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Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2‑HG in Vivo

ACS medicinal chemistry letters, 2012-10, Vol.3 (10), p.850-855

2012

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1-(3-Aryloxyaryl)benzimidazole sulfones are liver X receptor agonists

Bioorganic & medicinal chemistry letters, 2010-01, Vol.20 (2), p.526-530

2010

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4-(3-Aryloxyaryl)quinoline sulfones are potent liver X receptor agonists

Bioorganic & medicinal chemistry letters, 2010, Vol.20 (1), p.209-212

2010

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Aspartic Protease Inhibitors: Expedient Synthesis of 2-Substituted Statines

Organic letters, 2001-08, Vol.3 (17), p.2725-2728

2001

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Synthesis of 4-(3-biaryl)quinoline sulfones as potent liver X receptor agonists

Bioorganic & medicinal chemistry letters, 2010-05, Vol.20 (9), p.2903-2907

2010

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Biphenylsulfonyl-thiophene-carboxamidine inhibitors of the complement component C1s

Bioorganic & medicinal chemistry, 2008-03, Vol.18 (5), p.1603-1606

2008

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A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s

Bioorganic & medicinal chemistry letters, 2006-04, Vol.16 (8), p.2200-2204

2006

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Design and Enantioselective Synthesis of a Peptidomimetic of the Turn in the Helix−Turn−Helix DNA-Binding Protein Motif

Journal of organic chemistry, 1997-11, Vol.62 (24), p.8387-8393

1997

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Facile synthesis of d-amino acids from an l-serine-derived aziridine

Tetrahedron letters, 1998-12, Vol.39 (51), p.9389-9392

1998

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ChemInform Abstract: Facile Synthesis of D-Amino Acids from an L-Serine-Derived Aziridine

ChemInform, 1999-03, Vol.30 (10), p.no-no

1999

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ChemInform Abstract: Rare Protein Turns: γ-Turn, Helix-Turn-Helix, and cis-Proline Mimics

ChemInform, 2000-04, Vol.31 (15), p.no-no

2000

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ChemInform Abstract: Aspartic Protease Inhibitors: Expedient Synthesis of 2-Substituted Statines

ChemInform, 2001-11, Vol.32 (48), p.no-no

2001

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MTAP Deletions in Cancer Create Vulnerability to Targeting of the MAT2A/PRMT5/RIOK1 Axis

Cell reports (Cambridge), 2016-04, Vol.15 (3), p.574-587

2016

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IDH2 mutation-induced histone and DNA hypermethylation is progressively reversed by small-molecule inhibition

Blood, 2015-01, Vol.125 (2), p.296-303

2015

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Mutant IDH inhibits HNF-4α to block hepatocyte differentiation and promote biliary cancer

Nature (London), 2014-09, Vol.513 (7516), p.110-114

2014

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Targeted Inhibition of Mutant IDH2 in Leukemia Cells Induces Cellular Differentiation

Science (American Association for the Advancement of Science), 2013-05, Vol.340 (6132), p.622-626

2013

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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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Combination Targeted Therapy to Disrupt Aberrant Oncogenic Signaling and Reverse Epigenetic Dysfunction in IDH2 - and TET2 -Mutant Acute Myeloid Leukemia

Cancer discovery, 2017-05, Vol.7 (5), p.494-505

2017

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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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Abstract B115: Mitotic defects induced by MAT2A inhibitors guides translational drug combination strategies with AG-270 and taxanes

Molecular cancer therapeutics, 2019-12, Vol.18 (12_Supplement), p.B115-B115

2019

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AG-221, a Small Molecule Mutant IDH2 Inhibitor, Remodels the Epigenetic State of IDH2-Mutant Cells and Induces Alterations in Self-Renewal/Differentiation in IDH2-Mutant AML Model in Vivo

Blood, 2014-12, Vol.124 (21), p.437-437

2014

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Abstract 2296: IDH2 mutation induced histone and DNA hypermethylation is progressively reversed by small molecule inhibition

Cancer research (Chicago, Ill.), 2014-10, Vol.74 (19_Supplement), p.2296-2296

2014

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Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2‑HG in Vivo

1-(3-Aryloxyaryl)benzimidazole sulfones are liver X receptor agonists

4-(3-Aryloxyaryl)quinoline sulfones are potent liver X receptor agonists

Aspartic Protease Inhibitors: Expedient Synthesis of 2-Substituted Statines

Synthesis of 4-(3-biaryl)quinoline sulfones as potent liver X receptor agonists

Biphenylsulfonyl-thiophene-carboxamidine inhibitors of the complement component C1s

A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s

Design and Enantioselective Synthesis of a Peptidomimetic of the Turn in the Helix−Turn−Helix DNA-Binding Protein Motif

Facile synthesis of d-amino acids from an l-serine-derived aziridine

ChemInform Abstract: Facile Synthesis of D-Amino Acids from an L-Serine-Derived Aziridine

ChemInform Abstract: Rare Protein Turns: γ-Turn, Helix-Turn-Helix, and cis-Proline Mimics

ChemInform Abstract: Aspartic Protease Inhibitors: Expedient Synthesis of 2-Substituted Statines

MAT2A Inhibition Blocks the Growth of MTAP-Deleted Cancer Cells by Reducing PRMT5-Dependent mRNA Splicing and Inducing DNA Damage

MTAP Deletions in Cancer Create Vulnerability to Targeting of the MAT2A/PRMT5/RIOK1 Axis

Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers

IDH2 mutation-induced histone and DNA hypermethylation is progressively reversed by small-molecule inhibition

Mutant IDH inhibits HNF-4α to block hepatocyte differentiation and promote biliary cancer

Targeted Inhibition of Mutant IDH2 in Leukemia Cells Induces Cellular Differentiation

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

Combination Targeted Therapy to Disrupt Aberrant Oncogenic Signaling and Reverse Epigenetic Dysfunction in IDH2 - and TET2 -Mutant Acute Myeloid Leukemia

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

Abstract B115: Mitotic defects induced by MAT2A inhibitors guides translational drug combination strategies with AG-270 and taxanes

AG-221, a Small Molecule Mutant IDH2 Inhibitor, Remodels the Epigenetic State of IDH2-Mutant Cells and Induces Alterations in Self-Renewal/Differentiation in IDH2-Mutant AML Model in Vivo

Erratum: Corrigendum: Mutant IDH inhibits HNF-4α to block hepatocyte differentiation and promote biliary cancer

Abstract 2296: IDH2 mutation induced histone and DNA hypermethylation is progressively reversed by small molecule inhibition

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