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Biochemical characterization of protease activity of Nsp3 from SARS-CoV-2 and its inhibition by nanobodies

PloS one, 2021-07, Vol.16 (7), p.e0253364

2021

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Comparison of a High-Throughput High-Content Intracellular Leishmania donovani Assay with an Axenic Amastigote Assay

Antimicrobial Agents and Chemotherapy, 2013-07, Vol.57 (7), p.2913-2922

2013

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Targeting N-myristoylation for therapy of B-cell lymphomas

Nature communications, 2020-10, Vol.11 (1), p.5348-5348, Article 5348

2020

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Target validation: linking target and chemical properties to desired product profile

Current topics in medicinal chemistry, 2011-05, Vol.11 (10), p.1275

2011

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N -myristoyltransferase inhibitors as new leads to treat sleeping sickness

Nature, 2010-04, Vol.464 (7289), p.728-732

2010

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Design of the Global Health chemical diversity library v2 for screening against infectious diseases

PLoS neglected tropical diseases, 2023-12, Vol.17 (12), p.e0011799-e0011799

2023

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Fragment library design, synthesis and expansion: nurturing a synthesis and training platform

Drug discovery today, 2017-01, Vol.22 (1), p.43-56

2017

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Inhibiting Mycobacterium tuberculosis CoaBC by targeting an allosteric site

Nature communications, 2021-01, Vol.12 (1), p.143-143, Article 143

2021

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Lead Optimization of a Pyrazole Sulfonamide Series of Trypanosoma brucei N‑Myristoyltransferase Inhibitors: Identification and Evaluation of CNS Penetrant Compounds as Potential Treatments for Stage 2 Human African Trypanosomiasis

Journal of medicinal chemistry, 2014-12, Vol.57 (23), p.9855-9869

2014

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Exploring the Trypanosoma brucei Hsp83 potential as a target for structure guided drug design

PLoS neglected tropical diseases, 2013-10, Vol.7 (10), p.e2492

2013

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Identification of Inhibitors of Protein Kinase B Using Fragment-Based Lead Discovery

Journal of medicinal chemistry, 2007-05, Vol.50 (10), p.2293-2296

2007

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One Scaffold, Three Binding Modes: Novel and Selective Pteridine Reductase 1 Inhibitors Derived from Fragment Hits Discovered by Virtual Screening

Journal of medicinal chemistry, 2009-07, Vol.52 (14), p.4454-4465

2009

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Screening a protein kinase inhibitor library against Plasmodium falciparum

Malaria journal, 2017-11, Vol.16 (1), p.446-446, Article 446

2017

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De Novo Design of Protein Kinase Inhibitors by in Silico Identification of Hinge Region-Binding Fragments

ACS chemical biology, 2013-05, Vol.8 (5), p.1044-1052

2013

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Generation of Polar Semi‐Saturated Bicyclic Pyrazoles for Fragment‐Based Drug‐Discovery Campaigns

Chemistry : a European journal, 2018-07, Vol.24 (41), p.10443-10451

2018

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Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need

Nature reviews. Microbiology, 2017-04, Vol.15 (4), p.217-231

2017

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Diversity-oriented synthesis of bicyclic fragments containing privileged azines

Bioorganic & medicinal chemistry letters, 2019-01, Vol.29 (2), p.248-251

2019

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PE/PPE proteins mediate nutrient transport across the outer membrane of Mycobacterium tuberculosis

Science (American Association for the Advancement of Science), 2020-03, Vol.367 (6482), p.1147-1151

2020

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A target repurposing approach identifies N-myristoyltransferase as a new candidate drug target in filarial nematodes

PLoS neglected tropical diseases, 2014-09, Vol.8 (9), p.e3145-e3145

2014

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Structure–Activity Relationships of Pyrazolo[1,5‑a]pyrimidin-7(4H)‑ones as Antitubercular Agents

ACS infectious diseases, 2021-02, Vol.7 (2), p.479-492

2021

Volltextzugriff (PDF)

Ligand binding: evaluating the contribution of the water molecules network using the Fragment Molecular Orbital method

Journal of computer-aided molecular design, 2021-10, Vol.35 (10), p.1025-1036

2021

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Investigation of Trypanothione Reductase as a Drug Target in Trypanosoma brucei

ChemMedChem, 2009-12, Vol.4 (12), p.2060-2069

2009

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Biochemical characterization of protease activity of Nsp3 from SARS-CoV-2 and its inhibition by nanobodies

Comparison of a High-Throughput High-Content Intracellular Leishmania donovani Assay with an Axenic Amastigote Assay

Targeting N-myristoylation for therapy of B-cell lymphomas

Target validation: linking target and chemical properties to desired product profile

N -myristoyltransferase inhibitors as new leads to treat sleeping sickness

Design of the Global Health chemical diversity library v2 for screening against infectious diseases

Identification of N-(4-Piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a Novel Cyclin Dependent Kinase Inhibitor Using Fragment-Based X-Ray Crystallography and Structure Based Drug Design

Fragment library design, synthesis and expansion: nurturing a synthesis and training platform

Inhibiting Mycobacterium tuberculosis CoaBC by targeting an allosteric site

Lead Optimization of a Pyrazole Sulfonamide Series of Trypanosoma brucei N‑Myristoyltransferase Inhibitors: Identification and Evaluation of CNS Penetrant Compounds as Potential Treatments for Stage 2 Human African Trypanosomiasis

Exploring the Trypanosoma brucei Hsp83 potential as a target for structure guided drug design

Identification of Inhibitors of Protein Kinase B Using Fragment-Based Lead Discovery

One Scaffold, Three Binding Modes: Novel and Selective Pteridine Reductase 1 Inhibitors Derived from Fragment Hits Discovered by Virtual Screening

Screening a protein kinase inhibitor library against Plasmodium falciparum

De Novo Design of Protein Kinase Inhibitors by in Silico Identification of Hinge Region-Binding Fragments

Generation of Polar Semi‐Saturated Bicyclic Pyrazoles for Fragment‐Based Drug‐Discovery Campaigns

Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need

Diversity-oriented synthesis of bicyclic fragments containing privileged azines

PE/PPE proteins mediate nutrient transport across the outer membrane of Mycobacterium tuberculosis

A target repurposing approach identifies N-myristoyltransferase as a new candidate drug target in filarial nematodes

Spirocycle MmpL3 Inhibitors with Improved hERG and Cytotoxicity Profiles as Inhibitors of Mycobacterium tuberculosis Growth

Structure–Activity Relationships of Pyrazolo[1,5‑a]pyrimidin-7(4H)‑ones as Antitubercular Agents

Ligand binding: evaluating the contribution of the water molecules network using the Fragment Molecular Orbital method

Investigation of Trypanothione Reductase as a Drug Target in Trypanosoma brucei

Cyclin-dependent kinase 12 is a drug target for visceral leishmaniasis

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