Panagis Filippakopoulos

Principal Investigator

University of Oxford
Group: 
Bromodomains

Panagis obtained his BSc. in Chemistry from the Aristotelian University of Thessaloniki. He carried out his doctoral studies in Inorganic Chemistry at the University of Michigan with Prof. Dimitri Coucouvanis and received his PhD in 2004. He moved to Oxford University in the UK at the Structural Genomics Consortium where he focused on protein crystallography and biophysics, first as a postdoctoral scientist until 2007, then as a Team Leader until 2011. In December 2011 he received a Research Career Development Fellowship Award from the Wellcome Trust and took a post as a Principal Investigator at the Nuffield Department of Medicine in Oxford University. In November 2012 he became an affiliate of the Ludwig Institute for Cancer Research (LICR) in Oxford. His research interest is focused on structural comparisons of entire protein families and the discovery of shared and distinct mechanisms that determine substrate recognition and protein regulation, as well as the structure-guided design of specific inhibitors that modulate the function of proteins involved in epigenetic signaling, aiming to target them in disease.

Research Areas

The goal of our research is to address the structural and functional role of BET (Bromo and Extra Terminal) proteins in transcription initiation by establishing the network of their interactions and their structural involvement in the assembly of the transcriptional machinery. Importantly, we aim to understand how this network of interactions is perturbed in cancer, when members of the BET family are found fused to the NUT protein, acting as molecular switches, resulting in so called NUT-midline carcinomas (NMCs). Research of this type will help demystify cell cycle progression providing a link between cellular signalling and readout of epigenetic marks facilitating the design of translational research projects that aim to target BET proteins.

Group Members

  • Sarah Picaud
  • Eirini Xemantilotou
  • Takao Fujisawa
  • Beatriz Diez-Dacal
  • Chen-Yi Wang

Publications

Functions of bromodomain-containing proteins and their roles in homeostasis and cancer.
Fujisawa, T; Filippakopoulos, P;
Nature Reviews: Molecular Cell Biology. 2017 18:246-262. doi: 10.1038/nrm.2016.143
PMID: 28053347

Multivalent Histone and DNA Engagement by a PHD/BRD/PWWP Triple Reader Cassette Recruits ZMYND8 to K14ac-Rich Chromatin.
Savitsky, P; Krojer, T; Fujisawa, T; Lambert, JP; Picaud, S; Wang, CY; Shanle, EK; Krajewski, K; Friedrichsen, H; Kanapin, A; Goding, C; Schapira, M; Samsonova, A; Strahl, BD; Gingras, AC; Filippakopoulos, P;
Cell Reports. 2016 17:2724-2737. doi: 10.1016/j.celrep.2016.11.014
PMID: 27926874

Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia.
Picaud, S; Leonards, K; Lambert, JP; Dovey, O; Wells, C; Fedorov, O; Monteiro, O; Fujisawa, T; Wang, CY; Lingard, H; Tallant, C; Nikbin, N; Guetzoyan, L; Ingham, R; Ley, SV; Brennan, P; Muller, S; Samsonova, A; Gingras, AC; Schwaller, J; Vassiliou, G; Knapp, S; Filippakopoulos, P;
Science Advances. 2016 2:e1600760-. doi: 10.1126/sciadv.1600760
PMID: 27757418

Beating the odds: BETs in disease.
Wang, CY; Filippakopoulos, P;
Trends in Biochemical Sciences. 2015 40:468-479. doi:
PMID: 26145250

Targeting bromodomains: epigenetic readers of lysine acetylation.
Filippakopoulos, P; Knapp, S;
Nature Reviews Drug Discovery. 2014 13:337-356. doi:
PMID: 24751816

Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.
Ciceri, P; Müller, S; O'Mahony, A; Fedorov, O; Filippakopoulos, P; Hunt, JP; Lasater, EA; Pallares, G; Picaud, S; Wells, C; Martin, S; Wodicka, LM; Shah, NP; Treiber, DK; Knapp, S;
Nature Chemical Biology. 2014 10:305-312. doi:
PMID: 24584101

RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.
Picaud, S; Wells, C; Felletar, I; Brotherton, D; Martin, S; Savitsky, P; Diez-Dacal, B; Philpott, M; Bountra, C; Lingard, H; Fedorov, O; Müller, S; Brennan, PE; Knapp, S; Filippakopoulos, P;
Proceedings of the National Academy of Sciences of USA. 2013 110:19754-19759. doi:
PMID: 24248379

Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit.
Fish, PV; Filippakopoulos, P; Bish, G; Brennan, PE; Bunnage, ME; Cook, AS; Federov, O; Gerstenberger, BS; Jones, H; Knapp, S; Marsden, B; Nocka, K; Owen, DR; Philpott, M; Picaud, S; Primiano, MJ; Ralph, MJ; Sciammetta, N; Trzupek, JD;
Journal of Medicinal Chemistry. 2012 55:9831-9837. doi:
PMID: 23095041

Small-molecule inhibition of BRDT for male contraception.
Matzuk, MM; McKeown, MR; Filippakopoulos, P; Li, Q; Ma, L; Agno, JE; Lemieux, ME; Picaud, S; Yu, RN; Qi, J; Knapp, S; Bradner, JE;
Cell. 2012 150:673-684. doi: 10.1016/j.cell.2012.06.045
PMID: 22901802

The bromodomain interaction module
Filippakopoulos, P; Knapp, S;
FEBS Letters. 2012 586:2692-2704. doi: 10.1016/j.febslet.2012.04.045
PMID:

Selective inhibition of BET bromodomains.
Filippakopoulos, P; Qi, J; Picaud, S; Shen, Y; Smith, WB; Fedorov, O; Morse, EM; Keates, T; Hickman, TT; Felletar, I; Philpott, M; Munro, S; McKeown, MR; Wang, Y; Christie, AL; West, N; Cameron, MJ; Schwartz, B; Heightman, TD; La Thangue, N; French, CA; Wiest, O; Kung, AL; Knapp, S; Bradner, JE;
Nature. 2010 468:1067-1073. doi:
PMID: 20871596

Structural coupling of SH2-kinase domains links Fes and Abl substrate recognition and kinase activation.
Filippakopoulos, P; Kofler, M; Hantschel, O; Gish, GD; Grebien, F; Salah, E; Neudecker, P; Kay, LE; Turk, BE; Superti-Furga, G; Pawson, T; Knapp, S;
Cell. 2008 134:793-803. doi: 10.1016/j.cell.2008.07.047
PMID: 18775312

2017

Epigenetic pathway inhibitors represent potential drugs for treating pancreatic and bronchial neuroendocrine tumors.
Lines, KE; Stevenson, M; Filippakopoulos, P; Müller, S; Lockstone, HE; Wright, B; Grozinsky-Glasberg, S; Grossman, AB; Knapp, S; Buck, D; Bountra, C; Thakker, RV;
Oncogenesis. 2017 6:e332-. doi: 10.1038/oncsis.2017.30
PMID: 28504695

MOB1 Mediated Phospho-recognition in the Core Mammalian Hippo Pathway.
Couzens, AL; Xiong, S; Knight, JDR; Mao, DY; Guettler, S; Picaud, S; Kurinov, I; Filippakopoulos, P; Sicheri, F; Gingras, AC;
Molecular and Cellular Proteomics. 2017 16:1098-1110. doi: 10.1074/mcp.M116.065490
PMID: 28373298

Functions of bromodomain-containing proteins and their roles in homeostasis and cancer.
Fujisawa, T; Filippakopoulos, P;
Nature Reviews: Molecular Cell Biology. 2017 18:246-262. doi: 10.1038/nrm.2016.143
PMID: 28053347

2016

Multivalent Histone and DNA Engagement by a PHD/BRD/PWWP Triple Reader Cassette Recruits ZMYND8 to K14ac-Rich Chromatin.
Savitsky, P; Krojer, T; Fujisawa, T; Lambert, JP; Picaud, S; Wang, CY; Shanle, EK; Krajewski, K; Friedrichsen, H; Kanapin, A; Goding, C; Schapira, M; Samsonova, A; Strahl, BD; Gingras, AC; Filippakopoulos, P;
Cell Reports. 2016 17:2724-2737. doi: 10.1016/j.celrep.2016.11.014
PMID: 27926874

Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia.
Picaud, S; Leonards, K; Lambert, JP; Dovey, O; Wells, C; Fedorov, O; Monteiro, O; Fujisawa, T; Wang, CY; Lingard, H; Tallant, C; Nikbin, N; Guetzoyan, L; Ingham, R; Ley, SV; Brennan, P; Muller, S; Samsonova, A; Gingras, AC; Schwaller, J; Vassiliou, G; Knapp, S; Filippakopoulos, P;
Science Advances. 2016 2:e1600760-. doi: 10.1126/sciadv.1600760
PMID: 27757418

Discovery and optimization of a selective ligand for the Switch/Sucrose Non-Fermenting-related bromodomains of Polybromo protein-1 by the use of virtual screening and hydration analysis.
Myrianthopoulos, V; Gaboriaud-Kolar, N; Tallant, C; Hall, ML; Grigoriou, S; Brownlee, PM; Fedorov, O; Rogers, C; Heidenreich, D; Wanior, M; Drosos, N; Mexia, N; Savitsky, P; Bagratuni, T; Kastritis, E; Terpos, E; Filippakopoulos, P; Müller, S; Skaltsounis, AL; Downs, JA; Knapp, S; Mikros, E;
Journal of Medicinal Chemistry. 2016 :-. doi:
PMID: 27617704

Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit.
Gerstenberger, BS; Trzupek, JD; Tallant, C; Fedorov, O; Filippakopoulos, P; Brennan, PE; Fedele, V; Martin, S; Picaud, S; Rogers, C; Parikh, M; Taylor, A; Samas, B; O'Mahony, A; Berg, E; Pallares, G; Torrey, AD; Treiber, DK; Samardjiev, IJ; Nasipak, BT; Padilla-Benavides, T; Wu, Q; Imbalzano, AN; Nickerson, JA; Bunnage, ME; Müller, S; Knapp, S; Owen, DR;
Journal of Medicinal Chemistry. 2016 59:4800-4811. doi:
PMID: 27115555

Dual Targeting of Bromodomain and Extraterminal Domain Proteins, and WNT or MAPK Signaling, Inhibits c-MYC Expression and Proliferation of Colorectal Cancer Cells.
Tögel, L; Nightingale, R; Chueh, AC; Jayachandran, A; Tran, H; Phesse, T; Wu, R; Sieber, OM; Arango, D; Dhillon, AS; Dawson, MA; Diez-Dacal, B; Gahman, TC; Filippakopoulos, P; Shiau, AK; Mariadason, JM;
Molecular Cancer Therapeutics. 2016 15:1217-1226. doi:
PMID: 26983878

2015

Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy.
Picaud, S; Fedorov, O; Thanasopoulou, A; Leonards, K; Jones, K; Meier, J; Olzscha, H; Monteiro, O; Martin, S; Philpott, M; Tumber, A; Filippakopoulos, P; Yapp, C; Wells, C; Che, KH; Bannister, A; Robson, S; Kumar, U; Parr, N; Lee, K; Lugo, D; Jeffrey, P; Taylor, S; Vecellio, ML; Bountra, C; Brennan, PE; O'Mahony, A; Velichko, S; Müller, S; Hay, D; Daniels, DL; Urh, M; La Thangue, NB; Kouzarides, T; Prinjha, R; Schwaller, J; Knapp, S;
Cancer Research. 2015 75:5106-5119. doi:
PMID: 26552700

Regulation of signaling interactomes in cancer
Lambert, J-P; Zhou, Y; Couzens, A; Tsou, C-C; Picaud, S; Ivosev, G; Tate, S; Nesvizhskii, A; Filippakopoulos, P; Gingras, A-C;
Cancer Research. 2015 75:-. doi: 10.1158/1538-7445.COMPSYSBIO-IA19
PMID:

Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance.
Fedorov, O; Castex, J; Tallant, C; Owen, DR; Martin, S; Aldeghi, M; Monteiro, O; Filippakopoulos, P; Picaud, S; Trzupek, JD; Gerstenberger, BS; Bountra, C; Willmann, D; Wells, C; Philpott, M; Rogers, C; Biggin, PC; Brennan, PE; Bunnage, ME; Schüle, R; Günther, T; Knapp, S; Müller, S;
Science Advances. 2015 1:e1500723-. doi:
PMID: 26702435

BET Inhibition Upregulates SIRT1 and Alleviates Inflammatory Responses.
Kokkola, T; Suuronen, T; Pesonen, M; Filippakopoulos, P; Salminen, A; Jarho, EM; Lahtela-Kakkonen, M;
ChemBioChem: a European journal of chemical biology. 2015 16:1997-2001. doi: 10.1002/cbic.201500272
PMID: 26212199

Beating the odds: BETs in disease.
Wang, CY; Filippakopoulos, P;
Trends in Biochemical Sciences. 2015 40:468-479. doi:
PMID: 26145250

9H-purine scaffold reveals induced-fit pocket plasticity of the BRD9 bromodomain.
Picaud, S; Strocchia, M; Terracciano, S; Lauro, G; Mendez, J; Daniels, DL; Riccio, R; Bifulco, G; Bruno, I; Filippakopoulos, P;
Journal of Medicinal Chemistry. 2015 58:2718-2736. doi:
PMID: 25703523

SPOTing Acetyl-Lysine Dependent Interactions.
Picaud, S; Filippakopoulos, P;
Microarrays. 2015 4:370-388. doi:
PMID: 27600229

Genome-wide profiling of molecular recognition of histone PTMs
Filippakopoulos, P; Knapp, S;
. 2015 :173-184. doi: 10.1007/978-3-319-18102-8_8
PMID:

Molecular basis of histone tail recognition by human TIP5 PHD finger and bromodomain of the chromatin remodeling complex NoRC.
Tallant, C; Valentini, E; Fedorov, O; Overvoorde, L; Ferguson, FM; Filippakopoulos, P; Svergun, DI; Knapp, S; Ciulli, A;
Structure. 2015 23:80-92. doi:
PMID: 25533489

2014

Dual kinase/bromodomain inhibitors for rationally designed polypharmacology
Quinn, ER; Ciceri, P; Mueller-Knapp, S; O'Mahony, A; Fedorov, O; Filippakopoulos, P; Hunt, JP; Lasater, EA; Pallares, G; Picaud, S; Wells, C; Wodicka, LM; Shah, NP; Knapp, S; Treiber, DK;
Cancer Research. 2014 74:-. doi: 10.1158/1538-7445.AM2014-5387
PMID:

Corrigendum: Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.
Ciceri, P; Müller, S; O'Mahony, A; Fedorov, O; Filippakopoulos, P; Hunt, JP; Lasater, EA; Pallares, G; Picaud, S; Wells, C; Martin, S; Wodicka, LM; Shah, NP; Treiber, DK; Knapp, S;
Nature Chemical Biology. 2014 10:692-. doi: 10.1038/nchembio0814-692d
PMID: 25036311

Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains.
Hay, DA; Fedorov, O; Martin, S; Singleton, DC; Tallant, C; Wells, C; Picaud, S; Philpott, M; Monteiro, OP; Rogers, CM; Conway, SJ; Rooney, TP; Tumber, A; Yapp, C; Filippakopoulos, P; Bunnage, ME; Müller, S; Knapp, S; Schofield, CJ; Brennan, PE;
Journal of the American Chemical Society. 2014 136:9308-9319. doi:
PMID: 24946055

A series of potent CREBBP bromodomain ligands reveals an induced-fit pocket stabilized by a cation-π interaction.
Rooney, TP; Filippakopoulos, P; Fedorov, O; Picaud, S; Cortopassi, WA; Hay, DA; Martin, S; Tumber, A; Rogers, CM; Philpott, M; Wang, M; Thompson, AL; Heightman, TD; Pryde, DC; Cook, A; Paton, RS; Müller, S; Knapp, S; Brennan, PE; Conway, SJ;
Angewandte Chemie International Edition. 2014 53:6126-6130. doi:
PMID: 24821300

Targeting bromodomains: epigenetic readers of lysine acetylation.
Filippakopoulos, P; Knapp, S;
Nature Reviews Drug Discovery. 2014 13:337-356. doi:
PMID: 24751816

Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.
Ciceri, P; Müller, S; O'Mahony, A; Fedorov, O; Filippakopoulos, P; Hunt, JP; Lasater, EA; Pallares, G; Picaud, S; Wells, C; Martin, S; Wodicka, LM; Shah, NP; Treiber, DK; Knapp, S;
Nature Chemical Biology. 2014 10:305-312. doi:
PMID: 24584101

[1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains.
Fedorov, O; Lingard, H; Wells, C; Monteiro, OP; Picaud, S; Keates, T; Yapp, C; Philpott, M; Martin, SJ; Felletar, I; Marsden, BD; Filippakopoulos, P; Müller, S; Knapp, S; Brennan, PE;
Journal of Medicinal Chemistry. 2014 57:462-476. doi:
PMID: 24313754

2013

RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.
Picaud, S; Wells, C; Felletar, I; Brotherton, D; Martin, S; Savitsky, P; Diez-Dacal, B; Philpott, M; Bountra, C; Lingard, H; Fedorov, O; Müller, S; Brennan, PE; Knapp, S; Filippakopoulos, P;
Proceedings of the National Academy of Sciences of USA. 2013 110:19754-19759. doi:
PMID: 24248379

Discovery of novel small-molecule inhibitors of BRD4 using structure-based virtual screening.
Vidler, LR; Filippakopoulos, P; Fedorov, O; Picaud, S; Martin, S; Tomsett, M; Woodward, H; Brown, N; Knapp, S; Hoelder, S;
Journal of Medicinal Chemistry. 2013 56:8073-8088. doi:
PMID: 24090311

Chemical probes for bromodomains outside the BET family
Brennan, PE; Martin, SJ; Monteiro, O; Fedorov, O; Knapp, S; Hay, D; Wells, C; Filippakopoulos, P; Picaud, S; Muller-Knapp, S; Keates, T; Yapp, C; Philpott, M; Schofield, C; Burgess-Brown, N; Shrestha, L; Strain-Damerell, C;
ACS National Meeting Book of Abstracts. 2013 246:-. doi:
PMID:

PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains.
Picaud, S; Da Costa, D; Thanasopoulou, A; Filippakopoulos, P; Fish, PV; Philpott, M; Fedorov, O; Brennan, P; Bunnage, ME; Owen, DR; Bradner, JE; Taniere, P; O'Sullivan, B; Müller, S; Schwaller, J; Stankovic, T; Knapp, S;
Cancer Research. 2013 73:3336-3346. doi:
PMID: 23576556

Constitutively active ALK2 receptor mutants require type II receptor cooperation.
Bagarova, J; Vonner, AJ; Armstrong, KA; Börgermann, J; Lai, CS; Deng, DY; Beppu, H; Alfano, I; Filippakopoulos, P; Morrell, NW; Bullock, AN; Knaus, P; Mishina, Y; Yu, PB;
Molecular and Cellular Biology. 2013 33:2413-2424. doi: 10.1128/MCB.01595-12
PMID: 23572558

Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.
Hewings, DS; Fedorov, O; Filippakopoulos, P; Martin, S; Picaud, S; Tumber, A; Wells, C; Olcina, MM; Freeman, K; Gill, A; Ritchie, AJ; Sheppard, DW; Russell, AJ; Hammond, EM; Knapp, S; Brennan, PE; Conway, SJ;
Journal of Medicinal Chemistry. 2013 56:3217-3227. doi:
PMID: 23517011

Novel Inverse Binding Mode of Indirubin Derivatives Yields Improved Selectivity for DYRK Kinases.
Myrianthopoulos, V; Kritsanida, M; Gaboriaud-Kolar, N; Magiatis, P; Ferandin, Y; Durieu, E; Lozach, O; Cappel, D; Soundararajan, M; Filippakopoulos, P; Sherman, W; Knapp, S; Meijer, L; Mikros, E; Skaltsounis, AL;
ACS Medicinal Chemistry Letters. 2013 4:22-26. doi: 10.1021/ml300207a
PMID: 23336033

Stimulation of Hepatic Apolipoprotein A-I Production by Novel Thieno-Triazolodiazepines: Roles of the Classical Benzodiazepine Receptor, PAF Receptor, and Bromodomain Binding.
Kempen, HJ; Bellus, D; Fedorov, O; Nicklisch, S; Filippakopoulos, P; Picaud, S; Knapp, S;
Lipid Insights. 2013 6:47-54. doi:
PMID: 25278768

The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains.
Hay, D; Fedorov, O; Filippakopoulos, P; Martin, S; Philpott, M; Picaud, S; Hewings, DS; Uttakar, S; Heightman, TD; Conway, SJ; Knapp, S; Brennan, PE;
MedChemComm. 2013 4:140-144. doi:
PMID: 26682033

2012

Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit.
Fish, PV; Filippakopoulos, P; Bish, G; Brennan, PE; Bunnage, ME; Cook, AS; Federov, O; Gerstenberger, BS; Jones, H; Knapp, S; Marsden, B; Nocka, K; Owen, DR; Philpott, M; Picaud, S; Primiano, MJ; Ralph, MJ; Sciammetta, N; Trzupek, JD;
Journal of Medicinal Chemistry. 2012 55:9831-9837. doi:
PMID: 23095041

Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.
Tahtouh, T; Elkins, JM; Filippakopoulos, P; Soundararajan, M; Burgy, G; Durieu, E; Cochet, C; Schmid, RS; Lo, DC; Delhommel, F; Oberholzer, AE; Pearl, LH; Carreaux, F; Bazureau, JP; Knapp, S; Meijer, L;
Journal of Medicinal Chemistry. 2012 55:9312-9330. doi: 10.1021/jm301034u
PMID: 22998443

Developing small molecule inhibitors of the CREBBP bromodomain-histone interaction
Rooney, TPC; Fedorov, O; Filippakopoulos, P; Wang, M; Philpott, M; Cook, A; Heightman, TD; Knapp, S; Pryde, D; Brennan, PE; Conway, SJ;
ACS National Meeting Book of Abstracts. 2012 244:-. doi:
PMID:

Small-molecule inhibition of BRDT for male contraception.
Matzuk, MM; McKeown, MR; Filippakopoulos, P; Li, Q; Ma, L; Agno, JE; Lemieux, ME; Picaud, S; Yu, RN; Qi, J; Knapp, S; Bradner, JE;
Cell. 2012 150:673-684. doi: 10.1016/j.cell.2012.06.045
PMID: 22901802

Small-molecule inhibitors of the c-Fes protein-tyrosine kinase.
Hellwig, S; Miduturu, CV; Kanda, S; Zhang, J; Filippakopoulos, P; Salah, E; Deng, X; Choi, HG; Zhou, W; Hur, W; Knapp, S; Gray, NS; Smithgall, TE;
Chemistry and Biology. 2012 19:529-540. doi: 10.1016/j.chembiol.2012.01.020
PMID: 22520759

3,5-Dimethylisoxazoles inhibit the bromodomain-histone protein-protein interaction
Hewings, DS; Wang, M; Philpott, M; Fedorov, O; Uttarkar, S; Filippakopoulos, P; Picaud, S; Vuppusetty, C; Marsden, B; Heightman, TD; Knapp, S; Brennan, P; Conway, SJ;
ACS National Meeting Book of Abstracts. 2012 243:-. doi:
PMID:

Developing chemical probes for the BET bromodomains
Hewings, DS; Wang, M; Philpott, M; Fedorov, O; Uttarkar, S; Filippakopoulos, P; Picaud, S; Vuppusetty, C; Marsden, B; Heightman, TD; Knapp, S; Brennan, P; Conway, SJ;
ACS National Meeting Book of Abstracts. 2012 243:-. doi:
PMID:

The bromodomain interaction module
Filippakopoulos, P; Knapp, S;
FEBS Letters. 2012 586:2692-2704. doi: 10.1016/j.febslet.2012.04.045
PMID:

The therapeutic potential of acetyl-lysine and methyl-lysine effector domains
Brennan, P; Filippakopoulos, P; Knapp, S;
Drug Discovery Today: Therapeutic Strategies. 2012 :-. doi:
PMID:

The therapeutic potential of acetyl-lysine and methyl-lysine effector domains
Brennan, P; Filippakopoulos, P; Knapp, S;
Drug Discovery Today: Therapeutic Strategies. 2012 9:-. doi: 10.1016/j.ddstr.2012.04.001
PMID:

7,8-dichloro-1-oxo-β-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.
Huber, K; Brault, L; Fedorov, O; Gasser, C; Filippakopoulos, P; Bullock, AN; Fabbro, D; Trappe, J; Schwaller, J; Knapp, S; Bracher, F;
Journal of Medicinal Chemistry. 2012 55:403-413. doi:
PMID: 22136433

Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
Filippakopoulos, P; Picaud, S; Fedorov, O; Keller, M; Wrobel, M; Morgenstern, O; Bracher, F; Knapp, S;
Bioorganic and Medicinal Chemistry. 2012 20:1878-1886. doi:
PMID: 22137933

2011

Bromodomains as therapeutic targets.
Muller, S; Filippakopoulos, P; Knapp, S;
Expert Reviews in Molecular Medicine. 2011 13:e29-. doi: 10.1017/S1462399411001992
PMID: 21933453

High-throughput kinase profiling: a more efficient approach toward the discovery of new kinase inhibitors.
Miduturu, CV; Deng, X; Kwiatkowski, N; Yang, W; Brault, L; Filippakopoulos, P; Chung, E; Yang, Q; Schwaller, J; Knapp, S; King, RW; Lee, JD; Herrgard, S; Zarrinkar, P; Gray, NS;
Chemistry and Biology. 2011 18:868-879. doi: 10.1016/j.chembiol.2011.05.010
PMID: 21802008

Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing.
Debdab, M; Carreaux, F; Renault, S; Soundararajan, M; Fedorov, O; Filippakopoulos, P; Lozach, O; Babault, L; Tahtouh, T; Baratte, B; Ogawa, Y; Hagiwara, M; Eisenreich, A; Rauch, U; Knapp, S; Meijer, L; Bazureau, JP;
Journal of Medicinal Chemistry. 2011 54:4172-4186. doi:
PMID: 21615147

Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing.
Fedorov, O; Huber, K; Eisenreich, A; Filippakopoulos, P; King, O; Bullock, AN; Szklarczyk, D; Jensen, LJ; Fabbro, D; Trappe, J; Rauch, U; Bracher, F; Knapp, S;
Chemistry and Biology. 2011 18:67-76. doi:
PMID: 21276940

Structurally sophisticated octahedral metal complexes as highly selective protein kinase inhibitors
Feng, L; Geisselbrecht, Y; Blanck, S; Wilbuer, A; Atilla-Gokcumen, GE; Filippakopoulos, P; Kräling, K; Celik, MA; Harms, K; Maksimoska, J; Marmorstein, R; Frenking, G; Knapp, S; Essen, LO; Meggers, E;
Journal of the American Chemical Society. 2011 133:5976-5986. doi: 10.1021/ja1112996
PMID: 21446733

Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery.
Philpott, M; Yang, J; Tumber, T; Fedorov, O; Uttarkar, S; Filippakopoulos, P; Picaud, S; Keates, T; Felletar, I; Ciulli, A; Knapp, S; Heightman, TD;
Molecular Biosystems. 2011 7:2899-2908. doi:
PMID:

The crystal structure of human GLRX5: iron-sulfur cluster co-ordination, tetrameric assembly and monomer activity.
Johansson, C; Roos, AK; Montano, SJ; Sengupta, R; Filippakopoulos, P; Guo, K; von Delft, F; Holmgren, A; Oppermann, U; Kavanagh, KL;
Biochemical Journal. 2011 433:303-311. doi: 10.1042/BJ20101286
PMID: 21029046

2010

Selective inhibition of BET bromodomains.
Filippakopoulos, P; Qi, J; Picaud, S; Shen, Y; Smith, WB; Fedorov, O; Morse, EM; Keates, T; Hickman, TT; Felletar, I; Philpott, M; Munro, S; McKeown, MR; Wang, Y; Christie, AL; West, N; Cameron, MJ; Schwartz, B; Heightman, TD; La Thangue, N; French, CA; Wiest, O; Kung, AL; Knapp, S; Bradner, JE;
Nature. 2010 468:1067-1073. doi:
PMID: 20871596

Structural basis for Par-4 recognition by the SPRY domain- and SOCS box-containing proteins SPSB1, SPSB2, and SPSB4.
Filippakopoulos, P; Low, A; Sharpe, TD; Uppenberg, J; Yao, S; Kuang, Z; Savitsky, P; Lewis, RS; Nicholson, SE; Norton, RS; Bullock, AN;
Journal of Molecular Biology. 2010 401:389-402. doi: 10.1016/j.jmb.2010.06.017
PMID: 20561531

Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function.
Kwiatkowski, N; Jelluma, N; Filippakopoulos, P; Soundararajan, M; Manak, MS; Kwon, M; Choi, HG; Sim, T; Deveraux, QL; Rottmann, S; Pellman, D; Shah, JV; Kops, GJ; Knapp, S; Gray, NS;
Nature Chemical Biology. 2010 6:359-368. doi: 10.1038/nchembio.345
PMID: 20383151

New potent dual inhibitors of CK2 and Pim kinases: discovery and structural insights.
López-Ramos, M; Prudent, R; Moucadel, V; Sautel, CF; Barette, C; Lafanechère, L; Mouawad, L; Grierson, D; Schmidt, F; Florent, JC; Filippakopoulos, P; Bullock, AN; Knapp, S; Reiser, JB; Cochet, C;
The FASEB Journal. 2010 24:3171-3185. doi: 10.1096/fj.09-143743
PMID: 20400536

2009

SH2 domains: modulators of nonreceptor tyrosine kinase activity.
Filippakopoulos, P; Müller, S; Knapp, S;
Current Opinion in Structural Biology. 2009 19:643-649. doi: 10.1016/j.sbi.2009.10.001
PMID: 19926274

Structure and functional characterization of the atypical human kinase haspin.
Eswaran, J; Patnaik, D; Filippakopoulos, P; Wang, F; Stein, RL; Murray, JW; Higgins, JM; Knapp, S;
Proceedings of the National Academy of Sciences of USA. 2009 106:20198-20203. doi: 10.1073/pnas.0901989106
PMID: 19918057

Synthesis, kinase inhibitory potencies, and in vitro antiproliferative evaluation of new Pim kinase inhibitors.
Akué-Gédu, R; Rossignol, E; Azzaro, S; Knapp, S; Filippakopoulos, P; Bullock, AN; Bain, J; Cohen, P; Prudhomme, M; Anizon, F; Moreau, P;
Journal of Medicinal Chemistry. 2009 52:6369-6381. doi: 10.1021/jm901018f
PMID: 19788246

Large-scale structural analysis of the classical human protein tyrosine phosphatome.
Barr, AJ; Ugochukwu, E; Lee, WH; King, ON; Filippakopoulos, P; Alfano, I; Savitsky, P; Burgess-Brown, NA; Müller, S; Knapp, S;
Cell. 2009 136:352-363. doi: 10.1016/j.cell.2008.11.038
PMID: 19167335

Erratum: Extremely tight binding of a ruthenium complex to glycogen synthase kinase 3 (ChemBioChem (2008) vol. 9 (2933-2936))
Atilla-Gokcumen, GE; Pagano, N; Streu, C; Maksimoska, J; Filippakopoulos, P; Knapp, S; Meggers, E;
ChemBioChem: a European journal of chemical biology. 2009 10:198-. doi: 10.1002/cbic.200800489
PMID:

2008

Extremely tight binding of a ruthenium complex to glycogen synthase kinase 3.
Atilla-Gokcumen, GE; Pagano, N; Streu, C; Maksimoska, J; Filippakopoulos, P; Knapp, S; Meggers, E;
ChemBioChem: a European journal of chemical biology. 2008 9:2933-2936. doi: 10.1002/cbic.200800489
PMID: 19035373

Structural coupling of SH2-kinase domains links Fes and Abl substrate recognition and kinase activation.
Filippakopoulos, P; Kofler, M; Hantschel, O; Gish, GD; Grebien, F; Salah, E; Neudecker, P; Kay, LE; Turk, BE; Superti-Furga, G; Pawson, T; Knapp, S;
Cell. 2008 134:793-803. doi: 10.1016/j.cell.2008.07.047
PMID: 18775312

Similar biological activities of two isostructural ruthenium and osmium complexes.
Maksimoska, J; Williams, DS; Atilla-Gokcumen, GE; Smalley, KS; Carroll, PJ; Webster, RD; Filippakopoulos, P; Knapp, S; Herlyn, M; Meggers, E;
Chemistry: A European Journal. 2008 14:4816-4822. doi: 10.1002/chem.200800294
PMID: 18425743

2007

Structural and functional characterization of the human protein kinase ASK1.
Bunkoczi, G; Salah, E; Filippakopoulos, P; Fedorov, O; Müller, S; Sobott, F; Parker, SA; Zhang, H; Min, W; Turk, BE; Knapp, S;
Structure. 2007 15:1215-1226. doi:
PMID: 17937911

Structural analysis identifies imidazo[1,2-b]pyridazines as PIM kinase inhibitors with in vitro antileukemic activity.
Pogacic, V; Bullock, AN; Fedorov, O; Filippakopoulos, P; Gasser, C; Biondi, A; Meyer-Monard, S; Knapp, S; Schwaller, J;
Cancer Research. 2007 67:6916-6924. doi:
PMID: 17638903

Crystal Structures of the p21-activated kinases PAK4, PAK5, and PAK6 reveal catalytic domain plasticity of active group II PAKs.
Eswaran, J; Lee, WH; Debreczeni, JE; Filippakopoulos, P; Turnbull, A; Fedorov, O; Deacon, SW; Peterson, JR; Knapp, S;
Structure. 2007 15:201-213. doi:
PMID: 17292838

2004

Crown-ether functionalized Co(III) sailicylideneimine complexes as ditopic carriers for the facilitated transport of zwitterions across a chloroform barrier.
Filippakopoulos, P; Coucouvanis, D;
ACS National Meeting Book of Abstracts. 2004 227:U1294-U1294. doi:
PMID:

1998

CuII-herbicide complexes: Structure and bioactivity
Psomas, G; Dendrinou-Samara, C; Philippakopoulos, P; Tangoulis, V; Raptopoulou, CP; Samaras, E; Kessissoglou, DP;
Inorganica Chimica Acta. 1998 272:24-32. doi:
PMID:

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