Julian Blagg

Julian Blagg

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Julian Blagg

Julian Blagg

Publications by authors named "Julian Blagg"

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Metabolism of the dual FLT-3/Aurora kinase inhibitor CCT241736 in preclinical and human in vitro models: Implication for the choice of toxicology species.

Eur J Pharm Sci 2019 Nov 3;139:104899. Epub 2019 Apr 3.

Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, United Kingdom. Electronic address:

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http://dx.doi.org/10.1016/j.ejps.2019.04.004DOI Listing
November 2019

Catalytic inhibition of KDM1A in Ewing sarcoma is insufficient as a therapeutic strategy.

Pediatr Blood Cancer 2019 Sep 17;66(9):e27888. Epub 2019 Jun 17.

Sarcoma Molecular Pathology Team, Divisions of Molecular Pathology and Cancer Therapeutics, The Institute of Cancer Research, London, UK.

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http://dx.doi.org/10.1002/pbc.27888DOI Listing
September 2019

Ligand discrimination between active and inactive activation loop conformations of Aurora-A kinase is unmodified by phosphorylation.

Chem Sci 2019 Apr 4;10(14):4069-4076. Epub 2019 Mar 4.

Molecular Medicine , National Heart & Lung Institute , Imperial College London , SAF Building , London SW7 2AZ , UK.

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http://dx.doi.org/10.1039/c8sc03669aDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6461105PMC
April 2019

Combining Mutational Signatures, Clonal Fitness, and Drug Affinity to Define Drug-Specific Resistance Mutations in Cancer.

Cell Chem Biol 2018 11 23;25(11):1359-1371.e2. Epub 2018 Aug 23.

Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, UK. Electronic address:

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http://dx.doi.org/10.1016/j.chembiol.2018.07.013DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6242700PMC
November 2018

Evaluation of APOBEC3B Recognition Motifs by NMR Reveals Preferred Substrates.

ACS Chem Biol 2018 09 27;13(9):2427-2432. Epub 2018 Aug 27.

Cancer Research UK Cancer Therapeutics Unit , The Institute of Cancer Research , London SM2 5NG , U.K.

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http://dx.doi.org/10.1021/acschembio.8b00639DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6430498PMC
September 2018

Dynamic Equilibrium of the Aurora A Kinase Activation Loop Revealed by Single-Molecule Spectroscopy.

Angew Chem Int Ed Engl 2017 09 7;56(38):11409-11414. Epub 2017 Aug 7.

National Heart & Lung Institute, SAF Building, Imperial College London, London, SW7 2AZ, UK.

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http://dx.doi.org/10.1002/anie.201704654DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5601181PMC
September 2017

Choose and Use Your Chemical Probe Wisely to Explore Cancer Biology.

Cancer Cell 2017 07;32(1):9-25

Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, UK. Electronic address:

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http://dx.doi.org/10.1016/j.ccell.2017.06.005DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5511331PMC
July 2017

Targeting Androgen Receptor Aberrations in Castration-Resistant Prostate Cancer.

Clin Cancer Res 2016 Sep 21;22(17):4280-2. Epub 2016 Jun 21.

Prostate Cancer Targeted Therapy Group, Institute of Cancer Research and The Royal Marsden NHS Foundation Trust, Sutton, United Kingdom.

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http://dx.doi.org/10.1158/1078-0432.CCR-16-1137DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5302169PMC
September 2016

Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore.

Bioorg Med Chem Lett 2016 Mar 22;26(5):1443-51. Epub 2016 Jan 22.

Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London SW7 3RP, UK.

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http://dx.doi.org/10.1016/j.bmcl.2016.01.062DOI Listing
March 2016

Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance.

Cancer Res 2015 Aug 22;75(16):3340-54. Epub 2015 Jul 22.

Breakthrough Breast Cancer Research Centre, Division of Breast Cancer Research, The Institute of Cancer Research, London, United Kingdom. Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, United Kingdom.

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http://cancerres.aacrjournals.org/content/early/2015/07/21/0
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http://cancerres.aacrjournals.org/content/75/16/3340.full.pd
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http://cancerres.aacrjournals.org/cgi/doi/10.1158/0008-5472.
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http://dx.doi.org/10.1158/0008-5472.CAN-14-3272DOI Listing
August 2015

Aurora kinase inhibition: a new light in the sky?

J Med Chem 2015 Jul 25;58(13):5186-8. Epub 2015 Jun 25.

†Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K.

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http://dx.doi.org/10.1021/acs.jmedchem.5b00918DOI Listing
July 2015

MOARF, an Integrated Workflow for Multiobjective Optimization: Implementation, Synthesis, and Biological Evaluation.

J Chem Inf Model 2015 Jun 9;55(6):1169-80. Epub 2015 Jun 9.

Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, SM2 5NG, U.K.

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http://pubs.acs.org/doi/10.1021/acs.jcim.5b00073
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http://dx.doi.org/10.1021/acs.jcim.5b00073DOI Listing
June 2015

Diverse functionalization of Aurora-A kinase at specified surface and buried sites by native chemical modification.

PLoS One 2014 5;9(8):e103935. Epub 2014 Aug 5.

Cancer Research U.K. Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, United Kingdom.

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0103935PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4122486PMC
April 2015

Chemical biology approaches to target validation in cancer.

Curr Opin Pharmacol 2014 Aug 28;17:87-100. Epub 2014 Aug 28.

Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, UK. Electronic address:

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http://dx.doi.org/10.1016/j.coph.2014.07.007DOI Listing
August 2014

Insights into Aurora-A kinase activation using unnatural amino acids incorporated by chemical modification.

ACS Chem Biol 2013 Oct 7;8(10):2184-91. Epub 2013 Aug 7.

Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, Surrey, SM2 5NG, U.K.

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http://dx.doi.org/10.1021/cb400425tDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3805324PMC
October 2013

Scaffold-focused virtual screening: prospective application to the discovery of TTK inhibitors.

J Chem Inf Model 2013 May 14;53(5):1100-12. Epub 2013 May 14.

Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, Sutton, Surrey, United Kingdom.

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http://dx.doi.org/10.1021/ci400100cDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3665241PMC
May 2013

Regioselective C2-arylation of imidazo[4,5-b]pyridines.

Org Biomol Chem 2013 Apr;11(14):2335-47

Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, Haddow Laboratories, Sutton, Surrey SM2 5NG, UK.

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http://dx.doi.org/10.1039/c3ob27477bDOI Listing
April 2013

Benzimidazole inhibitors of the protein kinase CHK2: clarification of the binding mode by flexible side chain docking and protein-ligand crystallography.

Bioorg Med Chem 2012 Nov 21;20(22):6630-9. Epub 2012 Sep 21.

Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, Institute of Cancer Research, Haddow Laboratories, Sutton, Surrey, UK.

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http://dx.doi.org/10.1016/j.bmc.2012.09.024DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3778940PMC
November 2012

Plane of best fit: a novel method to characterize the three-dimensionality of molecules.

J Chem Inf Model 2012 Oct 26;52(10):2516-25. Epub 2012 Sep 26.

Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, 15 Cotswold Road, Sutton, Surrey, SM2 5NG, UK.

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http://dx.doi.org/10.1021/ci300293fDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3477823PMC
October 2012

Scaffold diversity of exemplified medicinal chemistry space.

J Chem Inf Model 2011 Sep 31;51(9):2174-85. Epub 2011 Aug 31.

Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, Sutton, Surrey, UK.

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http://dx.doi.org/10.1021/ci2001428DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3180201PMC
September 2011

Epigenetics: Targeting leukemia on the DOT.

Nat Chem Biol 2011 Aug 28;7(10):663-5. Epub 2011 Aug 28.

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http://dx.doi.org/10.1038/nchembio.661DOI Listing
August 2011

Analysis of water patterns in protein kinase binding sites.

Proteins 2011 Jul 9;79(7):2109-21. Epub 2011 May 9.

Section of Cancer Therapeutics, The Institute of Cancer Research, Haddow Laboratories, Sutton, Surrey SM2 5NG, United Kingdom.

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http://dx.doi.org/10.1002/prot.23032DOI Listing
July 2011

Structural basis of poly(ADP-ribose) recognition by the multizinc binding domain of checkpoint with forkhead-associated and RING Domains (CHFR).

J Biol Chem 2010 Dec 29;285(50):39348-58. Epub 2010 Sep 29.

Section of Structural Biology, Institute of Cancer Research, Chester Beatty Laboratories, 237 Fulham Road, London SW3 6JB, United Kingdom.

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http://dx.doi.org/10.1074/jbc.M110.159855DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2998101PMC
December 2010

Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells.

Bioorg Med Chem Lett 2010 Oct 21;20(20):5988-93. Epub 2010 Aug 21.

Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, Sutton, Surrey, United Kingdom.

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http://dx.doi.org/10.1016/j.bmcl.2010.08.091DOI Listing
October 2010

Crystal structure of an Aurora-A mutant that mimics Aurora-B bound to MLN8054: insights into selectivity and drug design.

Biochem J 2010 Mar 15;427(1):19-28. Epub 2010 Mar 15.

Section of Structural Biology, The Institute of Cancer Research, Chester Beatty Laboratories, 237 Fulham Road, London SW36JB, U.K.

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http://dx.doi.org/10.1042/BJ20091530DOI Listing
March 2010

The tetrahydrobiopterin pathway and pain.

Curr Opin Investig Drugs 2010 Jan;11(1):19-30

Solace Pharmaceuticals Ltd, 6 Denne Hill Business Centre, Denne Hill Farm, Womenswold, Canterbury, Kent CT5 3PJ, UK.

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January 2010

Design and synthesis of pyridazinone-based 5-HT(2C) agonists.

Bioorg Med Chem Lett 2009 Oct 6;19(19):5791-5. Epub 2009 Aug 6.

Department of Discovery Chemistry, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT139NJ, UK.

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http://dx.doi.org/10.1016/j.bmcl.2009.07.136DOI Listing
October 2009

Design and synthesis of piperazinylpyrimidinones as novel selective 5-HT(2C) agonists.

Bioorg Med Chem Lett 2009 Sep 6;19(18):5346-50. Epub 2009 Aug 6.

Department of Medicinal Chemistry, Pfizer Global Research and Development, Sandwich Laboratories, Sandwich, Kent CT13 9NJ, UK.

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http://dx.doi.org/10.1016/j.bmcl.2009.07.133DOI Listing
September 2009

Physicochemical drug properties associated with in vivo toxicological outcomes: a review.

Expert Opin Drug Metab Toxicol 2009 Aug;5(8):921-31

Pfizer Global Research and Development, Groton/New London Laboratories, Pfizer, Inc., Eastern Point Road, Groton, CT 06340, USA.

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http://dx.doi.org/10.1517/17425250903042318DOI Listing
August 2009

Small, non-peptide C5a receptor antagonists: part 2.

Bioorg Med Chem Lett 2008 Oct 31;18(20):5605-8. Epub 2008 Aug 31.

Department of Discovery Chemistry, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK.

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http://dx.doi.org/10.1016/j.bmcl.2008.08.101DOI Listing
October 2008

Small, non-peptide C5a receptor antagonists: part 1.

Bioorg Med Chem Lett 2008 Oct 31;18(20):5601-4. Epub 2008 Aug 31.

Department of Discovery Chemistry, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK.

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http://dx.doi.org/10.1016/j.bmcl.2008.08.106DOI Listing
October 2008

1-(2-Phenoxyphenyl)methanamines: SAR for dual serotonin/noradrenaline reuptake inhibition, metabolic stability and hERG affinity.

Bioorg Med Chem Lett 2008 Jan;18(2):596-9

Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK.

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http://dx.doi.org/10.1016/j.bmcl.2007.11.080DOI Listing
January 2008

The metabolism and toxicity of furosemide in the Wistar rat and CD-1 mouse: a chemical and biochemical definition of the toxicophore.

J Pharmacol Exp Ther 2007 Sep 7;322(3):1208-20. Epub 2007 Jun 7.

Drug Safety Research Group, Department of Pharmacology and Therapeutics, University of Liverpool, Sherrington Buildings, Ashton Street, Liverpool, Merseyside L69 3GE, UK.

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http://dx.doi.org/10.1124/jpet.107.125302DOI Listing
September 2007

Potent and selective nonpeptidic inhibitors of procollagen C-proteinase.

J Med Chem 2007 Jul 26;50(15):3442-56. Epub 2007 Jun 26.

Department of Discovery Chemistry, Pfizer Global Research and Development, Sandwich, Kent, CT13 9NJ, United Kingdom.

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http://dx.doi.org/10.1021/jm061010zDOI Listing
July 2007