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Items: 1 to 50 of 283

1.

Synthesis, 3D-structure and stability analyses of NRPa-308, a new promising anti-cancer agent.

Brachet E, Dumond A, Liu WQ, Fabre M, Selkti M, Raynaud F, Hermine O, Benhida R, Belmont P, Garbay C, Lepelletier Y, Ronco C, Pagès G, Demange L.

Bioorg Med Chem Lett. 2019 Oct 16:126710. doi: 10.1016/j.bmcl.2019.126710. [Epub ahead of print]

PMID:
31699610
2.

Synthesis of a benzoxazinthione derivative of tanaproget and pharmacological evaluation for PET imaging of PR expression.

Allott L, Miranda C, Hayes A, Raynaud F, Cawthorne C, Smith G.

EJNMMI Radiopharm Chem. 2019 Jan 10;4(1):1. doi: 10.1186/s41181-018-0054-z.

3.

Dynamic Emergence of Observed and Hidden Intra-tumor Heterogeneity.

Raynaud F, Mina M, Ciriello G.

iScience. 2019 Oct 10;21:157-167. doi: 10.1016/j.isci.2019.10.018. [Epub ahead of print]

4.

International Ring Trial of a High Resolution Targeted Metabolomics and Lipidomics Platform for Serum and Plasma Analysis.

Thompson JW, Adams KJ, Adamski J, Asad Y, Borts D, Bowden JA, Byram G, Dang V, Dunn WB, Fernandez F, Fiehn O, Gaul DA, Hühmer AF, Kalli A, Koal T, Koeniger S, Mandal R, Meier F, Naser FJ, O'Neil D, Pal A, Patti GJ, Pham-Tuan H, Prehn C, Raynaud FI, Shen T, Southam AD, St John-Williams L, Sulek K, Vasilopoulou CG, Viant M, Winder CL, Wishart D, Zhang L, Zheng J, Moseley MA.

Anal Chem. 2019 Nov 8. doi: 10.1021/acs.analchem.9b02908. [Epub ahead of print]

PMID:
31638379
5.

High Proliferation Rate and a Compromised Spindle Assembly Checkpoint Confers Sensitivity to the MPS1 Inhibitor BOS172722 in Triple-Negative Breast Cancers.

Anderhub SJ, Mak GW, Gurden MD, Faisal A, Drosopoulos K, Walsh K, Woodward HL, Innocenti P, Westwood IM, Naud S, Hayes A, Theofani E, Filosto S, Saville H, Burke R, van Montfort RLM, Raynaud FI, Blagg J, Hoelder S, Eccles SA, Linardopoulos S.

Mol Cancer Ther. 2019 Oct;18(10):1696-1707. doi: 10.1158/1535-7163.MCT-18-1203.

PMID:
31575759
6.

De novo phosphatidylcholine synthesis is required for autophagosome membrane formation and maintenance during autophagy.

Andrejeva G, Gowan S, Lin G, Wong Te Fong AL, Shamsaei E, Parkes HG, Mui J, Raynaud FI, Asad Y, Vizcay-Barrena G, Nikitorowicz-Buniak J, Valenti M, Howell L, Fleck RA, Martin LA, Kirkin V, Leach MO, Chung YL.

Autophagy. 2019 Sep 13:1-17. doi: 10.1080/15548627.2019.1659608. [Epub ahead of print]

PMID:
31517566
7.

Signalling involving MET and FAK supports cell division independent of the activity of the cell cycle-regulating CDK4/6 kinases.

Zhang C, Stockwell SR, Elbanna M, Ketteler R, Freeman J, Al-Lazikani B, Eccles S, De Haven Brandon A, Raynaud F, Hayes A, Clarke PA, Workman P, Mittnacht S.

Oncogene. 2019 Jul;38(30):5905-5920. doi: 10.1038/s41388-019-0850-2. Epub 2019 Jul 12.

8.

Differences in Signaling Patterns on PI3K Inhibition Reveal Context Specificity in KRAS-Mutant Cancers.

Stewart A, Coker EA, Pölsterl S, Georgiou A, Minchom AR, Carreira S, Cunningham D, O'Brien ME, Raynaud FI, de Bono JS, Al-Lazikani B, Banerji U.

Mol Cancer Ther. 2019 Aug;18(8):1396-1404. doi: 10.1158/1535-7163.MCT-18-0727. Epub 2019 Jul 1.

PMID:
31262731
9.

C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays.

Le Bihan YV, Lanigan RM, Atrash B, McLaughlin MG, Velupillai S, Malcolm AG, England KS, Ruda GF, Mok NY, Tumber A, Tomlin K, Saville H, Shehu E, McAndrew C, Carmichael L, Bennett JM, Jeganathan F, Eve P, Donovan A, Hayes A, Wood F, Raynaud FI, Fedorov O, Brennan PE, Burke R, van Montfort RLM, Rossanese OW, Blagg J, Bavetsias V.

Eur J Med Chem. 2019 Sep 1;177:316-337. doi: 10.1016/j.ejmech.2019.05.041. Epub 2019 May 17.

10.

ALK2 inhibitors display beneficial effects in preclinical models of ACVR1 mutant diffuse intrinsic pontine glioma.

Carvalho D, Taylor KR, Olaciregui NG, Molinari V, Clarke M, Mackay A, Ruddle R, Henley A, Valenti M, Hayes A, Brandon AH, Eccles SA, Raynaud F, Boudhar A, Monje M, Popov S, Moore AS, Mora J, Cruz O, Vinci M, Brennan PE, Bullock AN, Carcaboso AM, Jones C.

Commun Biol. 2019 May 9;2:156. doi: 10.1038/s42003-019-0420-8. eCollection 2019.

11.

Metabolism of the dual FLT-3/Aurora kinase inhibitor CCT241736 in preclinical and human in vitro models: Implication for the choice of toxicology species.

Wood FL, Shepherd S, Hayes A, Liu M, Grira K, Mok Y, Atrash B, Faisal A, Bavetsias V, Linardopoulos S, Blagg J, Raynaud FI.

Eur J Pharm Sci. 2019 Nov 1;139:104899. doi: 10.1016/j.ejps.2019.04.004. Epub 2019 Apr 3.

12.

Effect of acute total sleep deprivation on plasma melatonin, cortisol and metabolite rhythms in females.

Honma A, Revell VL, Gunn PJ, Davies SK, Middleton B, Raynaud FI, Skene DJ.

Eur J Neurosci. 2019 Mar 30. doi: 10.1111/ejn.14411. [Epub ahead of print]

PMID:
30929284
13.

Neuropilin-1 peptide-like ligands with proline mimetics, tested using the improved chemiluminescence affinity detection method.

Puszko AK, Sosnowski P, Tymecka D, Raynaud F, Hermine O, Lepelletier Y, Misicka A.

Medchemcomm. 2019 Jan 25;10(2):332-340. doi: 10.1039/c8md00537k. eCollection 2019 Feb 1.

PMID:
30881620
14.

EZH2 oncogenic mutations drive epigenetic, transcriptional, and structural changes within chromatin domains.

Donaldson-Collier MC, Sungalee S, Zufferey M, Tavernari D, Katanayeva N, Battistello E, Mina M, Douglass KM, Rey T, Raynaud F, Manley S, Ciriello G, Oricchio E.

Nat Genet. 2019 Mar;51(3):517-528. doi: 10.1038/s41588-018-0338-y. Epub 2019 Jan 28.

PMID:
30692681
15.

Correction: In vitro Biological Characterization of a Novel, Synthetic Diaryl Pyrazole Resorcinol Class of Heat Shock Protein 90 Inhibitors.

Sharp SY, Boxall K, Rowlands M, Prodromou C, Roe SM, Maloney A, Powers M, Clarke PA, Box G, Sanderson S, Patterson L, Matthews TP, Cheung KJ, Ball K, Hayes A, Raynaud F, Marais R, Pearl L, Eccles S, Aherne W, McDonald E, Workman P.

Cancer Res. 2019 Jan 1;79(1):287. doi: 10.1158/0008-5472.CAN-18-3578. No abstract available.

PMID:
30602624
16.

Design, Synthesis and Characterization of Covalent KDM5 Inhibitors.

Vazquez-Rodriguez S, Wright M, Rogers CM, Cribbs AP, Velupillai S, Philpott M, Lee H, Dunford JE, Huber KVM, Robers MB, Vasta JD, Thezenas ML, Bonham S, Kessler B, Bennett J, Fedorov O, Raynaud F, Donovan A, Blagg J, Bavetsias V, Oppermann U, Bountra C, Kawamura A, Brennan PE.

Angew Chem Int Ed Engl. 2019 Jan 8;58(2):515-519. doi: 10.1002/anie.201810179. Epub 2018 Dec 7.

17.

High dietary intake of palm oils compromises glucose tolerance whereas high dietary intake of olive oil compromises liver lipid metabolism and integrity.

Djohan YF, Badia E, Bonafos B, Fouret G, Lauret C, Dupuy AM, Pinot E, Sutra T, Gaillet S, Lambert K, Raynaud F, Gayrard N, Jover B, Monde AA, Cristol JP, Coudray C, Feillet-Coudray C.

Eur J Nutr. 2019 Dec;58(8):3091-3107. doi: 10.1007/s00394-018-1854-3. Epub 2018 Nov 3.

PMID:
30392135
18.

Pan-cancer inference of intra-tumor heterogeneity reveals associations with different forms of genomic instability.

Raynaud F, Mina M, Tavernari D, Ciriello G.

PLoS Genet. 2018 Sep 13;14(9):e1007669. doi: 10.1371/journal.pgen.1007669. eCollection 2018 Sep.

19.

Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4- d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N2-(2-Ethoxy-4-(4-methyl-4 H-1,2,4-triazol-3-yl)phenyl)-6-methyl- N8-neopentylpyrido[3,4- d]pyrimidine-2,8-diamine (BOS172722).

Woodward HL, Innocenti P, Cheung KJ, Hayes A, Roberts J, Henley AT, Faisal A, Mak GW, Box G, Westwood IM, Cronin N, Carter M, Valenti M, De Haven Brandon A, O'Fee L, Saville H, Schmitt J, Burke R, Broccatelli F, van Montfort RLM, Raynaud FI, Eccles SA, Linardopoulos S, Blagg J, Hoelder S.

J Med Chem. 2018 Sep 27;61(18):8226-8240. doi: 10.1021/acs.jmedchem.8b00690. Epub 2018 Sep 10.

20.

Correction to: An in vitro and in vivo study of the combination of the heat shock protein inhibitor 17-allylamino-17-demethoxygeldanamycin and carboplatin in human ovarian cancer models.

Banerji U, Sain N, Sharp SY, Valenti M, Asad Y, Ruddle R, Raynaud F, Walton M, Eccles SA, Judson I, Jackman AL, Workman P.

Cancer Chemother Pharmacol. 2018 Nov;82(5):911-912. doi: 10.1007/s00280-018-3674-9.

PMID:
30173339
21.

Vistusertib (dual m-TORC1/2 inhibitor) in combination with paclitaxel in patients with high-grade serous ovarian and squamous non-small-cell lung cancer.

Basu B, Krebs MG, Sundar R, Wilson RH, Spicer J, Jones R, Brada M, Talbot DC, Steele N, Ingles Garces AH, Brugger W, Harrington EA, Evans J, Hall E, Tovey H, de Oliveira FM, Carreira S, Swales K, Ruddle R, Raynaud FI, Purchase B, Dawes JC, Parmar M, Turner AJ, Tunariu N, Banerjee S, de Bono JS, Banerji U.

Ann Oncol. 2018 Sep 1;29(9):1918-1925. doi: 10.1093/annonc/mdy245.

22.

SNAP23-Kif5 complex controls mGlu1 receptor trafficking.

Raynaud F, Homburger V, Seveno M, Vigy O, Moutin E, Fagni L, Perroy J.

J Mol Cell Biol. 2018 Oct 1;10(5):423-436. doi: 10.1093/jmcb/mjy031.

PMID:
29762713
23.

NRPa-308, a new neuropilin-1 antagonist, exerts in vitro anti-angiogenic and anti-proliferative effects and in vivo anti-cancer effects in a mouse xenograft model.

Liu WQ, Lepelletier Y, Montès M, Borriello L, Jarray R, Grépin R, Leforban B, Loukaci A, Benhida R, Hermine O, Dufour S, Pagès G, Garbay C, Raynaud F, Hadj-Slimane R, Demange L.

Cancer Lett. 2018 Feb 1;414:88-98. doi: 10.1016/j.canlet.2017.10.039. Epub 2017 Oct 28.

PMID:
29111348
24.

Erratum to: investigation of metabolites for estimating blood deposition time.

Lech K, Liu F, Davies SK, Ackermann K, Ang JE, Middleton B, Revell VL, Raynaud FI, Hoveijn I, Hut RA, Skene DJ, Kayser M.

Int J Legal Med. 2018 Jan;132(1):33. doi: 10.1007/s00414-017-1670-y. No abstract available.

PMID:
28840223
25.

Investigation of metabolites for estimating blood deposition time.

Lech K, Liu F, Davies SK, Ackermann K, Ang JE, Middleton B, Revell VL, Raynaud FJ, Hoveijn I, Hut RA, Skene DJ, Kayser M.

Int J Legal Med. 2018 Jan;132(1):25-32. doi: 10.1007/s00414-017-1638-y. Epub 2017 Aug 5. Erratum in: Int J Legal Med. 2017 Aug 24;:.

26.

Conditional Selection of Genomic Alterations Dictates Cancer Evolution and Oncogenic Dependencies.

Mina M, Raynaud F, Tavernari D, Battistello E, Sungalee S, Saghafinia S, Laessle T, Sanchez-Vega F, Schultz N, Oricchio E, Ciriello G.

Cancer Cell. 2017 Aug 14;32(2):155-168.e6. doi: 10.1016/j.ccell.2017.06.010. Epub 2017 Jul 27.

27.

Development and validation of a LC-MS/MS method for the quantification of the checkpoint kinase 1 inhibitor SRA737 in human plasma.

Zangarini M, Berry P, Sludden J, Raynaud FI, Banerji U, Jones P, Edwards D, Veal GJ.

Bioanalysis. 2017 Jul;9(13):1001-1010. doi: 10.4155/bio-2017-0043. Epub 2017 Jul 10.

PMID:
28692309
28.

Modulation of Plasma Metabolite Biomarkers of the MAPK Pathway with MEK Inhibitor RO4987655: Pharmacodynamic and Predictive Potential in Metastatic Melanoma.

Ang JE, Pal A, Asad YJ, Henley AT, Valenti M, Box G, de Haven Brandon A, Revell VL, Skene DJ, Venturi M, Rueger R, Meresse V, Eccles SA, de Bono JS, Kaye SB, Workman P, Banerji U, Raynaud FI.

Mol Cancer Ther. 2017 Oct;16(10):2315-2323. doi: 10.1158/1535-7163.MCT-16-0881. Epub 2017 Jun 21.

29.

APN/CD13 is over-expressed by Psoriatic fibroblasts and is modulated by CGRP and IL-4 but not by retinoic acid treatment.

Gerbaud P, Guibourdenche J, Jarray R, Conti M, Palmic P, Leclerc-Mercier S, Bruneau J, Hermine O, Lepelletier Y, Raynaud F.

J Cell Physiol. 2018 Feb;233(2):958-967. doi: 10.1002/jcp.25941. Epub 2017 May 23.

PMID:
28387421
30.

Characterisation of CCT271850, a selective, oral and potent MPS1 inhibitor, used to directly measure in vivo MPS1 inhibition vs therapeutic efficacy.

Faisal A, Mak GWY, Gurden MD, Xavier CPR, Anderhub SJ, Innocenti P, Westwood IM, Naud S, Hayes A, Box G, Valenti MR, De Haven Brandon AK, O'Fee L, Schmitt J, Woodward HL, Burke R, vanMontfort RLM, Blagg J, Raynaud FI, Eccles SA, Hoelder S, Linardopoulos S.

Br J Cancer. 2017 Apr 25;116(9):1166-1176. doi: 10.1038/bjc.2017.75. Epub 2017 Mar 23.

31.

Assessing histone demethylase inhibitors in cells: lessons learned.

Hatch SB, Yapp C, Montenegro RC, Savitsky P, Gamble V, Tumber A, Ruda GF, Bavetsias V, Fedorov O, Atrash B, Raynaud F, Lanigan R, Carmichael L, Tomlin K, Burke R, Westaway SM, Brown JA, Prinjha RK, Martinez ED, Oppermann U, Schofield CJ, Bountra C, Kawamura A, Blagg J, Brennan PE, Rossanese O, Müller S.

Epigenetics Chromatin. 2017 Mar 1;10:9. doi: 10.1186/s13072-017-0116-6. eCollection 2017.

32.

Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen.

Cheeseman MD, Chessum NE, Rye CS, Pasqua AE, Tucker MJ, Wilding B, Evans LE, Lepri S, Richards M, Sharp SY, Ali S, Rowlands M, O'Fee L, Miah A, Hayes A, Henley AT, Powers M, Te Poele R, De Billy E, Pellegrino L, Raynaud F, Burke R, van Montfort RL, Eccles SA, Workman P, Jones K.

J Med Chem. 2017 Jan 12;60(1):180-201. doi: 10.1021/acs.jmedchem.6b01055. Epub 2016 Dec 22.

33.

Interlaboratory Reproducibility of a Targeted Metabolomics Platform for Analysis of Human Serum and Plasma.

Siskos AP, Jain P, Römisch-Margl W, Bennett M, Achaintre D, Asad Y, Marney L, Richardson L, Koulman A, Griffin JL, Raynaud F, Scalbert A, Adamski J, Prehn C, Keun HC.

Anal Chem. 2017 Jan 3;89(1):656-665. doi: 10.1021/acs.analchem.6b02930. Epub 2016 Dec 13.

34.

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.

35.

Discovery of 4,6-disubstituted pyrimidines as potent inhibitors of the heat shock factor 1 (HSF1) stress pathway and CDK9.

Rye CS, Chessum NE, Lamont S, Pike KG, Faulder P, Demeritt J, Kemmitt P, Tucker J, Zani L, Cheeseman MD, Isaac R, Goodwin L, Boros J, Raynaud F, Hayes A, Henley AT, de Billy E, Lynch CJ, Sharp SY, Te Poele R, Fee LO, Foote KM, Green S, Workman P, Jones K.

Medchemcomm. 2016 Aug 1;7(8):1580-1586. Epub 2016 Jun 13.

36.

Comprehensive Genetic Landscape of Uveal Melanoma by Whole-Genome Sequencing.

Royer-Bertrand B, Torsello M, Rimoldi D, El Zaoui I, Cisarova K, Pescini-Gobert R, Raynaud F, Zografos L, Schalenbourg A, Speiser D, Nicolas M, Vallat L, Klein R, Leyvraz S, Ciriello G, Riggi N, Moulin AP, Rivolta C.

Am J Hum Genet. 2016 Nov 3;99(5):1190-1198. doi: 10.1016/j.ajhg.2016.09.008. Epub 2016 Oct 13.

37.

Pyrido[3,4-d]pyrimidin-4(3H)-one metabolism mediated by aldehyde oxidase is blocked by C2-substitution.

Hayes A, Mok NY, Liu M, Thai C, Henley AT, Atrash B, Lanigan RM, Sejberg J, Le Bihan YV, Bavetsias V, Blagg J, Raynaud FI.

Xenobiotica. 2017 Sep;47(9):771-777. doi: 10.1080/00498254.2016.1230245. Epub 2016 Oct 26.

38.

Intercellular ultrafast Ca(2+) wave in vascular smooth muscle cells: numerical and experimental study.

Quijano JC, Raynaud F, Nguyen D, Piacentini N, Meister JJ.

Sci Rep. 2016 Aug 10;6:31271. doi: 10.1038/srep31271.

39.

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.

40.

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.

41.

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.

42.

p53 Loss in MYC-Driven Neuroblastoma Leads to Metabolic Adaptations Supporting Radioresistance.

Yogev O, Barker K, Sikka A, Almeida GS, Hallsworth A, Smith LM, Jamin Y, Ruddle R, Koers A, Webber HT, Raynaud FI, Popov S, Jones C, Petrie K, Robinson SP, Keun HC, Chesler L.

Cancer Res. 2016 May 15;76(10):3025-35. doi: 10.1158/0008-5472.CAN-15-1939. Epub 2016 Mar 29.

43.

Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737).

Osborne JD, Matthews TP, McHardy T, Proisy N, Cheung KM, Lainchbury M, Brown N, Walton MI, Eve PD, Boxall KJ, Hayes A, Henley AT, Valenti MR, De Haven Brandon AK, Box G, Jamin Y, Robinson SP, Westwood IM, van Montfort RL, Leonard PM, Lamers MB, Reader JC, Aherne GW, Raynaud FI, Eccles SA, Garrett MD, Collins I.

J Med Chem. 2016 Jun 9;59(11):5221-37. doi: 10.1021/acs.jmedchem.5b01938. Epub 2016 May 23.

44.

Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach.

Innocenti P, Woodward HL, Solanki S, Naud S, Westwood IM, Cronin N, Hayes A, Roberts J, Henley AT, Baker R, Faisal A, Mak GW, Box G, Valenti M, De Haven Brandon A, O'Fee L, Saville H, Schmitt J, Matijssen B, Burke R, van Montfort RL, Raynaud FI, Eccles SA, Linardopoulos S, Blagg J, Hoelder S.

J Med Chem. 2016 Apr 28;59(8):3671-88. doi: 10.1021/acs.jmedchem.5b01811. Epub 2016 Apr 7.

45.

Plasma Metabolomic Changes following PI3K Inhibition as Pharmacodynamic Biomarkers: Preclinical Discovery to Phase I Trial Evaluation.

Ang JE, Pandher R, Ang JC, Asad YJ, Henley AT, Valenti M, Box G, de Haven Brandon A, Baird RD, Friedman L, Derynck M, Vanhaesebroeck B, Eccles SA, Kaye SB, Workman P, de Bono JS, Raynaud FI.

Mol Cancer Ther. 2016 Jun;15(6):1412-24. doi: 10.1158/1535-7163.MCT-15-0815. Epub 2016 Apr 5.

46.

Synthesis and Evaluation of a 2,11-Cembranoid-Inspired Library.

Welford AJ, Caldwell JJ, Liu M, Richards M, Brown N, Lomas C, Tizzard GJ, Pitak MB, Coles SJ, Eccles SA, Raynaud FI, Collins I.

Chemistry. 2016 Apr 11;22(16):5657-64. doi: 10.1002/chem.201505093. Epub 2016 Mar 1.

47.

Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore.

Schiemann K, Mallinger A, Wienke D, Esdar C, Poeschke O, Busch M, Rohdich F, Eccles SA, Schneider R, Raynaud FI, Czodrowski P, Musil D, Schwarz D, Urbahns K, Blagg J.

Bioorg Med Chem Lett. 2016 Mar 1;26(5):1443-51. doi: 10.1016/j.bmcl.2016.01.062. Epub 2016 Jan 22.

PMID:
26852363
48.

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.

49.

8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors.

Bavetsias V, Lanigan RM, Ruda GF, Atrash B, McLaughlin MG, Tumber A, Mok NY, Le Bihan YV, Dempster S, Boxall KJ, Jeganathan F, Hatch SB, Savitsky P, Velupillai S, Krojer T, England KS, Sejberg J, Thai C, Donovan A, Pal A, Scozzafava G, Bennett JM, Kawamura A, Johansson C, Szykowska A, Gileadi C, Burgess-Brown NA, von Delft F, Oppermann U, Walters Z, Shipley J, Raynaud FI, Westaway SM, Prinjha RK, Fedorov O, Burke R, Schofield CJ, Westwood IM, Bountra C, Müller S, van Montfort RL, Brennan PE, Blagg J.

J Med Chem. 2016 Feb 25;59(4):1388-409. doi: 10.1021/acs.jmedchem.5b01635. Epub 2016 Jan 7.

50.

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.

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