Edinburgh Drug Discovery

Recent Publications

Commitment to the dissemination of knowledge and leadership in our field has led us to produce numerous drug discovery publications.

An Edinburgh Drug Discovery researcher writes chemical compounds

Our publications in the field of drug discovery research span a wide range of topics including research articles on novel targets, compounds and drug delivery systems in myriad disease areas, new methods and assays to promote drug discovery, perspective pieces on progress in the field and review articles.

The following articles are selected from our portfolio and listed by most recently published.

Selected articles from 2015

A magnetic bead-based ligand binding assay to facilitate human kynurenine 3-monooxygenase drug discovery

K. Wilson, D. J. Mole, N. Z. Homer, J. P. Iredale, M. Auer and S. P. Webster J Biomol Screen (2015):  20(2): 292-8

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Palladium-mediated dealkylation of N-propargyl-floxuridine as a bioorthogonal oxygen-independent prodrug strategy

J. T. Weiss, N. O. Carragher and A. Unciti-Broceta Sci Rep (2015):  5: 9329

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Bioorthogonal catalysis: Rise of the nanobots

A. Unciti-Broceta Nat Chem (2015):  7(7): 538-9

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Cognitive and disease-modifying effects of 11ss-hydroxysteroid dehydrogenase type 1 inhibition in male Tg2576 mice, a model of Alzheimer's disease

K. Sooy, J. Noble, A. McBride, M. Binnie, J. L. Yau, J. R. Seckl, B. R. Walker and S. P. Webster Endocrinology (2015): en20151395

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UFSRAT: Ultra-fast Shape Recognition with Atom Types--the discovery of novel bioactive small molecular scaffolds for FKBP12 and 11betaHSD1

S. Shave, E. A. Blackburn, J. Adie, D. R. Houston, M. Auer, S. P. Webster, P. Taylor and M. D. Walkinshaw PLoS One (2015):  10(2): e0116570

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Amide-controlled, one-pot synthesis of tri-substituted purines generates structural diversity and analogues with trypanocidal activity

M. J. Pineda de las Infantas y Villatoro, J. D. Unciti-Broceta, R. Contreras-Montoya, J. A. Garcia-Salcedo, M. A. Gallo Mezo, A. Unciti-Broceta and J. J. Diaz-Mochon Sci Rep (2015):  5: 9139

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Synthesis of 6,8,9 poly-substituted purine analogue libraries as pro-apoptotic inducers of human leukemic lymphocytes and DAPK-1 inhibitors

M. J. Pineda de las Infantas, S. Torres-Rusillo, J. D. Unciti-Broceta, P. Fernandez-Rubio, M. A. Luque-Gonzalez, M. A. Gallo, A. Unciti-Broceta, I. J. Molina and J. J. Diaz-Mochon Org Biomol Chem (2015):  13(18): 5224-34

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Axl inhibitors in cancer: A medicinal chemistry perspective 

S.H. Meyers, V.G. Brunton, A. Unciti-Broceta   Journal of Medicinal Chemistry (2015): 

Potent organo-osmium compound shifts metabolism in epithelial ovarian cancer cells

J. M. Hearn, I. Romero-Canelon, A. F. Munro, Y. Fu, A. M. Pizarro, M. J. Garnett, U. McDermott, N. O. Carragher and P. J. Sadler Proc Natl Acad Sci U S A (2015):  112(29): E3800-5

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Paradox-breaking RAF inhibitors that also target SRC are effective in drug-resistant BRAF mutant melanoma

M. R. Girotti, F. Lopes, N. Preece, D. Niculescu-Duvaz, A. Zambon, L. Davies, S. Whittaker, G. Saturno, A. Viros, M. Pedersen, B. M. Suijkerbuijk, D. Menard, R. McLeary, L. Johnson, L. Fish, S. Ejiama, B. Sanchez-Laorden, J. Hohloch, N. Carragher, K. Macleod, G. Ashton, A. A. Marusiak, A. Fusi, J. Brognard, M. Frame, P. Lorigan, R. Marais and C. Springer Cancer Cell (2015):  27(1): 85-96

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Selected articles from 2014

Bacterial expression of human kynurenine 3-monooxygenase: solubility, activity, purification

K. Wilson, D. J. Mole, M. Binnie, N. Z. Homer, X. Zheng, B. A. Yard, J. P. Iredale, M. Auer and S. P. Webster Protein Expr Purif (2014):  95: 96-103

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N-alkynyl derivatives of 5-fluorouracil: susceptibility to palladium-mediated dealkylation and toxigenicity in cancer cell culture

J. T. Weiss, C. Fraser, B. Rubio-Ruiz, S. H. Myers, R. Crispin, J. C. Dawson, V. G. Brunton, E. E. Patton, N. O. Carragher and A. Unciti-Broceta Front Chem (2014):  2: 56

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Extracellular palladium-catalysed dealkylation of 5-fluoro-1-propargyl-uracil as a bioorthogonally activated prodrug approach

J. T. Weiss, J. C. Dawson, K. G. Macleod, W. Rybski, C. Fraser, C. Torres-Sanchez, E. E. Patton, M. Bradley, N. O. Carragher and A. Unciti-Broceta Nat Commun (2014):  5: 3277

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Development and bioorthogonal activation of palladium-labile prodrugs of gemcitabine

J. T. Weiss, J. C. Dawson, C. Fraser, W. Rybski, C. Torres-Sanchez, M. Bradley, E. E. Patton, N. O. Carragher and A. Unciti-Broceta J Med Chem (2014):  57(12): 5395-404

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Lead discovery for human kynurenine 3-monooxygenase by high-throughput RapidFire mass spectrometry

D. M. Lowe, M. Gee, C. Haslam, B. Leavens, E. Christodoulou, P. Hissey, P. Hardwicke, A. Argyrou, S. P. Webster, D. J. Mole, K. Wilson, M. Binnie, B. A. Yard, T. Dean, J. Liddle, I. Uings and J. P. Hutchinson J Biomol Screen (2014):  19(4): 508-15

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Quantitative phenotypic and pathway profiling guides rational drug combination strategies

J. C. Dawson and N. O. Carragher Front Pharmacol (2014):  5: 118

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Developments in preclinical cancer imaging: innovating the discovery of therapeutics

J. R. Conway, N. O. Carragher and P. Timpson Nat Rev Cancer (2014):  14(5): 314-28

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Elevated hepatic 11beta-hydroxysteroid dehydrogenase type 1 induces insulin resistance in uremia

A. Chapagain, P. W. Caton, J. Kieswich, P. Andrikopoulos, N. Nayuni, J. H. Long, S. M. Harwood, S. P. Webster, M. J. Raftery, C. Thiemermann, B. R. Walker, J. R. Seckl, R. Corder and M. M. Yaqoob Proc Natl Acad Sci U S A (2014):  111(10): 3817-22

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Selected articles from 2013

A yeast chemical genetic screen identifies inhibitors of human telomerase

L. H. Wong, A. Unciti-Broceta, M. Spitzer, R. White, M. Tyers and L. Harrington Chem Biol (2013):  20(3): 333-40

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Intravital FLIM-FRET imaging reveals dasatinib-induced spatial control of src in pancreatic cancer

M. Nobis, E. J. McGhee, J. P. Morton, J. P. Schwarz, S. A. Karim, J. Quinn, M. Edward, A. D. Campbell, L. C. McGarry, T. R. Evans, V. G. Brunton, M. C. Frame, N. O. Carragher, Y. Wang, O. J. Sansom, P. Timpson and K. I. Anderson Cancer Res (2013):  73(15): 4674-86

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Advanced intravital subcellular imaging reveals vital three-dimensional signalling events driving cancer cell behaviour and drug responses in live tissue

M. Nobis, N. O. Carragher, E. J. McGhee, J. P. Morton, O. J. Sansom, K. I. Anderson and P. Timpson FEBS J (2013):  280(21): 5177-97

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Comparison of methods for image-based profiling of cellular morphological responses to small-molecule treatment

V. Ljosa, P. D. Caie, R. Ter Horst, K. L. Sokolnicki, E. L. Jenkins, S. Daya, M. E. Roberts, T. R. Jones, S. Singh, A. Genovesio, P. A. Clemons, N. O. Carragher and A. E. Carpenter J Biomol Screen (2013):  18(10): 1321-9

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Dasatinib inhibits mammary tumour development in a genetically engineered mouse model

S. A. Karim, H. Creedon, H. Patel, N. O. Carragher, J. P. Morton, W. J. Muller, T. R. Evans, B. Gusterson, O. J. Sansom and V. G. Brunton J Pathol (2013):  230(4): 430-40

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High-content analysis to leverage a robust phenotypic profiling approach to vascular modulation

B. J. Isherwood, R. E. Walls, M. E. Roberts, T. M. Houslay, S. R. Brave, S. T. Barry and N. O. Carragher J Biomol Screen (2013):  18(10): 1246-59

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Ret inhibition decreases growth and metastatic potential of estrogen receptor positive breast cancer cells

A. Gattelli, I. Nalvarte, A. Boulay, T. C. Roloff, M. Schreiber, N. Carragher, K. K. Macleod, M. Schlederer, S. Lienhard, L. Kenner, M. I. Torres-Arzayus and N. E. Hynes EMBO Mol Med (2013):  5(9): 1335-50

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Mass spectrometry imaging for dissecting steroid intracrinology within target tissues

D. F. Cobice, C. L. Mackay, R. J. Goodwin, A. McBride, P. R. Langridge-Smith, S. P. Webster, B. R. Walker and R. Andrew Anal Chem (2013):  85(23): 11576-84

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Publications Archive

For articles dated up to 2012, please visit our archived publications.

Read our archived articles.