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Approaches to discover non-ATP site kinase inhibitors

MedChemComm, 2013, Vol.4 (1), p.41-51

2013

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The role of 11beta-hydroxysteroid dehydrogenase in metabolic disease and therapeutic potential of 11beta-hsd1 inhibitors

Current medicinal chemistry, 2008-03, Vol.15 (7), p.642-649

Saiah, Eddine

2008

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Sestrin modulator NV-5138 produces rapid antidepressant effects via direct mTORC1 activation

The Journal of clinical investigation, 2019-06, Vol.129 (6), p.2542-2554

2019

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Discovery of NV-5138, the first selective Brain mTORC1 activator

Scientific reports, 2019-03, Vol.9 (1), p.4107, Article 4107

2019

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A small molecule inhibitor of Rheb selectively targets mTORC1 signaling

Nature communications, 2018-02, Vol.9 (1), p.548-12, Article 548

2018

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Huntington's disease phenotypes are improved via mTORC1 modulation by small molecule therapy

PloS one, 2022-08, Vol.17 (8), p.e0273710

2022

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Huntington’s disease phenotypes are improved via mTORC1 modulation by small molecule therapy

PloS one, 2022-08, Vol.17 (8), p.e0273710-e0273710

2022

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Discovery of Small-Molecule Selective mTORC1 Inhibitors via Direct Inhibition of Glucose Transporters

Cell chemical biology, 2019-09, Vol.26 (9), p.1203-1213.e13

2019

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Diazine Indole Acetic Acids as Potent, Selective, and Orally Bioavailable Antagonists of Chemoattractant Receptor Homologous Molecule Expressed on Th2 Cells (CRTH2) for the Treatment of Allergic Inflammatory Diseases

Journal of medicinal chemistry, 2012-06, Vol.55 (11), p.5088-5109

2012

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Discovery and gram-scale synthesis of BMS-593214, a potent, selective FVIIa inhibitor

Bioorganic & medicinal chemistry letters, 2013-04, Vol.23 (8), p.2432-2435

2013

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Small molecule coagulation cascade inhibitors in the clinic

Current topics in medicinal chemistry, 2005-01, Vol.5 (16), p.1677-1695

2005

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Discovery of potent and selective matrix metalloprotease 12 inhibitors for the potential treatment of chronic obstructive pulmonary disease (COPD)

Bioorganic & medicinal chemistry letters, 2012-01, Vol.22 (1), p.138-143

2012

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Discovery of HSD-621 as a Potential Agent for the Treatment of Type 2 Diabetes

ACS medicinal chemistry letters, 2013-01, Vol.4 (1), p.118-123

2013

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Sestrin modulator NV-5138 produces rapid antidepressant effects via direct mTORC1 activation

The Journal of clinical investigation, 2019-06, Vol.129 (6), p.2542-2554

2019

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Small Molecules That Target Protein Misfolding

Journal of medicinal chemistry, 2012-12, Vol.55 (24), p.10823-10843

2012

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Recent developments in targeting protein misfolding diseases

Bioorganic & medicinal chemistry letters, 2013-04, Vol.23 (7), p.1935-1944

2013

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Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases

Journal of medicinal chemistry, 2020-11, Vol.63 (22), p.13561-13577

2020

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Comparative Pharmacokinetics and Metabolism Studies in Lean and Diet- Induced Obese Mice: An Animal Efficacy Model for 11β -Hydroxysteroid Dehydrogenase Type 1 (11β -HSD1) Inhibitors

Drug metabolism letters, 2011-01, Vol.5 (1), p.55-63

2011

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Sestrin modulator NV-5138 produces rapid antidepressant effects via direct mTORCI activation

The Journal of clinical investigation, 2019-06, Vol.129 (6), p.2542

2019

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SIRT2- and NRF2-Targeting Thiazole-Containing Compound with Therapeutic Activity in Huntington's Disease Models

Cell chemical biology, 2016-07, Vol.23 (7), p.849-861

2016

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Discovery of Isoquinolinone Indole Acetic Acids as Antagonists of Chemoattractant Receptor Homologous Molecule Expressed on Th2 Cells (CRTH2) for the Treatment of Allergic Inflammatory Diseases

Journal of medicinal chemistry, 2014-02, Vol.57 (4), p.1299-1322

2014

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Phosphonium-mediated cyclization of N-(2-aminophenyl)thioureas: efficient synthesis of 2-aminobenzimidazoles

Tetrahedron letters, 2011-08, Vol.52 (32), p.4149-4152

2011

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Chemistry and biology of the 2β-alkyl-3β-phenyl analogues of cocaine : subnanomolar affinity ligands that suggest a new pharmacophore model at the C-2 position

Journal of medicinal chemistry, 1995-08, Vol.38 (16), p.3086-3093

1995

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Approaches to discover non-ATP site kinase inhibitorsThis article is part of a MedChemComm 'New Talents' issue highlighting the work of outstanding rising scientists in medicinal chemistry research

2012-12

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Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841)

Journal of medicinal chemistry, 2018-10, Vol.61 (19), p.8597-8612

2018

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Approaches to discover non-ATP site kinase inhibitors

The role of 11beta-hydroxysteroid dehydrogenase in metabolic disease and therapeutic potential of 11beta-hsd1 inhibitors

Sestrin modulator NV-5138 produces rapid antidepressant effects via direct mTORC1 activation

Discovery of NV-5138, the first selective Brain mTORC1 activator

A small molecule inhibitor of Rheb selectively targets mTORC1 signaling

Huntington's disease phenotypes are improved via mTORC1 modulation by small molecule therapy

Huntington’s disease phenotypes are improved via mTORC1 modulation by small molecule therapy

Discovery of Small-Molecule Selective mTORC1 Inhibitors via Direct Inhibition of Glucose Transporters

Diazine Indole Acetic Acids as Potent, Selective, and Orally Bioavailable Antagonists of Chemoattractant Receptor Homologous Molecule Expressed on Th2 Cells (CRTH2) for the Treatment of Allergic Inflammatory Diseases

Discovery and gram-scale synthesis of BMS-593214, a potent, selective FVIIa inhibitor

Small molecule coagulation cascade inhibitors in the clinic

Discovery of potent and selective matrix metalloprotease 12 inhibitors for the potential treatment of chronic obstructive pulmonary disease (COPD)

Discovery of HSD-621 as a Potential Agent for the Treatment of Type 2 Diabetes

Sestrin modulator NV-5138 produces rapid antidepressant effects via direct mTORC1 activation

Small Molecules That Target Protein Misfolding

Recent developments in targeting protein misfolding diseases

Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases

Comparative Pharmacokinetics and Metabolism Studies in Lean and Diet- Induced Obese Mice: An Animal Efficacy Model for 11β -Hydroxysteroid Dehydrogenase Type 1 (11β -HSD1) Inhibitors

Sestrin modulator NV-5138 produces rapid antidepressant effects via direct mTORCI activation

SIRT2- and NRF2-Targeting Thiazole-Containing Compound with Therapeutic Activity in Huntington's Disease Models

Discovery of Isoquinolinone Indole Acetic Acids as Antagonists of Chemoattractant Receptor Homologous Molecule Expressed on Th2 Cells (CRTH2) for the Treatment of Allergic Inflammatory Diseases

Phosphonium-mediated cyclization of N-(2-aminophenyl)thioureas: efficient synthesis of 2-aminobenzimidazoles

Chemistry and biology of the 2β-alkyl-3β-phenyl analogues of cocaine : subnanomolar affinity ligands that suggest a new pharmacophore model at the C-2 position

Approaches to discover non-ATP site kinase inhibitorsThis article is part of a MedChemComm 'New Talents' issue highlighting the work of outstanding rising scientists in medicinal chemistry research

Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841)

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