Jan Eickhoff
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View article: Evaluating Triazole-Substituted Pyrrolopyrimidines as CSF1R Inhibitors
Evaluating Triazole-Substituted Pyrrolopyrimidines as CSF1R Inhibitors Open
6-Aryl-7H-pyrrolo[2,3-d]pyrimidin-4-amines have promising properties as colony-stimulating factor 1 receptor (CSF1R) inhibitors. Inspired by these antagonists, two series of 1,2,3-triazole analogues (28 compounds) were synthesized and eval…
View article: Design and Synthesis of Pyridine-Based Pyrrolo[2,3-d]pyrimidine Analogs as CSF1R Inhibitors: Molecular Hybridization and Scaffold Hopping Approach
Design and Synthesis of Pyridine-Based Pyrrolo[2,3-d]pyrimidine Analogs as CSF1R Inhibitors: Molecular Hybridization and Scaffold Hopping Approach Open
Background/Objectives: Colony stimulating factor 1 receptor kinase (CSF1R) is a well-validated molecular target in drug discovery for various reasons. Based on the structure of an early lead molecule identified in our lab and the marketed …
View article: Development of a live cell assay for real-time monitoring the interactions between the Hippo pathway components 14-3-3 and TAZ
Development of a live cell assay for real-time monitoring the interactions between the Hippo pathway components 14-3-3 and TAZ Open
The Hippo pathway plays an important role in organ size control and tissue homeostasis. Dysregulation is involved in many pathologies, including cancer, which has attracted interest in targeting the Hippo pathway. Since the upstream compon…
View article: An Antiherpesviral Host-Directed Strategy Based on CDK7 Covalently Binding Drugs: Target-Selective, Picomolar-Dose, Cross-Virus Reactivity
An Antiherpesviral Host-Directed Strategy Based on CDK7 Covalently Binding Drugs: Target-Selective, Picomolar-Dose, Cross-Virus Reactivity Open
The repertoire of currently available antiviral drugs spans therapeutic applications against a number of important human pathogens distributed worldwide. These include cases of the pandemic severe acute respiratory coronavirus type 2 (SARS…
View article: Pyrrolopyrimidine based CSF1R inhibitors: Attempted departure from Flatland
Pyrrolopyrimidine based CSF1R inhibitors: Attempted departure from Flatland Open
The colony-stimulating factor 1 receptor (CSF1R) is an attractive target for inflammation disorders and cancers. Based on a series of pyrrolo[2,3-d]pyrimidine containing two carbo-aromatic rings, we have searched for new CSF1R inhibitors h…
View article: ComplexEye: a multi-lens array microscope for high-throughput embedded immune cell migration analysis
ComplexEye: a multi-lens array microscope for high-throughput embedded immune cell migration analysis Open
Autonomous migration is essential for the function of immune cells such as neutrophils and plays an important role in numerous diseases. The ability to routinely measure or target it would offer a wealth of clinical applications. Video mic…
View article: Combined Treatment with Host-Directed and Anticytomegaloviral Kinase Inhibitors: Mechanisms, Synergisms and Drug Resistance Barriers
Combined Treatment with Host-Directed and Anticytomegaloviral Kinase Inhibitors: Mechanisms, Synergisms and Drug Resistance Barriers Open
Despite the availability of currently approved antiviral drugs, infections with human cytomegalovirus (HCMV) still cause clinically challenging, sometimes life-threatening situations. There is an urgent need for enhanced anti-HCMV drugs th…
View article: ComplexEye - a multi lens array microscope for High-Throughput embedded immune cell migration analysis
ComplexEye - a multi lens array microscope for High-Throughput embedded immune cell migration analysis Open
This dataset contains raw high-resolution movies of migrating neutrophils, which were recorded using the ComplexEye, an array microscope with 16 independent aberration-corrected glass lenses spaced at the pitch of a 96-well plate. Please s…
View article: ComplexEye - a multi lens array microscope for High-Throughput embedded immune cell migration analysis
ComplexEye - a multi lens array microscope for High-Throughput embedded immune cell migration analysis Open
This dataset contains raw high-resolution movies of migrating neutrophils, which were recorded using the ComplexEye, an array microscope with 16 independent aberration-corrected glass lenses spaced at the pitch of a 96-well plate. Please s…
View article: Characterization of the Antibacterial Activity of Quinone-Based Compounds Originating from the Alnumycin Biosynthetic Gene Cluster of a Streptomyces Isolate
Characterization of the Antibacterial Activity of Quinone-Based Compounds Originating from the Alnumycin Biosynthetic Gene Cluster of a Streptomyces Isolate Open
Bacteria of the genus Streptomyces produce various specialized metabolites. Single biosynthetic gene clusters (BGCs) can give rise to different products that can vary in terms of their biological activities. For example, for alnumycin and …
View article: ComplexEye - a multi lens array microscope for High-Throughput embedded immune cell migration analysis
ComplexEye - a multi lens array microscope for High-Throughput embedded immune cell migration analysis Open
This dataset contains raw high-resolution movies of migrating neutrophils, which were recorded using an array microscope with 16 independent aberration-corrected glass lenses spaced at the pitch of a 96-well plate.
View article: Synthesis and Development of Highly Selective Pyrrolo[2,3-<i>d</i>]pyrimidine CSF1R Inhibitors Targeting the Autoinhibited Form
Synthesis and Development of Highly Selective Pyrrolo[2,3-<i>d</i>]pyrimidine CSF1R Inhibitors Targeting the Autoinhibited Form Open
Colony-stimulating factor-1 receptor (CSF1R) is a receptor tyrosine kinase that controls the differentiation and maintenance of most tissue-resident macrophages, and the inhibition of CSF1R has been suggested as a possible therapy for a ra…
View article: Assessment of Covalently Binding Warhead Compounds in the Validation of the Cytomegalovirus Nuclear Egress Complex as an Antiviral Target
Assessment of Covalently Binding Warhead Compounds in the Validation of the Cytomegalovirus Nuclear Egress Complex as an Antiviral Target Open
Herpesviral nuclear egress is a regulated process of viral capsid nucleocytoplasmic release. Due to the large capsid size, a regular transport via the nuclear pores is unfeasible, so that a multistage-regulated export pathway through the n…
View article: Assessment of covalently binding warhead compounds in the validation of the cytomegalovirus nuclear egress complex as an antiviral target
Assessment of covalently binding warhead compounds in the validation of the cytomegalovirus nuclear egress complex as an antiviral target Open
Supplementary to the publication: "Assessment of covalently binding warhead compounds in the validation of the cytomegalovirus nuclear egress complex as an antiviral target" (2023), published in Cells Raw images of the Figures 4, 10, 11 an…
View article: Assessment of covalently binding warhead compounds in the validation of the cytomegalovirus nuclear egress complex as an antiviral target
Assessment of covalently binding warhead compounds in the validation of the cytomegalovirus nuclear egress complex as an antiviral target Open
Supplementary to the publication: "Assessment of covalently binding warhead compounds in the validation of the cytomegalovirus nuclear egress complex as an antiviral target" (2023), published in Cells Raw images of the Figures 4, 10, 11 an…
View article: Supplementary Figure 1 from Proteomic Characterization of the Angiogenesis Inhibitor SU6668 Reveals Multiple Impacts on Cellular Kinase Signaling
Supplementary Figure 1 from Proteomic Characterization of the Angiogenesis Inhibitor SU6668 Reveals Multiple Impacts on Cellular Kinase Signaling Open
Supplementary Figure 1 from Proteomic Characterization of the Angiogenesis Inhibitor SU6668 Reveals Multiple Impacts on Cellular Kinase Signaling
View article: Supplementary Figure 1 from Proteomic Characterization of the Angiogenesis Inhibitor SU6668 Reveals Multiple Impacts on Cellular Kinase Signaling
Supplementary Figure 1 from Proteomic Characterization of the Angiogenesis Inhibitor SU6668 Reveals Multiple Impacts on Cellular Kinase Signaling Open
Supplementary Figure 1 from Proteomic Characterization of the Angiogenesis Inhibitor SU6668 Reveals Multiple Impacts on Cellular Kinase Signaling
View article: Data from Proteomic Characterization of the Angiogenesis Inhibitor SU6668 Reveals Multiple Impacts on Cellular Kinase Signaling
Data from Proteomic Characterization of the Angiogenesis Inhibitor SU6668 Reveals Multiple Impacts on Cellular Kinase Signaling Open
Knowledge about molecular drug action is critical for the development of protein kinase inhibitors for cancer therapy. Here, we establish a chemical proteomic approach to profile the anticancer drug SU6668, which was originally designed as…
View article: Data from Proteomic Characterization of the Angiogenesis Inhibitor SU6668 Reveals Multiple Impacts on Cellular Kinase Signaling
Data from Proteomic Characterization of the Angiogenesis Inhibitor SU6668 Reveals Multiple Impacts on Cellular Kinase Signaling Open
Knowledge about molecular drug action is critical for the development of protein kinase inhibitors for cancer therapy. Here, we establish a chemical proteomic approach to profile the anticancer drug SU6668, which was originally designed as…
View article: Supplementary Methods from Proteomic Characterization of the Angiogenesis Inhibitor SU6668 Reveals Multiple Impacts on Cellular Kinase Signaling
Supplementary Methods from Proteomic Characterization of the Angiogenesis Inhibitor SU6668 Reveals Multiple Impacts on Cellular Kinase Signaling Open
Supplementary Methods from Proteomic Characterization of the Angiogenesis Inhibitor SU6668 Reveals Multiple Impacts on Cellular Kinase Signaling
View article: Supplementary Methods from Proteomic Characterization of the Angiogenesis Inhibitor SU6668 Reveals Multiple Impacts on Cellular Kinase Signaling
Supplementary Methods from Proteomic Characterization of the Angiogenesis Inhibitor SU6668 Reveals Multiple Impacts on Cellular Kinase Signaling Open
Supplementary Methods from Proteomic Characterization of the Angiogenesis Inhibitor SU6668 Reveals Multiple Impacts on Cellular Kinase Signaling
View article: Negishi Cross‐Coupling in the Preparation of Benzyl Substituted Pyrrolo[2,3‐<i>d</i>]pyrimidine Based CSF1R Inhibitors
Negishi Cross‐Coupling in the Preparation of Benzyl Substituted Pyrrolo[2,3‐<i>d</i>]pyrimidine Based CSF1R Inhibitors Open
The colony‐stimulating factor 1 receptor (CSF1R) is a protein kinase emerging as an attractive target with clinical relevance in cancer, CNS and inflammatory diseases. Molecular docking experiments followed by synthesis and structure–activ…
View article: Assessment of covalently binding warhead compounds in the validation of the cytomegalovirus nuclear egress complex as an antiviral target
Assessment of covalently binding warhead compounds in the validation of the cytomegalovirus nuclear egress complex as an antiviral target Open
Supplementary to the publication: "Assessment of covalently binding warhead compounds in the validation of the cytomegalovirus nuclear egress complex as an antiviral target" (2023), published in Cells Raw images of the Figures 2, 8 and 11
View article: Assessment of covalently binding warhead compounds in the validation of the cytomegalovirus nuclear egress complex as an antiviral target
Assessment of covalently binding warhead compounds in the validation of the cytomegalovirus nuclear egress complex as an antiviral target Open
Supplementary to the publication: "Assessment of covalently binding warhead compounds in the validation of the cytomegalovirus nuclear egress complex as an antiviral target" (2023), published in Cells Raw images of the Figures 2, 7 and 10
View article: A cell-based chemical-genetic screen for amino acid stress response inhibitors reveals torins reverse stress kinase GCN2 signaling
A cell-based chemical-genetic screen for amino acid stress response inhibitors reveals torins reverse stress kinase GCN2 signaling Open
mTORC1 and GCN2 are serine/threonine kinases that control how cells adapt to amino acid availability. mTORC1 responds to amino acids to promote translation and cell growth while GCN2 senses limiting amino acids to hinder translation via eI…
View article: Combinatorial Drug Treatments Reveal Promising Anticytomegaloviral Profiles for Clinically Relevant Pharmaceutical Kinase Inhibitors (PKIs)
Combinatorial Drug Treatments Reveal Promising Anticytomegaloviral Profiles for Clinically Relevant Pharmaceutical Kinase Inhibitors (PKIs) Open
Human cytomegalovirus (HCMV) is a human pathogenic herpesvirus associated with a variety of clinical symptoms. Current antiviral therapy is not always effective, so that improved drug classes and drug-targeting strategies are needed. Parti…
View article: Kinase Chemodiversity from the Arctic: The Breitfussins
Kinase Chemodiversity from the Arctic: The Breitfussins Open
In this work, we demonstrate that the indole-oxazole-pyrrole framework of the breitfussin family of natural products is a promising scaffold for kinase inhibition. Six new halogenated natural products, breitfussin C-H (3 - 8) were isolated…