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Items: 28

1.

Structure-Guided Discovery of a Selective Mcl-1 Inhibitor with Cellular Activity.

Szlávik Z, Ondi L, Csékei M, Paczal A, Szabó ZB, Radics G, Murray J, Davidson J, Chen I, Davis B, Hubbard RE, Pedder C, Dokurno P, Surgenor A, Smith J, Robertson A, LeToumelin-Braizat G, Cauquil N, Zarka M, Demarles D, Perron-Sierra F, Claperon A, Colland F, Geneste O, Kotschy A.

J Med Chem. 2019 Aug 8;62(15):6913-6924. doi: 10.1021/acs.jmedchem.9b00134. Epub 2019 Jul 24.

PMID:
31339316
2.

Design of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors Using a Crystallographic Surrogate Derived from Checkpoint Kinase 1 (CHK1).

Williamson DS, Smith GP, Acheson-Dossang P, Bedford ST, Chell V, Chen IJ, Daechsel JCA, Daniels Z, David L, Dokurno P, Hentzer M, Herzig MC, Hubbard RE, Moore JD, Murray JB, Newland S, Ray SC, Shaw T, Surgenor AE, Terry L, Thirstrup K, Wang Y, Christensen KV.

J Med Chem. 2017 Nov 9;60(21):8945-8962. doi: 10.1021/acs.jmedchem.7b01186. Epub 2017 Oct 27.

PMID:
29023112
3.

Application of Off-Rate Screening in the Identification of Novel Pan-Isoform Inhibitors of Pyruvate Dehydrogenase Kinase.

Brough PA, Baker L, Bedford S, Brown K, Chavda S, Chell V, D'Alessandro J, Davies NG, Davis B, Le Strat L, Macias AT, Maddox D, Mahon PC, Massey AJ, Matassova N, McKenna S, Meissner JW, Moore JD, Murray JB, Northfield CJ, Parry C, Parsons R, Roughley SD, Shaw T, Simmonite H, Stokes S, Surgenor A, Stefaniak E, Robertson A, Wang Y, Webb P, Whitehead N, Wood M.

J Med Chem. 2017 Mar 23;60(6):2271-2286. doi: 10.1021/acs.jmedchem.6b01478. Epub 2017 Feb 15.

PMID:
28199108
4.

The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models.

Kotschy A, Szlavik Z, Murray J, Davidson J, Maragno AL, Le Toumelin-Braizat G, Chanrion M, Kelly GL, Gong JN, Moujalled DM, Bruno A, Csekei M, Paczal A, Szabo ZB, Sipos S, Radics G, Proszenyak A, Balint B, Ondi L, Blasko G, Robertson A, Surgenor A, Dokurno P, Chen I, Matassova N, Smith J, Pedder C, Graham C, Studeny A, Lysiak-Auvity G, Girard AM, Gravé F, Segal D, Riffkin CD, Pomilio G, Galbraith LC, Aubrey BJ, Brennan MS, Herold MJ, Chang C, Guasconi G, Cauquil N, Melchiore F, Guigal-Stephan N, Lockhart B, Colland F, Hickman JA, Roberts AW, Huang DC, Wei AH, Strasser A, Lessene G, Geneste O.

Nature. 2016 Oct 27;538(7626):477-482. doi: 10.1038/nature19830. Epub 2016 Oct 19.

PMID:
27760111
5.

VER-246608, a novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase kinase, disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells.

Moore JD, Staniszewska A, Shaw T, D'Alessandro J, Davis B, Surgenor A, Baker L, Matassova N, Murray J, Macias A, Brough P, Wood M, Mahon PC.

Oncotarget. 2014 Dec 30;5(24):12862-76.

6.

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.

PMID:
23018093
7.

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.

PMID:
21526763
8.

Discovery of cell-active phenyl-imidazole Pin1 inhibitors by structure-guided fragment evolution.

Potter A, Oldfield V, Nunns C, Fromont C, Ray S, Northfield CJ, Bryant CJ, Scrace SF, Robinson D, Matossova N, Baker L, Dokurno P, Surgenor AE, Davis B, Richardson CM, Murray JB, Moore JD.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6483-8. doi: 10.1016/j.bmcl.2010.09.063. Epub 2010 Sep 17.

PMID:
20932746
9.

Structure-guided design of alpha-amino acid-derived Pin1 inhibitors.

Potter AJ, Ray S, Gueritz L, Nunns CL, Bryant CJ, Scrace SF, Matassova N, Baker L, Dokurno P, Robinson DA, Surgenor AE, Davis B, Murray JB, Richardson CM, Moore JD.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):586-90. doi: 10.1016/j.bmcl.2009.11.090. Epub 2009 Nov 22. Erratum in: Bioorg Med Chem Lett. 2010 Aug 15;20(16):e1.

PMID:
19969456
10.

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.

PMID:
19610616
11.

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.

PMID:
19256508
12.

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.

13.

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.

PMID:
18020435
14.

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.

PMID:
17570665
15.

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.

16.

Identification of chemically diverse Chk1 inhibitors by receptor-based virtual screening.

Foloppe N, Fisher LM, Howes R, Potter A, Robertson AG, Surgenor AE.

Bioorg Med Chem. 2006 Jul 15;14(14):4792-802. Epub 2006 Mar 29.

PMID:
16574416
17.

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.

PMID:
16480864
18.

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.

PMID:
16460658
19.

Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR.

Richardson CM, Williamson DS, Parratt MJ, Borgognoni J, Cansfield AD, Dokurno P, Francis GL, Howes R, Moore JD, Murray JB, Robertson A, Surgenor AE, Torrance CJ.

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1353-7. Epub 2005 Dec 1.

PMID:
16325401
20.

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.

PMID:
16213716
21.

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.

PMID:
16202589
22.

Structure-based design of novel Chk1 inhibitors: insights into hydrogen bonding and protein-ligand affinity.

Foloppe N, Fisher LM, Howes R, Kierstan P, Potter A, Robertson AG, Surgenor AE.

J Med Chem. 2005 Jun 30;48(13):4332-45.

PMID:
15974586
23.

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.

PMID:
15974572
24.

Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2.

Williamson DS, Parratt MJ, Bower JF, Moore JD, Richardson CM, Dokurno P, Cansfield AD, Francis GL, Hebdon RJ, Howes R, Jackson PS, Lockie AM, Murray JB, Nunns CL, Powles J, Robertson A, Surgenor AE, Torrance CJ.

Bioorg Med Chem Lett. 2005 Feb 15;15(4):863-7.

PMID:
15686876
25.

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.

26.

Adenine derived inhibitors of the molecular chaperone HSP90-SAR explained through multiple X-ray structures.

Dymock B, Barril X, Beswick M, Collier A, Davies N, Drysdale M, Fink A, Fromont C, Hubbard RE, Massey A, Surgenor A, Wright L.

Bioorg Med Chem Lett. 2004 Jan 19;14(2):325-8.

PMID:
14698151
27.

Structure-based design of peptidomimetic antagonists of p56(lck) SH2 domain.

Hobbs CJ, Bit RA, Cansfield AD, Harris B, Hill CH, Hilyard KL, Kilford IR, Kitas E, Kroehn A, Lovell P, Pole D, Rugman P, Sherborne BS, Smith IE, Vesey DR, Walmsley DL, Whittaker D, Williams G, Wilson F, Banner D, Surgenor A, Borkakoti N.

Bioorg Med Chem Lett. 2002 May 20;12(10):1365-9.

PMID:
11992778
28.

Comparison of peptide aldehydes with alpha 1-antitrypsin as elastase inhibitors for use in emphysema.

Roberts NA, Surgenor AE.

Biochem Biophys Res Commun. 1986 Sep 30;139(3):896-902.

PMID:
2429659

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