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A chemical biology toolbox to study protein methyltransferases and epigenetic signaling

Nature communications, 2019-01, Vol.10 (1), p.19-14, Article 19

2019

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Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6

Journal of medicinal chemistry, 2016-10, Vol.59 (19), p.9124-9139

2016

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

Journal of medicinal chemistry, 2016-03, Vol.59 (6), p.2478-2496

2016

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

Journal of medicinal chemistry, 2016-07, Vol.59 (14), p.6838-6847

2016

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Discovery of a Dual PRMT5–PRMT7 Inhibitor

ACS medicinal chemistry letters, 2015-04, Vol.6 (4), p.408-412

2015

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Exploiting an Allosteric Binding Site of PRMT3 Yields Potent and Selective Inhibitors

Journal of medicinal chemistry, 2013-03, Vol.56 (5), p.2110-2124

2013

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An Allosteric Inhibitor of Protein Arginine Methyltransferase 3

Structure (London), 2012-08, Vol.20 (8), p.1425-1435

2012

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Novel HDAC6 isoform selective chiral small molecule histone deacetylase inhibitors

Bioorganic & medicinal chemistry letters, 2009-02, Vol.19 (3), p.688-692

2009

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A non-traditional crystal-based compound screening method targeting the ATP binding site of Plasmodium falciparum GRP78 for identification of novel nucleoside analogues

Frontiers in molecular biosciences, 2022-10, Vol.9, p.956095-956095

2022

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Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors

Bioorganic & medicinal chemistry letters, 2009-10, Vol.19 (19), p.5684-5688

2009

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The First Boron-Tethered Radical Cyclizations and Intramolecular Homolytic Substitutions at Boron

Angewandte Chemie (International ed.), 1999-06, Vol.38 (12), p.1798-1800

1999

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SP-013 - Leveraging an open science approach for PET radiotracer discovery: radiolabelling and preliminary neuroimaging of 11C-labelled activin receptor-like kinase 2 inhibitors

Nuclear medicine and biology, 2021-05, Vol.96-97, p.S41-S41

2021

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Leveraging an open science approach for PET radiotracer discovery: radiolabelling and preliminary neuroimaging of 11C-labelled activin receptor-like kinase 2 inhibitors

Nuclear medicine and biology, 2021-05, Vol.96-97, p.S41

2021

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Evidence That Compound I Is the Active Species in Both the Hydroxylase and Lyase Steps by Which P450scc Converts Cholesterol to Pregnenolone: EPR/ENDOR/Cryoreduction/Annealing Studies

Biochemistry (Easton), 2015-12, Vol.54 (48), p.7089-7097

2015

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Discovery of Conformationally Constrained ALK2 Inhibitors

Journal of medicinal chemistry, 2024-03, Vol.67 (6), p.4707-4725

2024

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A Potent, Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 3 (PRMT3)

Angewandte Chemie (International ed.), 2015-04, Vol.54 (17), p.5166-5170

2015

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Functional interdependence of BRD4 and DOT1L in MLL leukemia

Nature structural & molecular biology, 2016-07, Vol.23 (7), p.673

2016

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Potassium allyl- and crotyltrifluoroborates: Stable and efficient agents for allylation and crotylation

Tetrahedron letters, 1999-06, Vol.40 (23), p.4289-4292

1999

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Leveraging an Open Science Drug Discovery Model to Develop CNS-Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma

Journal of medicinal chemistry, 2020-09, Vol.63 (17), p.10061-10085

2020

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A general carbometalation, three component coupling strategy for the synthesis of α,β-unsaturated γ-sultines including thio-rofecoxib, a selective COX-2 inhibitor

Bioorganic & medicinal chemistry letters, 2005-04, Vol.15 (8), p.2057-2060

2005

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

Biochemical journal, 2013-01, Vol.449 (1), p.151-159

2013

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Probing the SAM Binding Site of SARS-CoV-2 Nsp14 In Vitro Using SAM Competitive Inhibitors Guides Developing Selective Bisubstrate Inhibitors

SLAS discovery, 2021-10, Vol.26 (9), p.1200-1211

2021

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Targeting ALK2: An Open Science Approach to Developing Therapeutics for the Treatment of Diffuse Intrinsic Pontine Glioma

Journal of medicinal chemistry, 2020-05, Vol.63 (9), p.4978-4996

2020

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A chemical biology toolbox to study protein methyltransferases and epigenetic signaling

Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6

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

MLL5 Orchestrates a Cancer Self-Renewal State by Repressing the Histone Variant H3.3 and Globally Reorganizing Chromatin

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

Discovery of a Dual PRMT5–PRMT7 Inhibitor

Exploiting an Allosteric Binding Site of PRMT3 Yields Potent and Selective Inhibitors

An Allosteric Inhibitor of Protein Arginine Methyltransferase 3

Novel HDAC6 isoform selective chiral small molecule histone deacetylase inhibitors

A non-traditional crystal-based compound screening method targeting the ATP binding site of Plasmodium falciparum GRP78 for identification of novel nucleoside analogues

Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors

The First Boron-Tethered Radical Cyclizations and Intramolecular Homolytic Substitutions at Boron

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

SP-013 - Leveraging an open science approach for PET radiotracer discovery: radiolabelling and preliminary neuroimaging of 11C-labelled activin receptor-like kinase 2 inhibitors

Leveraging an open science approach for PET radiotracer discovery: radiolabelling and preliminary neuroimaging of 11C-labelled activin receptor-like kinase 2 inhibitors

Evidence That Compound I Is the Active Species in Both the Hydroxylase and Lyase Steps by Which P450scc Converts Cholesterol to Pregnenolone: EPR/ENDOR/Cryoreduction/Annealing Studies

Discovery of Conformationally Constrained ALK2 Inhibitors

A Potent, Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 3 (PRMT3)

Functional interdependence of BRD4 and DOT1L in MLL leukemia

Potassium allyl- and crotyltrifluoroborates: Stable and efficient agents for allylation and crotylation

Leveraging an Open Science Drug Discovery Model to Develop CNS-Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma

A general carbometalation, three component coupling strategy for the synthesis of α,β-unsaturated γ-sultines including thio-rofecoxib, a selective COX-2 inhibitor

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

Probing the SAM Binding Site of SARS-CoV-2 Nsp14 In Vitro Using SAM Competitive Inhibitors Guides Developing Selective Bisubstrate Inhibitors

Targeting ALK2: An Open Science Approach to Developing Therapeutics for the Treatment of Diffuse Intrinsic Pontine Glioma

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