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Axons Matter: The Promise of Treating Neurodegenerative Disorders by Targeting SARM1-Mediated Axonal Degeneration

Trends in pharmacological sciences (Regular ed.), 2020-04, Vol.41 (4), p.281-293

2020

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NAD + cleavage activity by animal and plant TIR domains in cell death pathways

Science (American Association for the Advancement of Science), 2019-08, Vol.365 (6455), p.793-799

2019

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Highly selective inhibition of Bruton's tyrosine kinase attenuates skin and brain disease in murine lupus

Arthritis research & therapy, 2018-01, Vol.20 (1), p.10-10, Article 10

2018

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Evolution of the Total Synthesis of (−)-Okilactomycin Exploiting a Tandem Oxy-Cope Rearrangement/Oxidation, a Petasis−Ferrier Union/Rearrangement, and Ring-Closing Metathesis

Journal of the American Chemical Society, 2009-02, Vol.131 (6), p.2348-2358

2009

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Small Molecule SARM1 Inhibitors Recapitulate the SARM1−/− Phenotype and Allow Recovery of a Metastable Pool of Axons Fated to Degenerate

Cell reports (Cambridge), 2021-01, Vol.34 (1), p.108588-108588, Article 108588

2021

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Pharmacological SARM1 inhibition protects axon structure and function in paclitaxel-induced peripheral neuropathy

Brain (London, England : 1878), 2021-11, Vol.144 (10), p.3226-3238

2021

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cADPR is a gene dosage-sensitive biomarker of SARM1 activity in healthy, compromised, and degenerating axons

Experimental neurology, 2020-07, Vol.329, p.113252-113252, Article 113252

2020

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SARM1 is a metabolic sensor activated by an increased NMN/NAD+ ratio to trigger axon degeneration

Neuron (Cambridge, Mass.), 2021-04, Vol.109 (7), p.1118-1136.e11

2021

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Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: Part 2, optimization for blood pressure reduction in spontaneously hypertensive rats

Bioorganic & medicinal chemistry letters, 2010-09, Vol.20 (17), p.5153-5156

2010

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Structural basis of SARM1 activation, substrate recognition, and inhibition by small molecules

Molecular cell, 2022-05, Vol.82 (9), p.1643-1659.e10

2022

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Kinase Crystal Miner: A Powerful Approach to Repurposing 3D Hinge Binding Fragments and Its Application to Finding Novel Bruton Tyrosine Kinase Inhibitors

Journal of chemical information and modeling, 2017-09, Vol.57 (9), p.2152-2160

2017

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The Novel, Clinical-Stage Soluble Guanylate Cyclase Activator BI 685509 Protects from Disease Progression in Models of Renal Injury and Disease

The Journal of pharmacology and experimental therapeutics, 2023-03, Vol.384 (3), p.382

2023

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A Soluble Guanylate Cyclase Activator Inhibits the Progression of Diabetic Nephropathy in the ZSF1 Rat

The Journal of pharmacology and experimental therapeutics, 2016-03, Vol.356 (3), p.712

2016

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BTK inhibition ameliorates kidney disease in spontaneous lupus nephritis

Clinical immunology (Orlando, Fla.), 2018-12, Vol.197, p.205-218

2018

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Crystal and cryo-EM structures provide insight into how pro-neurodegenerative SARM1 is activated and cleaves NAD

Acta crystallographica. Section A, Foundations and advances, 2021-08, Vol.77 (a2), p.C431-C431

2021

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Therapeutic Blockade of Immune Complex-Mediated Glomerulonephritis by Highly Selective Inhibition of Bruton's Tyrosine Kinase

Scientific reports, 2016-05, Vol.6 (1), p.26164, Article 26164

2016

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BTK inhibition ameliorates renal, skin, and brain disease in a spontaneous murine model of systemic lupus erythematosus

The Journal of immunology (1950), 2018-05, Vol.200 (1_Supplement), p.175-175.4

2018

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Total Synthesis of (−)-Okilactomycin

Journal of the American Chemical Society, 2007-12, Vol.129 (48), p.14872-14874

2007

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Remission induction of established nephritis by therapeutic administration of a novel BTK inhibitor in an inducible model of lupus nephritis

The Journal of immunology (1950), 2017-05, Vol.198 (1_Supplement), p.224-224.16

2017

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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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Discovery and optimization of oxadiazole-based FLAP inhibitors

Bioorganic & medicinal chemistry letters, 2017-10, Vol.27 (20), p.4652-4659

2017

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Therapeutic blockade of immune complex-mediated glomerulonephritis by highly selective inhibition of Bruton’s tyrosine kinase

The Journal of immunology (1950), 2016-05, Vol.196 (1_Supplement), p.210-210.9

2016

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Development of an Asymmetric Synthesis of a Chiral Quaternary FLAP Inhibitor

Journal of organic chemistry, 2015-02, Vol.80 (3), p.1651-1660

2015

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Early Development Scale-Up of a Structurally-Challenging 5‑Lipoxygenase Activating Protein (FLAP) Inhibitor

Organic process research & development, 2017-09, Vol.21 (9), p.1427-1434

2017

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Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: Part 3, aryl substituted pyrrolidines

Bioorganic & medicinal chemistry letters, 2010-06, Vol.20 (12), p.3746-3749

2010

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Axons Matter: The Promise of Treating Neurodegenerative Disorders by Targeting SARM1-Mediated Axonal Degeneration

NAD + cleavage activity by animal and plant TIR domains in cell death pathways

Highly selective inhibition of Bruton's tyrosine kinase attenuates skin and brain disease in murine lupus

Evolution of the Total Synthesis of (−)-Okilactomycin Exploiting a Tandem Oxy-Cope Rearrangement/Oxidation, a Petasis−Ferrier Union/Rearrangement, and Ring-Closing Metathesis

Small Molecule SARM1 Inhibitors Recapitulate the SARM1−/− Phenotype and Allow Recovery of a Metastable Pool of Axons Fated to Degenerate

Pharmacological SARM1 inhibition protects axon structure and function in paclitaxel-induced peripheral neuropathy

cADPR is a gene dosage-sensitive biomarker of SARM1 activity in healthy, compromised, and degenerating axons

SARM1 is a metabolic sensor activated by an increased NMN/NAD+ ratio to trigger axon degeneration

Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: Part 2, optimization for blood pressure reduction in spontaneously hypertensive rats

Structural basis of SARM1 activation, substrate recognition, and inhibition by small molecules

Kinase Crystal Miner: A Powerful Approach to Repurposing 3D Hinge Binding Fragments and Its Application to Finding Novel Bruton Tyrosine Kinase Inhibitors

The Novel, Clinical-Stage Soluble Guanylate Cyclase Activator BI 685509 Protects from Disease Progression in Models of Renal Injury and Disease

A Soluble Guanylate Cyclase Activator Inhibits the Progression of Diabetic Nephropathy in the ZSF1 Rat

BTK inhibition ameliorates kidney disease in spontaneous lupus nephritis

Crystal and cryo-EM structures provide insight into how pro-neurodegenerative SARM1 is activated and cleaves NAD

Therapeutic Blockade of Immune Complex-Mediated Glomerulonephritis by Highly Selective Inhibition of Bruton's Tyrosine Kinase

BTK inhibition ameliorates renal, skin, and brain disease in a spontaneous murine model of systemic lupus erythematosus

Total Synthesis of (−)-Okilactomycin

Remission induction of established nephritis by therapeutic administration of a novel BTK inhibitor in an inducible model of lupus nephritis

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)

Discovery and optimization of oxadiazole-based FLAP inhibitors

Therapeutic blockade of immune complex-mediated glomerulonephritis by highly selective inhibition of Bruton’s tyrosine kinase

Development of an Asymmetric Synthesis of a Chiral Quaternary FLAP Inhibitor

Early Development Scale-Up of a Structurally-Challenging 5‑Lipoxygenase Activating Protein (FLAP) Inhibitor

Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: Part 3, aryl substituted pyrrolidines

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