Search Results - "EICKHOFF, Jan"
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Modulators of 14-3‑3 Protein–Protein Interactions
Published in Journal of medicinal chemistry (10-05-2018)“…Direct interactions between proteins are essential for the regulation of their functions in biological pathways. Targeting the complex network of…”
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A cell-based chemical-genetic screen for amino acid stress response inhibitors reveals torins reverse stress kinase GCN2 signaling
Published in The Journal of biological chemistry (01-12-2022)“…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…”
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3
A novel CDK7 inhibitor of the Pyrazolotriazine class exerts broad-spectrum antiviral activity at nanomolar concentrations
Published in Antimicrobial agents and chemotherapy (01-04-2015)“…Protein kinases represent central and multifunctional regulators of a balanced virus-host interaction. Cyclin-dependent protein kinase 7 (CDK7) plays crucial…”
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Identification of Atuveciclib (BAY 1143572), the First Highly Selective, Clinical PTEFb/CDK9 Inhibitor for the Treatment of Cancer
Published in ChemMedChem (08-11-2017)“…Selective inhibition of exclusively transcription‐regulating PTEFb/CDK9 is a promising new approach in cancer therapy. Starting from lead compound BAY‐958,…”
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Stabilization of protein-protein interactions in drug discovery
Published in Expert opinion on drug discovery (02-09-2017)“…PPIs are involved in every disease and specific modulation of these PPIs with small molecules would significantly improve our prospects of developing…”
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Cytomegalovirus cyclin-dependent kinase ortholog vCDK/pUL97 undergoes regulatory interaction with human cyclin H and CDK7 to codetermine viral replication efficiency
Published in Virus research (02-10-2023)“…• Consistent upregulation of cyclin H in various human cell types by strains of HCMV. • Reduced or increased vCDK/pUL97 kinase activity as a consequence of…”
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Cyclin-Dependent Kinase 7 Controls mRNA Synthesis by Affecting Stability of Preinitiation Complexes, Leading to Altered Gene Expression, Cell Cycle Progression, and Survival of Tumor Cells
Published in Molecular and cellular biology (01-10-2014)“…Cyclin-dependent kinase 7 (CDK7) activates cell cycle CDKs and is a member of the general transcription factor TFIIH. Although there is substantial evidence…”
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Combinatorial Drug Treatments Reveal Promising Anticytomegaloviral Profiles for Clinically Relevant Pharmaceutical Kinase Inhibitors (PKIs)
Published in International journal of molecular sciences (08-01-2021)“…Human cytomegalovirus (HCMV) is a human pathogenic herpesvirus associated with a variety of clinical symptoms. Current antiviral therapy is not always…”
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Combined Treatment with Host-Directed and Anticytomegaloviral Kinase Inhibitors: Mechanisms, Synergisms and Drug Resistance Barriers
Published in Pharmaceutics (27-11-2023)“…Despite the availability of currently approved antiviral drugs, infections with human cytomegalovirus (HCMV) still cause clinically challenging, sometimes…”
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Development of a live cell assay for real-time monitoring the interactions between the Hippo pathway components 14-3-3 and TAZ
Published in SLAS discovery (01-12-2024)“…The Hippo pathway plays an important role in organ size control and tissue homeostasis. Dysregulation is involved in many pathologies, including cancer, which…”
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Dual Inhibition of GSK3β and CDK5 Protects the Cytoskeleton of Neurons from Neuroinflammatory-Mediated Degeneration In Vitro and In Vivo
Published in Stem cell reports (05-03-2019)“…Neuroinflammation is a hallmark of neurological disorders and is accompanied by the production of neurotoxic agents such as nitric oxide. We used stem…”
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An Antiherpesviral Host-Directed Strategy Based on CDK7 Covalently Binding Drugs: Target-Selective, Picomolar-Dose, Cross-Virus Reactivity
Published in Pharmaceutics (23-01-2024)“…The repertoire of currently available antiviral drugs spans therapeutic applications against a number of important human pathogens distributed worldwide. These…”
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Assessment of Covalently Binding Warhead Compounds in the Validation of the Cytomegalovirus Nuclear Egress Complex as an Antiviral Target
Published in Cells (Basel, Switzerland) (01-04-2023)“…Herpesviral nuclear egress is a regulated process of viral capsid nucleocytoplasmic release. Due to the large capsid size, a regular transport via the nuclear…”
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Characterization of the Antibacterial Activity of Quinone-Based Compounds Originating from the Alnumycin Biosynthetic Gene Cluster of a Streptomyces Isolate
Published in Antibiotics (Basel) (28-06-2023)“…Bacteria of the genus produce various specialized metabolites. Single biosynthetic gene clusters (BGCs) can give rise to different products that can vary in…”
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Recruitment of cyclin-dependent kinase 9 to nuclear compartments during cytomegalovirus late replication: importance of an interaction between viral pUL69 and cyclin T1
Published in Journal of general virology (01-07-2011)“…Cyclin-dependent protein kinases (CDKs) are important regulators of cellular processes and are functionally integrated into the replication of human…”
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ComplexEye: a multi-lens array microscope for high-throughput embedded immune cell migration analysis
Published in Nature communications (11-12-2023)“…Autonomous migration is essential for the function of immune cells such as neutrophils and plays an important role in numerous diseases. The ability to…”
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Cyclin-dependent Kinases Phosphorylate the Cytomegalovirus RNA Export Protein pUL69 and Modulate Its Nuclear Localization and Activity
Published in The Journal of biological chemistry (27-03-2009)“…Replication of human cytomegalovirus (HCMV) is subject to regulation by cellular protein kinases. Recently, we and others reported that inhibition of…”
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Proteomic characterization of the angiogenesis inhibitor SU6668 reveals multiple impacts on cellular kinase signaling
Published in Cancer research (Chicago, Ill.) (01-08-2005)“…Knowledge about molecular drug action is critical for the development of protein kinase inhibitors for cancer therapy. Here, we establish a chemical proteomic…”
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The Role of RIP2 in p38 MAPK Activation in the Stressed Heart
Published in The Journal of biological chemistry (02-05-2008)“…The activation of p38 MAPK by dual phosphorylation aggravates myocardial ischemic injury and depresses cardiac contractile function. SB203580, an…”
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A bead-based GPCR phosphorylation immunoassay for high-throughput ligand profiling and GRK inhibitor screening
Published in Communications biology (09-11-2022)“…Analysis of agonist-driven phosphorylation of G protein-coupled receptors (GPCRs) can provide valuable insights into the receptor activation state and ligand…”
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