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Chemical Genetics―Based Target Identification in Drug Discovery

Annual review of pharmacology and toxicology, 2012-01, Vol.52 (1), p.57-78

2012

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Use of Intramolecular 1,5-Sulfur–Oxygen and 1,5-Sulfur–Halogen Interactions in the Design of N‑Methyl-5-aryl‑N‑(2,2,6,6-tetramethylpiperidin-4-yl)-1,3,4-thiadiazol-2-amine SMN2 Splicing Modulators

Journal of medicinal chemistry, 2021-04, Vol.64 (8), p.4744-4761

2021

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Identification of NVP-TNKS656: The Use of Structure–Efficiency Relationships To Generate a Highly Potent, Selective, and Orally Active Tankyrase Inhibitor

Journal of medicinal chemistry, 2013-08, Vol.56 (16), p.6495-6511

2013

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Discovery of Icenticaftor (QBW251), a Cystic Fibrosis Transmembrane Conductance Regulator Potentiator with Clinical Efficacy in Cystic Fibrosis and Chronic Obstructive Pulmonary Disease

Journal of medicinal chemistry, 2021-06, Vol.64 (11), p.7241-7260

2021

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Discovery of Small Molecule Splicing Modulators of Survival Motor Neuron‑2 (SMN2) for the Treatment of Spinal Muscular Atrophy (SMA)

Journal of medicinal chemistry, 2018-12, Vol.61 (24), p.11021-11036

2018

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Conformationally Restricted (+)-Cacospongionolide B Analogues. Influence on Secretory Phospholipase A2 Inhibition

Journal of organic chemistry, 2007-03, Vol.72 (5), p.1545-1552

2007

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Total Syntheses of (+)- and (−)-Cacospongionolide B: New Insight into Structural Requirements for Phospholipase A2 Inhibition

Journal of the American Chemical Society, 2002-10, Vol.124 (39), p.11584-11585

2002

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PIKfyve, a Class III PI Kinase, Is the Target of the Small Molecular IL-12/IL-23 Inhibitor Apilimod and a Player in Toll-like Receptor Signaling

Chemistry & biology, 2013-07, Vol.20 (7), p.912-921

2013

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Accelerating the discovery of new drug targets with chemical proteomics

IDrugs : the investigational drugs journal, 2010-12, Vol.13 (12), p.862

2010

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Total Syntheses of (+)- and (−)-Cacospongionolide B, Cacospongionolide E, and Related Analogues. Preliminary Study of Structural Features Required for Phospholipase A2 Inhibition

Journal of organic chemistry, 2004-08, Vol.69 (17), p.5712-5719

2004

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[1,2,4]Triazol-3-ylsulfanylmethyl)-3-phenyl-[1,2,4]oxadiazoles: Antagonists of the Wnt Pathway That Inhibit Tankyrases 1 and 2 via Novel Adenosine Pocket Binding

Journal of medicinal chemistry, 2012-02, Vol.55 (3), p.1127-1136

2012

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Structure of human tankyrase 1 in complex with small-molecule inhibitors PJ34 and XAV939

Acta crystallographica. Section F, Structural biology and crystallization communications, 2012-02, Vol.68 (2), p.115-118

2012

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Total syntheses of (+)- and (-)-cacospongionolide B: new insight into structural requirements for phospholipase A(2) inhibition

Journal of the American Chemical Society, 2002-10, Vol.124 (39), p.11584-11585

2002

Volltextzugriff (PDF)

Conformationally Restricted (+)-Cacospongionolide B Analogues. Influence on Secretory Phospholipase A 2 Inhibition

Journal of organic chemistry, 2007-03, Vol.72 (5), p.1545-1552

2007

Volltextzugriff (PDF)

Total Syntheses of (+)- and (−)-Cacospongionolide B: New Insight into Structural Requirements for Phospholipase A 2 Inhibition

Journal of the American Chemical Society, 2002-10, Vol.124 (39), p.11584-11585

2002

Volltextzugriff (PDF)

Total Syntheses of (+)- and (−)-Cacospongionolide B, Cacospongionolide E, and Related Analogues. Preliminary Study of Structural Features Required for Phospholipase A 2 Inhibition

Journal of organic chemistry, 2004-08, Vol.69 (17), p.5712-5719

2004

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Total syntheses of (+)- and (-)-cacospongionolide B: Investigation into structural requirements for phospholipase A(2) inhibition

Cheung, Atwood Kim

2003

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PIKfyve, a class III PI-kinase, is the target of the small molecular IL12/23 inhibitor apilimod and a new player in toll-like receptor signaling

Chemistry & biology, 2013-07, Vol.20 (7), p.912-921

2013

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Total Syntheses of (+)‐ and (‐)‐Cacospongionolide B: New Insight into Structural Requirements for Phospholipase A 2 Inhibition

ChemInform, 2003-02, Vol.34 (6)

2003

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Total Syntheses of (+)- and (-)-Cacospongionolide B: New Insight into Structural Requirements for Phospholipase A2 Inhibition

ChemInform, 2003-02, Vol.34 (6), p.no-no

2003

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Total Syntheses of (+)- and (-)-Cacospongionolide B, Cacospongionolide E, and Related Analogues. Preliminary Study of Structural Features Required for Phospholipase A2 Inhibition

ChemInform, 2004-12, Vol.35 (52), p.no-no

2004

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Total Syntheses of (+)‐ and (‐)‐Cacospongionolide B, Cacospongionolide E, and Related Analogues. Preliminary Study of Structural Features Required for Phospholipase A 2 Inhibition

ChemInform, 2004-12, Vol.35 (52)

2004

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Protecting the global ocean for biodiversity, food and climate

Nature (London), 2021-04, Vol.592 (7854), p.397-402

2021

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Chemical Genetics―Based Target Identification in Drug Discovery

SMN2 splice modulators enhance U1-pre-mRNA association and rescue SMA mice

Use of Intramolecular 1,5-Sulfur–Oxygen and 1,5-Sulfur–Halogen Interactions in the Design of N‑Methyl-5-aryl‑N‑(2,2,6,6-tetramethylpiperidin-4-yl)-1,3,4-thiadiazol-2-amine SMN2 Splicing Modulators

Identification of NVP-TNKS656: The Use of Structure–Efficiency Relationships To Generate a Highly Potent, Selective, and Orally Active Tankyrase Inhibitor

Discovery of Icenticaftor (QBW251), a Cystic Fibrosis Transmembrane Conductance Regulator Potentiator with Clinical Efficacy in Cystic Fibrosis and Chronic Obstructive Pulmonary Disease

Discovery of Small Molecule Splicing Modulators of Survival Motor Neuron‑2 (SMN2) for the Treatment of Spinal Muscular Atrophy (SMA)

Conformationally Restricted (+)-Cacospongionolide B Analogues. Influence on Secretory Phospholipase A2 Inhibition

Total Syntheses of (+)- and (−)-Cacospongionolide B: New Insight into Structural Requirements for Phospholipase A2 Inhibition

PIKfyve, a Class III PI Kinase, Is the Target of the Small Molecular IL-12/IL-23 Inhibitor Apilimod and a Player in Toll-like Receptor Signaling

Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling

Accelerating the discovery of new drug targets with chemical proteomics

Total Syntheses of (+)- and (−)-Cacospongionolide B, Cacospongionolide E, and Related Analogues. Preliminary Study of Structural Features Required for Phospholipase A2 Inhibition

[1,2,4]Triazol-3-ylsulfanylmethyl)-3-phenyl-[1,2,4]oxadiazoles: Antagonists of the Wnt Pathway That Inhibit Tankyrases 1 and 2 via Novel Adenosine Pocket Binding

Structure of human tankyrase 1 in complex with small-molecule inhibitors PJ34 and XAV939

Total syntheses of (+)- and (-)-cacospongionolide B: new insight into structural requirements for phospholipase A(2) inhibition

Conformationally Restricted (+)-Cacospongionolide B Analogues. Influence on Secretory Phospholipase A 2 Inhibition

Total Syntheses of (+)- and (−)-Cacospongionolide B: New Insight into Structural Requirements for Phospholipase A 2 Inhibition

Total Syntheses of (+)- and (−)-Cacospongionolide B, Cacospongionolide E, and Related Analogues. Preliminary Study of Structural Features Required for Phospholipase A 2 Inhibition

Total syntheses of (+)- and (-)-cacospongionolide B: Investigation into structural requirements for phospholipase A(2) inhibition

PIKfyve, a class III PI-kinase, is the target of the small molecular IL12/23 inhibitor apilimod and a new player in toll-like receptor signaling

Total Syntheses of (+)‐ and (‐)‐Cacospongionolide B: New Insight into Structural Requirements for Phospholipase A 2 Inhibition

Total Syntheses of (+)- and (-)-Cacospongionolide B: New Insight into Structural Requirements for Phospholipase A2 Inhibition

Total Syntheses of (+)- and (-)-Cacospongionolide B, Cacospongionolide E, and Related Analogues. Preliminary Study of Structural Features Required for Phospholipase A2 Inhibition

Total Syntheses of (+)‐ and (‐)‐Cacospongionolide B, Cacospongionolide E, and Related Analogues. Preliminary Study of Structural Features Required for Phospholipase A 2 Inhibition

Protecting the global ocean for biodiversity, food and climate

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