List of works - Panagis Filippakopoulos

3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands

scientific article

7,8-Dichloro-1-oxo-β-carbolines as a Versatile Scaffold for the Development of Potent and Selective Kinase Inhibitors with Unusual Binding Modes

scientific article

9H-purine scaffold reveals induced-fit pocket plasticity of the BRD9 bromodomain

scientific article

A TFEB nuclear export signal integrates amino acid supply and glucose availability.

scientific article published on 11 July 2018

A Tail-Based Mechanism Drives Nucleosome Demethylation by the LSD2/NPAC Multimeric Complex

scientific article published on 01 April 2019

A chemical toolbox for the study of bromodomains and epigenetic signaling

scientific article published on 23 April 2019

A series of potent CREBBP bromodomain ligands reveals an induced-fit pocket stabilized by a cation-π interaction

scientific article published on 12 May 2014

BET Inhibition Upregulates SIRT1 and Alleviates Inflammatory Responses

scientific article published on 25 July 2015

BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability

scientific article published on 15 May 2018

BET inhibition disrupts transcription but retains enhancer-promoter contact

scientific article published on 11 January 2021

BRAF/MAPK and GSK3 signaling converges to control MITF nuclear export

article published in the Proceedings of the National Academy of Sciences of the United States of America

Beating the odds: BETs in disease

scientific article published on 03 July 2015

Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family

scientific article

Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery

scientific article published in 2011

Constitutively active ALK2 receptor mutants require type II receptor cooperation

scientific article published on 09 April 2013

Crystal Structures of the p21-Activated Kinases PAK4, PAK5, and PAK6 Reveal Catalytic Domain Plasticity of Active Group II PAKs

scientific article

Development and preclinical validation of a novel covalent ubiquitin receptor Rpn13 degrader in multiple myeloma

scientific article published on 08 April 2019

Direct interaction between the PRDM3 and PRDM16 tumor suppressors and the NuRD chromatin remodeling complex

scientific article published on 20 November 2018

Discovery and Optimization of a Selective Ligand for the Switch/Sucrose Nonfermenting-Related Bromodomains of Polybromo Protein-1 by the Use of Virtual Screening and Hydration Analysis

scientific article

Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains

scientific article (publication date: 2 July 2014)

Discovery of Novel Small-Molecule Inhibitors of BRD4 Using Structure-Based Virtual Screening

scientific article

Dissecting the Role of BET Bromodomain Proteins BRD2 and BRD4 in Human NK Cell Function

scientific article published on 26 February 2021

Dual Targeting of Bromodomain and Extraterminal Domain Proteins, and WNT or MAPK Signaling, Inhibits c-MYC Expression and Proliferation of Colorectal Cancer Cells.

scientific article published on 16 March 2016

Dual kinase-bromodomain inhibitors for rationally designed polypharmacology

scientific article

Effects of epigenetic pathway inhibitors on corticotroph tumour AtT20 cells

scientific article published on 01 March 2020

Emerging tools to investigate bromodomain functions

scientific article published on 11 November 2019

Epigenetic pathway inhibitors represent potential drugs for treating pancreatic and bronchial neuroendocrine tumors.

scientific article published on 15 May 2017

Epigenetic targeting of bromodomain protein BRD4 counteracts cancer cachexia and prolongs survival.

scientific article published on 22 November 2017

Erratum: Corrigendum: Dual kinase-bromodomain inhibitors for rationally designed polypharmacology

scholarly article published in Nature Chemical Biology

Evaluation of linker length effects on a BET bromodomain probe

scientific article published on 01 August 2019

Extremely Tight Binding of a Ruthenium Complex to Glycogen Synthase Kinase 3

scientific article

Functions of bromodomain-containing proteins and their roles in homeostasis and cancer.

scientific article published on 5 January 2017

Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy

scientific article

Genome-Wide Profiling of Molecular Recognition of Histone PTMs

article

High-throughput kinase profiling: a more efficient approach toward the discovery of new kinase inhibitors

scientific article

Histone recognition and large-scale structural analysis of the human bromodomain family

scientific article

Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit

scientific article

Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit

scientific article

Identification of a Major Determinant for Serine-Threonine Kinase Phosphoacceptor Specificity

scientific article

Interactome Rewiring Following Pharmacological Targeting of BET Bromodomains

scientific article published on 13 December 2018

Large-scale structural analysis of the classical human protein tyrosine phosphatome

scientific article

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.

scientific article published on 26 May 2011

MOB1 Mediated Phospho-recognition in the Core Mammalian Hippo Pathway

scientific article

Molecular basis of histone tail recognition by human TIP5 PHD finger and bromodomain of the chromatin remodeling complex NoRC.

scientific article published on 18 December 2014

Multivalent Histone and DNA Engagement by a PHD/BRD/PWWP Triple Reader Cassette Recruits ZMYND8 to K14ac-Rich Chromatin

scientific article published on December 2016

New potent dual inhibitors of CK2 and Pim kinases: discovery and structural insights

scientific article

Novel Inverse Binding Mode of Indirubin Derivatives Yields Improved Selectivity for DYRK Kinases

scientific article published on November 2012

Nut Directs p300-Dependent, Genome-Wide H4 Hyperacetylation in Male Germ Cells

scientific article published on 01 September 2018

Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

scientific article

PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains

scientific article

Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia.

scientific article published on 12 October 2016

RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain

scientific article

SH2 domains: modulators of nonreceptor tyrosine kinase activity

scientific article

SPOTing Acetyl-Lysine Dependent Interactions

scientific article

Selective inhibition of BET bromodomains

scientific article

Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B

scientific article

Similar Biological Activities of Two Isostructural Ruthenium and Osmium Complexes

scientific article

Small molecule inhibitors reveal an indispensable scaffolding role of RIPK2 in NOD2 signaling

scientific article published on 19 July 2018

Small-Molecule Inhibitors of the c-Fes Protein-Tyrosine Kinase

scientific article

Small-molecule inhibition of BRDT for male contraception

scientific article

Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function

scientific article

Specific CLK Inhibitors from a Novel Chemotype for Regulation of Alternative Splicing

scientific article

Stimulation of Hepatic Apolipoprotein A-I Production by Novel Thieno-Triazolodiazepines: Roles of the Classical Benzodiazepine Receptor, PAF Receptor, and Bromodomain Binding

scientific article published on 22 December 2013

Structural Basis for Recruitment of DAPK1 to the KLHL20 E3 Ligase

scientific article published on 03 July 2019

Structural Genomics and Drug Discovery for Chromatin-Related Protein Complexes Involved in Histone Tail Recognition

Structural analysis identifies imidazo[1,2-b]pyridazines as PIM kinase inhibitors with in vitro antileukemic activity

scientific article

Structural and Functional Characterization of the Human Protein Kinase ASK1

scientific article

Structural basis for Par-4 recognition by the SPRY domain- and SOCS box-containing proteins SPSB1, SPSB2, and SPSB4

scientific article

Structural coupling of SH2-kinase domains links Fes and Abl substrate recognition and kinase activation

scientific article

Structurally Sophisticated Octahedral Metal Complexes as Highly Selective Protein Kinase Inhibitors

scientific article

Structure and functional characterization of the atypical human kinase haspin

scientific article

Structures of Down Syndrome Kinases, DYRKs, Reveal Mechanisms of Kinase Activation and Substrate Recognition

scientific article

Structures of PGAM5 Provide Insight into Active Site Plasticity and Multimeric Assembly

scientific article published on 10 June 2017

Synthesis, kinase inhibitory potencies, and in vitro antiproliferative evaluation of new Pim kinase inhibitors

scientific article

Targeting bromodomains: epigenetic readers of lysine acetylation

scientific article (publication date: May 2014)

The C-terminal extension landscape of naturally presented HLA-I ligands

article published in the Proceedings of the National Academy of Sciences of the United States of America

The bromodomain interaction module ⬇️

scientific article published on 03 May 2012

The crystal structure of human GLRX5: iron-sulfur cluster co-ordination, tetrameric assembly and monomer activity

scientific article

The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains

scientific article published on January 2013

The structure of nontypeable Haemophilus influenzae SapA in a closed conformation reveals a constricted ligand-binding cavity and a novel RNA binding motif

scientific article published on 15 October 2021

The therapeutic potential of acetyl-lysine and methyl-lysine effector domains

Tryptophan-mediated interactions between tristetraprolin and the CNOT9 subunit are required for CCR4-NOT deadenylase complex recruitment.

scientific article published on 29 December 2017

What Is the BET on Solid Tumors?

scientific article published on 30 May 2018

[1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains

scientific article

List of works by Panagis Filippakopoulos

3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands

7,8-Dichloro-1-oxo-β-carbolines as a Versatile Scaffold for the Development of Potent and Selective Kinase Inhibitors with Unusual Binding Modes

9H-purine scaffold reveals induced-fit pocket plasticity of the BRD9 bromodomain

A TFEB nuclear export signal integrates amino acid supply and glucose availability.

A Tail-Based Mechanism Drives Nucleosome Demethylation by the LSD2/NPAC Multimeric Complex

A chemical toolbox for the study of bromodomains and epigenetic signaling

A series of potent CREBBP bromodomain ligands reveals an induced-fit pocket stabilized by a cation-π interaction

BET Inhibition Upregulates SIRT1 and Alleviates Inflammatory Responses

BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability

BET inhibition disrupts transcription but retains enhancer-promoter contact

BRAF/MAPK and GSK3 signaling converges to control MITF nuclear export

Beating the odds: BETs in disease

Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family

Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery

Constitutively active ALK2 receptor mutants require type II receptor cooperation

Crystal Structures of the p21-Activated Kinases PAK4, PAK5, and PAK6 Reveal Catalytic Domain Plasticity of Active Group II PAKs

Development and preclinical validation of a novel covalent ubiquitin receptor Rpn13 degrader in multiple myeloma

Direct interaction between the PRDM3 and PRDM16 tumor suppressors and the NuRD chromatin remodeling complex

Discovery and Optimization of a Selective Ligand for the Switch/Sucrose Nonfermenting-Related Bromodomains of Polybromo Protein-1 by the Use of Virtual Screening and Hydration Analysis

Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains

Discovery of Novel Small-Molecule Inhibitors of BRD4 Using Structure-Based Virtual Screening

Dissecting the Role of BET Bromodomain Proteins BRD2 and BRD4 in Human NK Cell Function

Dual Targeting of Bromodomain and Extraterminal Domain Proteins, and WNT or MAPK Signaling, Inhibits c-MYC Expression and Proliferation of Colorectal Cancer Cells.

Dual kinase-bromodomain inhibitors for rationally designed polypharmacology

Effects of epigenetic pathway inhibitors on corticotroph tumour AtT20 cells

Emerging tools to investigate bromodomain functions

Epigenetic pathway inhibitors represent potential drugs for treating pancreatic and bronchial neuroendocrine tumors.

Epigenetic targeting of bromodomain protein BRD4 counteracts cancer cachexia and prolongs survival.

Erratum: Corrigendum: Dual kinase-bromodomain inhibitors for rationally designed polypharmacology

Evaluation of linker length effects on a BET bromodomain probe

Extremely Tight Binding of a Ruthenium Complex to Glycogen Synthase Kinase 3

Functions of bromodomain-containing proteins and their roles in homeostasis and cancer.

Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy

Genome-Wide Profiling of Molecular Recognition of Histone PTMs

High-throughput kinase profiling: a more efficient approach toward the discovery of new kinase inhibitors

Histone recognition and large-scale structural analysis of the human bromodomain family

Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit

Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit

Identification of a Major Determinant for Serine-Threonine Kinase Phosphoacceptor Specificity

Interactome Rewiring Following Pharmacological Targeting of BET Bromodomains

Large-scale structural analysis of the classical human protein tyrosine phosphatome

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.

MOB1 Mediated Phospho-recognition in the Core Mammalian Hippo Pathway

Molecular basis of histone tail recognition by human TIP5 PHD finger and bromodomain of the chromatin remodeling complex NoRC.

Multivalent Histone and DNA Engagement by a PHD/BRD/PWWP Triple Reader Cassette Recruits ZMYND8 to K14ac-Rich Chromatin

New potent dual inhibitors of CK2 and Pim kinases: discovery and structural insights

Novel Inverse Binding Mode of Indirubin Derivatives Yields Improved Selectivity for DYRK Kinases

Nut Directs p300-Dependent, Genome-Wide H4 Hyperacetylation in Male Germ Cells

Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains

Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia.

RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain

SH2 domains: modulators of nonreceptor tyrosine kinase activity

SPOTing Acetyl-Lysine Dependent Interactions

Selective inhibition of BET bromodomains

Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B

Similar Biological Activities of Two Isostructural Ruthenium and Osmium Complexes

Small molecule inhibitors reveal an indispensable scaffolding role of RIPK2 in NOD2 signaling

Small-Molecule Inhibitors of the c-Fes Protein-Tyrosine Kinase

Small-molecule inhibition of BRDT for male contraception

Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function

Specific CLK Inhibitors from a Novel Chemotype for Regulation of Alternative Splicing

Stimulation of Hepatic Apolipoprotein A-I Production by Novel Thieno-Triazolodiazepines: Roles of the Classical Benzodiazepine Receptor, PAF Receptor, and Bromodomain Binding

Structural Basis for Recruitment of DAPK1 to the KLHL20 E3 Ligase

Structural Genomics and Drug Discovery for Chromatin-Related Protein Complexes Involved in Histone Tail Recognition

Structural analysis identifies imidazo[1,2-b]pyridazines as PIM kinase inhibitors with in vitro antileukemic activity

Structural and Functional Characterization of the Human Protein Kinase ASK1

Structural basis for Par-4 recognition by the SPRY domain- and SOCS box-containing proteins SPSB1, SPSB2, and SPSB4

Structural coupling of SH2-kinase domains links Fes and Abl substrate recognition and kinase activation

Structurally Sophisticated Octahedral Metal Complexes as Highly Selective Protein Kinase Inhibitors

Structure and functional characterization of the atypical human kinase haspin

Structures of Down Syndrome Kinases, DYRKs, Reveal Mechanisms of Kinase Activation and Substrate Recognition

Structures of PGAM5 Provide Insight into Active Site Plasticity and Multimeric Assembly

Synthesis, kinase inhibitory potencies, and in vitro antiproliferative evaluation of new Pim kinase inhibitors

Targeting bromodomains: epigenetic readers of lysine acetylation

The C-terminal extension landscape of naturally presented HLA-I ligands

The bromodomain interaction module ⬇️

The crystal structure of human GLRX5: iron-sulfur cluster co-ordination, tetrameric assembly and monomer activity

The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains