Search Results - "WITTWER, Matthias"
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Fundamental aspects of DMPK optimization of targeted protein degraders
Published in Drug discovery today (01-06-2020)“…•Degraders are an emerging modality which fall into the ‘beyond rule of 5’ space.•Poor permeability and solubility are critical features limiting oral…”
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Transporters in Drug Development: 2018 ITC Recommendations for Transporters of Emerging Clinical Importance
Published in Clinical pharmacology and therapeutics (01-11-2018)“…This white paper provides updated International Transporter Consortium (ITC) recommendations on transporters that are important in drug development following…”
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Considerations and recommendations for assessment of plasma protein binding and drug-drug interactions for siRNA therapeutics
Published in Nucleic acids research (24-06-2022)“…At the time of writing, although siRNA therapeutics are approved for human use, no official regulatory guidance specific to this modality is available. In the…”
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Renal Transporters in Drug Development
Published in Annual review of pharmacology and toxicology (01-01-2013)“…The kidney plays a vital role in the body's defense against potentially toxic xenobiotics and metabolic waste products through elimination pathways. In…”
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Transporters in Drug Development: International Transporter Consortium Update on Emerging Transporters of Clinical Importance
Published in Clinical pharmacology and therapeutics (01-09-2022)“…During its fourth transporter workshop in 2021, the International Transporter Consortium (ITC) provided updates on emerging clinically relevant transporters…”
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Discovery of Potent, Selective Multidrug and Toxin Extrusion Transporter 1 (MATE1, SLC47A1) Inhibitors Through Prescription Drug Profiling and Computational Modeling
Published in Journal of medicinal chemistry (14-02-2013)“…The human multidrug and toxin extrusion (MATE) transporter 1 contributes to the tissue distribution and excretion of many drugs. Inhibition of MATE1 may result…”
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The genome of Naegleria lovaniensis, the basis for a comparative approach to unravel pathogenicity factors of the human pathogenic amoeba N. fowleri
Published in BMC genomics (05-09-2018)“…Members of the genus Naegleria are free-living eukaryotes with the capability to transform from the amoeboid form into resting cysts or moving flagellates in…”
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Targeted protein degraders: a call for collective action to advance safety assessment
Published in Nature reviews. Drug discovery (01-06-2022)“…Targeted protein degraders (TPDs) are emerging classes of therapeutics that have the potential to address difficult drug targets in new ways. In 2021, experts…”
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Involvement of CB1 and CB2 receptors in neuroprotective effects of cannabinoids in experimental TDP-43 related frontotemporal dementia using male mice
Published in Biomedicine & pharmacotherapy (01-05-2024)“…The elevation of endocannabinoid levels through inhibiting their degradation afforded neuroprotection in CaMKIIα-TDP-43 mice, a conditional transgenic model of…”
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Identification of ( R )-[ 18 F]YH134 for Monoacylglycerol Lipase Neuroimaging and Exploration of Its Use for Central Nervous System and Peripheral Drug Development
Published in Journal of Nuclear Medicine (01-02-2024)“…This study aimed to evaluate ( )-[ F]YH134 as a novel PET tracer for imaging monoacylglycerol lipase (MAGL). Considering the ubiquitous expression of MAGL…”
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Identification of cryptic Anopheles mosquito species by molecular protein profiling
Published in PloS one (28-02-2013)“…Vector control is the mainstay of malaria control programmes. Successful vector control profoundly relies on accurate information on the target mosquito…”
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The Effect of Famotidine, a MATE1-Selective Inhibitor, on the Pharmacokinetics and Pharmacodynamics of Metformin
Published in Clinical pharmacokinetics (01-06-2016)“…Introduction Pharmacokinetic outcomes of transporter-mediated drug–drug interactions (TMDDIs) are increasingly being evaluated clinically. The goal of our…”
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ITC Commentary on Metformin Clinical Drug–Drug Interaction Study Design That Enables an Efficacy‐ and Safety‐Based Dose Adjustment Decision
Published in Clinical pharmacology and therapeutics (01-11-2018)“…Metformin drug-drug interaction (DDI) studies are conducted during development of drugs that inhibit organic cation transporters and/or multidrug and toxin…”
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Discovery of a NAPE-PLD inhibitor that modulates emotional behavior in mice
Published in Nature chemical biology (01-06-2020)“…N -acylethanolamines (NAEs), which include the endocannabinoid anandamide, represent an important family of signaling lipids in the brain. The lack of chemical…”
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A potent and selective inhibitor for the modulation of MAGL activity in the neurovasculature
Published in PloS one (09-09-2022)“…Chronic inflammation and blood–brain barrier dysfunction are key pathological hallmarks of neurological disorders such as multiple sclerosis, Alzheimer’s…”
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Involvement of CB 1 and CB 2 receptors in neuroprotective effects of cannabinoids in experimental TDP-43 related frontotemporal dementia using male mice
Published in Biomedicine & pharmacotherapy (01-05-2024)“…The elevation of endocannabinoid levels through inhibiting their degradation afforded neuroprotection in CaMKIIα-TDP-43 mice, a conditional transgenic model of…”
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Associations of the intestinal microbiome with the complement system in neovascular age-related macular degeneration
Published in Npj genomic medicine (01-09-2020)“…Age-related macular degeneration (AMD) is a leading cause of severe vision loss in the aged population. The etiology of AMD is multifactorial including…”
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Multi-parameter optimization: Development of a morpholin-3-one derivative with an improved kinetic profile for imaging monoacylglycerol lipase in the brain
Published in European journal of medicinal chemistry (05-12-2022)“…Monoacylglycerol lipase (MAGL) is a gatekeeper in regulating endocannabinoid signaling and has gained substantial attention as a therapeutic target for…”
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Discovery, synthesis and evaluation of novel reversible monoacylglycerol lipase radioligands bearing a morpholine-3-one scaffold
Published in Nuclear medicine and biology (01-05-2022)“…Monoacylglycerol lipase (MAGL) is a serine hydrolase that plays an important role in the endocannabinoid degradation in the brain. It has recently emerged as a…”
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Functional characterization of Francisella tularensis subspecies holarctica genotypes during tick cell and macrophage infections using a proteogenomic approach
Published in Frontiers in cellular and infection microbiology (04-03-2024)“…Tularemia is a vector-borne disease caused by the Gram-negative bacterium . Known hosts and vectors in Europe are hare and ticks. is transmitted from ticks and…”
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