51(2):196-218. Epub 2007 Nov 20.


The SeeDs approach: integrating fragments into drug discovery.

Hubbard RE, Davis B, Chen I, Drysdale MJ.

Curr Top Med Chem. 2007;7(16):1568-81. Review.


Discovery of a potent CDK2 inhibitor with a novel binding mode, using virtual screening and initial, structure-guided lead scoping.

Richardson CM, Nunns CL, Williamson DS, Parratt MJ, Dokurno P, Howes R, Borgognoni J, Drysdale MJ, Finch H, Hubbard RE, Jackson PS, Kierstan P, Lentzen G, Moore JD, Murray JB, Simmonite H, Surgenor AE, Torrance CJ.

Bioorg Med Chem Lett. 2007 Jul 15;17(14):3880-5. Epub 2007 May 6.


Inhibition of the heat shock protein 90 molecular chaperone in vitro and in vivo by novel, synthetic, potent resorcinylic pyrazole/isoxazole amide analogues.

Sharp SY, Prodromou C, Boxall K, Powers MV, Holmes JL, Box G, Matthews TP, Cheung KM, Kalusa A, James K, Hayes A, Hardcastle A, Dymock B, Brough PA, Barril X, Cansfield JE, Wright L, Surgenor A, Foloppe N, Hubbard RE, Aherne W, Pearl L, Jones K, McDonald E, Raynaud F, Eccles S, Drysdale M, Workman P.

Mol Cancer Ther. 2007 Apr;6(4):1198-211.


Murine innate immune response to virulent toxigenic and nontoxigenic Bacillus anthracis strains.

Drysdale M, Olson G, Koehler TM, Lipscomb MF, Lyons CR.

Infect Immun. 2007 Apr;75(4):1757-64. Epub 2007 Jan 22.


Toxin-deficient mutants of Bacillus anthracis are lethal in a murine model for pulmonary anthrax.

Heninger S, Drysdale M, Lovchik J, Hutt J, Lipscomb MF, Koehler TM, Lyons CR.

Infect Immun. 2006 Nov;74(11):6067-74. Epub 2006 Aug 21.


Targeting Hsp90 for the treatment of cancer.

Drysdale MJ, Brough PA, Massey A, Jensen MR, Schoepfer J.

Curr Opin Drug Discov Devel. 2006 Jul;9(4):483-95. Review.


Discovery and development of pyrazole-scaffold Hsp90 inhibitors.

McDonald E, Jones K, Brough PA, Drysdale MJ, Workman P.

Curr Top Med Chem. 2006;6(11):1193-203. Review.


Preclinical pharmacokinetics and metabolism of a novel diaryl pyrazole resorcinol series of heat shock protein 90 inhibitors.

Smith NF, Hayes A, James K, Nutley BP, McDonald E, Henley A, Dymock B, Drysdale MJ, Raynaud FI, Workman P.

Mol Cancer Ther. 2006 Jun;5(6):1628-37.


4-Amino derivatives of the Hsp90 inhibitor CCT018159.

Barril X, Beswick MC, Collier A, Drysdale MJ, Dymock BW, Fink A, Grant K, Howes R, Jordan AM, Massey A, Surgenor A, Wayne J, Workman P, Wright L.

Bioorg Med Chem Lett. 2006 May 1;16(9):2543-8. Epub 2006 Feb 9.


A fluorescence polarization assay for inhibitors of Hsp90.

Howes R, Barril X, Dymock BW, Grant K, Northfield CJ, Robertson AG, Surgenor A, Wayne J, Wright L, James K, Matthews T, Cheung KM, McDonald E, Workman P, Drysdale MJ.

Anal Biochem. 2006 Mar 15;350(2):202-13. Epub 2006 Jan 23.


The conducting and reporting of rural health research: rurality and rural population issues.

Robinson A, Burley M, McGrail MR, Drysdale M, Jones R, Rickard CM.

Rural Remote Health. 2005 Oct-Dec;5(4):427. Epub 2005 Oct 14. Review.


The planning of rural health research: rurality and rural population issues.

McGrail MR, Jones R, Robinson A, Rickard CM, Burley M, Drysdale M.

Rural Remote Health. 2005 Oct-Dec;5(4):426. Epub 2005 Oct 14. Review.


3-(5-Chloro-2,4-dihydroxyphenyl)-pyrazole-4-carboxamides as inhibitors of the Hsp90 molecular chaperone.

Brough PA, Barril X, Beswick M, Dymock BW, Drysdale MJ, Wright L, Grant K, Massey A, Surgenor A, Workman P.

Bioorg Med Chem Lett. 2005 Dec 1;15(23):5197-201. Epub 2005 Oct 5.


Structure-based discovery of a new class of Hsp90 inhibitors.

Barril X, Brough P, Drysdale M, Hubbard RE, Massey A, Surgenor A, Wright L.

Bioorg Med Chem Lett. 2005 Dec 1;15(23):5187-91. Epub 2005 Oct 3.


Transcriptional analysis of the Bacillus anthracis capsule regulators.

Drysdale M, Bourgogne A, Koehler TM.

J Bacteriol. 2005 Aug;187(15):5108-14.


Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design.

Dymock BW, Barril X, Brough PA, Cansfield JE, Massey A, McDonald E, Hubbard RE, Surgenor A, Roughley SD, Webb P, Workman P, Wright L, Drysdale MJ.

J Med Chem. 2005 Jun 30;48(13):4212-5.


Capsule synthesis by Bacillus anthracis is required for dissemination in murine inhalation anthrax.

Drysdale M, Heninger S, Hutt J, Chen Y, Lyons CR, Koehler TM.

EMBO J. 2005 Jan 12;24(1):221-7. Epub 2004 Dec 16.


Design and characterization of libraries of molecular fragments for use in NMR screening against protein targets.

Baurin N, Aboul-Ela F, Barril X, Davis B, Drysdale M, Dymock B, Finch H, Fromont C, Richardson C, Simmonite H, Hubbard RE.

J Chem Inf Comput Sci. 2004 Nov-Dec;44(6):2157-66.


Structure-activity relationships in purine-based inhibitor binding to HSP90 isoforms.

Wright L, Barril X, Dymock B, Sheridan L, Surgenor A, Beswick M, Drysdale M, Collier A, Massey A, Davies N, Fink A, Fromont C, Aherne W, Boxall K, Sharp S, Workman P, Hubbard RE.

Chem Biol. 2004 Jun;11(6):775-85.


The detection of non-O157 E. coli in food by immunomagnetic separation.

Drysdale M, MacRae M, Strachan NJ, Reid TM, Ogden ID.

J Appl Microbiol. 2004;97(1):220-4.

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