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New approaches for the treatment of Alzheimer’s disease

Bioorganic & medicinal chemistry letters, 2019-01, Vol.29 (2), p.125-133

2019

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Epigenetic protein families: a new frontier for drug discovery

Nature reviews. Drug discovery, 2012-05, Vol.11 (5), p.384-400

2012

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Bridging solubility between drug discovery and development

Drug discovery today, 2012-05, Vol.17 (9-10), p.486-495

2012

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Carboxylesterase Notum Is a Druggable Target to Modulate Wnt Signaling

Journal of medicinal chemistry, 2021-04, Vol.64 (8), p.4289-4311

2021

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PFI-1, a Highly Selective Protein Interaction Inhibitor, Targeting BET Bromodomains

Cancer research (Chicago, Ill.), 2013-06, Vol.73 (11), p.3336-3346

2013

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Structural Insights into Notum Covalent Inhibition

Journal of medicinal chemistry, 2021-08, Vol.64 (15), p.11354-11363

2021

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5‑Phenyl-1,3,4-oxadiazol-2(3H)‑ones Are Potent Inhibitors of Notum Carboxylesterase Activity Identified by the Optimization of a Crystallographic Fragment Screening Hit

Journal of medicinal chemistry, 2020-11, Vol.63 (21), p.12942-12956

2020

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Design of a Potent, Selective, and Brain-Penetrant Inhibitor of Wnt-Deactivating Enzyme Notum by Optimization of a Crystallographic Fragment Hit

Journal of medicinal chemistry, 2022-05, Vol.65 (10), p.7212-7230

2022

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

Journal of medicinal chemistry, 2012-11, Vol.55 (22), p.9831-9837

2012

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Small-molecule inhibitors of carboxylesterase Notum

Future medicinal chemistry, 2021-06, Vol.13 (11), p.1001-1015

2021

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Virtual Screening Directly Identifies New Fragment-Sized Inhibitors of Carboxylesterase Notum with Nanomolar Activity

Journal of medicinal chemistry, 2022-01, Vol.65 (1), p.562-578

2022

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Large-scale synthesis of Notum inhibitor 1-(2,4-dichloro-3-(trifluoromethyl)-phenyl)-1H-1,2,3-triazole (ARUK3001185) employing a modified Sakai reaction as the key step

RSC advances, 2022-09, Vol.12 (41), p.26497-26503

2022

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

Proceedings of the National Academy of Sciences - PNAS, 2014-09, Vol.111 (35), p.12853-12858

2014

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Scaffold-hopping identifies furano[2,3-d]pyrimidine amides as potent Notum inhibitors

Bioorganic & medicinal chemistry letters, 2020-02, Vol.30 (3), p.126751, Article 126751

2020

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Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and In Vivo Efficacy in the Plasmodium falciparum NSG Mouse Model

Journal of medicinal chemistry, 2020-11, Vol.63 (21), p.13013-13030

2020

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

Journal of medicinal chemistry, 2017-08, Vol.60 (16), p.6998-7011

2017

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Antimalarial Lead-Optimization Studies on a 2,6-Imidazopyridine Series within a Constrained Chemical Space To Circumvent Atypical Dose–Response Curves against Multidrug Resistant Parasite Strains

Journal of medicinal chemistry, 2018-10, Vol.61 (20), p.9371-9385

2018

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Designed switch from covalent to non-covalent inhibitors of carboxylesterase Notum activity

European journal of medicinal chemistry, 2023-05, Vol.251, p.115132-115132, Article 115132

2023

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An improved, scalable synthesis of Notum inhibitor LP-922056 using 1-chloro-1,2-benziodoxol-3-one as a superior electrophilic chlorinating agent

Beilstein journal of organic chemistry, 2019-11, Vol.15 (1), p.2790-2797

2019

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Structural Analysis and Development of Notum Fragment Screening Hits

ACS chemical neuroscience, 2022-07, Vol.13 (13), p.2060-2077

2022

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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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New small molecule inhibitors of histone methyl transferase DOT1L with a nitrile as a non-traditional replacement for heavy halogen atoms

Bioorganic & medicinal chemistry letters, 2016-09, Vol.26 (18), p.4518-4522

2016

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Discovery of 2-phenoxyacetamides as inhibitors of the Wnt-depalmitoleating enzyme NOTUM from an X-ray fragment screen

MedChemComm, 2019-08, Vol.1 (8), p.1361-1369

2019

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

Journal of medicinal chemistry, 2017-01, Vol.60 (2), p.668-680

2017

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New approaches for the treatment of Alzheimer’s disease

Epigenetic protein families: a new frontier for drug discovery

Bridging solubility between drug discovery and development

NOTUM from Apc-mutant cells biases clonal competition to initiate cancer

Carboxylesterase Notum Is a Druggable Target to Modulate Wnt Signaling

PFI-1, a Highly Selective Protein Interaction Inhibitor, Targeting BET Bromodomains

Structural Insights into Notum Covalent Inhibition

5‑Phenyl-1,3,4-oxadiazol-2(3H)‑ones Are Potent Inhibitors of Notum Carboxylesterase Activity Identified by the Optimization of a Crystallographic Fragment Screening Hit

Design of a Potent, Selective, and Brain-Penetrant Inhibitor of Wnt-Deactivating Enzyme Notum by Optimization of a Crystallographic Fragment Hit

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

Small-molecule inhibitors of carboxylesterase Notum

Virtual Screening Directly Identifies New Fragment-Sized Inhibitors of Carboxylesterase Notum with Nanomolar Activity

Large-scale synthesis of Notum inhibitor 1-(2,4-dichloro-3-(trifluoromethyl)-phenyl)-1H-1,2,3-triazole (ARUK3001185) employing a modified Sakai reaction as the key step

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

Scaffold-hopping identifies furano[2,3-d]pyrimidine amides as potent Notum inhibitors

Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and In Vivo Efficacy in the Plasmodium falciparum NSG Mouse Model

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

Antimalarial Lead-Optimization Studies on a 2,6-Imidazopyridine Series within a Constrained Chemical Space To Circumvent Atypical Dose–Response Curves against Multidrug Resistant Parasite Strains

Designed switch from covalent to non-covalent inhibitors of carboxylesterase Notum activity

An improved, scalable synthesis of Notum inhibitor LP-922056 using 1-chloro-1,2-benziodoxol-3-one as a superior electrophilic chlorinating agent

Structural Analysis and Development of Notum Fragment Screening Hits

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

New small molecule inhibitors of histone methyl transferase DOT1L with a nitrile as a non-traditional replacement for heavy halogen atoms

Discovery of 2-phenoxyacetamides as inhibitors of the Wnt-depalmitoleating enzyme NOTUM from an X-ray fragment screen

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

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