J. Flanagan

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Computational Prediction of Amino Acids Governing Protein-Membrane Interaction for the PIP3 Cell Signaling System.

Jane R. Allison, W. A. Irvine, J. Flanagan, 2019, Structure.

One for the Price of Two…Are Bivalent Ligands Targeting Cannabinoid Receptor Dimers Capable of Simultaneously Binding to both Receptors?

M. Glass, J. Flanagan, Karan Govindpani, 2016, Trends in pharmacological sciences.

Glutathione transferases.

J. Hayes, J. Flanagan, I. Jowsey, 2005, Annual review of pharmacology and toxicology.

Synthesis and structure-activity relationships for 1-(4-(piperidin-1-ylsulfonyl)phenyl)pyrrolidin-2-ones as novel non-carboxylate inhibitors of the aldo-keto reductase enzyme AKR1C3.

W. Denny, A. Turnbull, J. Flanagan, 2013, European journal of medicinal chemistry.

Small-molecule CSF1R kinase inhibitors; review of patents 2015-present

W. Denny, J. Flanagan, 2020, Expert opinion on therapeutic patents.

Crystal Structures of Three Classes of Non-Steroidal Anti-Inflammatory Drugs in Complex with Aldo-Keto Reductase 1C3

Andrew P. Turnbull, A. Turnbull, J. Flanagan, 2012, PloS one.

Role of conserved Asp293 of cytochrome P450 2C9 in substrate recognition and catalytic activity.

M. Sutcliffe, C. Wolf, G. Roberts, 2003, The Biochemical journal.

Sequence-Structure-Function Classification of a Catalytically Diverse Oxidoreductase Superfamily in Mycobacteria.

C. Jackson, P. Carr, J. Flanagan, 2015, Journal of molecular biology.

Human Glutathione Transferase T2-2 Discloses Some Evolutionary Strategies for Optimization of Substrate Binding to the Active Site of Glutathione Transferases*

R. Paolesse, M. Parker, A. Caccuri, 2001, The Journal of Biological Chemistry.

Ab initio calculations on hidden modulators of theta class glutathione transferase activity

G. Chelvanayagam, M. Parker, J. Flanagan, 2000, Proteins.

Mutagenic analysis of conserved arginine residues in and around the novel sulfate binding pocket of the human Theta class glutathione transferase T2‐2

G. Chelvanayagam, J. Rossjohn, M. Parker, 1999, Protein science : a publication of the Protein Society.

Role of conserved Asp 293 of cytochrome P 450 2 C 9 in substrate recognition and catalytic activity

M. Sutcliffe, C. Wolf, G. Roberts, 2022 .

Binding mode of the breakthrough inhibitor AZD9291 to epidermal growth factor receptor revealed.

J. Smaill, J. Flanagan, M. McKeage, 2015, Journal of structural biology.

An inflammatory role for the mammalian carboxypeptidase inhibitor latexin: relationship to cystatins and the tumor suppressor TIG1.

D. Hume, T. Ravasi, C. Wells, 2005, Structure.

A new selective pharmacological enhancer of the Orai1 Ca2+ channel reveals roles for Orai1 in smooth and skeletal muscle functions.

W. Denny, I. Vetter, I. Azimi, 2020, ACS pharmacology & translational science.

Combining properties of different classes of PI3Kα inhibitors to understand the molecular features that confer selectivity.

W. Denny, G. Rewcastle, C. Buchanan, 2017, The Biochemical journal.

Inhibition of NMDA receptor function with an anti-GluN1-S2 antibody impairs human platelet function and thrombosis

M. During, Peng Sun, Ting-Yu Chen, 2017, Platelets.

Targeting the Warburg Effect in cancer; relationships for 2-arylpyridazinones as inhibitors of the key glycolytic enzyme 6-phosphofructo-2-kinase/2,6-bisphosphatase 3 (PFKFB3).

W. Denny, C. K. Watts, D. G. Brooke, 2014, Bioorganic & medicinal chemistry.

Discovery and evaluation of inhibitors to the immunosuppressive enzyme indoleamine 2,3-dioxygenase 1 (IDO1): Probing the active site-inhibitor interactions.

B. Palmer, J. Flanagan, L. Ching, 2017, European journal of medicinal chemistry.

Evaluation of Novel Inhibitors of Tryptophan Dioxygenases for Enzyme and Species Selectivity Using Engineered Tumour Cell Lines Expressing Either Murine or Human IDO1 or TDO2

S. Gamage, B. Palmer, J. Flanagan, 2022, Pharmaceuticals.

Structure, function and inhibition of the phosphoinositide 3-kinase p110α enzyme.

P. Shepherd, J. Flanagan, 2014, Biochemical Society transactions.

Discovery of pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors.

Claire L. Lill, W. Denny, G. Rewcastle, 2012, Bioorganic & medicinal chemistry.

Orthogonal assays for the identification of inhibitors of the single-stranded nucleic acid binding protein YB-1

C. Print, G. Rewcastle, A. Lasham, 2019, Acta pharmaceutica Sinica. B.

3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3.

W. Denny, A. Turnbull, D. G. Brooke, 2012, Journal of medicinal chemistry.

Targeting growth hormone function: strategies and therapeutic applications

J. Flanagan, J. Perry, M. Hay, 2019, Signal Transduction and Targeted Therapy.

Identification and characterization of GSTT3, a third murine Theta class glutathione transferase.

W. Pearson, M. Parker, J. Flanagan, 2002, The Biochemical journal.

Identification and molecular modeling of a novel, plant-like, human purple acid phosphatase.

D. Hume, L. Guddat, J. Flanagan, 2006, Gene.

Novel pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors: Exploring the benzenesulfonohydrazide SAR.

Claire L. Lill, K. Y. Tsang, W. Denny, 2012, Bioorganic & medicinal chemistry.

Structural insights into RAMP modification of secretin family G protein-coupled receptors: implications for drug development.

J. Archbold, D. Hay, J. Flanagan, 2011, Trends in pharmacological sciences.

4-Pyridylanilinothiazoles that selectively target von Hippel-Lindau deficient renal cell carcinoma cells by inducing autophagic cell death.

P. Sutphin, W. Denny, A. Giaccia, 2010, Journal of medicinal chemistry.

Formation of fluorophores from the kynurenine pathway metabolite N-formylkynurenine and cyclic amines involves transamidation and carbon-carbon bond formation at the 2-position of the amine.

B. Palmer, J. Flanagan, L. Ching, 2015, Biochimica et biophysica acta.

Evaluation of known and novel inhibitors of Orai1-mediated store operated Ca2+ entry in MDA-MB-231 breast cancer cells using a Fluorescence Imaging Plate Reader assay.

W. Denny, I. Vetter, I. Azimi, 2017, Bioorganic & medicinal chemistry.

Human Glutathione Transferase T2-2 Discloses Some Evolutionary Strategies for Optimization of the Catalytic Activity of Glutathione Transferases*

G. Chelvanayagam, R. Paolesse, M. Parker, 2001, The Journal of Biological Chemistry.

Probing the molecular basis of substrate specificity and catalysis in the theta class glutathione transferases

J. Flanagan, 1999 .

SAR studies of 4-pyridyl heterocyclic anilines that selectively induce autophagic cell death in von Hippel-Lindau-deficient renal cell carcinoma cells.

A. Giaccia, J. Flanagan, M. Bonnet, 2011, Bioorganic & medicinal chemistry.

Discovery and characterisation of hydrazines as inhibitors of the immune suppressive enzyme, indoleamine 2,3-dioxygenase 1 (IDO1).

B. Palmer, J. Jamie, J. Flanagan, 2013, Bioorganic & medicinal chemistry.

Formation of an N-formylkynurenine-derived fluorophore and its use for measuring indoleamine 2,3-dioxygenase 1 activity

B. Palmer, J. Jamie, J. Flanagan, 2013, Analytical and Bioanalytical Chemistry.

Why Is Quinidine an Inhibitor of Cytochrome P450 2D6?

M. Sutcliffe, Jean‐Didier Maréchal, C. Wolf, 2005, Journal of Biological Chemistry.

Rational design of an AKR1C3-resistant analog of PR-104 for enzyme-prodrug therapy.

J. Smaill, J. Flanagan, J. Copp, 2016, Biochemical pharmacology.

Rational design of an AKR 1 C 3-resistant analog of PR-104 for enzyme-prodrug therapy

J. Smaill, J. Flanagan, J. Copp, 2016 .

Diverse mechanisms activate the PI 3-kinase/mTOR pathway in melanomas: implications for the use of PI 3-kinase inhibitors to overcome resistance to inhibitors of BRAF and MEK

Khanh B. Tran, G. Rewcastle, P. Shepherd, 2021, BMC cancer.

Targeting GLUT1 and the Warburg Effect in Renal Cell Carcinoma by Chemical Synthetic Lethality

P. Sutphin, W. Denny, E. Graves, 2011, Science Translational Medicine.

Mammalian class Sigma glutathione S-transferases: catalytic properties and tissue-specific expression of human and rat GSH-dependent prostaglandin D2 synthases.

P. Murdock, J. Hayes, Stephen A. Smith, 2001, The Biochemical journal.

Evidence That GRIN2A Mutations in Melanoma Correlate with Decreased Survival

M. During, M. Askarian-Amiri, R. Isaacs, 2014, Front. Oncol..

High-throughput screening campaigns against a PI3Kα isoform bearing the H1047R mutation identified potential inhibitors with novel scaffolds

W. Denny, G. Rewcastle, C. Buchanan, 2018, Acta Pharmacologica Sinica.

Structure of AKR1C3 with 3-phenoxybenzoic acid bound.

J. Flanagan, Y. Yosaatmadja, C. Squire, 2012, Acta crystallographica. Section F, Structural biology and crystallization communications.

Exploring the isoform selectivity of TGX-221 related pyrido[1,2-a]pyrimidinone-based Class IA PI 3-kinase inhibitors: synthesis, biological evaluation and molecular modelling.

Claire L. Lill, W. Denny, G. Rewcastle, 2015, Bioorganic & medicinal chemistry.

A drug targeting only p110α can block phosphoinositide 3-kinase signalling and tumour growth in certain cell types

W. Denny, G. Rewcastle, C. Buchanan, 2011, The Biochemical journal.

Synthesis and biological evaluation of sulfonamide analogues of the phosphatidylinositol 3-kinase inhibitor ZSTK474.

K. Y. Tsang, S. Gamage, W. Denny, 2017, Bioorganic & medicinal chemistry.

Synthesis and biological evaluation of novel phosphatidylinositol 3-kinase inhibitors: Solubilized 4-substituted benzimidazole analogs of 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474).

Claire L. Lill, S. Gamage, W. Denny, 2013, European journal of medicinal chemistry.

Synthesis and biological evaluation of novel analogues of the pan class I phosphatidylinositol 3-kinase (PI3K) inhibitor 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474).

Claire L. Lill, S. Gamage, W. Denny, 2011, Journal of medicinal chemistry.

A single discrete Rab5-binding site in phosphoinositide 3-kinase β is required for tumor cell invasion

David J. Hamelin, Zahra Erami, A. Bresnick, 2019, The Journal of Biological Chemistry.

Identifying novel targets in renal cell carcinoma: design and synthesis of affinity chromatography reagents.

A. Giaccia, J. Flanagan, M. Bonnet, 2014, Bioorganic & medicinal chemistry.

DMXAA (Vadimezan, ASA404) is a multi-kinase inhibitor targeting VEGFR2 in particular.

G. Rewcastle, C. Buchanan, P. Shepherd, 2012, Clinical science.

Synthesis and Evaluation of Imidazo[1,2-a]pyridine Analogues of the ZSTK474 Class of Phosphatidylinositol 3-Kinase Inhibitors.

K. Y. Tsang, J. A. Spicer, S. Gamage, 2019, Chemistry, an Asian journal.

Structural Evolution of the ABC Transporter Subfamily B

T. Huber, J. Flanagan, 2007, Evolutionary bioinformatics online.

Sigma-class glutathione transferases

J. Flanagan, M. Smythe, 2011, Drug metabolism reviews.

Human theta class glutathione transferase: the crystal structure reveals a sulfate-binding pocket within a buried active site.

G Chelvanayagam, J Rossjohn, M W Parker, 1998, Structure.

Engineering a Multifunctional Nitroreductase for Improved Activation of Prodrugs and PET Probes for Cancer Gene Therapy.

J. Smaill, J. Flanagan, J. Copp, 2017, Cell chemical biology.

Dichloromethane mediated in vivo selection and functional characterization of rat glutathione S-transferase theta 1-1 variants.

G. Chelvanayagam, S. Vuilleumier, J. Rossjohn, 2001, European journal of biochemistry.

Chan Chemical Synthetic Lethality Targeting GLUT 1 and the Warburg Effect in Renal Cell Carcinoma by

P. Sutphin, W. Denny, E. Graves, 2011 .

Identification of Small-Molecule Positive Modulators of Calcitonin-like Receptor-Based Receptors.

G. Pairaudeau, C. Reynolds, A. Pioszak, 2020, ACS pharmacology & translational science.

Inhibitors of Discoidin Domain Receptor (DDR) Kinases for Cancer and Inflammation

W. Denny, J. Flanagan, 2021, Biomolecules.

Morpholylureas are a new class of potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase (AKR1C3).

W. Denny, A. Turnbull, D. G. Brooke, 2014, Bioorganic & medicinal chemistry.

Influence of Aldo-keto Reductase 1C3 in Prostate Cancer - A Mini Review.

L. Ferguson, J. Flanagan, N. Karunasinghe, 2017, Current cancer drug targets.

Identification of a non-purple tartrate-resistant acid phosphatase: an evolutionary link to Ser/Thr protein phosphatases?

D. Hume, L. Guddat, T. Huber, 2008, BMC Research Notes.

An SAR study of hydroxy-trifluoromethylpyrazolines as inhibitors of Orai1-mediated store operated Ca2+ entry in MDA-MB-231 breast cancer cells using a convenient Fluorescence Imaging Plate Reader assay.

W. Denny, I. Vetter, I. Azimi, 2018, Bioorganic & medicinal chemistry.

A homology model for the human theta‐class glutathione transferase T1–1

G Chelvanayagam, J Rossjohn, M W Parker, 1998, Proteins.

Variable-length Ester-based Staples for α-Helical Peptides Using A Double Thiol-ene Reaction.

M. Brimble, J. Flanagan, P. Harris, 2020, Chemistry.

Phe120 contributes to the regiospecificity of cytochrome P450 2D6: mutation leads to the formation of a novel dextromethorphan metabolite.

Gordon C K Roberts, Jean-Didier Maréchal, C Roland Wolf, 2004, The Biochemical journal.

3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic acids; a New Class of Highly Potent and Selective Inhibitors of the Type 5 17-beta-hydroxysteroid Dehydrogenase AKR1C3

W. Denny, A. Turnbull, D. G. Brooke, 2012 .

High-throughput screening campaigns against a PI3Kα isoform bearing the H1047R mutation identified potential inhibitors with novel scaffolds

W. Denny, G. Rewcastle, C. Buchanan, 2018, Acta Pharmacologica Sinica.

Identification and characterisation of new inhibitors for the human hematopoietic prostaglandin D2 synthase.

D. Hume, Angelika N. Christ, J. Hayes, 2010, European journal of medicinal chemistry.

Residues Glutamate 216 and Aspartate 301 Are Key Determinants of Substrate Specificity and Product Regioselectivity in Cytochrome P450 2D6*

Gordon C K Roberts, C Roland Wolf, Mark J I Paine, 2003, The Journal of Biological Chemistry.

Novel pyrazolo[1,5-a]pyridines as PI3K inhibitors: variation of the central linker group

Claire L. Lill, K. Y. Tsang, W. Denny, 2014 .

Parallel discovery of selective and dual inhibitors of tryptophan dioxygenases IDO1 and TDO2 with a newly-modified enzymatic assay.

B. Palmer, J. Flanagan, L. Ching, 2021, Bioorganic & medicinal chemistry.

One for the Price of Two…Are Bivalent Ligands Targeting Cannabinoid Receptor Dimers Capable of Simultaneously Binding to both Receptors?

M. Glass, J. Flanagan, Karan Govindpani, 2016, TIPS - Trends in Pharmacological Sciences.