Search Results - "Durk, Matthew"
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Optimized arylomycins are a new class of Gram-negative antibiotics
Published in Nature (London) (01-09-2018)“…Multidrug-resistant bacteria are spreading at alarming rates, and despite extensive efforts no new class of antibiotic with activity against Gram-negative…”
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2
Complex DDI by Fenebrutinib and the Use of Transporter Endogenous Biomarkers to Elucidate the Mechanism of DDI
Published in Clinical pharmacology and therapeutics (01-01-2020)“…Mechanistic understanding of complex clinical drug–drug interactions (DDIs) with potential involvement of multiple elimination pathways has been challenging,…”
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3
1α,25-Dihydroxyvitamin D3 reduces cerebral amyloid-β accumulation and improves cognition in mouse models of Alzheimer's disease
Published in The Journal of neuroscience (21-05-2014)“…We demonstrate a role of the vitamin D receptor (VDR) in reducing cerebral soluble and insoluble amyloid-β (Aβ) peptides. Short-term treatment of two human…”
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4
Design and Measurement of Drug Tissue Concentration Asymmetry and Tissue Exposure-Effect (Tissue PK-PD) Evaluation
Published in Journal of medicinal chemistry (14-07-2022)“…The “free drug hypothesis” assumes that, in the absence of transporters, the steady state free plasma concentrations equal to that at the site of action that…”
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5
Elucidating a Potential Mechanism of Permeability Enhancer Sodium N-[8-(2-hydroxybenzoyl) amino] Caprylate in Rats: Evidence of Lymphatic Absorption of Cyanocobalamin using the Mesenteric Lymph Duct Cannulated Rat
Published in Journal of pharmaceutical sciences (01-12-2022)“…Oral administration is the most popular and convenient route for drug delivery, yet the success of oral drug delivery is dependent on the ADME properties of…”
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6
Inhaled JAK inhibitor GDC-0214 reduces exhaled nitric oxide in patients with mild asthma: A randomized, controlled, proof-of-activity trial
Published in Journal of allergy and clinical immunology (01-09-2021)“…The Janus kinase (JAK) pathway mediates the activity of many asthma-relevant cytokines, including IL-4 and IL-13. GDC-0214 is a potent, inhaled, small-molecule…”
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7
Use of Subcutaneous and Intraperitoneal Administration Methods to Facilitate Cassette Dosing in Microdialysis Studies in Rats
Published in Drug metabolism and disposition (01-07-2018)“…Microdialysis is a powerful technique allowing for real-time measurement of unbound drug concentrations in brain interstitial fluid (ISF) in conscious animals…”
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Design and Evaluation of Highly Selective Human Immunoproteasome Inhibitors Reveal a Compensatory Process That Preserves Immune Cell Viability
Published in Journal of medicinal chemistry (08-08-2019)“…The pan-proteasome inhibitor bortezomib demonstrated clinical efficacy in off-label trials of Systemic Lupus Erythematosus. One potential mechanism of this…”
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9
Vitamin D Receptor Activation Down-regulates the Small Heterodimer Partner and Increases CYP7A1 to Lower Cholesterol
Published in Gastroenterology (New York, N.Y. 1943) (01-04-2014)“…Background & Aims Little is known about the effects of the vitamin D receptor (VDR) on hepatic activity of human cholesterol 7α-hydroxylase (CYP7A1) and…”
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10
Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5‑Fluoro-4-(3H)‑quinazolinone Aryl Urea pan-RAF Kinase Inhibitor
Published in Journal of medicinal chemistry (08-04-2021)“…Optimization of a series of aryl urea RAF inhibitors led to the identification of type II pan-RAF inhibitor GNE-0749 (7), which features a fluoroquinazolinone…”
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11
Understanding the Effect of Hydroxypropyl‐β‐Cyclodextrin on Fenebrutinib Absorption in an Itraconazole–Fenebrutinib Drug–Drug Interaction Study
Published in Clinical pharmacology and therapeutics (01-12-2020)“…Cyclodextrins are widely used pharmaceutical excipients, particularly for insoluble compounds dosed orally, such as the oral solution of itraconazole, which is…”
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1α,25-Dihydroxyvitamin D3-liganded vitamin D receptor increases expression and transport activity of P-glycoprotein in isolated rat brain capillaries and human and rat brain microvessel endothelial cells
Published in Journal of neurochemistry (01-12-2012)“…Induction of the multidrug resistance protein 1 (MDR1)/P‐glycoprotein (P‐gp) by the vitamin D receptor (VDR) was investigated in isolated rat brain capillaries…”
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13
Effects of inhaled JAK inhibitor GDC-4379 on exhaled nitric oxide and peripheral biomarkers of inflammation
Published in Pulmonary pharmacology & therapeutics (01-08-2022)“…Janus Kinases (JAKs) mediate activity of many asthma-relevant cytokines. GDC-0214, an inhaled small molecule JAK1 inhibitor, has previously been shown to…”
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14
Physiologically‐Based Pharmacokinetic Model‐Informed Drug Development for Fenebrutinib: Understanding Complex Drug‐Drug Interactions
Published in CPT: pharmacometrics and systems pharmacology (01-06-2020)“…Fenebrutinib is a CYP3A substrate and time‐dependent inhibitor, as well as a BCRP and OATP1B transporter inhibitor in vitro. Physiologically‐based…”
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Phase I and scintigraphy studies to evaluate safety, tolerability, pharmacokinetics, and lung deposition of inhaled GDC‐0214 in healthy volunteers
Published in Clinical and translational science (01-05-2022)“…Several inflammatory cytokines that promote inflammation and pathogenesis in asthma signal through the Janus kinase 1 (JAK1) pathway. This phase I, randomized,…”
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Impact of age, hypercholesterolemia, and the vitamin D receptor on brain endogenous β‐amyloid peptide accumulation in mice
Published in Biopharmaceutics & drug disposition (01-09-2021)“…Age, hypercholesterolemia, and vitamin D deficiency are risk factors that increase the brain accumulation of pathogenic β‐amyloid peptides (40 and 42),…”
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17
Lipid Tales: Optimizing Arylomycin Membrane Anchors
Published in ACS medicinal chemistry letters (09-11-2023)“…Multidrug-resistant bacteria are spreading at alarming rates, and despite extensive efforts, no new antibiotic class with activity against Gram-negative…”
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18
Biorelevant Dissolution Models for a Weak Base To Facilitate Formulation Development and Overcome Reduced Bioavailability Caused by Hypochlordyria or Achlorhydria
Published in Molecular pharmaceutics (02-10-2017)“…In this study, two dissolution models were developed to achieve in vitro–in vivo relationship for immediate release formulations of Compound-A, a poorly…”
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Physiologically-based pharmacokinetic modeling for absorption, transport, metabolism and excretion
Published in Journal of pharmacokinetics and pharmacodynamics (01-12-2010)“…The seminal paper on the liver physiologically-based pharmacokinetic (PBPK) model by Rowland et al. (J Pharmacokinet Biopharm 1:123–136, 1973 ) that described…”
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Vitamin D Receptor Activation Induces P-Glycoprotein and Increases Brain Efflux of Quinidine:An Intracerebral Microdialysis Study in Conscious Rats
Published in Pharmaceutical research (01-03-2015)“…Purpose Since the vitamin D receptor (VDR) was found to up-regulate cerebral P-glycoprotein expression in vitro and in mice, we extend our findings to rats by…”
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