List of works - Paul E. Brennan

5-Carboxy-8-hydroxyquinoline is a Broad Spectrum 2-Oxoglutarate Oxygenase Inhibitor which Causes Iron Translocation.

scientific article published on August 2013

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

scientific article

A Chemical Probe for Tudor Domain Protein Spindlin1 to Investigate Chromatin Function

scientific article published on 15 October 2019

A chemical toolbox for the study of bromodomains and epigenetic signaling

scientific article published on 23 April 2019

A poised fragment library enables rapid synthetic expansion yielding the first reported inhibitors of PHIP(2), an atypical bromodomain† †Electronic supplementary information (ESI) available. See DOI: 10.1039/c5sc03115j.

scientific article published on 22 December 2015

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

A structure-based approach towards identification of inhibitory fragments for eleven-nineteen-leukemia protein (ENL)

scientific article published on 26 November 2018

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

article

Advances and challenges in understanding histone demethylase biology.

scientific article

An Activity-Based Probe Targeting Non-Catalytic, Highly Conserved Amino Acid Residues within Bromodomains.

scientific article published on 27 December 2018

Assessing histone demethylase inhibitors in cells: lessons learned.

scientific article

BET inhibition as a new strategy for the treatment of gastric cancer

scientific article

BRD3 and BRD4 BET Bromodomain Proteins Differentially Regulate Skeletal Myogenesis.

scientific article published on 21 July 2017

Bench-Stable Transfer Reagent Facilitates the Generation of Trifluoromethyl-sulfonimidamides

scientific article published on 06 July 2018

Betti reaction enables efficient synthesis of 8-hydroxyquinoline inhibitors of 2-oxoglutarate oxygenases

scientific article published in 2015

CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses

scientific article

Deciphering the true antiproliferative target of an MK2 activation inhibitor in glioblastoma.

scientific article

Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies

scientific article published on 9 January 2017

Design of a Chemical Probe for the Bromodomain and Plant Homeodomain Finger-Containing (BRPF) Family of Proteins.

scientific article published on 17 July 2017

Design, Synthesis and Characterization of Covalent KDM5 Inhibitors

scientific article published on 07 December 2018

Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors

scientific article

Development of chemical probes for the bromodomains of BRD7 and BRD9.

scientific article published on March 2016

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

scientific article (publication date: 2 July 2014)

Discovery of Pyrrolo[3,2- d]pyrimidin-4-one Derivatives as a New Class of Potent and Cell-Active Inhibitors of P300/CBP-Associated Factor Bromodomain

scientific article published on 30 April 2019

Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF.

scientific article published on 14 May 2015

Discovery of a Highly Selective Cell-Active Inhibitor of the Histone Lysine Demethylases KDM2/7.

scientific article

Discovery of a PCAF Bromodomain Chemical Probe

scientific article published on 14 December 2016

Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1)

scientific article published on 24 July 2019

Discovery of a novel allosteric inhibitor scaffold for polyadenosine-diphosphate-ribose polymerase 14 (PARP14) macrodomain 2.

scientific article published on 12 March 2018

Discovery of an MLLT1/3 YEATS Domain Chemical Probe

scientific article published on 16 November 2018

Exploring the role of water in molecular recognition: predicting protein ligandability using a combinatorial search of surface hydration sites

scientific article published in July 2016

Fragment-based hit identification: thinking in 3D.

scientific article

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

scientific article

Halogen-Aromatic π Interactions Modulate Inhibitor Residence Times.

scientific article

Highly selective inhibition of histone demethylases by de novo macrocyclic peptides

scientific article published on 06 April 2017

Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex

scientific article published on 27 April 2016

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

Identifying Small-Molecule Binding Sites for Epigenetic Proteins at Domain-Domain Interfaces.

scientific article published on 26 March 2018

Inflammatory Signaling by NOD-RIPK2 Is Inhibited by Clinically Relevant Type II Kinase Inhibitors.

scientific article

Inhibition of histone H3K27 demethylases inactivates brachyury (TBXT) and promotes chordoma cell death

scientific article published on 27 August 2020

K2P channel gating mechanisms revealed by structures of TREK-2 and a complex with Prozac

scientific article published in March 2015

Kalirin as a Novel Treatment Target for Cognitive Dysfunction in Schizophrenia

scientific article published on 20 December 2021

LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor

scientific article

Mild, calcium catalysed Beckmann rearrangements

scientific article published on 4 January 2018

Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor

scientific article published in December 2014

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

Palladium-containing perovskites: recoverable and reuseable catalysts for Suzuki couplingsElectronic supplementary information (ESI) available: experimental details. See http://www.rsc.org/suppdata/cc/b3/b308465e/

scientific article published on 01 November 2003

Plant Growth Regulator Daminozide Is a Selective Inhibitor of Human KDM2/7 Histone Demethylases

scientific article

Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells

scientific article

Potent and selective alpha1A adrenoceptor partial agonists--novel imidazole frameworks.

scientific article

Progress in the development and application of small molecule inhibitors of bromodomain-acetyl-lysine interactions

scientific article published on 27 September 2012

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

Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence.

scientific article

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

scientific article

Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening

scientific article published on 22 May 2019

Recent Progress in Histone Demethylase Inhibitors

scientific article published on 28 December 2015

Selective targeting of Bromodomains of the Bromodomain-PHD Fingers family impairs osteoclast differentiation

scientific article published on 29 August 2017

Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance.

scientific article published on 13 November 2015

Structural analysis of human KDM5B guides histone demethylase inhibitor development

scientific article

Structure of the Human Protein Kinase ZAK in Complex with Vemurafenib

scientific article

Structure-Based Design of Highly Selective Inhibitors of the CREB Binding Protein Bromodomain

scientific article published on 4 April 2017

Structure-Based Identification of Inhibitory Fragments Targeting the p300/CBP-Associated Factor Bromodomain

scientific article published on 5 January 2016

Synthesis of carbohydrate derivatives using solid-phase work-up and scavenging techniques

scientific article

TargetDB: A target information aggregation tool and tractability predictor

scientific article published on 02 September 2020

Targeting the Small GTPase Superfamily through Their Regulatory Proteins

scientific article published on 30 January 2020

The SGC beyond structural genomics: redefining the role of 3D structures by coupling genomic stratification with fragment-based discovery.

scientific article published on 8 November 2017

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

scientific article published on January 2013

The promise and peril of chemical probes

scientific article

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

scientific article

List of works by Paul E. Brennan

5-Carboxy-8-hydroxyquinoline is a Broad Spectrum 2-Oxoglutarate Oxygenase Inhibitor which Causes Iron Translocation.

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

A Chemical Probe for Tudor Domain Protein Spindlin1 to Investigate Chromatin Function

A chemical toolbox for the study of bromodomains and epigenetic signaling

A poised fragment library enables rapid synthetic expansion yielding the first reported inhibitors of PHIP(2), an atypical bromodomain† †Electronic supplementary information (ESI) available. See DOI: 10.1039/c5sc03115j.

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

A structure-based approach towards identification of inhibitory fragments for eleven-nineteen-leukemia protein (ENL)

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

Advances and challenges in understanding histone demethylase biology.

An Activity-Based Probe Targeting Non-Catalytic, Highly Conserved Amino Acid Residues within Bromodomains.

Assessing histone demethylase inhibitors in cells: lessons learned.

BET inhibition as a new strategy for the treatment of gastric cancer

BRD3 and BRD4 BET Bromodomain Proteins Differentially Regulate Skeletal Myogenesis.

Bench-Stable Transfer Reagent Facilitates the Generation of Trifluoromethyl-sulfonimidamides

Betti reaction enables efficient synthesis of 8-hydroxyquinoline inhibitors of 2-oxoglutarate oxygenases

CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses

Deciphering the true antiproliferative target of an MK2 activation inhibitor in glioblastoma.

Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies

Design of a Chemical Probe for the Bromodomain and Plant Homeodomain Finger-Containing (BRPF) Family of Proteins.

Design, Synthesis and Characterization of Covalent KDM5 Inhibitors

Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors

Development of chemical probes for the bromodomains of BRD7 and BRD9.

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

Discovery of Pyrrolo[3,2- d]pyrimidin-4-one Derivatives as a New Class of Potent and Cell-Active Inhibitors of P300/CBP-Associated Factor Bromodomain

Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF.

Discovery of a Highly Selective Cell-Active Inhibitor of the Histone Lysine Demethylases KDM2/7.

Discovery of a PCAF Bromodomain Chemical Probe

Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1)

Discovery of a novel allosteric inhibitor scaffold for polyadenosine-diphosphate-ribose polymerase 14 (PARP14) macrodomain 2.

Discovery of an MLLT1/3 YEATS Domain Chemical Probe

Exploring the role of water in molecular recognition: predicting protein ligandability using a combinatorial search of surface hydration sites

Fragment-based hit identification: thinking in 3D.

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

Halogen-Aromatic π Interactions Modulate Inhibitor Residence Times.

Highly selective inhibition of histone demethylases by de novo macrocyclic peptides

Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex

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

Identifying Small-Molecule Binding Sites for Epigenetic Proteins at Domain-Domain Interfaces.

Inflammatory Signaling by NOD-RIPK2 Is Inhibited by Clinically Relevant Type II Kinase Inhibitors.

Inhibition of histone H3K27 demethylases inactivates brachyury (TBXT) and promotes chordoma cell death

K2P channel gating mechanisms revealed by structures of TREK-2 and a complex with Prozac

Kalirin as a Novel Treatment Target for Cognitive Dysfunction in Schizophrenia

LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor

Mild, calcium catalysed Beckmann rearrangements

Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor

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

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

Palladium-containing perovskites: recoverable and reuseable catalysts for Suzuki couplingsElectronic supplementary information (ESI) available: experimental details. See http://www.rsc.org/suppdata/cc/b3/b308465e/

Plant Growth Regulator Daminozide Is a Selective Inhibitor of Human KDM2/7 Histone Demethylases

Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells

Potent and selective alpha1A adrenoceptor partial agonists--novel imidazole frameworks.

Progress in the development and application of small molecule inhibitors of bromodomain-acetyl-lysine interactions

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

Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence.

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

Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening

Recent Progress in Histone Demethylase Inhibitors

Selective targeting of Bromodomains of the Bromodomain-PHD Fingers family impairs osteoclast differentiation

Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance.

Structural analysis of human KDM5B guides histone demethylase inhibitor development

Structure of the Human Protein Kinase ZAK in Complex with Vemurafenib

Structure-Based Design of Highly Selective Inhibitors of the CREB Binding Protein Bromodomain

Structure-Based Identification of Inhibitory Fragments Targeting the p300/CBP-Associated Factor Bromodomain

Synthesis of carbohydrate derivatives using solid-phase work-up and scavenging techniques

TargetDB: A target information aggregation tool and tractability predictor

Targeting the Small GTPase Superfamily through Their Regulatory Proteins

The SGC beyond structural genomics: redefining the role of 3D structures by coupling genomic stratification with fragment-based discovery.

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

The promise and peril of chemical probes

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