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Items: 1 to 50 of 156

1.

Correction: Synthesis of highly substituted 2-spiropiperidines.

Griggs SD, Thompson N, Tape DT, Fabre M, Clarke PA.

Org Biomol Chem. 2018 Aug 10. doi: 10.1039/c8ob90117a. [Epub ahead of print]

PMID:
30095852
2.

Synthesis of highly substituted 2-spiropiperidines.

Griggs SD, Thompson N, Tape DT, Fabre M, Clarke PA.

Org Biomol Chem. 2018 Aug 1. doi: 10.1039/c8ob01272e. [Epub ahead of print] Erratum in: Org Biomol Chem. 2018 Aug 10;:.

PMID:
30067258
3.

Strategies for the synthesis of spiropiperidines - a review of the last 10 years.

Griggs SD, Tape DT, Clarke PA.

Org Biomol Chem. 2018 Jul 11. doi: 10.1039/c8ob01271g. [Epub ahead of print] Review.

PMID:
29993083
4.

Water-soluble substituted chitosan derivatives as technology platform for inhalation delivery of siRNA.

Capel V, Vllasaliu D, Watts P, Clarke PA, Luxton D, Grabowska AM, Mantovani G, Stolnik S.

Drug Deliv. 2018 Nov;25(1):644-653. doi: 10.1080/10717544.2018.1440668.

PMID:
29493294
5.

Patient-derived organoids model treatment response of metastatic gastrointestinal cancers.

Vlachogiannis G, Hedayat S, Vatsiou A, Jamin Y, Fernández-Mateos J, Khan K, Lampis A, Eason K, Huntingford I, Burke R, Rata M, Koh DM, Tunariu N, Collins D, Hulkki-Wilson S, Ragulan C, Spiteri I, Moorcraft SY, Chau I, Rao S, Watkins D, Fotiadis N, Bali M, Darvish-Damavandi M, Lote H, Eltahir Z, Smyth EC, Begum R, Clarke PA, Hahne JC, Dowsett M, de Bono J, Workman P, Sadanandam A, Fassan M, Sansom OJ, Eccles S, Starling N, Braconi C, Sottoriva A, Robinson SP, Cunningham D, Valeri N.

Science. 2018 Feb 23;359(6378):920-926. doi: 10.1126/science.aao2774.

PMID:
29472484
6.

Oncogenic RAC1 and NRAS drive resistance to endoplasmic reticulum stress through MEK/ERK signalling.

Bright MD, Clarke PA, Workman P, Davies FE.

Cell Signal. 2018 Apr;44:127-137. doi: 10.1016/j.cellsig.2018.01.004. Epub 2018 Jan 9.

7.

Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766).

Chessum NEA, Sharp SY, Caldwell JJ, Pasqua AE, Wilding B, Colombano G, Collins I, Ozer B, Richards M, Rowlands M, Stubbs M, Burke R, McAndrew PC, Clarke PA, Workman P, Cheeseman MD, Jones K.

J Med Chem. 2018 Feb 8;61(3):918-933. doi: 10.1021/acs.jmedchem.7b01406. Epub 2018 Jan 5.

8.

Molecular profiling and combinatorial activity of CCT068127: a potent CDK2 and CDK9 inhibitor.

Whittaker SR, Barlow C, Martin MP, Mancusi C, Wagner S, Self A, Barrie E, Te Poele R, Sharp S, Brown N, Wilson S, Jackson W, Fischer PM, Clarke PA, Walton MI, McDonald E, Blagg J, Noble M, Garrett MD, Workman P.

Mol Oncol. 2018 Mar;12(3):287-304. doi: 10.1002/1878-0261.12148. Epub 2018 Jan 28.

9.

Prebiotic synthesis of 2-deoxy-d-ribose from interstellar building blocks promoted by amino esters or amino nitriles.

Steer AM, Bia N, Smith DK, Clarke PA.

Chem Commun (Camb). 2017 Sep 25;53(75):10362-10365. doi: 10.1039/c7cc06083a. Epub 2017 Sep 8.

PMID:
28884758
10.

In vitro nuclear magnetic resonance spectroscopy metabolic biomarkers for the combination of temozolomide with PI3K inhibition in paediatric glioblastoma cells.

Al-Saffar NMS, Agliano A, Marshall LV, Jackson LE, Balarajah G, Sidhu J, Clarke PA, Jones C, Workman P, Pearson ADJ, Leach MO.

PLoS One. 2017 Jul 13;12(7):e0180263. doi: 10.1371/journal.pone.0180263. eCollection 2017.

11.

Pediatric and adult glioblastoma radiosensitization induced by PI3K/mTOR inhibition causes early metabolic alterations detected by nuclear magnetic resonance spectroscopy.

Agliano A, Balarajah G, Ciobota DM, Sidhu J, Clarke PA, Jones C, Workman P, Leach MO, Al-Saffar NMS.

Oncotarget. 2017 Jul 18;8(29):47969-47983. doi: 10.18632/oncotarget.18206.

12.

A Two-Step Synthesis of 2-Spiropiperidines.

Griggs SD, Thompson N, Tape DT, Fabre M, Clarke PA.

Chemistry. 2017 Jul 12;23(39):9262-9265. doi: 10.1002/chem.201702467. Epub 2017 Jun 22.

PMID:
28561323
13.

The stereodivergent formation of 2,6-cis and 2,6-trans-tetrahydropyrans: experimental and computational investigation of the mechanism of a thioester oxy-Michael cyclization.

Ermanis K, Hsiao YT, Kaya U, Jeuken A, Clarke PA.

Chem Sci. 2017 Jan 1;8(1):482-490. doi: 10.1039/c6sc03478k. Epub 2016 Aug 30.

14.

Overexpression of EZH2 in multiple myeloma is associated with poor prognosis and dysregulation of cell cycle control.

Pawlyn C, Bright MD, Buros AF, Stein CK, Walters Z, Aronson LI, Mirabella F, Jones JR, Kaiser MF, Walker BA, Jackson GH, Clarke PA, Bergsagel PL, Workman P, Chesi M, Morgan GJ, Davies FE.

Blood Cancer J. 2017 Mar 31;7(3):e549. doi: 10.1038/bcj.2017.27.

15.

Inhibitors of cyclin-dependent kinases as cancer therapeutics.

Whittaker SR, Mallinger A, Workman P, Clarke PA.

Pharmacol Ther. 2017 May;173:83-105. doi: 10.1016/j.pharmthera.2017.02.008. Epub 2017 Feb 5. Review.

PMID:
28174091
16.

Assessing the mechanism and therapeutic potential of modulators of the human Mediator complex-associated protein kinases.

Clarke PA, Ortiz-Ruiz MJ, TePoele R, Adeniji-Popoola O, Box G, Court W, Czasch S, El Bawab S, Esdar C, Ewan K, Gowan S, De Haven Brandon A, Hewitt P, Hobbs SM, Kaufmann W, Mallinger A, Raynaud F, Roe T, Rohdich F, Schiemann K, Simon S, Schneider R, Valenti M, Weigt S, Blagg J, Blaukat A, Dale TC, Eccles SA, Hecht S, Urbahns K, Workman P, Wienke D.

Elife. 2016 Dec 9;5. pii: e20722. doi: 10.7554/eLife.20722.

17.

Individual patient oesophageal cancer 3D models for tailored treatment.

Saunders JH, Onion D, Collier P, Dorrington MS, Argent RH, Clarke PA, Reece-Smith AM, Parsons SL, Grabowska AM.

Oncotarget. 2017 Apr 11;8(15):24224-24236. doi: 10.18632/oncotarget.12500.

18.

Endoplasmic Reticulum Stress Protein GRP78 Modulates Lipid Metabolism to Control Drug Sensitivity and Antitumor Immunity in Breast Cancer.

Cook KL, Soto-Pantoja DR, Clarke PA, Cruz MI, Zwart A, Wärri A, Hilakivi-Clarke L, Roberts DD, Clarke R.

Cancer Res. 2016 Oct 1;76(19):5657-5670.

19.

Sex steroid-induced DNA methylation changes and inflammation response in prostate cancer.

Wang S, Clarke PAG, Davis R, Mumuni S, Kwabi-Addo B.

Cytokine. 2016 Oct;86:110-118. doi: 10.1016/j.cyto.2016.07.006. Epub 2016 Aug 5.

PMID:
27500645
20.

Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening.

Czodrowski P, Mallinger A, Wienke D, Esdar C, Pöschke O, Busch M, Rohdich F, Eccles SA, Ortiz-Ruiz MJ, Schneider R, Raynaud FI, Clarke PA, Musil D, Schwarz D, Dale T, Urbahns K, Blagg J, Schiemann K.

J Med Chem. 2016 Oct 27;59(20):9337-9349. Epub 2016 Oct 7.

21.

Inhibition of mTOR-kinase destabilizes MYCN and is a potential therapy for MYCN-dependent tumors.

Vaughan L, Clarke PA, Barker K, Chanthery Y, Gustafson CW, Tucker E, Renshaw J, Raynaud F, Li X, Burke R, Jamin Y, Robinson SP, Pearson A, Maira M, Weiss WA, Workman P, Chesler L.

Oncotarget. 2016 Sep 6;7(36):57525-57544. doi: 10.18632/oncotarget.10544.

22.

Synthesis of 2,6-trans- and 3,3,6-trisubstituted tetrahydropyran-4-ones from Maitland-Japp derived 2H-dihydropyran-4-ones: a total synthesis of diospongin B.

Clarke PA, Nasir NM, Sellars PB, Peter AM, Lawson CA, Burroughs JL.

Org Biomol Chem. 2016 Jul 12;14(28):6840-52. doi: 10.1039/c6ob01182a.

PMID:
27340028
23.

2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19.

Mallinger A, Schiemann K, Rink C, Sejberg J, Honey MA, Czodrowski P, Stubbs M, Poeschke O, Busch M, Schneider R, Schwarz D, Musil D, Burke R, Urbahns K, Workman P, Wienke D, Clarke PA, Raynaud FI, Eccles SA, Esdar C, Rohdich F, Blagg J.

ACS Med Chem Lett. 2016 Mar 28;7(6):573-8. doi: 10.1021/acsmedchemlett.6b00022. eCollection 2016 Jun 9.

24.

3-Dimensional Patient-Derived Lung Cancer Assays Reveal Resistance to Standards-of-Care Promoted by Stromal Cells but Sensitivity to Histone Deacetylase Inhibitors.

Onion D, Argent RH, Reece-Smith AM, Craze ML, Pineda RG, Clarke PA, Ratan HL, Parsons SL, Lobo DN, Duffy JP, Atherton JC, McKenzie AJ, Kumari R, King P, Hall BM, Grabowska AM.

Mol Cancer Ther. 2016 Apr;15(4):753-63. doi: 10.1158/1535-7163.MCT-15-0598. Epub 2016 Feb 12.

25.

Blocking the survival of the nastiest by HSP90 inhibition.

Workman P, Clarke PA, Al-Lazikani B.

Oncotarget. 2016 Jan 26;7(4):3658-61. doi: 10.18632/oncotarget.6971.

26.

Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.

Mallinger A, Schiemann K, Rink C, Stieber F, Calderini M, Crumpler S, Stubbs M, Adeniji-Popoola O, Poeschke O, Busch M, Czodrowski P, Musil D, Schwarz D, Ortiz-Ruiz MJ, Schneider R, Thai C, Valenti M, de Haven Brandon A, Burke R, Workman P, Dale T, Wienke D, Clarke PA, Esdar C, Raynaud FI, Eccles SA, Rohdich F, Blagg J.

J Med Chem. 2016 Feb 11;59(3):1078-101. doi: 10.1021/acs.jmedchem.5b01685. Epub 2016 Jan 21.

27.

Mechanistic interrogation of the asymmetric lithiation-trapping of N-thiopivaloyl azetidine and pyrrolidine.

Rayner PJ, Smith JC, Denneval C, O'Brien P, Clarke PA, Horan RA.

Chem Commun (Camb). 2016 Jan 25;52(7):1354-7. doi: 10.1039/c5cc08690f. Epub 2015 Dec 1.

PMID:
26620913
28.

A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.

Dale T, Clarke PA, Esdar C, Waalboer D, Adeniji-Popoola O, Ortiz-Ruiz MJ, Mallinger A, Samant RS, Czodrowski P, Musil D, Schwarz D, Schneider K, Stubbs M, Ewan K, Fraser E, TePoele R, Court W, Box G, Valenti M, de Haven Brandon A, Gowan S, Rohdich F, Raynaud F, Schneider R, Poeschke O, Blaukat A, Workman P, Schiemann K, Eccles SA, Wienke D, Blagg J.

Nat Chem Biol. 2015 Dec;11(12):973-980. doi: 10.1038/nchembio.1952. Epub 2015 Oct 26.

29.

Drugging PI3K in cancer: refining targets and therapeutic strategies.

Yap TA, Bjerke L, Clarke PA, Workman P.

Curr Opin Pharmacol. 2015 Aug;23:98-107. doi: 10.1016/j.coph.2015.05.016. Epub 2015 Jun 25. Review.

30.

Transdisciplinary synthesis for ecosystem science, policy and management: The Australian experience.

Lynch AJ, Thackway R, Specht A, Beggs PJ, Brisbane S, Burns EL, Byrne M, Capon SJ, Casanova MT, Clarke PA, Davies JM, Dovers S, Dwyer RG, Ens E, Fisher DO, Flanigan M, Garnier E, Guru SM, Kilminster K, Locke J, Mac Nally R, McMahon KM, Mitchell PJ, Pierson JC, Rodgers EM, Russell-Smith J, Udy J, Waycott M.

Sci Total Environ. 2015 Nov 15;534:173-84. doi: 10.1016/j.scitotenv.2015.04.100. Epub 2015 May 6.

PMID:
25957785
31.

A Maitland-Japp inspired synthesis of dihydropyran-4-ones and their stereoselective conversion to functionalised tetrahydropyran-4-ones.

Clarke PA, Sellars PB, Nasir NM.

Org Biomol Chem. 2015 Apr 28;13(16):4743-50. doi: 10.1039/c5ob00292c.

PMID:
25804802
32.

Monoclonal Antibodies Targeting LecLex-Related Glycans with Potent Antitumor Activity.

Chua JX, Vankemmelbeke M, McIntosh RS, Clarke PA, Moss R, Parsons T, Spendlove I, Zaitoun AM, Madhusudan S, Durrant LG.

Clin Cancer Res. 2015 Jul 1;21(13):2963-74. doi: 10.1158/1078-0432.CCR-14-3030. Epub 2015 Mar 16.

33.

An online spatial database of Australian Indigenous Biocultural Knowledge for contemporary natural and cultural resource management.

Pert PL, Ens EJ, Locke J, Clarke PA, Packer JM, Turpin G.

Sci Total Environ. 2015 Nov 15;534:110-21. doi: 10.1016/j.scitotenv.2015.01.073. Epub 2015 Feb 11.

PMID:
25682266
34.

Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.

Mallinger A, Crumpler S, Pichowicz M, Waalboer D, Stubbs M, Adeniji-Popoola O, Wood B, Smith E, Thai C, Henley AT, Georgi K, Court W, Hobbs S, Box G, Ortiz-Ruiz MJ, Valenti M, De Haven Brandon A, TePoele R, Leuthner B, Workman P, Aherne W, Poeschke O, Dale T, Wienke D, Esdar C, Rohdich F, Raynaud F, Clarke PA, Eccles SA, Stieber F, Schiemann K, Blagg J.

J Med Chem. 2015 Feb 26;58(4):1717-35. doi: 10.1021/jm501436m. Epub 2015 Feb 13.

35.

First-in-human phase I study of pictilisib (GDC-0941), a potent pan-class I phosphatidylinositol-3-kinase (PI3K) inhibitor, in patients with advanced solid tumors.

Sarker D, Ang JE, Baird R, Kristeleit R, Shah K, Moreno V, Clarke PA, Raynaud FI, Levy G, Ware JA, Mazina K, Lin R, Wu J, Fredrickson J, Spoerke JM, Lackner MR, Yan Y, Friedman LS, Kaye SB, Derynck MK, Workman P, de Bono JS.

Clin Cancer Res. 2015 Jan 1;21(1):77-86. doi: 10.1158/1078-0432.CCR-14-0947. Epub 2014 Nov 4.

36.

Surgical delivery of drug releasing poly(lactic-co-glycolic acid)/poly(ethylene glycol) paste with in vivo effects against glioblastoma.

Smith SJ, Rahman CV, Clarke PA, Ritchie AA, Gould TW, Ward JH, Shakesheff KM, Grundy RG, Rahman R.

Ann R Coll Surg Engl. 2014 Oct;96(7):495-501. doi: 10.1308/003588414X13946184903568.

37.

Lactate and choline metabolites detected in vitro by nuclear magnetic resonance spectroscopy are potential metabolic biomarkers for PI3K inhibition in pediatric glioblastoma.

Al-Saffar NM, Marshall LV, Jackson LE, Balarajah G, Eykyn TR, Agliano A, Clarke PA, Jones C, Workman P, Pearson AD, Leach MO.

PLoS One. 2014 Aug 1;9(8):e103835. doi: 10.1371/journal.pone.0103835. eCollection 2014.

38.

Hydroxychloroquine inhibits autophagy to potentiate antiestrogen responsiveness in ER+ breast cancer.

Cook KL, Wärri A, Soto-Pantoja DR, Clarke PA, Cruz MI, Zwart A, Clarke R.

Clin Cancer Res. 2014 Jun 15;20(12):3222-32. doi: 10.1158/1078-0432.CCR-13-3227. Erratum in: Clin Cancer Res. 2016 Jun 1;22(11):2825.

39.

Knockdown of estrogen receptor-α induces autophagy and inhibits antiestrogen-mediated unfolded protein response activation, promoting ROS-induced breast cancer cell death.

Cook KL, Clarke PA, Parmar J, Hu R, Schwartz-Roberts JL, Abu-Asab M, Wärri A, Baumann WT, Clarke R.

FASEB J. 2014 Sep;28(9):3891-905. doi: 10.1096/fj.13-247353. Epub 2014 May 23.

40.

E3 ubiquitin ligase Cullin-5 modulates multiple molecular and cellular responses to heat shock protein 90 inhibition in human cancer cells.

Samant RS, Clarke PA, Workman P.

Proc Natl Acad Sci U S A. 2014 May 6;111(18):6834-9. doi: 10.1073/pnas.1322412111. Epub 2014 Apr 23.

41.

Strategies for the construction of tetrahydropyran rings in the synthesis of natural products.

Nasir NM, Ermanis K, Clarke PA.

Org Biomol Chem. 2014 Jun 7;12(21):3323-35. doi: 10.1039/c4ob00423j. Epub 2014 Apr 17. Review.

PMID:
24744139
42.

Mitochondria directly donate their membrane to form autophagosomes during a novel mechanism of parkin-associated mitophagy.

Cook KL, Soto-Pantoja DR, Abu-Asab M, Clarke PA, Roberts DD, Clarke R.

Cell Biosci. 2014 Mar 27;4(1):16. doi: 10.1186/2045-3701-4-16.

43.

Modelling the effect of GRP78 on anti-oestrogen sensitivity and resistance in breast cancer.

Parmar JH, Cook KL, Shajahan-Haq AN, Clarke PA, Tavassoly I, Clarke R, Tyson JJ, Baumann WT.

Interface Focus. 2013 Aug 6;3(4):20130012. doi: 10.1098/rsfs.2013.0012.

44.

Restricting direct interaction of CDC37 with HSP90 does not compromise chaperoning of client proteins.

Smith JR, de Billy E, Hobbs S, Powers M, Prodromou C, Pearl L, Clarke PA, Workman P.

Oncogene. 2015 Jan 2;34(1):15-26. doi: 10.1038/onc.2013.519. Epub 2013 Dec 2.

45.

Mode of cell death induced by the HSP90 inhibitor 17-AAG (tanespimycin) is dependent on the expression of pro-apoptotic BAX.

Powers MV, Valenti M, Miranda S, Maloney A, Eccles SA, Thomas G, Clarke PA, Workman P.

Oncotarget. 2013 Nov;4(11):1963-75.

46.

Adjuvant chemotherapy for brain tumors delivered via a novel intra-cavity moldable polymer matrix.

Rahman CV, Smith SJ, Morgan PS, Langmack KA, Clarke PA, Ritchie AA, Macarthur DC, Rose FR, Shakesheff KM, Grundy RG, Ruman Rahman.

PLoS One. 2013 Oct 14;8(10):e77435. doi: 10.1371/journal.pone.0077435. eCollection 2013.

47.

The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design.

Couty S, Westwood IM, Kalusa A, Cano C, Travers J, Boxall K, Chow CL, Burns S, Schmitt J, Pickard L, Barillari C, McAndrew PC, Clarke PA, Linardopoulos S, Griffin RJ, Aherne GW, Raynaud FI, Workman P, Jones K, van Montfort RL.

Oncotarget. 2013 Oct;4(10):1647-61.

48.

HSF1 in Translation.

de Billy E, Clarke PA, Workman P.

Cancer Cell. 2013 Aug 12;24(2):147-9. doi: 10.1016/j.ccr.2013.07.017.

49.

Combining trail with PI3 kinase or HSP90 inhibitors enhances apoptosis in colorectal cancer cells via suppression of survival signaling.

Saturno G, Valenti M, De Haven Brandon A, Thomas GV, Eccles S, Clarke PA, Workman P.

Oncotarget. 2013 Aug;4(8):1185-98.

50.

Genome-based cancer therapeutics: targets, kinase drug resistance and future strategies for precision oncology.

Workman P, Al-Lazikani B, Clarke PA.

Curr Opin Pharmacol. 2013 Aug;13(4):486-96. doi: 10.1016/j.coph.2013.06.004. Epub 2013 Jun 28. Review.

PMID:
23810823

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