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Items: 1 to 50 of 62

1.

Engineering Escherichia coli NfsB To Activate a Hypoxia-Resistant Analogue of the PET Probe EF5 To Enable Non-Invasive Imaging during Enzyme Prodrug Therapy.

Williams EM, Rich MH, Mowday AM, Ashoorzadeh A, Copp JN, Guise CP, Anderson RF, Flanagan JU, Smaill JB, Patterson AV, Ackerley DF.

Biochemistry. 2019 Sep 3;58(35):3700-3710. doi: 10.1021/acs.biochem.9b00376. Epub 2019 Aug 20.

PMID:
31403283
2.

Targeting growth hormone function: strategies and therapeutic applications.

Lu M, Flanagan JU, Langley RJ, Hay MP, Perry JK.

Signal Transduct Target Ther. 2019 Feb 8;4:3. doi: 10.1038/s41392-019-0036-y. eCollection 2019. Review.

3.

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

Gamage SA, Spicer JA, Tsang KY, O'Connor PD, Flanagan JU, Lee WJ, Dickson JMJ, Shepherd PR, Denny WA, Rewcastle GW.

Chem Asian J. 2019 Apr 15;14(8):1249-1261. doi: 10.1002/asia.201801762. Epub 2019 Mar 12.

PMID:
30714356
4.

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

Heitz SD, Hamelin DJ, Hoffmann RM, Greenberg N, Salloum G, Erami Z, Khalil BD, Shymanets A, Steidle EA, Gong GQ, Nürnberg B, Burke JE, Flanagan JU, Bresnick AR, Backer JM.

J Biol Chem. 2019 Mar 22;294(12):4621-4633. doi: 10.1074/jbc.RA118.006032. Epub 2019 Jan 18.

PMID:
30659094
5.

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

Irvine WA, Flanagan JU, Allison JR.

Structure. 2019 Feb 5;27(2):371-380.e3. doi: 10.1016/j.str.2018.10.014. Epub 2018 Dec 6.

PMID:
30528597
6.

Identification, structure modification, and characterization of potential small-molecule SGK3 inhibitors with novel scaffolds.

Gong GQ, Wang K, Dai XC, Zhou Y, Basnet R, Chen Y, Yang DH, Lee WJ, Buchanan CM, Flanagan JU, Shepherd PR, Chen Y, Wang MW.

Acta Pharmacol Sin. 2018 Dec;39(12):1902-1912. doi: 10.1038/s41401-018-0087-6. Epub 2018 Jul 23.

PMID:
30038340
7.

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

Wang J, Gong GQ, Zhou Y, Lee WJ, Buchanan CM, Denny WA, Rewcastle GW, Kendall JD, Dickson JMJ, Flanagan JU, Shepherd PR, Yang DH, Wang MW.

Acta Pharmacol Sin. 2018 Nov;39(11):1816-1822. doi: 10.1038/s41401-018-0057-z. Epub 2018 Jul 10.

PMID:
29991713
8.

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.

Stevenson RJ, Azimi I, Flanagan JU, Inserra M, Vetter I, Monteith GR, Denny WA.

Bioorg Med Chem. 2018 Jul 23;26(12):3406-3413. doi: 10.1016/j.bmc.2018.05.012. Epub 2018 May 9.

PMID:
29776832
9.

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

Gamage SA, Giddens AC, Tsang KY, Flanagan JU, Kendall JD, Lee WJ, Baguley BC, Buchanan CM, Jamieson SMF, Shepherd PR, Denny WA, Rewcastle GW.

Bioorg Med Chem. 2017 Oct 15;25(20):5859-5874. doi: 10.1016/j.bmc.2017.09.025. Epub 2017 Sep 20.

PMID:
28958845
10.

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

Gong GQ, Kendall JD, Dickson JMJ, Rewcastle GW, Buchanan CM, Denny WA, Shepherd PR, Flanagan JU.

Biochem J. 2017 Jun 26;474(13):2261-2276. doi: 10.1042/BCJ20161098.

PMID:
28526744
11.

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

Karunasinghe N, Masters J, Flanagan JU, Ferguson LR.

Curr Cancer Drug Targets. 2017;17(7):603-616. doi: 10.2174/1568009617666170330115722.

PMID:
28359237
12.

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

Green TN, Hamilton JR, Morel-Kopp MC, Zheng Z, Chen TT, Hearn JI, Sun PP, Flanagan JU, Young D, Barber PA, During MJ, Ward CM, Kalev-Zylinska ML.

Platelets. 2017 Dec;28(8):799-811. doi: 10.1080/09537104.2017.1280149. Epub 2017 Feb 21.

PMID:
28277064
13.

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

Copp JN, Mowday AM, Williams EM, Guise CP, Ashoorzadeh A, Sharrock AV, Flanagan JU, Smaill JB, Patterson AV, Ackerley DF.

Cell Chem Biol. 2017 Mar 16;24(3):391-403. doi: 10.1016/j.chembiol.2017.02.005. Epub 2017 Mar 2.

14.

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

Tomek P, Palmer BD, Flanagan JU, Sun C, Raven EL, Ching LM.

Eur J Med Chem. 2017 Jan 27;126:983-996. doi: 10.1016/j.ejmech.2016.12.029. Epub 2016 Dec 13.

PMID:
28011425
15.

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.

Azimi I, Flanagan JU, Stevenson RJ, Inserra M, Vetter I, Monteith GR, Denny WA.

Bioorg Med Chem. 2017 Jan 1;25(1):440-449. doi: 10.1016/j.bmc.2016.11.007. Epub 2016 Nov 7.

PMID:
27856238
16.

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

Mowday AM, Ashoorzadeh A, Williams EM, Copp JN, Silva S, Bull MR, Abbattista MR, Anderson RF, Flanagan JU, Guise CP, Ackerley DF, Smaill JB, Patterson AV.

Biochem Pharmacol. 2016 Sep 15;116:176-87. doi: 10.1016/j.bcp.2016.07.015. Epub 2016 Jul 22.

PMID:
27453434
17.

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

Glass M, Govindpani K, Furkert DP, Hurst DP, Reggio PH, Flanagan JU.

Trends Pharmacol Sci. 2016 May;37(5):353-363. doi: 10.1016/j.tips.2016.01.010. Epub 2016 Feb 22. Review.

PMID:
26917061
18.

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

Yosaatmadja Y, Silva S, Dickson JM, Patterson AV, Smaill JB, Flanagan JU, McKeage MJ, Squire CJ.

J Struct Biol. 2015 Dec;192(3):539-544. doi: 10.1016/j.jsb.2015.10.018. Epub 2015 Nov 2.

PMID:
26522274
19.

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.

Tomek P, Palmer BD, Kendall JD, Flanagan JU, Ching LM.

Biochim Biophys Acta. 2015 Sep;1850(9):1772-80. doi: 10.1016/j.bbagen.2015.04.007. Epub 2015 Apr 20.

PMID:
25907332
20.

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.

Marshall AJ, Lill CL, Chao M, Kolekar SV, Lee WJ, Marshall ES, Baguley BC, Shepherd PR, Denny WA, Flanagan JU, Rewcastle GW.

Bioorg Med Chem. 2015 Jul 1;23(13):3796-808. doi: 10.1016/j.bmc.2015.03.073. Epub 2015 Apr 4.

PMID:
25890698
21.

Evidence That GRIN2A Mutations in Melanoma Correlate with Decreased Survival.

D'mello SA, Flanagan JU, Green TN, Leung EY, Askarian-Amiri ME, Joseph WR, McCrystal MR, Isaacs RJ, Shaw JH, Furneaux CE, During MJ, Finlay GJ, Baguley BC, Kalev-Zylinska ML.

Front Oncol. 2014 Jan 13;3:333. doi: 10.3389/fonc.2013.00333. eCollection 2014 Jan 13.

22.

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

Flanagan JU, Shepherd PR.

Biochem Soc Trans. 2014 Feb;42(1):120-4. doi: 10.1042/BST20130255. Review.

PMID:
24450638
23.

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

Flanagan JU, Atwell GJ, Heinrich DM, Brooke DG, Silva S, Rigoreau LJ, Trivier E, Turnbull AP, Raynham T, Jamieson SM, Denny WA.

Bioorg Med Chem. 2014 Feb 1;22(3):967-77. doi: 10.1016/j.bmc.2013.12.050. Epub 2014 Jan 2.

PMID:
24411201
24.

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).

Brooke DG, van Dam EM, Watts CK, Khoury A, Dziadek MA, Brooks H, Graham LJ, Flanagan JU, Denny WA.

Bioorg Med Chem. 2014 Feb 1;22(3):1029-39. doi: 10.1016/j.bmc.2013.12.041. Epub 2013 Dec 30.

PMID:
24398380
25.

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

Bonnet M, Flanagan JU, Chan DA, Giaccia AJ, Hay MP.

Bioorg Med Chem. 2014 Jan 15;22(2):711-20. doi: 10.1016/j.bmc.2013.12.028. Epub 2013 Dec 20.

26.

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

Fung SP, Wang H, Tomek P, Squire CJ, Flanagan JU, Palmer BD, Bridewell DJ, Tijono SM, Jamie JF, Ching LM.

Bioorg Med Chem. 2013 Dec 15;21(24):7595-603. doi: 10.1016/j.bmc.2013.10.037. Epub 2013 Nov 6.

PMID:
24262887
27.

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).

Rewcastle GW, Gamage SA, Flanagan JU, Kendall JD, Denny WA, Baguley BC, Buchanan CM, Chao M, Kestell P, Kolekar S, Lee WJ, Lill CL, Malik A, Singh R, Jamieson SM, Shepherd PR.

Eur J Med Chem. 2013 Jun;64:137-47. doi: 10.1016/j.ejmech.2013.03.038. Epub 2013 Apr 6.

PMID:
23644197
28.

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.

Heinrich DM, Flanagan JU, Jamieson SM, Silva S, Rigoreau LJ, Trivier E, Raynham T, Turnbull AP, Denny WA.

Eur J Med Chem. 2013 Apr;62:738-44. doi: 10.1016/j.ejmech.2013.01.047. Epub 2013 Feb 9.

PMID:
23454516
29.

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

Tomek P, Palmer BD, Flanagan JU, Fung SP, Bridewell DJ, Jamie JF, Ching LM.

Anal Bioanal Chem. 2013 Mar;405(8):2515-24. doi: 10.1007/s00216-012-6650-y. Epub 2013 Jan 12.

PMID:
23314482
30.

Crystal structures of three classes of non-steroidal anti-inflammatory drugs in complex with aldo-keto reductase 1C3.

Flanagan JU, Yosaatmadja Y, Teague RM, Chai MZ, Turnbull AP, Squire CJ.

PLoS One. 2012;7(8):e43965. doi: 10.1371/journal.pone.0043965. Epub 2012 Aug 28.

31.

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

Jamieson SM, Brooke DG, Heinrich D, Atwell GJ, Silva S, Hamilton EJ, Turnbull AP, Rigoreau LJ, Trivier E, Soudy C, Samlal SS, Owen PJ, Schroeder E, Raynham T, Flanagan JU, Denny WA.

J Med Chem. 2012 Sep 13;55(17):7746-58. doi: 10.1021/jm3007867. Epub 2012 Aug 21.

PMID:
22877157
32.

Structure of AKR1C3 with 3-phenoxybenzoic acid bound.

Jackson VJ, Yosaatmadja Y, Flanagan JU, Squire CJ.

Acta Crystallogr Sect F Struct Biol Cryst Commun. 2012 Apr 1;68(Pt 4):409-13. doi: 10.1107/S1744309112009049. Epub 2012 Mar 27.

33.

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

Kendall JD, Giddens AC, Tsang KY, Frédérick R, Marshall ES, Singh R, Lill CL, Lee WJ, Kolekar S, Chao M, Malik A, Yu S, Chaussade C, Buchanan C, Rewcastle GW, Baguley BC, Flanagan JU, Jamieson SM, Denny WA, Shepherd PR.

Bioorg Med Chem. 2012 Jan 1;20(1):58-68. doi: 10.1016/j.bmc.2011.11.031. Epub 2011 Nov 25.

PMID:
22177407
34.

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

Kendall JD, O'Connor PD, Marshall AJ, Frédérick R, Marshall ES, Lill CL, Lee WJ, Kolekar S, Chao M, Malik A, Yu S, Chaussade C, Buchanan C, Rewcastle GW, Baguley BC, Flanagan JU, Jamieson SM, Denny WA, Shepherd PR.

Bioorg Med Chem. 2012 Jan 1;20(1):69-85. doi: 10.1016/j.bmc.2011.11.029. Epub 2011 Nov 25.

PMID:
22177405
35.

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

Buchanan CM, Shih JH, Astin JW, Rewcastle GW, Flanagan JU, Crosier PS, Shepherd PR.

Clin Sci (Lond). 2012 May 1;122(10):449-57. doi: 10.1042/CS20110412.

PMID:
22142330
36.

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).

Rewcastle GW, Gamage SA, Flanagan JU, Frederick R, Denny WA, Baguley BC, Kestell P, Singh R, Kendall JD, Marshall ES, Lill CL, Lee WJ, Kolekar S, Buchanan CM, Jamieson SM, Shepherd PR.

J Med Chem. 2011 Oct 27;54(20):7105-26. doi: 10.1021/jm200688y. Epub 2011 Sep 27.

PMID:
21882832
37.

Targeting GLUT1 and the Warburg effect in renal cell carcinoma by chemical synthetic lethality.

Chan DA, Sutphin PD, Nguyen P, Turcotte S, Lai EW, Banh A, Reynolds GE, Chi JT, Wu J, Solow-Cordero DE, Bonnet M, Flanagan JU, Bouley DM, Graves EE, Denny WA, Hay MP, Giaccia AJ.

Sci Transl Med. 2011 Aug 3;3(94):94ra70. doi: 10.1126/scitranslmed.3002394.

38.

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

Archbold JK, Flanagan JU, Watkins HA, Gingell JJ, Hay DL.

Trends Pharmacol Sci. 2011 Oct;32(10):591-600. doi: 10.1016/j.tips.2011.05.007. Epub 2011 Jun 29. Review.

PMID:
21722971
39.

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

Jamieson S, Flanagan JU, Kolekar S, Buchanan C, Kendall JD, Lee WJ, Rewcastle GW, Denny WA, Singh R, Dickson J, Baguley BC, Shepherd PR.

Biochem J. 2011 Aug 15;438(1):53-62. doi: 10.1042/BJ20110502.

40.

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

Bonnet M, Flanagan JU, Chan DA, Lai EW, Nguyen P, Giaccia AJ, Hay MP.

Bioorg Med Chem. 2011 Jun 1;19(11):3347-56. doi: 10.1016/j.bmc.2011.04.042. Epub 2011 Apr 24.

41.

Sigma-class glutathione transferases.

Flanagan JU, Smythe ML.

Drug Metab Rev. 2011 May;43(2):194-214. doi: 10.3109/03602532.2011.560157. Epub 2011 Mar 22. Review.

PMID:
21425928
42.

Development and characterization of new inhibitors of the human and mouse hematopoietic prostaglandin D(2) synthases.

Christ AN, Labzin L, Bourne GT, Fukunishi H, Weber JE, Sweet MJ, Smythe ML, Flanagan JU.

J Med Chem. 2010 Aug 12;53(15):5536-48. doi: 10.1021/jm100194a.

PMID:
20684598
43.

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

Hay MP, Turcotte S, Flanagan JU, Bonnet M, Chan DA, Sutphin PD, Nguyen P, Giaccia AJ, Denny WA.

J Med Chem. 2010 Jan 28;53(2):787-97. doi: 10.1021/jm901457w.

44.

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

Weber JE, Oakley AJ, Christ AN, Clark AG, Hayes JD, Hall R, Hume DA, Board PG, Smythe ML, Flanagan JU.

Eur J Med Chem. 2010 Feb;45(2):447-54. doi: 10.1016/j.ejmech.2009.10.025. Epub 2009 Oct 23.

PMID:
19939518
45.

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

Hadler KS, Huber T, Cassady AI, Weber J, Robinson J, Burrows A, Kelly G, Guddat LW, Hume DA, Schenk G, Flanagan JU.

BMC Res Notes. 2008 Sep 4;1:78. doi: 10.1186/1756-0500-1-78.

46.

Structural evolution of the ABC transporter subfamily B.

Flanagan JU, Huber T.

Evol Bioinform Online. 2007 Nov 8;3:309-16.

47.

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

Flanagan JU, Cassady AI, Schenk G, Guddat LW, Hume DA.

Gene. 2006 Aug 1;377:12-20. Epub 2006 Apr 5.

PMID:
16793224
48.

Modelling the structure of latexin-carboxypeptidase A complex based on chemical cross-linking and molecular docking.

Mouradov D, Craven A, Forwood JK, Flanagan JU, García-Castellanos R, Gomis-Rüth FX, Hume DA, Martin JL, Kobe B, Huber T.

Protein Eng Des Sel. 2006 Jan;19(1):9-16. Epub 2005 Oct 25.

PMID:
16249216
49.

Why is quinidine an inhibitor of cytochrome P450 2D6? The role of key active-site residues in quinidine binding.

McLaughlin LA, Paine MJ, Kemp CA, Maréchal JD, Flanagan JU, Ward CJ, Sutcliffe MJ, Roberts GC, Wolf CR.

J Biol Chem. 2005 Nov 18;280(46):38617-24. Epub 2005 Sep 14.

50.

Glutathione transferases.

Hayes JD, Flanagan JU, Jowsey IR.

Annu Rev Pharmacol Toxicol. 2005;45:51-88. Review.

PMID:
15822171

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