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Items: 1 to 50 of 101

1.

Adventures in Scaffold Morphing: Discovery of Fused Ring Heterocyclic Checkpoint Kinase 1 (CHK1) Inhibitors.

Yang B, Vasbinder MM, Hird AW, Su Q, Wang H, Yu Y, Toader D, Lyne PD, Read JA, Breed J, Ioannidis S, Deng C, Grondine M, DeGrace N, Whitston D, Brassil P, Janetka JW.

J Med Chem. 2018 Feb 8;61(3):1061-1073. doi: 10.1021/acs.jmedchem.7b01490. Epub 2018 Jan 19.

PMID:
29301085
2.

A study of the reactivity of S(VI)-F containing warheads with nucleophilic amino-acid side chains under physiological conditions.

Mukherjee H, Debreczeni J, Breed J, Tentarelli S, Aquila B, Dowling JE, Whitty A, Grimster NP.

Org Biomol Chem. 2017 Nov 22;15(45):9685-9695. doi: 10.1039/c7ob02028g.

PMID:
29119993
3.

Structural and functional characterization of a DARPin which inhibits Ras nucleotide exchange.

Guillard S, Kolasinska-Zwierz P, Debreczeni J, Breed J, Zhang J, Bery N, Marwood R, Tart J, Overman R, Stocki P, Mistry B, Phillips C, Rabbitts T, Jackson R, Minter R.

Nat Commun. 2017 Jul 14;8:16111. doi: 10.1038/ncomms16111.

4.

Structural Characterisation Reveals Mechanism of IL-13-Neutralising Monoclonal Antibody Tralokinumab as Inhibition of Binding to IL-13Rα1 and IL-13Rα2.

Popovic B, Breed J, Rees DG, Gardener MJ, Vinall LM, Kemp B, Spooner J, Keen J, Minter R, Uddin F, Colice G, Wilkinson T, Vaughan T, May RD.

J Mol Biol. 2017 Jan 20;429(2):208-219. doi: 10.1016/j.jmb.2016.12.005. Epub 2016 Dec 9.

5.

Discovery of cofactor-specific, bactericidal Mycobacterium tuberculosis InhA inhibitors using DNA-encoded library technology.

Soutter HH, Centrella P, Clark MA, Cuozzo JW, Dumelin CE, Guie MA, Habeshian S, Keefe AD, Kennedy KM, Sigel EA, Troast DM, Zhang Y, Ferguson AD, Davies G, Stead ER, Breed J, Madhavapeddi P, Read JA.

Proc Natl Acad Sci U S A. 2016 Dec 6;113(49):E7880-E7889. Epub 2016 Nov 18.

6.

Successful percutaneous management of symptomatic central posterior epidural Baastrup cyst: a potential surgical sparing option?

Breed J, Goldschlager T, Chandra RV.

Spine J. 2016 Sep;16(9):e631-3. doi: 10.1016/j.spinee.2016.04.005. Epub 2016 Apr 8.

PMID:
27067606
7.

MTH1 Substrate Recognition--An Example of Specific Promiscuity.

Nissink JW, Bista M, Breed J, Carter N, Embrey K, Read J, Winter-Holt JJ.

PLoS One. 2016 Mar 21;11(3):e0151154. doi: 10.1371/journal.pone.0151154. eCollection 2016.

8.

Landscape of activating cancer mutations in FGFR kinases and their differential responses to inhibitors in clinical use.

Patani H, Bunney TD, Thiyagarajan N, Norman RA, Ogg D, Breed J, Ashford P, Potterton A, Edwards M, Williams SV, Thomson GS, Pang CS, Knowles MA, Breeze AL, Orengo C, Phillips C, Katan M.

Oncotarget. 2016 Apr 26;7(17):24252-68. doi: 10.18632/oncotarget.8132.

9.

Potent and Selective Inhibitors of MTH1 Probe Its Role in Cancer Cell Survival.

Kettle JG, Alwan H, Bista M, Breed J, Davies NL, Eckersley K, Fillery S, Foote KM, Goodwin L, Jones DR, Käck H, Lau A, Nissink JW, Read J, Scott JS, Taylor B, Walker G, Wissler L, Wylot M.

J Med Chem. 2016 Mar 24;59(6):2346-61. doi: 10.1021/acs.jmedchem.5b01760. Epub 2016 Feb 16.

PMID:
26878898
10.

Structural insights into FGFR kinase isoform selectivity: diverse binding modes of AZD4547 and ponatinib in complex with FGFR1 and FGFR4.

Tucker JA, Klein T, Breed J, Breeze AL, Overman R, Phillips C, Norman RA.

Structure. 2014 Dec 2;22(12):1764-1774. doi: 10.1016/j.str.2014.09.019. Epub 2014 Nov 20.

11.

Cathepsin C inhibitors: property optimization and identification of a clinical candidate.

Furber M, Tiden AK, Gardiner P, Mete A, Ford R, Millichip I, Stein L, Mather A, Kinchin E, Luckhurst C, Barber S, Cage P, Sanganee H, Austin R, Chohan K, Beri R, Thong B, Wallace A, Oreffo V, Hutchinson R, Harper S, Debreczeni J, Breed J, Wissler L, Edman K.

J Med Chem. 2014 Mar 27;57(6):2357-67. doi: 10.1021/jm401705g. Epub 2014 Mar 14.

PMID:
24592859
12.

Protein-ligand crystal structures can guide the design of selective inhibitors of the FGFR tyrosine kinase.

Norman RA, Schott AK, Andrews DM, Breed J, Foote KM, Garner AP, Ogg D, Orme JP, Pink JH, Roberts K, Rudge DA, Thomas AP, Leach AG.

J Med Chem. 2012 Jun 14;55(11):5003-12. doi: 10.1021/jm3004043. Epub 2012 May 21.

PMID:
22612866
13.

Discovery of checkpoint kinase inhibitor (S)-5-(3-fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by structure-based design and optimization of thiophenecarboxamide ureas.

Oza V, Ashwell S, Almeida L, Brassil P, Breed J, Deng C, Gero T, Grondine M, Horn C, Ioannidis S, Liu D, Lyne P, Newcombe N, Pass M, Read J, Ready S, Rowsell S, Su M, Toader D, Vasbinder M, Yu D, Yu Y, Xue Y, Zabludoff S, Janetka J.

J Med Chem. 2012 Jun 14;55(11):5130-42. doi: 10.1021/jm300025r. Epub 2012 Jun 4.

PMID:
22551018
14.

Synthesis and evaluation of triazolones as checkpoint kinase 1 inhibitors.

Oza V, Ashwell S, Brassil P, Breed J, Ezhuthachan J, Deng C, Grondine M, Horn C, Liu D, Lyne P, Newcombe N, Pass M, Read J, Su M, Toader D, Yu D, Yu Y, Zabludoff S.

Bioorg Med Chem Lett. 2012 Mar 15;22(6):2330-7. doi: 10.1016/j.bmcl.2012.01.043. Epub 2012 Feb 1.

PMID:
22342147
15.

Inhibitors of acetyltransferase domain of N-acetylglucosamine-1-phosphate-uridyltransferase/glucosamine-1-phosphate-acetyltransferase (GlmU). Part 1: Hit to lead evaluation of a novel arylsulfonamide series.

Green OM, McKenzie AR, Shapiro AB, Otterbein L, Ni H, Patten A, Stokes S, Albert R, Kawatkar S, Breed J.

Bioorg Med Chem Lett. 2012 Feb 15;22(4):1510-9. doi: 10.1016/j.bmcl.2012.01.016. Epub 2012 Jan 14.

PMID:
22297115
16.

Discovery of a novel class of triazolones as checkpoint kinase inhibitors--hit to lead exploration.

Oza V, Ashwell S, Brassil P, Breed J, Deng C, Ezhuthachan J, Haye H, Horn C, Janetka J, Lyne P, Newcombe N, Otterbien L, Pass M, Read J, Roswell S, Su M, Toader D, Yu D, Yu Y, Valentine A, Webborn P, White A, Zabludoff S, Zheng X.

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5133-8. doi: 10.1016/j.bmcl.2010.07.015. Epub 2010 Jul 29.

PMID:
20673630
17.

Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors.

Anderson M, Andrews DM, Barker AJ, Brassington CA, Breed J, Byth KF, Culshaw JD, Finlay MR, Fisher E, McMiken HH, Green CP, Heaton DW, Nash IA, Newcombe NJ, Oakes SE, Pauptit RA, Roberts A, Stanway JJ, Thomas AP, Tucker JA, Walker M, Weir HM.

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5487-92. doi: 10.1016/j.bmcl.2008.09.024. Epub 2008 Sep 10.

PMID:
18815031
18.

N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.

Hennequin LF, Allen J, Breed J, Curwen J, Fennell M, Green TP, Lambert-van der Brempt C, Morgentin R, Norman RA, Olivier A, Otterbein L, Plé PA, Warin N, Costello G.

J Med Chem. 2006 Nov 2;49(22):6465-88.

PMID:
17064066
19.

Molecular determinants for substrate specificity of the ligand-binding protein OpuAC from Bacillus subtilis for the compatible solutes glycine betaine and proline betaine.

Horn C, Sohn-Bösser L, Breed J, Welte W, Schmitt L, Bremer E.

J Mol Biol. 2006 Mar 24;357(2):592-606. Epub 2006 Jan 13.

PMID:
16445940
20.

Prevention of MKK6-dependent activation by binding to p38alpha MAP kinase.

Sullivan JE, Holdgate GA, Campbell D, Timms D, Gerhardt S, Breed J, Breeze AL, Bermingham A, Pauptit RA, Norman RA, Embrey KJ, Read J, VanScyoc WS, Ward WH.

Biochemistry. 2005 Dec 20;44(50):16475-90.

PMID:
16342939
21.

SAR and inhibitor complex structure determination of a novel class of potent and specific Aurora kinase inhibitors.

Heron NM, Anderson M, Blowers DP, Breed J, Eden JM, Green S, Hill GB, Johnson T, Jung FH, McMiken HH, Mortlock AA, Pannifer AD, Pauptit RA, Pink J, Roberts NJ, Rowsell S.

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1320-3. Epub 2005 Dec 5.

PMID:
16337122
22.

Structure-based design of protein tyrosine phosphatase-1B inhibitors.

Black E, Breed J, Breeze AL, Embrey K, Garcia R, Gero TW, Godfrey L, Kenny PW, Morley AD, Minshull CA, Pannifer AD, Read J, Rees A, Russell DJ, Toader D, Tucker J.

Bioorg Med Chem Lett. 2005 May 16;15(10):2503-7.

PMID:
15863305
23.

Novel, potent and selective anilinoquinazoline and anilinopyrimidine inhibitors of p38 MAP kinase.

Cumming JG, McKenzie CL, Bowden SG, Campbell D, Masters DJ, Breed J, Jewsbury PJ.

Bioorg Med Chem Lett. 2004 Nov 1;14(21):5389-94.

PMID:
15454232
24.

Imidazo[1,2-b]pyridazines: a potent and selective class of cyclin-dependent kinase inhibitors.

Byth KF, Cooper N, Culshaw JD, Heaton DW, Oakes SE, Minshull CA, Norman RA, Pauptit RA, Tucker JA, Breed J, Pannifer A, Rowsell S, Stanway JJ, Valentine AL, Thomas AP.

Bioorg Med Chem Lett. 2004 May 3;14(9):2249-52.

PMID:
15081018
25.

Crystal structure of human thymidine phosphorylase in complex with a small molecule inhibitor.

Norman RA, Barry ST, Bate M, Breed J, Colls JG, Ernill RJ, Luke RW, Minshull CA, McAlister MS, McCall EJ, McMiken HH, Paterson DS, Timms D, Tucker JA, Pauptit RA.

Structure. 2004 Jan;12(1):75-84.

26.

Cation-pi interactions as determinants for binding of the compatible solutes glycine betaine and proline betaine by the periplasmic ligand-binding protein ProX from Escherichia coli.

Schiefner A, Breed J, Bösser L, Kneip S, Gade J, Holtmann G, Diederichs K, Welte W, Bremer E.

J Biol Chem. 2004 Feb 13;279(7):5588-96. Epub 2003 Nov 11.

27.

Structure and interactions of NCAM Ig1-2-3 suggest a novel zipper mechanism for homophilic adhesion.

Soroka V, Kolkova K, Kastrup JS, Diederichs K, Breed J, Kiselyov VV, Poulsen FM, Larsen IK, Welte W, Berezin V, Bock E, Kasper C.

Structure. 2003 Oct;11(10):1291-301.

28.

Imidazo[1,2-a]pyridines: a potent and selective class of cyclin-dependent kinase inhibitors identified through structure-based hybridisation.

Anderson M, Beattie JF, Breault GA, Breed J, Byth KF, Culshaw JD, Ellston RP, Green S, Minshull CA, Norman RA, Pauptit RA, Stanway J, Thomas AP, Jewsbury PJ.

Bioorg Med Chem Lett. 2003 Sep 15;13(18):3021-6.

PMID:
12941325
29.

Crystal structure analysis of the exocytosis-sensitive phosphoprotein, pp63/parafusin (phosphoglucomutase), from Paramecium reveals significant conformational variability.

Müller S, Diederichs K, Breed J, Kissmehl R, Hauser K, Plattner H, Welte W.

J Mol Biol. 2002 Jan 11;315(2):141-53.

PMID:
11779235
30.

Purification, crystallization and preliminary crystallographic analysis of the periplasmic binding protein ProX from Escherichia coli.

Breed J, Kneip S, Gade J, Welte W, Bremer E.

Acta Crystallogr D Biol Crystallogr. 2001 Mar;57(Pt 3):448-50.

PMID:
11223528
31.

Three-dimensional structure of the nonaheme cytochrome c from Desulfovibrio desulfuricans Essex in the Fe(III) state at 1.89 A resolution.

Umhau S, Fritz G, Diederichs K, Breed J, Welte W, Kroneck PM.

Biochemistry. 2001 Feb 6;40(5):1308-16.

PMID:
11170457
32.
33.

Crystal structure of MalK, the ATPase subunit of the trehalose/maltose ABC transporter of the archaeon Thermococcus litoralis.

Diederichs K, Diez J, Greller G, Müller C, Breed J, Schnell C, Vonrhein C, Boos W, Welte W.

EMBO J. 2000 Nov 15;19(22):5951-61.

34.

Alamethicin channels in a membrane: molecular dynamics simulations.

Tieleman DP, Breed J, Berendsen HJ, Sansom MS.

Faraday Discuss. 1998;(111):209-23; discussion 225-46.

PMID:
10822611
35.

Comparison of in vivo and in vitro phosphorylation of the exocytosis-sensitive protein PP63/parafusin by differential MALDI mass spectrometric peptide mapping.

Kussmann M, Hauser K, Kissmehl R, Breed J, Plattner H, Roepstorff P.

Biochemistry. 1999 Jun 15;38(24):7780-90.

PMID:
10387018
36.

Prediction by a neural network of outer membrane beta-strand protein topology.

Diederichs K, Freigang J, Umhau S, Zeth K, Breed J.

Protein Sci. 1998 Nov;7(11):2413-20.

37.

A randomized trial in primary biliary cirrhosis comparing ursodeoxycholic acid in daily doses of either 10 mg/kg or 20 mg/kg. Dutch Multicentre PBC Study Group.

Van Hoogstraten HJ, De Smet MB, Renooij W, Breed JG, Engels LG, Den Ouden-Muller JW, Rijk MC, Smit AM, Zwertbroek R, Hop WC, van Berge Henegouwen GP, Schalm SW, van Buuren HR.

Aliment Pharmacol Ther. 1998 Oct;12(10):965-71.

38.

Treatment of elderly patients with isolated systolic hypertension with isosorbide dinitrate in an asymmetric dosing schedule.

Starmans-Kool MJ, Kleinjans HA, Lustermans FA, Kragten JA, Breed JG, Van Bortel LM.

J Hum Hypertens. 1998 Aug;12(8):557-61.

PMID:
9759991
39.
40.

Pharmacokinetics of a slower clearing tissue plasminogen activator variant, TNK-tPA, in patients with acute myocardial infarction.

Modi NB, Eppler S, Breed J, Cannon CP, Braunwald E, Love TW.

Thromb Haemost. 1998 Jan;79(1):134-9.

PMID:
9459338
41.

Ion channel stability and hydrogen bonding. Molecular modelling of channels formed by synthetic alamethicin analogues.

Breed J, Kerr ID, Molle G, Duclohier H, Sansom MS.

Biochim Biophys Acta. 1997 Dec 4;1330(2):103-9.

42.

Intrinsic rectification of ion flux in alamethicin channels: studies with an alamethicin dimer.

Woolley GA, Biggin PC, Schultz A, Lien L, Jaikaran DC, Breed J, Crowhurst K, Sansom MS.

Biophys J. 1997 Aug;73(2):770-8.

43.

Alamethicin channels - modelling via restrained molecular dynamics simulations.

Breed J, Biggin PC, Kerr ID, Smart OS, Sansom MS.

Biochim Biophys Acta. 1997 Apr 26;1325(2):235-49.

44.

The structure of porin from Paracoccus denitrificans at 3.1 A resolution.

Hirsch A, Breed J, Saxena K, Richter OM, Ludwig B, Diederichs K, Welte W.

FEBS Lett. 1997 Mar 10;404(2-3):208-10.

45.

A novel method for structure-based prediction of ion channel conductance properties.

Smart OS, Breed J, Smith GR, Sansom MS.

Biophys J. 1997 Mar;72(3):1109-26.

46.

Simulation studies of alamethicin-bilayer interactions.

Biggin PC, Breed J, Son HS, Sansom MS.

Biophys J. 1997 Feb;72(2 Pt 1):627-36.

47.

TNK-tissue plasminogen activator in acute myocardial infarction. Results of the Thrombolysis in Myocardial Infarction (TIMI) 10A dose-ranging trial.

Cannon CP, McCabe CH, Gibson CM, Ghali M, Sequeira RF, McKendall GR, Breed J, Modi NB, Fox NL, Tracy RP, Love TW, Braunwald E.

Circulation. 1997 Jan 21;95(2):351-6.

48.
49.

Engineering stabilized ion channels: covalent dimers of alamethicin.

You S, Peng S, Lien L, Breed J, Sansom MS, Woolley GA.

Biochemistry. 1996 May 21;35(20):6225-32.

PMID:
8639562
50.

Molecular dynamics simulations of water within models of ion channels.

Breed J, Sankararamakrishnan R, Kerr ID, Sansom MS.

Biophys J. 1996 Apr;70(4):1643-61.

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