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Widespread potential for growth-factor-driven resistance to anticancer kinase inhibitors

Nature (London), 2012-07, Vol.487 (7408), p.505-509

2012

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Fibroblast Activation Protein Cleaves and Inactivates Fibroblast Growth Factor 21

The Journal of biological chemistry, 2016-03, Vol.291 (11), p.5986-5996

2016

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Nav1.7 inhibitors for the treatment of chronic pain

Bioorganic & medicinal chemistry letters, 2018-10, Vol.28 (19), p.3141-3149

2018

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GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway

Molecular cancer therapeutics, 2011-12, Vol.10 (12), p.2426-2436

2011

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Structural basis of Nav1.7 inhibition by an isoform-selective small-molecule antagonist

Science (American Association for the Advancement of Science), 2015-12, Vol.350 (6267), p.1491-1491

2015

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Activation of caspases-8 and -10 by FLIPL

Biochemical journal, 2004-09, Vol.382 (2), p.651-657

2004

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GDC-0449—A potent inhibitor of the hedgehog pathway

Bioorganic & medicinal chemistry letters, 2009-10, Vol.19 (19), p.5576-5581

2009

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Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Nav1.7 Inhibitors for the Treatment of Chronic Pain

Journal of medicinal chemistry, 2019-04, Vol.62 (8), p.4091-4109

2019

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Selective NaV1.7 Antagonists with Long Residence Time Show Improved Efficacy against Inflammatory and Neuropathic Pain

Cell reports (Cambridge), 2018-09, Vol.24 (12), p.3133-3145

2018

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Discovery of (Thienopyrimidin-2-yl)aminopyrimidines as Potent, Selective, and Orally Available Pan-PI3-Kinase and Dual Pan-PI3-Kinase/mTOR Inhibitors for the Treatment of Cancer

Journal of medicinal chemistry, 2010-02, Vol.53 (3), p.1086-1097

2010

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A Unified Model for Apical Caspase Activation

Molecular cell, 2003-02, Vol.11 (2), p.529-541

2003

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Discovery of Acyl-sulfonamide Nav1.7 Inhibitors GDC-0276 and GDC-0310

Journal of medicinal chemistry, 2021-03, Vol.64 (6), p.2953-2966

2021

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Discovery of Acyl-sulfonamide Na v 1.7 Inhibitors GDC-0276 and GDC-0310

Journal of medicinal chemistry, 2021-03, Vol.64 (6), p.2953-2966

2021

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Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNa V 1.7 Inhibitors for the Treatment of Pain

Journal of medicinal chemistry, 2018-06, Vol.61 (11), p.4810

2018

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Rational Design of Phosphoinositide 3-Kinase α Inhibitors That Exhibit Selectivity over the Phosphoinositide 3-Kinase β Isoform

Journal of medicinal chemistry, 2011-11, Vol.54 (22), p.7815-7833

2011

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Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor

Bioorganic & medicinal chemistry letters, 2010-04, Vol.20 (8), p.2408-2411

2010

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Potent and Highly Selective Benzimidazole Inhibitors of PI3-Kinase Delta

Journal of medicinal chemistry, 2012-09, Vol.55 (17), p.7686-7695

2012

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Discovery of Aryl Sulfonamides as Isoform-Selective Inhibitors of NaV1.7 with Efficacy in Rodent Pain Models

ACS medicinal chemistry letters, 2016-03, Vol.7 (3), p.277-282

2016

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Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Na v 1.7 Inhibitors for the Treatment of Chronic Pain

Journal of medicinal chemistry, 2019-04, Vol.62 (8), p.4091-4109

2019

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Discovery and preclinical development of vismodegib

Expert opinion on drug discovery, 2014-08, Vol.9 (8), p.969-984

2014

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Discovery of Novel PI3-Kinase δ Specific Inhibitors for the Treatment of Rheumatoid Arthritis: Taming CYP3A4 Time-Dependent Inhibition

Journal of medicinal chemistry, 2012-06, Vol.55 (12), p.5887-5900

2012

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Design of Selective Benzoxazepin PI3Kδ Inhibitors Through Control of Dihedral Angles

ACS medicinal chemistry letters, 2017-09, Vol.8 (9), p.936-940

2017

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Identification of GNE-293, a potent and selective PI3Kδ inhibitor: Navigating in vitro genotoxicity while improving potency and selectivity

Bioorganic & medicinal chemistry letters, 2013-09, Vol.23 (17), p.4953-4959

2013

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Widespread potential for growth-factor-driven resistance to anticancer kinase inhibitors

Fibroblast Activation Protein Cleaves and Inactivates Fibroblast Growth Factor 21

Nav1.7 inhibitors for the treatment of chronic pain

GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway

Discovery of a Potent, Selective, and Orally Available Class I Phosphatidylinositol 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Kinase Inhibitor (GDC-0980) for the Treatment of Cancer

Structural basis of Nav1.7 inhibition by an isoform-selective small-molecule antagonist

Activation of caspases-8 and -10 by FLIPL

GDC-0449—A potent inhibitor of the hedgehog pathway

Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Nav1.7 Inhibitors for the Treatment of Chronic Pain

Selective NaV1.7 Antagonists with Long Residence Time Show Improved Efficacy against Inflammatory and Neuropathic Pain

Discovery of (Thienopyrimidin-2-yl)aminopyrimidines as Potent, Selective, and Orally Available Pan-PI3-Kinase and Dual Pan-PI3-Kinase/mTOR Inhibitors for the Treatment of Cancer

Identification of Selective Acyl Sulfonamide–Cycloalkylether Inhibitors of the Voltage-Gated Sodium Channel (NaV) 1.7 with Potent Analgesic Activity

A Unified Model for Apical Caspase Activation

Discovery of Acyl-sulfonamide Nav1.7 Inhibitors GDC-0276 and GDC-0310

Discovery of Acyl-sulfonamide Na v 1.7 Inhibitors GDC-0276 and GDC-0310

Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNa V 1.7 Inhibitors for the Treatment of Pain

Rational Design of Phosphoinositide 3-Kinase α Inhibitors That Exhibit Selectivity over the Phosphoinositide 3-Kinase β Isoform

Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor

Potent and Highly Selective Benzimidazole Inhibitors of PI3-Kinase Delta

Discovery of Aryl Sulfonamides as Isoform-Selective Inhibitors of NaV1.7 with Efficacy in Rodent Pain Models

Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Na v 1.7 Inhibitors for the Treatment of Chronic Pain

Discovery and preclinical development of vismodegib

Discovery of Novel PI3-Kinase δ Specific Inhibitors for the Treatment of Rheumatoid Arthritis: Taming CYP3A4 Time-Dependent Inhibition

Design of Selective Benzoxazepin PI3Kδ Inhibitors Through Control of Dihedral Angles

Identification of GNE-293, a potent and selective PI3Kδ inhibitor: Navigating in vitro genotoxicity while improving potency and selectivity

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