Search Results - "Irlbacher, Horst"
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Novel Class of Potent and Cellularly Active Inhibitors Devalidates MTH1 as Broad-Spectrum Cancer Target
Published in ACS chemical biology (18-08-2017)“…MTH1 is a hydrolase responsible for sanitization of oxidized purine nucleoside triphosphates to prevent their incorporation into replicating DNA. Early tool…”
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Targeting the aryl hydrocarbon receptor (AhR) with BAY 2416964: a selective small molecule inhibitor for cancer immunotherapy
Published in Journal for immunotherapy of cancer (01-11-2023)“…BackgroundThe metabolism of tryptophan to kynurenines (KYN) by indoleamine-2,3-dioxygenase or tryptophan-2,3-dioxygenase is a key pathway of constitutive and…”
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Cnksr3 is a direct mineralocorticoid receptor target gene and plays a key role in the regulation of the epithelial sodium channel
Published in The FASEB journal (01-11-2009)“…Aldosterone is the principal hormonal regulator of sodium homeostasis in vertebrates. It exerts its actions through the mineralocorticoid receptor (MR) that…”
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Control of replication initiation and heterochromatin formation in Saccharomyces cerevisiae by a regulator of meiotic gene expression
Published in Genes & development (01-08-2005)“…Heterochromatinization at the silent mating-type loci HMR and HML in Saccharomyces cerevisiae is achieved by targeting the Sir complex to these regions via a…”
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Control of replication initiation by the Sum1/Rfm1/Hst1 histone deacetylase
Published in BMC molecular biology (06-11-2008)“…Replication initiation at origins of replication in the yeast genome takes place on chromatin as a template, raising the question how histone modifications,…”
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Discovery of BAY-985, a Highly Selective TBK1/IKKε Inhibitor
Published in Journal of medicinal chemistry (23-01-2020)“…The serine/threonine kinase TBK1 (TANK-binding kinase 1) and its homologue IKKε are noncanonical members of the inhibitor of the nuclear factor κB (IκB) kinase…”
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Discovery and In Vitro Characterization of BAY 2686013, an Allosteric Small Molecule Antagonist of the Human Pituitary Adenylate Cyclase-Activating Polypeptide Receptor
Published in Molecular pharmacology (01-09-2023)“…The human pituitary adenylate cyclase-activating polypeptide receptor (hPAC -R), a class B G-protein-coupled receptor (GPCR) identified almost 30 years ago,…”
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Discovery and Characterization of the Potent and Highly Selective 1,7-Naphthyridine-Based Inhibitors BAY-091 and BAY-297 of the Kinase PIP4K2A
Published in Journal of medicinal chemistry (11-11-2021)“…PIP4K2A is an insufficiently studied type II lipid kinase that catalyzes the conversion of phosphatidylinositol-5-phosphate (PI5P) into phosphatidylinositol…”
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Discovery and optimization of pyridyl-cycloalkyl-carboxylic acids as inhibitors of microsomal prostaglandin E synthase-1 for the treatment of endometriosis
Published in Bioorganic & medicinal chemistry letters (15-09-2019)“…[Display omitted] Here we report on novel and potent pyridyl-cycloalkyl-carboxylic acid inhibitors of microsomal prostaglandin E synthase-1 (PTGES). PTGES…”
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Abstract 4454: Identification of BAY-218, a potent and selective small-molecule AhR inhibitor, as a new modality to counteract tumor immunosuppression
Published in Cancer research (Chicago, Ill.) (01-07-2019)“…Abstract Re-constitution of anti-tumor T-cell responses by clinically-approved immune checkpoint inhibitors (ICIs) targeting CTLA4 or PD-1/PD-L1 represents a…”
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Abstract 1288: Blocking tumor-associated immune suppression with BAY-218, a novel, selective aryl hydrocarbon receptor (AhR) inhibitor
Published in Cancer research (Chicago, Ill.) (01-07-2019)“…Abstract Tumor cells co-opt multiple pathways in order to evade attack by infiltrating immune cells. One such mechanism is the upregulation of…”
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Abstract 4460: Targeting the redox-protective protein MTH1 for cancer therapy: A novel way to exploit the unique redox status of cancer cells
Published in Cancer research (Chicago, Ill.) (01-08-2015)“…Abstract Cancer cells are characterized by an increase in the rate of reactive oxygen species (ROS) production and an altered redox environment compared to…”
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Abstract 689: Identification and optimization of novel chemical matter via a structure-based approach resulting in a probe for MTH1
Published in Cancer research (Chicago, Ill.) (01-07-2018)“…Abstract Cancer cells can form reactive oxygen species (ROS) due to altered redox regulation that affect desoxynucleosides triphosphates (dNTP) in particular…”
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Differential expression of antenna and core genes in Prochlorococcus PCC 9511 (Oxyphotobacteria) grown under a modulated light-dark cycle
Published in Environmental microbiology (01-03-2001)“…The continuous changes in incident solar light occurring during the day oblige oxyphototrophs, such as the marine prokaryote Prochlorococcus, to modulate the…”
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