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Development of nitrile-based peptidic inhibitors of cysteine cathepsins

Current topics in medicinal chemistry, 2010-02, Vol.10 (3), p.294-322

2010

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Structural Optimization of Azadipeptide Nitriles Strongly Increases Association Rates and Allows the Development of Selective Cathepsin Inhibitors

Journal of medicinal chemistry, 2011-01, Vol.54 (1), p.396-400

2011

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Facing the gem-Dialkyl Effect in Enzyme Inhibitor Design: Preparation of Homocycloleucine-Based Azadipeptide Nitriles

Chemistry : a European journal, 2011-10, Vol.17 (41), p.11419-11423

2011

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Azadipeptide Nitriles: Highly Potent and Proteolytically Stable Inhibitors of Papain-Like Cysteine Proteases

Angewandte Chemie (International ed.), 2008-05, Vol.47 (23), p.4331-4334

2008

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A New Objective Method to Compare Different Color Reactions for the Detection of Cyclic Ureides

Analytical Sciences, 2005, Vol.21(12), pp.1561-1564

2005

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Chemical introduction of the green fluorescence: imaging of cysteine cathepsins by an irreversibly locked GFP fluorophore

Organic & biomolecular chemistry, 2013-09, Vol.11 (35), p.5913-5921

2013

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Synthesis and preliminary radiopharmacological characterisation of an 11 C-labelled azadipeptide nitrile as potential PET tracer for imaging of cysteine cathepsins

Journal of labelled compounds & radiopharmaceuticals, 2019-06, Vol.62 (8), p.448-459

2019

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Synthesis and preliminary radiopharmacological characterisation of an 11C‐labelled azadipeptide nitrile as potential PET tracer for imaging of cysteine cathepsins

Journal of labelled compounds & radiopharmaceuticals, 2019-06, Vol.62 (8), p.448-459

2019

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Fluorescent nitrile-based inhibitors of cysteine cathepsins

Bioorganic & medicinal chemistry letters, 2012-12, Vol.22 (24), p.7715-7718

2012

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Selective Nitrile Inhibitors To Modulate the Proteolytic Synergism of Cathepsins S and F

Journal of medicinal chemistry, 2012-06, Vol.55 (12), p.5982-5986

2012

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Active Site Mapping of Human Cathepsin F with Dipeptide Nitrile Inhibitors

ChemMedChem, 2015-08, Vol.10 (8), p.1365-1377

2015

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Synthesis and Radiopharmacological Characterisation of a Fluorine-18-Labelled Azadipeptide Nitrile as a Potential PET Tracer for invivo Imaging of Cysteine Cathepsins

ChemMedChem, 2013-08, Vol.8 (8), p.1330

2013

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α,β → β,γ double bond migration in corallopyronin A biosynthesis

Chemical science (Cambridge), 2013-01, Vol.4 (11), p.4175

2013

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Chemical introduction of the green fluorescence: imaging of cysteine cathepsins by an irreversibly locked GFP fluorophoreElectronic supplementary information (ESI) available: Inhibition assays for cathepsins L, S, K, and B, spectral properties of 12, as well as 13C NMR spectra of 2, 4, 5, 7, 8, 9, 11, and 12. See DOI: 10.1039/c3ob41341a

2013-08

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Active Site Mapping of Human CathepsinF with Dipeptide Nitrile Inhibitors

ChemMedChem, 2015-08, Vol.10 (8), p.1365

2015

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Inside Cover: Synthesis and Radiopharmacological Characterisation of a Fluorine-18-Labelled Azadipeptide Nitrile as a Potential PET Tracer for invivo Imaging of Cysteine Cathepsins (ChemMedChem 8/2013)

ChemMedChem, 2013-08, Vol.8 (8), p.1230

2013

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Inside Cover: Synthesis and Radiopharmacological Characterisation of a Fluorine-18-Labelled Azadipeptide Nitrile as a Potential PET Tracer for in vivo Imaging of Cysteine Cathepsins (ChemMedChem 8/2013)

ChemMedChem, 2013-08, Vol.8 (8), p.1230-1230

2013

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Synthesis and Radiopharmacological Characterisation of a Fluorine-18-Labelled Azadipeptide Nitrile as a Potential PET Tracer for in vivo Imaging of Cysteine Cathepsins

ChemMedChem, 2013-08, Vol.8 (8), p.1330-1344

2013

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Antimalarial activity of azadipeptide nitriles

Bioorganic & medicinal chemistry letters, 2010-01, Vol.20 (1), p.252-255

2010

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New Cathepsin Inhibitors to Explore the Fluorophilic Properties of the S2 Pocket of Cathepsin B: Design, Synthesis, and Biological Evaluation

Chemistry : a European journal, 2011-05, Vol.17 (19), p.5256-5260

2011

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Azadipeptidnitrile - hochpotente und proteolysestabile Inhibitoren Papain-ähnlicher Cysteinproteasen

Angewandte Chemie, 2008-05, Vol.120 (23), p.4403-4406

2008

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New Cathepsin Inhibitors to Explore the Fluorophilic Properties of the S 2 Pocket of Cathepsin B: Design, Synthesis, and Biological Evaluation

Chemistry : a European journal, 2011-05, Vol.17 (19), p.5256-5260

2011

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Synthesis and elastase-inhibiting activity of 2-pyridinyl-isothiazol-3(2 H)-one 1,1-dioxides

Bioorganic & medicinal chemistry, 2008-09, Vol.16 (17), p.8127-8135

2008

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Inhibitors of Cathepsins K and S Identified Using the DynaMAD Virtual Screening Algorithm

ChemMedChem, 2010-01, Vol.5 (1), p.61-64

2010

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Hit Expansion through Computational Selectivity Searching

ChemMedChem, 2009-01, Vol.4 (1), p.52-54

2009

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Development of nitrile-based peptidic inhibitors of cysteine cathepsins

Structural Optimization of Azadipeptide Nitriles Strongly Increases Association Rates and Allows the Development of Selective Cathepsin Inhibitors

Facing the gem-Dialkyl Effect in Enzyme Inhibitor Design: Preparation of Homocycloleucine-Based Azadipeptide Nitriles

Azadipeptide Nitriles: Highly Potent and Proteolytically Stable Inhibitors of Papain-Like Cysteine Proteases

A New Objective Method to Compare Different Color Reactions for the Detection of Cyclic Ureides

Chemical introduction of the green fluorescence: imaging of cysteine cathepsins by an irreversibly locked GFP fluorophore

Synthesis and preliminary radiopharmacological characterisation of an 11 C-labelled azadipeptide nitrile as potential PET tracer for imaging of cysteine cathepsins

Synthesis and preliminary radiopharmacological characterisation of an 11C‐labelled azadipeptide nitrile as potential PET tracer for imaging of cysteine cathepsins

Fluorescent nitrile-based inhibitors of cysteine cathepsins

Selective Nitrile Inhibitors To Modulate the Proteolytic Synergism of Cathepsins S and F

Active Site Mapping of Human Cathepsin F with Dipeptide Nitrile Inhibitors

Synthesis and Radiopharmacological Characterisation of a Fluorine-18-Labelled Azadipeptide Nitrile as a Potential PET Tracer for invivo Imaging of Cysteine Cathepsins

α,β → β,γ double bond migration in corallopyronin A biosynthesis

Active Site Mapping of Human CathepsinF with Dipeptide Nitrile Inhibitors

Inside Cover: Synthesis and Radiopharmacological Characterisation of a Fluorine-18-Labelled Azadipeptide Nitrile as a Potential PET Tracer for invivo Imaging of Cysteine Cathepsins (ChemMedChem 8/2013)

Inside Cover: Synthesis and Radiopharmacological Characterisation of a Fluorine-18-Labelled Azadipeptide Nitrile as a Potential PET Tracer for in vivo Imaging of Cysteine Cathepsins (ChemMedChem 8/2013)

Synthesis and Radiopharmacological Characterisation of a Fluorine-18-Labelled Azadipeptide Nitrile as a Potential PET Tracer for in vivo Imaging of Cysteine Cathepsins

Antimalarial activity of azadipeptide nitriles

New Cathepsin Inhibitors to Explore the Fluorophilic Properties of the S2 Pocket of Cathepsin B: Design, Synthesis, and Biological Evaluation

Azadipeptidnitrile - hochpotente und proteolysestabile Inhibitoren Papain-ähnlicher Cysteinproteasen

New Cathepsin Inhibitors to Explore the Fluorophilic Properties of the S 2 Pocket of Cathepsin B: Design, Synthesis, and Biological Evaluation

Synthesis and elastase-inhibiting activity of 2-pyridinyl-isothiazol-3(2 H)-one 1,1-dioxides

Inhibitors of Cathepsins K and S Identified Using the DynaMAD Virtual Screening Algorithm

Hit Expansion through Computational Selectivity Searching

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