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Structure and inhibition mechanism of the catalytic domain of human squalene epoxidase

Nature communications, 2019-01, Vol.10 (1), p.97-10, Article 97

2019

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Vorasidenib (AG-881): A First-in-Class, Brain-Penetrant Dual Inhibitor of Mutant IDH1 and 2 for Treatment of Glioma

ACS medicinal chemistry letters, 2020-02, Vol.11 (2), p.101-107

2020

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Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous MTAP Deletion

Journal of medicinal chemistry, 2021-04, Vol.64 (8), p.4430-4449

2021

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Structure‐Based Design of AG‐946, a Pyruvate Kinase Activator

ChemMedChem, 2024-03, Vol.19 (5), p.e202300559-n/a

2024

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High-throughput mutagenesis reveals unique structural features of human ADAR1

Nature communications, 2020-10, Vol.11 (1), p.5130-13, Article 5130

2020

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Leveraging Structure-Based Drug Design to Identify Next-Generation MAT2A Inhibitors, Including Brain-Penetrant and Peripherally Efficacious Leads

Journal of medicinal chemistry, 2022-03, Vol.65 (6), p.4600-4615

2022

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Allostery Illuminated: Harnessing AI and Machine Learning for Drug Discovery

ACS medicinal chemistry letters, 2024-09, Vol.15 (9), p.1449-1455

2024

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Distinct Hepatic PKA and CDK Signaling Pathways Control Activity-Independent Pyruvate Kinase Phosphorylation and Hepatic Glucose Production

Cell reports (Cambridge), 2019-12, Vol.29 (11), p.3394-3404.e9

2019

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Discovery of Potent, Selective Chymase Inhibitors via Fragment Linking Strategies

Journal of medicinal chemistry, 2013-06, Vol.56 (11), p.4465-4481

2013

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Synthesis, SAR, and Series Evolution of Novel Oxadiazole-Containing 5‑Lipoxygenase Activating Protein Inhibitors: Discovery of 2‑[4-(3-{(R)‑1-[4-(2-Amino-pyrimidin-5-yl)-phenyl]-1-cyclopropyl-ethyl}-[1,2,4]oxadiazol-5-yl)-pyrazol-1-yl]‑N,N‑dimethyl-acetamide (BI 665915)

Journal of medicinal chemistry, 2015-02, Vol.58 (4), p.1669-1690

2015

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Crystal structure of human GDF11

Acta crystallographica. Section F, Structural biology communications, 2016-03, Vol.72 (3), p.160-164

2016

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Fragment-Based Discovery of Indole Inhibitors of Matrix Metalloproteinase-13

Journal of medicinal chemistry, 2011-12, Vol.54 (23), p.8174-8187

2011

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Integrated Strategies for Identifying Leads That Target the NS3 Helicase of the Hepatitis C Virus

Journal of medicinal chemistry, 2014-03, Vol.57 (5), p.2074-2090

2014

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Structural Basis for Autoinhibition and Mutational Activation of Eukaryotic Initiation Factor 2α Protein Kinase GCN2[boxs]

The Journal of biological chemistry, 2005-08, Vol.280 (32), p.29289-29299

2005

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Correction to Fragment-Based Discovery of Indole Inhibitors of Matrix Metalloproteinase-13

Journal of medicinal chemistry, 2015-08, Vol.58 (15), p.6318-6318

2015

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Lateral energy transfer model for adjacent light-harvesting antennae rods of C-phycocyanins

Biochimica et biophysica acta, 2006-03, Vol.1757 (3), p.161-165

2006

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Crystal Structure of Shikimate 5-Dehydrogenase (SDH) Bound to NADP: Insights into Function and Evolution

Structure (London), 2003-08, Vol.11 (8), p.1005-1013

2003

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Crystal Structure of a Light-Harvesting Protein C-Phycocyanin from Spirulina platensis

Biochemical and biophysical research communications, 2001-04, Vol.282 (4), p.893-898

2001

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Abstract B075: Identifying functional allosteric binding sites using a systematic and scalable AMPS screening platform for drug discovery

Molecular cancer therapeutics, 2023-12, Vol.22 (12_Supplement), p.B075-B075

2023

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Abstract 3504: A chemical biology screen identifies a unique vulnerability of neuroendocrine cancer cells to SQLE inhibition

Cancer research (Chicago, Ill.), 2018-07, Vol.78 (13_Supplement), p.3504-3504

2018

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Role of a two-residue spacer in an α,β-didehydrophenylalanine containing hexapeptide: crystal and solution structure of Boc-Val-ΔPhe-Leu-Ala-ΔPhe-Ala-OMe

Journal of peptide science, 2003-01, Vol.9 (1), p.54-63

2003

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Crystal Structure of Shikimate 5-Dehydrogenase (SDH) Bound to NADP

Structure (London), 2003-08, Vol.11 (8), p.1005-1013

2003

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A chemical biology screen identifies a vulnerability of neuroendocrine cancer cells to SQLE inhibition

Nature communications, 2019-01, Vol.10 (1), p.96-14, Article 96

2019

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Structure and inhibition mechanism of the catalytic domain of human squalene epoxidase

Vorasidenib (AG-881): A First-in-Class, Brain-Penetrant Dual Inhibitor of Mutant IDH1 and 2 for Treatment of Glioma

Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous MTAP Deletion

Structure‐Based Design of AG‐946, a Pyruvate Kinase Activator

High-throughput mutagenesis reveals unique structural features of human ADAR1

Leveraging Structure-Based Drug Design to Identify Next-Generation MAT2A Inhibitors, Including Brain-Penetrant and Peripherally Efficacious Leads

Allostery Illuminated: Harnessing AI and Machine Learning for Drug Discovery

Selective Vulnerability to Pyrimidine Starvation in Hematologic Malignancies Revealed by AG-636, a Novel Clinical-Stage Inhibitor of Dihydroorotate Dehydrogenase

Distinct Hepatic PKA and CDK Signaling Pathways Control Activity-Independent Pyruvate Kinase Phosphorylation and Hepatic Glucose Production

Discovery of Potent, Selective Chymase Inhibitors via Fragment Linking Strategies

Synthesis, SAR, and Series Evolution of Novel Oxadiazole-Containing 5‑Lipoxygenase Activating Protein Inhibitors: Discovery of 2‑[4-(3-{(R)‑1-[4-(2-Amino-pyrimidin-5-yl)-phenyl]-1-cyclopropyl-ethyl}-[1,2,4]oxadiazol-5-yl)-pyrazol-1-yl]‑N,N‑dimethyl-acetamide (BI 665915)

Crystal structure of human GDF11

Fragment-Based Discovery of Indole Inhibitors of Matrix Metalloproteinase-13

Integrated Strategies for Identifying Leads That Target the NS3 Helicase of the Hepatitis C Virus

Structural Basis for Autoinhibition and Mutational Activation of Eukaryotic Initiation Factor 2α Protein Kinase GCN2[boxs]

Correction to Fragment-Based Discovery of Indole Inhibitors of Matrix Metalloproteinase-13

Lateral energy transfer model for adjacent light-harvesting antennae rods of C-phycocyanins

Crystal Structure of Shikimate 5-Dehydrogenase (SDH) Bound to NADP: Insights into Function and Evolution

AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations

Crystal Structure of a Light-Harvesting Protein C-Phycocyanin from Spirulina platensis

Abstract B075: Identifying functional allosteric binding sites using a systematic and scalable AMPS screening platform for drug discovery

Abstract 3504: A chemical biology screen identifies a unique vulnerability of neuroendocrine cancer cells to SQLE inhibition

Role of a two-residue spacer in an α,β-didehydrophenylalanine containing hexapeptide: crystal and solution structure of Boc-Val-ΔPhe-Leu-Ala-ΔPhe-Ala-OMe

Crystal Structure of Shikimate 5-Dehydrogenase (SDH) Bound to NADP

A chemical biology screen identifies a vulnerability of neuroendocrine cancer cells to SQLE inhibition

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