List of works - Peter J. Brown

(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells

scientific article

A CONVENIENT SYNTHESIS OF THIOFIBRATE ANALOGS FROM ARYL SULFONYL CHLORIDES

scientific article published in January 2001

A DNA-Encoded Library of Chemical Compounds Based on Common Scaffolding Structures Reveals the Impact of Ligand Geometry on Protein Recognition

scientific article published on 01 June 2018

A First-in-Class, Highly Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 6

scientific article published on 8 April 2021

A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases

scientific article published on 24 November 2015

A cellular chemical probe targeting the chromodomains of Polycomb repressive complex 1

scientific article

A chemical biology toolbox to study protein methyltransferases and epigenetic signaling

scientific article published in Nature Communications

A chemical probe of CARM1 alters epigenetic plasticity against breast cancer cell invasion

scientific article published on 28 October 2019

A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells

scientific article

A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3)

scientific article

A scintillation proximity assay for histone demethylases

scientific article published on 08 July 2014

AKT drives SOX2 overexpression and cancer cell stemness in esophageal cancer by protecting SOX2 from UBR5-mediated degradation

scientific article published on 20 March 2019

Accessing protein methyltransferase and demethylase enzymology using microfluidic capillary electrophoresis

scientific article

Activation of peroxisome proliferator-activated receptor-alpha protects the heart from ischemia/reperfusion injury

scientific article published on 13 October 2003

Alkenyl sulphoxides as precursors to cyclopentenones and prostanoid β-side chains

scientific article published in 1983

An allosteric inhibitor of protein arginine methyltransferase 3

scientific article

An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1

scientific article

Assay interference and off-target liabilities of reported histone acetyltransferase inhibitors

scientific article published on 15 November 2017

Author Correction: Pharmacological inhibition of PRMT7 links arginine monomethylation to the cellular stress response

scientific article published on 26 May 2020

Bromo-deaza-SAH: a potent and selective DOT1L inhibitor

scientific article published on 30 January 2013

Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors

scientific article

Chemical probes targeting epigenetic proteins: Applications beyond oncology

scientific article

Conformational dynamics of the TTD-PHD histone reader module of the UHRF1 epigenetic regulator reveals multiple histone-binding states, allosteric regulation, and druggability

scientific article published on 26 October 2017

Correction: A chemical probe of CARM1 alters epigenetic plasticity against breast cancer cell invasion

scientific article published on 15 October 2020

Design and synthesis of an array of selective androgen receptor modulators.

scientific article published on January 2007

Design and synthesis of selective, small molecule inhibitors of coactivator-associated arginine methyltransferase 1 (CARM1).

scientific article published on 13 July 2016

Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (BAY-598) for the Protein Lysine Methyltransferase SMYD2

scientific article

Discovery and Development of Potent and Selective Inhibitors of Histone Methyltransferase G9a

scientific article

Discovery of A-893, A New Cell-Active Benzoxazinone Inhibitor of Lysine Methyltransferase SMYD2.

scientific article published on 29 April 2015

Discovery of Peptidomimetic Ligands of EED as Allosteric Inhibitors of PRC2.

scientific article published on 6 February 2017

Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3).

scientific article

Discovery of Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase.

scientific article

Discovery of Small-Molecule Antagonists of the H3K9me3 Binding to UHRF1 Tandem Tudor Domain

scientific article published on 21 March 2018

Discovery of Small-Molecule Antagonists of the PWWP Domain of NSD2

scientific article published in February 2021

Discovery of a 2,4-Diamino-7-aminoalkoxyquinazoline as a Potent and Selective Inhibitor of Histone Lysine Methyltransferase G9a

scientific article

Discovery of a Dual PRMT5-PRMT7 Inhibitor

scientific article published on 2 March 2015

Discovery of a Potent Class I Protein Arginine Methyltransferase Fragment Inhibitor

scientific article

Discovery of a Potent and Selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) Inhibitor by Virtual Screening

scientific article

Discovery of a chemical probe for PRDM9

scientific article published on 17 December 2019

Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain

scientific article published on 6 January 2013

Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8

scientific article (publication date: 14 August 2014)

Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP.

scientific article published on 31 October 2013

Discovery of selective activators of PRC2 mutant EED-I363M

scientific article published on 25 April 2019

Donated chemical probes for open science.

scientific article published on 20 April 2018

Epigenetic chemical probes.

scientific article published on 24 October 2012

Evaluation of the therapeutic potential of PPARalpha agonists for X-linked adrenoleukodystrophy.

scientific article

Exploiting an allosteric binding site of PRMT3 yields potent and selective inhibitors

scientific article

Fatty acids and eicosanoids regulate gene expression through direct interactions with peroxisome proliferator-activated receptors alpha and gamma

scientific article

Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3

scientific article published on 08 July 2019

Functional interdependence of BRD4 and DOT1L in MLL leukemia

scientific article published on 13 June 2016

Generation of Secondary Alkyl Amines on Solid Support by Borane Reduction: Application to the Parallel Synthesis of PPAR Ligands

scientific article published in July 1997

Genome-wide profiling of histone H3 lysine 27 and lysine 4 trimethylation in multiple myeloma reveals the importance of Polycomb gene targeting and highlights EZH2 as a potential therapeutic target.

scientific article published on 7 January 2016

HMG-CoA reductase inhibitors 4. Tetrazole series: conformational constraints and structural requirements at the hydrophobic domain

scientific article published in January 1992

Hemi-methylated DNA regulates DNA methylation inheritance through allosteric activation of H3 ubiquitylation by UHRF1

scientific article

Identification and characterization of the first fragment hits for SETDB1 Tudor domain

scientific article published on 12 July 2019

Identification of a fragment-like small molecule ligand for the methyl-lysine binding protein, 53BP1.

scientific article

Identification of novel functionally selective κ-opioid receptor scaffolds

scientific article

Identification of small molecule allosteric modulators of 5,10-methylenetetrahydrofolate reductase (MTHFR) by targeting its unique regulatory domain

scientific article published in April 2021

Identification of structure-activity relationships from screening a structurally compact DNA-encoded chemical library

scientific article published on 3 February 2015

LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity

scientific article published on 23 April 2018

LLY-507, a Cell-active, Potent, and Selective Inhibitor of Protein-lysine Methyltransferase SMYD2.

scientific article published on 30 March 2015

Nahuoic acid A produced by a Streptomyces sp. isolated from a marine sediment is a selective SAM-competitive inhibitor of the histone methyltransferase SETD8.

scientific article published on 28 December 2012

Open access chemical probes for epigenetic targets

scientific article

Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines

scientific article

Pharmacological inhibition of PRMT7 links arginine monomethylation to the cellular stress response

scientific article published on 14 May 2020

Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia

scientific article

Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines

scientific article

Revealing the Protein Propionylation Activity of the Histone Acetyltransferase Males absent on the first (MOF).

scientific article published on 10 January 2018

SET9-Mediated Regulation of TGF-β Signaling Links Protein Methylation to Pulmonary Fibrosis

scientific article published on 08 June 2016

SETD7 Controls Intestinal Regeneration and Tumorigenesis by Regulating Wnt/β-Catenin and Hippo/YAP Signaling

scientific article published on April 2016

Selection, application, and validation of a set of molecular descriptors for nuclear receptor ligands.

scientific article

Selective, Small-Molecule Co-Factor Binding Site Inhibition of a Su(var)3-9, Enhancer of Zeste, Trithorax Domain Containing Lysine Methyltransferase

scientific article published on 03 September 2019

Sinefungin derivatives as inhibitors and structure probes of protein lysine methyltransferase SETD2

scientific article

Small-Molecule Ligands of Methyl-Lysine Binding Proteins

scientific article

Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5

scientific article published on January 2013

Structural and functional consequences of the STAT5BN642H driver mutation.

scientific article published on 7 June 2019

Structural basis of arginine asymmetrical dimethylation by PRMT6.

scientific article published on August 2016

Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists

scientific article published in June 2010

Structure of the Catalytic Domain of EZH2 Reveals Conformational Plasticity in Cofactor and Substrate Binding Sites and Explains Oncogenic Mutations

scientific article

Structure-Activity Relationship Studies for Enhancer of Zeste Homologue 2 (EZH2) and Enhancer of Zeste Homologue 1 (EZH1) Inhibitors

scientific article published on 28 July 2016

Structure-Based Design of a Covalent Inhibitor of the SET Domain-Containing Protein 8 (SETD8) Lysine Methyltransferase

scientific article

Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1).

scientific article

Structure-activity relationship studies of G9a-like protein (GLP) inhibitors

scientific article published on 19 June 2017

Structure-activity relationship studies of SETD8 inhibitors.

scientific article

Structure–activity relationships of methyl-lysine reader antagonists

scientific article published in 2012

Synthesis of (.+-.)-10,22-dioxokopsane and (.+-.)-kopsanone, heptacyclic indole alkaloids. Synthetic and mechanistic studies

scientific article published in 1984

Synthesis, Optimization, and Evaluation of Novel Small Molecules as Antagonists of WDR5-MLL Interaction

scientific article published on 04 February 2013

TP-064, a potent and selective small molecule inhibitor of PRMT4 for multiple myeloma.

scientific article published on 6 April 2018

Tankyrase 1 Inhibitors with Drug-like Properties Identified by Screening a DNA-Encoded Chemical Library

scientific article published on 10 June 2015

The SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity

scientific article published on 23 January 2017

The dynamic conformational landscape of the protein methyltransferase SETD8.

scientific article published on 13 May 2019

The indole 2-3-quinodimethane strategy for the synthesis of indole alkaloids

scientific article published in January 1984

The promise and peril of chemical probes

scientific article

Turning a Substrate Peptide into a Potent Inhibitor for the Histone Methyltransferase SETD8.

scientific article published on 11 October 2016

List of works by Peter J. Brown

(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells

A CONVENIENT SYNTHESIS OF THIOFIBRATE ANALOGS FROM ARYL SULFONYL CHLORIDES

A DNA-Encoded Library of Chemical Compounds Based on Common Scaffolding Structures Reveals the Impact of Ligand Geometry on Protein Recognition

A First-in-Class, Highly Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 6

A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases

A cellular chemical probe targeting the chromodomains of Polycomb repressive complex 1

A chemical biology toolbox to study protein methyltransferases and epigenetic signaling

A chemical probe of CARM1 alters epigenetic plasticity against breast cancer cell invasion

A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells

A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3)

A scintillation proximity assay for histone demethylases

AKT drives SOX2 overexpression and cancer cell stemness in esophageal cancer by protecting SOX2 from UBR5-mediated degradation

Accessing protein methyltransferase and demethylase enzymology using microfluidic capillary electrophoresis

Activation of peroxisome proliferator-activated receptor-alpha protects the heart from ischemia/reperfusion injury

Alkenyl sulphoxides as precursors to cyclopentenones and prostanoid β-side chains

An allosteric inhibitor of protein arginine methyltransferase 3

An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1

Assay interference and off-target liabilities of reported histone acetyltransferase inhibitors

Author Correction: Pharmacological inhibition of PRMT7 links arginine monomethylation to the cellular stress response

Bromo-deaza-SAH: a potent and selective DOT1L inhibitor

Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors

Chemical probes targeting epigenetic proteins: Applications beyond oncology

Conformational dynamics of the TTD-PHD histone reader module of the UHRF1 epigenetic regulator reveals multiple histone-binding states, allosteric regulation, and druggability

Correction: A chemical probe of CARM1 alters epigenetic plasticity against breast cancer cell invasion

Design and synthesis of an array of selective androgen receptor modulators.

Design and synthesis of selective, small molecule inhibitors of coactivator-associated arginine methyltransferase 1 (CARM1).

Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (BAY-598) for the Protein Lysine Methyltransferase SMYD2

Discovery and Development of Potent and Selective Inhibitors of Histone Methyltransferase G9a

Discovery of A-893, A New Cell-Active Benzoxazinone Inhibitor of Lysine Methyltransferase SMYD2.

Discovery of Peptidomimetic Ligands of EED as Allosteric Inhibitors of PRC2.

Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3).

Discovery of Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase.

Discovery of Small-Molecule Antagonists of the H3K9me3 Binding to UHRF1 Tandem Tudor Domain

Discovery of Small-Molecule Antagonists of the PWWP Domain of NSD2

Discovery of a 2,4-Diamino-7-aminoalkoxyquinazoline as a Potent and Selective Inhibitor of Histone Lysine Methyltransferase G9a

Discovery of a Dual PRMT5-PRMT7 Inhibitor

Discovery of a Potent Class I Protein Arginine Methyltransferase Fragment Inhibitor

Discovery of a Potent and Selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) Inhibitor by Virtual Screening

Discovery of a chemical probe for PRDM9

Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain

Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8

Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP.

Discovery of selective activators of PRC2 mutant EED-I363M

Donated chemical probes for open science.

Epigenetic chemical probes.

Evaluation of the therapeutic potential of PPARalpha agonists for X-linked adrenoleukodystrophy.

Exploiting an allosteric binding site of PRMT3 yields potent and selective inhibitors

Fatty acids and eicosanoids regulate gene expression through direct interactions with peroxisome proliferator-activated receptors alpha and gamma

Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3

Functional interdependence of BRD4 and DOT1L in MLL leukemia

Generation of Secondary Alkyl Amines on Solid Support by Borane Reduction: Application to the Parallel Synthesis of PPAR Ligands

Genome-wide profiling of histone H3 lysine 27 and lysine 4 trimethylation in multiple myeloma reveals the importance of Polycomb gene targeting and highlights EZH2 as a potential therapeutic target.

HMG-CoA reductase inhibitors 4. Tetrazole series: conformational constraints and structural requirements at the hydrophobic domain

Hemi-methylated DNA regulates DNA methylation inheritance through allosteric activation of H3 ubiquitylation by UHRF1

Identification and characterization of the first fragment hits for SETDB1 Tudor domain

Identification of a fragment-like small molecule ligand for the methyl-lysine binding protein, 53BP1.

Identification of novel functionally selective κ-opioid receptor scaffolds

Identification of small molecule allosteric modulators of 5,10-methylenetetrahydrofolate reductase (MTHFR) by targeting its unique regulatory domain

Identification of structure-activity relationships from screening a structurally compact DNA-encoded chemical library

LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity

LLY-507, a Cell-active, Potent, and Selective Inhibitor of Protein-lysine Methyltransferase SMYD2.

Nahuoic acid A produced by a Streptomyces sp. isolated from a marine sediment is a selective SAM-competitive inhibitor of the histone methyltransferase SETD8.

Open access chemical probes for epigenetic targets

Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines

Pharmacological inhibition of PRMT7 links arginine monomethylation to the cellular stress response

Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia

Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines

Revealing the Protein Propionylation Activity of the Histone Acetyltransferase Males absent on the first (MOF).

SET9-Mediated Regulation of TGF-β Signaling Links Protein Methylation to Pulmonary Fibrosis

SETD7 Controls Intestinal Regeneration and Tumorigenesis by Regulating Wnt/β-Catenin and Hippo/YAP Signaling

Selection, application, and validation of a set of molecular descriptors for nuclear receptor ligands.

Selective, Small-Molecule Co-Factor Binding Site Inhibition of a Su(var)3-9, Enhancer of Zeste, Trithorax Domain Containing Lysine Methyltransferase

Sinefungin derivatives as inhibitors and structure probes of protein lysine methyltransferase SETD2

Small-Molecule Ligands of Methyl-Lysine Binding Proteins

Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5

Structural and functional consequences of the STAT5BN642H driver mutation.

Structural basis of arginine asymmetrical dimethylation by PRMT6.

Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists

Structure of the Catalytic Domain of EZH2 Reveals Conformational Plasticity in Cofactor and Substrate Binding Sites and Explains Oncogenic Mutations