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

Trevarton A, Zhou Y, Yang D, Rewcastle GW, Flanagan JU, Braithwaite A, Shepherd PR, Print CG, Wang MW, Lasham A.

Acta Pharm Sin B. 2019 Sep;9(5):997-1007. doi: 10.1016/j.apsb.2018.12.011. Epub 2019 Jan 3.


For Better or Worse: The Potential for Dose Limiting the On-Target Toxicity of PI 3-Kinase Inhibitors.

Buchanan CM, Lee KL, Shepherd PR.

Biomolecules. 2019 Aug 22;9(9). pii: E402. doi: 10.3390/biom9090402. Review.


The CSF1 receptor inhibitor pexidartinib (PLX3397) reduces tissue macrophage levels without affecting glucose homeostasis in mice.

Merry TL, Brooks AES, Masson SW, Adams SE, Jaiswal JK, Jamieson SMF, Shepherd PR.

Int J Obes (Lond). 2020 Jan;44(1):245-253. doi: 10.1038/s41366-019-0355-7. Epub 2019 Mar 29.


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

Giddens AC, Gamage SA, Kendall JD, Lee WJ, Baguley BC, Buchanan CM, Jamieson SMF, Dickson JMJ, Shepherd PR, Denny WA, Rewcastle GW.

Bioorg Med Chem. 2019 Apr 15;27(8):1529-1545. doi: 10.1016/j.bmc.2019.02.050. Epub 2019 Feb 25.


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.


Macrophages enhance Vegfa-driven angiogenesis in an embryonic zebrafish tumour xenograft model.

Britto DD, Wyroba B, Chen W, Lockwood RA, Tran KB, Shepherd PR, Hall CJ, Crosier KE, Crosier PS, Astin JW.

Dis Model Mech. 2018 Nov 29;11(12). pii: dmm035998. doi: 10.1242/dmm.035998.


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.


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.


Feeding and GLP-1 receptor activation stabilize β-catenin in specific hypothalamic nuclei in male rats.

McEwen HJL, Cognard E, Ladyman SR, Khant-Aung Z, Tups A, Shepherd PR, Grattan DR.

J Neuroendocrinol. 2018 May 11:e12607. doi: 10.1111/jne.12607. [Epub ahead of print]


Discordant association of the CREBRF rs373863828 A allele with increased BMI and protection from type 2 diabetes in Māori and Pacific (Polynesian) people living in Aotearoa/New Zealand.

Krishnan M, Major TJ, Topless RK, Dewes O, Yu L, Thompson JMD, McCowan L, de Zoysa J, Stamp LK, Dalbeth N, Harré Hindmarsh J, Rapana N, Deka R, Eng WWH, Weeks DE, Minster RL, McGarvey ST, Viali S, Naseri T, Sefuiva Reupena M, Wilcox P, Grattan D, Shepherd PR, Shelling AN, Murphy R, Merriman TR.

Diabetologia. 2018 Jul;61(7):1603-1613. doi: 10.1007/s00125-018-4623-1. Epub 2018 May 2.


Identification of Pik3ca Mutation as a Genetic Driver of Prostate Cancer That Cooperates with Pten Loss to Accelerate Progression and Castration-Resistant Growth.

Pearson HB, Li J, Meniel VS, Fennell CM, Waring P, Montgomery KG, Rebello RJ, Macpherson AA, Koushyar S, Furic L, Cullinane C, Clarkson RW, Smalley MJ, Simpson KJ, Phesse TJ, Shepherd PR, Humbert PO, Sansom OJ, Phillips WA.

Cancer Discov. 2018 Jun;8(6):764-779. doi: 10.1158/2159-8290.CD-17-0867. Epub 2018 Mar 26.


β-catenin is important for the development of an insulin responsive pool of GLUT4 glucose transporters in 3T3-L1 adipocytes.

Dissanayake WC, Sorrenson B, Cognard E, Hughes WE, Shepherd PR.

Exp Cell Res. 2018 May 1;366(1):49-54. doi: 10.1016/j.yexcr.2018.03.011. Epub 2018 Mar 11.


Re: "Widespread prevalence of a CREBRF variant among Māori and Pacific children is associated with weight and height in early childhood".

Major TJ, Krishnan M, Topless RK, Dewes O, Thompson J, Zoysa J, Stamp LK, Dalbeth N, Deka R, Weeks DE, Minster RL, Wilcox P, Grattan D, Shepherd PR, Shelling AN, Murphy R, Merriman TR.

Int J Obes (Lond). 2018 Jul;42(7):1389-1391. doi: 10.1038/s41366-018-0025-1. Epub 2018 Mar 6. No abstract available.


The role of adherens junction proteins in the regulation of insulin secretion.

Dissanayake WC, Sorrenson B, Shepherd PR.

Biosci Rep. 2018 Mar 21;38(2). pii: BSR20170989. doi: 10.1042/BSR20170989. Print 2018 Apr 27. Review.


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.


Biological characterization of SN32976, a selective inhibitor of PI3K and mTOR with preferential activity to PI3Kα, in comparison to established pan PI3K inhibitors.

Rewcastle GW, Kolekar S, Buchanan CM, Gamage SA, Giddens AC, Tsang KY, Kendall JD, Singh R, Lee WJ, Smith GC, Han W, Matthews DJ, Denny WA, Shepherd PR, Jamieson SMF.

Oncotarget. 2017 Jul 18;8(29):47725-47740. doi: 10.18632/oncotarget.17730.


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.


Niclosamide reduces glucagon sensitivity via hepatic PKA inhibition in obese mice: Implications for glucose metabolism improvements in type 2 diabetes.

Chowdhury MK, Turner N, Bentley NL, Das A, Wu LE, Richani D, Bustamante S, Gilchrist RB, Morris MJ, Shepherd PR, Smith GC.

Sci Rep. 2017 Jan 5;7:40159. doi: 10.1038/srep40159.


Novel pyrazolo[1,5-a]pyridines with improved aqueous solubility as p110α-selective PI3 kinase inhibitors.

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

Bioorg Med Chem Lett. 2017 Jan 15;27(2):187-190. doi: 10.1016/j.bmcl.2016.11.078. Epub 2016 Nov 25.


A Critical Role for β-Catenin in Modulating Levels of Insulin Secretion from β-Cells by Regulating Actin Cytoskeleton and Insulin Vesicle Localization.

Sorrenson B, Cognard E, Lee KL, Dissanayake WC, Fu Y, Han W, Hughes WE, Shepherd PR.

J Biol Chem. 2016 Dec 9;291(50):25888-25900. Epub 2016 Oct 24.


NRAS and EPHB6 mutation rates differ in metastatic melanomas of patients in the North Island versus South Island of New Zealand.

Jones AM, Ferguson P, Gardner J, Rooker S, Sutton T, Ahn A, Chatterjee A, Bickley VM, Sarwar M, Emanuel P, Kenwright D, Shepherd PR, Eccles MR.

Oncotarget. 2016 Jul 5;7(27):41017-41030. doi: 10.18632/oncotarget.9351.


Targeted inhibition of dominant PI3-kinase catalytic isoforms increase expression of stem cell genes in glioblastoma cancer stem cell models.

Jones NM, Rowe MR, Shepherd PR, McConnell MJ.

Int J Oncol. 2016 Jul;49(1):207-16. doi: 10.3892/ijo.2016.3510. Epub 2016 May 9.


Niclosamide blocks glucagon phosphorylation of Ser552 on β-catenin in primary rat hepatocytes via PKA signalling.

Chowdhury MK, Wu LE, Coleman JL, Smith NJ, Morris MJ, Shepherd PR, Smith GC.

Biochem J. 2016 May 1;473(9):1247-55. doi: 10.1042/BCJ20160121. Epub 2016 Mar 10.


Inhibitors of pan-PI3K Signaling Synergize with BRAF or MEK Inhibitors to Prevent BRAF-Mutant Melanoma Cell Growth.

Sweetlove M, Wrightson E, Kolekar S, Rewcastle GW, Baguley BC, Shepherd PR, Jamieson SM.

Front Oncol. 2015 Jun 16;5:135. doi: 10.3389/fonc.2015.00135. eCollection 2015.


Glucagon phosphorylates serine 552 of β-catenin leading to increased expression of cyclin D1 and c-Myc in the isolated rat liver.

Chowdhury MK, Montgomery MK, Morris MJ, Cognard E, Shepherd PR, Smith GC.

Arch Physiol Biochem. 2015;121(3):88-96. doi: 10.3109/13813455.2015.1048693. Epub 2015 Jul 1.


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.


Biochemical Journal strengthens links in Asia.

Shepherd PR.

Biochem J. 2014 Nov 15;464(1):1. doi: 10.1042/BJ20140874. No abstract available.


Clozapine directly increases insulin and glucagon secretion from islets: implications for impairment of glucose tolerance.

Smith GC, Zhang ZY, Mulvey T, Petersen N, Lach S, Xiu P, Phillips A, Han W, Wang MW, Shepherd PR.

Schizophr Res. 2014 Aug;157(1-3):128-33. doi: 10.1016/j.schres.2014.05.003. Epub 2014 Jun 3.


The activation of the Akt/PKB signalling pathway in the brains of clozapine-exposed rats is linked to hyperinsulinemia and not a direct drug effect.

Smith GC, McEwen H, Steinberg JD, Shepherd PR.

Psychopharmacology (Berl). 2014 Dec;231(23):4553-60. doi: 10.1007/s00213-014-3608-0. Epub 2014 May 7.


Targeting class IA PI3K isoforms selectively impairs cell growth, survival, and migration in glioblastoma.

Höland K, Boller D, Hagel C, Dolski S, Treszl A, Pardo OE, Cwiek P, Salm F, Leni Z, Shepherd PR, Styp-Rekowska B, Djonov V, von Bueren AO, Frei K, Arcaro A.

PLoS One. 2014 Apr 9;9(4):e94132. doi: 10.1371/journal.pone.0094132. eCollection 2014.


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.


Cholesterol-induced mammary tumorigenesis is enhanced by adiponectin deficiency: role of LDL receptor upregulation.

Liu J, Xu A, Lam KS, Wong NS, Chen J, Shepherd PR, Wang Y.

Oncotarget. 2013 Oct;4(10):1804-18.


Hypothalamic WNT signalling is impaired during obesity and reinstated by leptin treatment in male mice.

Benzler J, Andrews ZB, Pracht C, Stöhr S, Shepherd PR, Grattan DR, Tups A.

Endocrinology. 2013 Dec;154(12):4737-45. doi: 10.1210/en.2013-1746. Epub 2013 Oct 8.


Enzyme activity effects of N-terminal His-tag attached to catalytic sub-unit of phosphoinositide-3-kinase.

Dickson JM, Lee WJ, Shepherd PR, Buchanan CM.

Biosci Rep. 2013 Nov 5;33(6). pii: e00079. doi: 10.1042/BSR20130075.


Oncogenic mutations of p110α isoform of PI 3-kinase upregulate its protein kinase activity.

Buchanan CM, Dickson JM, Lee WJ, Guthridge MA, Kendall JD, Shepherd PR.

PLoS One. 2013 Aug 1;8(8):e71337. doi: 10.1371/journal.pone.0071337. Print 2013.


Phosphatidylinositol 3-phosphate 5-kinase (PIKfyve) is an AMPK target participating in contraction-stimulated glucose uptake in skeletal muscle.

Liu Y, Lai YC, Hill EV, Tyteca D, Carpentier S, Ingvaldsen A, Vertommen D, Lantier L, Foretz M, Dequiedt F, Courtoy PJ, Erneux C, Viollet B, Shepherd PR, Tavaré JM, Jensen J, Rider MH.

Biochem J. 2013 Oct 15;455(2):195-206. doi: 10.1042/BJ20130644.


Extended treatment with selective phosphatidylinositol 3-kinase and mTOR inhibitors has effects on metabolism, growth, behaviour and bone strength.

Smith GC, Ong WK, Costa JL, Watson M, Cornish J, Grey A, Gamble GD, Dickinson M, Leung S, Rewcastle GW, Han W, Shepherd PR.

FEBS J. 2013 Nov;280(21):5337-49. doi: 10.1111/febs.12428. Epub 2013 Aug 12.


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.


Protein kinase activity of phosphoinositide 3-kinase regulates cytokine-dependent cell survival.

Thomas D, Powell JA, Green BD, Barry EF, Ma Y, Woodcock J, Fitter S, Zannettino AC, Pitson SM, Hughes TP, Lopez AF, Shepherd PR, Wei AH, Ekert PG, Guthridge MA.

PLoS Biol. 2013;11(3):e1001515. doi: 10.1371/journal.pbio.1001515. Epub 2013 Mar 19.


G protein-coupled receptor-mediated activation of p110β by Gβγ is required for cellular transformation and invasiveness.

Dbouk HA, Vadas O, Shymanets A, Burke JE, Salamon RS, Khalil BD, Barrett MO, Waldo GL, Surve C, Hsueh C, Perisic O, Harteneck C, Shepherd PR, Harden TK, Smrcka AV, Taussig R, Bresnick AR, Nürnberg B, Williams RL, Backer JM.

Sci Signal. 2012 Dec 4;5(253):ra89. doi: 10.1126/scisignal.2003264.


Identification of a pathway by which glucose regulates β-catenin signalling via the cAMP/protein kinase A pathway in β-cell models.

Cognard E, Dargaville CG, Hay DL, Shepherd PR.

Biochem J. 2013 Feb 1;449(3):803-11. doi: 10.1042/BJ20121454.


Hypothalamic glycogen synthase kinase 3β has a central role in the regulation of food intake and glucose metabolism.

Benzler J, Ganjam GK, Krüger M, Pinkenburg O, Kutschke M, Stöhr S, Steger J, Koch CE, Ölkrug R, Schwartz MW, Shepherd PR, Grattan DR, Tups A.

Biochem J. 2012 Oct 1;447(1):175-84. doi: 10.1042/BJ20120834.


Beta-testing of PI3-kinase inhibitors: is beta better?

Shepherd PR, Denny WA.

Cancer Discov. 2012 May;2(5):393-4. doi: 10.1158/2159-8290.CD-12-0122.


Definition of the binding mode of a new class of phosphoinositide 3-kinase α-selective inhibitors using in vitro mutagenesis of non-conserved amino acids and kinetic analysis.

Zheng Z, Amran SI, Zhu J, Schmidt-Kittler O, Kinzler KW, Vogelstein B, Shepherd PR, Thompson PE, Jennings IG.

Biochem J. 2012 Jun 15;444(3):529-35. doi: 10.1042/BJ20120499.


Concurrent resistance and aerobic exercise stimulates both myofibrillar and mitochondrial protein synthesis in sedentary middle-aged men.

Donges CE, Burd NA, Duffield R, Smith GC, West DW, Short MJ, Mackenzie R, Plank LD, Shepherd PR, Phillips SM, Edge JA.

J Appl Physiol (1985). 2012 Jun;112(12):1992-2001. doi: 10.1152/japplphysiol.00166.2012. Epub 2012 Apr 5.


Comparison of growth factor signalling pathway utilisation in cultured normal melanocytes and melanoma cell lines.

Kim JE, Stones C, Joseph WR, Leung E, Finlay GJ, Shelling AN, Phillips WA, Shepherd PR, Baguley BC.

BMC Cancer. 2012 Apr 4;12:141. doi: 10.1186/1471-2407-12-141.


IκB kinase β (IKKβ) does not mediate feedback inhibition of the insulin signalling cascade.

Lancaster GI, Skiba B, Yang C, Nicholls HT, Langley KG, Chan MH, Bruce CR, Rewcastle GW, Shepherd PR, Karin M, Febbraio MA.

Biochem J. 2012 Mar 15;442(3):723-32. doi: 10.1042/BJ20112037. Erratum in: Biochem J. 2013 May 15;452(1):171.


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.


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.


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.


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