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Pharmacological targeting of the unfolded protein response for disease intervention

Nature chemical biology, 2019-08, Vol.15 (8), p.764

2019

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Targeting PERK signaling with the small molecule GSK2606414 prevents neurodegeneration in a model of Parkinson's disease

Neurobiology of disease, 2018-04, Vol.112, p.136-148

2018

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Oral treatment targeting the unfolded protein response prevents neurodegeneration and clinical disease in prion-infected mice

Science translational medicine, 2013-10, Vol.5 (206), p.206ra138

2013

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Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1

Biochemical journal, 2011-01, Vol.433 (2), p.357-369

2011

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Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development

ACS medicinal chemistry letters, 2013-10, Vol.4 (10), p.964-968

2013

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Broad Kinase Inhibition Mitigates Early Neuronal Dysfunction in Tauopathy

International journal of molecular sciences, 2021-01, Vol.22 (3), p.1186

2021

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Protein kinase R(PKR)-like endoplasmic reticulum kinase (PERK) inhibitors: a patent review (2010-2015)

Expert opinion on therapeutic patents, 2017-01, Vol.27 (1), p.37-48

Axten, Jeffrey M.

2017

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Characterization of a Novel PERK Kinase Inhibitor with Antitumor and Antiangiogenic Activity

Cancer research (Chicago, Ill.), 2013-03, Vol.73 (6), p.1993-2002

2013

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PERK inhibition delays neurodegeneration and improves motor function in a mouse model of Marinesco-Sjögren syndrome

Human molecular genetics, 2018-07, Vol.27 (14), p.2477-2489

2018

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A highly selective, cell-permeable furin inhibitor BOS-318 rescues key features of cystic fibrosis airway disease

Cell chemical biology, 2022-06, Vol.29 (6), p.947-957.e8

2022

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The First Total Syntheses of Ircinol A, Ircinal A, and Manzamines A and D

Journal of the American Chemical Society, 1998-07, Vol.120 (25), p.6425-6426

1998

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Enantioselective Synthesis of d -threo-Methylphenidate

Journal of the American Chemical Society, 1999-07, Vol.121 (27), p.6511-6512

1999

Volltextzugriff (PDF)

Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases

Bioorganic & medicinal chemistry letters, 2011-12, Vol.21 (24), p.7489-7495

2011

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Structure-Based Design of Potent and Selective 3-Phosphoinositide-Dependent Kinase-1 (PDK1) Inhibitors

Journal of medicinal chemistry, 2011-03, Vol.54 (6), p.1871-1895

2011

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Conversion of 2-deoxyglucose-induced growth inhibition to cell death in normoxic tumor cells

Cancer chemotherapy and pharmacology, 2013-07, Vol.72 (1), p.251-262

2013

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Rapid synthesis of diversely functionalized 3,4,7-trisubstituted indoles

Tetrahedron letters, 2011-06, Vol.52 (26), p.3376-3378

2011

Volltextzugriff (PDF)

TLR2 agonism reverses chemotherapy-induced neutropenia in Macaca fascicularis

Blood advances, 2017-12, Vol.1 (26), p.2553-2562

2017

Volltextzugriff (PDF)

Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery

ACS medicinal chemistry letters, 2010-11, Vol.1 (8), p.439-442

2010

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Acylprolinamides: A new class of peptide deformylase inhibitors with in vivo antibacterial activity

Bioorganic & medicinal chemistry letters, 2012-06, Vol.22 (12), p.4028-4032

2012

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Discovery of a new series of Aurora inhibitors through truncation of GSK1070916

Bioorganic & medicinal chemistry letters, 2010-04, Vol.20 (8), p.2552-2555

2010

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Benzyl 2-Cyano-3,3-Dimethyl-1-pyrrolidinecarboxylate, a Versatile Intermediate for the Synthesis of 3,3-Dimethylproline Derivatives

Journal of organic chemistry, 2008-05, Vol.73 (10), p.3946-3949

2008

Volltextzugriff (PDF)

Furin Inhibition as a Mechanism to Reduce Aberrant ENaC‐Mediated Sodium Transport and Rehydrate the Airways in Cystic Fibrosis Lung Disease

The FASEB journal, 2019-04, Vol.33 (S1), p.802.26-802.26

2019

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An efficient and practical synthesis of 2,4-substituted pyrido[4,3-d]pyrimidin-5(6H)-ones

Tetrahedron letters, 2019-12, Vol.60 (49), p.151312, Article 151312

2019

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A Stereoselective Synthesis of dl-threo-Methylphenidate: Preparation and Biological Evaluation of Novel Analogues

Journal of organic chemistry, 1998-12, Vol.63 (26), p.9628-9629

1998

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Pharmacological targeting of the unfolded protein response for disease intervention

Targeting PERK signaling with the small molecule GSK2606414 prevents neurodegeneration in a model of Parkinson's disease

Oral treatment targeting the unfolded protein response prevents neurodegeneration and clinical disease in prion-infected mice

Discovery of 7‑Methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro‑1H‑indol-5-yl)‑7H‑pyrrolo[2,3‑d]pyrimidin-4-amine (GSK2606414), a Potent and Selective First-in-Class Inhibitor of Protein Kinase R (PKR)-like Endoplasmic Reticulum Kinase (PERK)

Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1

Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development

Broad Kinase Inhibition Mitigates Early Neuronal Dysfunction in Tauopathy

Protein kinase R(PKR)-like endoplasmic reticulum kinase (PERK) inhibitors: a patent review (2010-2015)

Characterization of a Novel PERK Kinase Inhibitor with Antitumor and Antiangiogenic Activity

PERK inhibition delays neurodegeneration and improves motor function in a mouse model of Marinesco-Sjögren syndrome

A highly selective, cell-permeable furin inhibitor BOS-318 rescues key features of cystic fibrosis airway disease

The First Total Syntheses of Ircinol A, Ircinal A, and Manzamines A and D

Enantioselective Synthesis of d -threo-Methylphenidate

Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases

Structure-Based Design of Potent and Selective 3-Phosphoinositide-Dependent Kinase-1 (PDK1) Inhibitors

Conversion of 2-deoxyglucose-induced growth inhibition to cell death in normoxic tumor cells

Rapid synthesis of diversely functionalized 3,4,7-trisubstituted indoles

TLR2 agonism reverses chemotherapy-induced neutropenia in Macaca fascicularis

Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery

Acylprolinamides: A new class of peptide deformylase inhibitors with in vivo antibacterial activity

Discovery of a new series of Aurora inhibitors through truncation of GSK1070916

Benzyl 2-Cyano-3,3-Dimethyl-1-pyrrolidinecarboxylate, a Versatile Intermediate for the Synthesis of 3,3-Dimethylproline Derivatives

Furin Inhibition as a Mechanism to Reduce Aberrant ENaC‐Mediated Sodium Transport and Rehydrate the Airways in Cystic Fibrosis Lung Disease

An efficient and practical synthesis of 2,4-substituted pyrido[4,3-d]pyrimidin-5(6H)-ones

A Stereoselective Synthesis of dl-threo-Methylphenidate: Preparation and Biological Evaluation of Novel Analogues

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