novel, small molecule inhibitor of Hsc70/Hsp70 potentiates Hsp90 inhibitor induced apoptosis in HCT116 colon carcinoma cells von Massey, Andrew J, Williamson, Douglas S, Browne, Helen, Murray, James B, Dokurno, Pawel, Shaw, Terry, Macias, Alba T, Daniels, Zoe, Geoffroy, Stephanie, Dopson, Melanie, Lavan, Paul, Matassova, Natalia, Francis, Geraint L, Graham, Christopher J, Parsons, Rachel, Wang, Yikang, Padfield, Antony, Comer, Mike, Drysdale, Martin J, Wood, Mike

Volltext

Accepting from the best donor; analysis of long-lifetime donor fluorescent protein pairings to optimise dynamic FLIM-based FRET experiments von Martin, Kirsty J, McGhee, Ewan J, Schwarz, Juliana P, Drysdale, Martin, Brachmann, Saskia M, Stucke, Volker, Sansom, Owen J, Anderson, Kurt I

Volltext

Discovery of a First-in-Class Inhibitor of the PRMT5–Substrate Adaptor Interaction von McKinney, David C, McMillan, Brian J, Ranaghan, Matthew J, Moroco, Jamie A, Brousseau, Merissa, Mullin-Bernstein, Zachary, O’Keefe, Meghan, McCarren, Patrick, Mesleh, Michael F, Mulvaney, Kathleen M, Robinson, Foxy, Singh, Ritu, Bajrami, Besnik, Wagner, Florence F, Hilgraf, Robert, Drysdale, Martin J, Campbell, Arthur J, Skepner, Adam, Timm, David E, Porter, Dale, Kaushik, Virendar K, Sellers, William R, Ianari, Alessandra

Volltext

Novel, Potent Small-Molecule Inhibitors of the Molecular Chaperone Hsp90 Discovered through Structure-Based Design von Dymock, Brian W, Barril, Xavier, Brough, Paul A, Cansfield, Julie E, Massey, Andrew, McDonald, Edward, Hubbard, Roderick E, Surgenor, Allan, Roughley, Stephen D, Webb, Paul, Workman, Paul, Wright, Lisa, Drysdale, Martin J

Volltext

Colorectal Tumors Require NUAK1 for Protection from Oxidative Stress von Port, Jennifer, Muthalagu, Nathiya, Raja, Meera, Ceteci, Fatih, Monteverde, Tiziana, Kruspig, Björn, Hedley, Ann, Kalna, Gabriela, Lilla, Sergio, Neilson, Lisa, Brucoli, Martina, Gyuraszova, Katarina, Tait-Mulder, Jacqueline, Mezna, Mokdad, Svambaryte, Silvija, Bryson, Amy, Sumpton, David, McVie, Allan, Nixon, Colin, Drysdale, Martin, Esumi, Hiroyasu, Murray, Graeme I, Sansom, Owen J, Zanivan, Sara R, Murphy, Daniel J

Volltext

Novel Adenosine-Derived Inhibitors of 70 kDa Heat Shock Protein, Discovered Through Structure-Based Design von Williamson, Douglas S, Borgognoni, Jenifer, Clay, Alexandra, Daniels, Zoe, Dokurno, Pawel, Drysdale, Martin J, Foloppe, Nicolas, Francis, Geraint L, Graham, Christopher J, Howes, Rob, Macias, Alba T, Murray, James B, Parsons, Rachel, Shaw, Terry, Surgenor, Allan E, Terry, Lindsey, Wang, Yikang, Wood, Mike, Massey, Andrew J

Volltext

Adenosine-Derived Inhibitors of 78 kDa Glucose Regulated Protein (Grp78) ATPase: Insights into Isoform Selectivity von Macias, Alba T, Williamson, Douglas S, Allen, Nicola, Borgognoni, Jenifer, Clay, Alexandra, Daniels, Zoe, Dokurno, Pawel, Drysdale, Martin J, Francis, Geraint L, Graham, Christopher J, Howes, Rob, Matassova, Natalia, Murray, James B, Parsons, Rachel, Shaw, Terry, Surgenor, Allan E, Terry, Lindsey, Wang, Yikang, Wood, Mike, Massey, Andrew J

Volltext

Targeting conserved water molecules: Design of 4-aryl-5-cyanopyrrolo[2,3-d]pyrimidine Hsp90 inhibitors using fragment-based screening and structure-based optimization von Davies, Nicholas G.M., Browne, Helen, Davis, Ben, Drysdale, Martin J., Foloppe, Nicolas, Geoffrey, Stephanie, Gibbons, Ben, Hart, Terance, Hubbard, Roderick, Jensen, Michael Rugaard, Mansell, Howard, Massey, Andrew, Matassova, Natalia, Moore, Jonathan D., Murray, James, Pratt, Robert, Ray, Stuart, Robertson, Alan, Roughley, Stephen D., Schoepfer, Joseph, Scriven, Kirsten, Simmonite, Heather, Stokes, Stephen, Surgenor, Allan, Webb, Paul, Wood, Mike, Wright, Lisa, Brough, Paul

Volltext

Preclinical antitumor activity of the orally available heat shock protein 90 inhibitor NVP-BEP800 von Massey, Andrew J, Schoepfer, Joseph, Brough, Paul A, Brueggen, Josef, Chène, Patrick, Drysdale, Martin J, Pfaar, Ulrike, Radimerski, Thomas, Ruetz, Stephan, Schweitzer, Alain, Wood, Mike, Garcia-Echeverria, Carlos, Jensen, Michael Rugaard

Volltext

Inhibition of the heat shock protein 90 molecular chaperone in vitro and in vivo by novel, synthetic, potent resorcinylic pyrazole/isoxazole amide analogues von Sharp, Swee Y, Prodromou, Chrisostomos, Boxall, Kathy, Powers, Marissa V, Holmes, Joanna L, Box, Gary, Matthews, Thomas P, Cheung, Kwai-Ming J, Kalusa, Andrew, James, Karen, Hayes, Angela, Hardcastle, Anthea, Dymock, Brian, Brough, Paul A, Barril, Xavier, Cansfield, Julie E, Wright, Lisa, Surgenor, Allan, Foloppe, Nicolas, Hubbard, Roderick E, Aherne, Wynne, Pearl, Laurence, Jones, Keith, McDonald, Edward, Raynaud, Florence, Eccles, Sue, Drysdale, Martin, Workman, Paul

Volltext

4-Amino derivatives of the Hsp90 inhibitor CCT018159 von Barril, Xavier, Beswick, Mandy C., Collier, Adam, Drysdale, Martin J., Dymock, Brian W., Fink, Alexandra, Grant, Kate, Howes, Robert, Jordan, Allan M., Massey, Andrew, Surgenor, Allan, Wayne, Joanne, Workman, Paul, Wright, Lisa

Volltext

Preclinical pharmacokinetics and metabolism of a novel diaryl pyrazole resorcinol series of heat shock protein 90 inhibitors von Smith, Nicola F, Hayes, Angela, James, Karen, Nutley, Bernard P, McDonald, Edward, Henley, Alan, Dymock, Brian, Drysdale, Martin J, Raynaud, Florence I, Workman, Paul

Volltext

Discovery of a potent CDK2 inhibitor with a novel binding mode, using virtual screening and initial, structure-guided lead scoping von Richardson, Christine M., Nunns, Claire L., Williamson, Douglas S., Parratt, Martin J., Dokurno, Pawel, Howes, Rob, Borgognoni, Jenifer, Drysdale, Martin J., Finch, Harry, Hubbard, Roderick E., Jackson, Philip S., Kierstan, Peter, Lentzen, Georg, Moore, Jonathan D., Murray, James B., Simmonite, Heather, Surgenor, Allan E., Torrance, Christopher J.

Volltext

Adenine derived inhibitors of the molecular chaperone HSP90—SAR explained through multiple X-ray structures von Dymock, Brian, Barril, Xavier, Beswick, Mandy, Collier, Adam, Davies, Nicholas, Drysdale, Martin, Fink, Alexandra, Fromont, Christophe, Hubbard, Roderick E., Massey, Andrew, Surgenor, Allan, Wright, Lisa

Volltext

Fragment-based hit identification: thinking in 3D von Morley, Andrew D., Pugliese, Angelo, Birchall, Kristian, Bower, Justin, Brennan, Paul, Brown, Nathan, Chapman, Tim, Drysdale, Martin, Gilbert, Ian H., Hoelder, Swen, Jordan, Allan, Ley, Steven V., Merritt, Andy, Miller, David, Swarbrick, Martin E., Wyatt, Paul G.

Volltext

Inhibition of inducible nitric oxide synthase by acetamidine derivatives of hetero-substituted lysine and homolysine von YOUNG, R. J, BEAMS, R. M, FRENCH, C, HODGSON, S. T, HODSON, H. F, KLEANTHOUS, S, RIDER, P, SANDERS, D, SAWYER, D. A, SCOTT, K. J, SHEARER, B. G, STOCKER, R, CARTER, K, SMITH, S, TACKLEY, M. C, KNOWLES, R. G, CLARK, H. A. R, COE, D. M, CHAMBERS, C. L, DAVIES, P. I, DAWSON, J, DRYSDALE, M. J, FRANZMAN, K. W

Volltext

A fully automated procedure for the parallel, multidimensional purification and nucleotide loading of the human GTPases KRas, Rac1 and RalB von Gray, Christopher H., Konczal, Jennifer, Mezna, Mokdad, Ismail, Shehab, Bower, Justin, Drysdale, Martin

Volltext

A Central Role for Biophysics in Cancer Drug Discovery - Development of Candidate Small Molecule Inhibitors in Mutant KRas von Gohlke, Andrea, Bower, Justin, Brown, Peter N., Cameron, Ken S., Drysdale, Martin, Goodwin, Gillian, Gray, Christopher, Konczal, Jen, McArthur, Duncan, McKinnon, Heather, Mezna, Mokdad, Pugliese, Angelo, Schuettelkopf, Alexander W.

Volltext

ChemInform Abstract: Fragment-Based Drug Discovery: The Shape of Things to Come von Drysdale, Martin J.

Volltext

Abstract C086: NP1867, a potent, selective, covalent small molecule inhibitor of DNA Mismatch Repair (MMR) protein PMS2, functionally inhibits MMR in cells and elicits COSMIC mutat... von Blagg, Julian, Riou, Philippe, Hervieu, Alexia, Piumatti, Eleonora, Rospo, Giuseppe, Arunachalam, Sasi, Meier, Bettina, Weeks, Sam, Rodriguez, Maria, Parmar, Kalpesh, Patel, Pradip, Peall, Adam, Tongue, Paige, McLaren, Tess, Workman, Robert, Bago, Ruzica, Robjohns, Stuart, Beaumont, Rebecca, Briggs, Mike, Langley, Gareth, Nichols, Charles, Clark, David, Winship, Paul, Rousseau, Benoit, Baker, Matthew, Drysdale, Martin, Germano, Giovanni, Bardelli, Alberto

Volltext