Optimized arylomycins are a new class of Gram-negative antibiotics

…, D Yan, Y Chen, Y Chen, JJ Crawford, MR Durk… - Nature, 2018 - nature.com
Multidrug-resistant bacteria are spreading at alarming rates, and despite extensive efforts
no new class of antibiotic with activity against Gram-negative bacteria has been approved in …

1α, 25-Dihydroxyvitamin D3 reduces cerebral amyloid-β accumulation and improves cognition in mouse models of Alzheimer's disease

MR Durk, K Han, ECY Chow, R Ahrens… - Journal of …, 2014 - Soc Neuroscience
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 amyloid precursor protein-…

Design and measurement of drug tissue concentration asymmetry and tissue exposure-effect (Tissue PK-PD) evaluation

…, J Shen, J Lade, K Grove, MR Durk… - Journal of Medicinal …, 2022 - ACS Publications
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 elicit pharmacologic effects. …

Physiologically-based pharmacokinetic modeling for absorption, transport, metabolism and excretion

KS Pang, MR Durk - Journal of pharmacokinetics and pharmacodynamics, 2010 - Springer
The seminal paper on the liver physiologically-based pharmacokinetic (PBPK) model by
Rowland et al. (J Pharmacokinet Biopharm 1:123–136, 1973 ) that described the influence of …

Vitamin D receptor activation down-regulates the small heterodimer partner and increases CYP7A1 to lower cholesterol

…, L Magomedova, HP Quach, R Patel, MR Durk… - Gastroenterology, 2014 - Elsevier
Background & Aims Little is known about the effects of the vitamin D receptor (VDR) on hepatic
activity of human cholesterol 7α-hydroxylase (CYP7A1) and cholesterol metabolism. We …

1α,25‐Dihydroxyvitamin D3‐liganded vitamin D receptor increases expression and transport activity of P‐glycoprotein in isolated rat brain capillaries and human and …

MR Durk, GNY Chan, CR Campos… - Journal of …, 2012 - Wiley Online Library
… ‐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 - Durk - …

1α, 25-Dihydroxyvitamin D3 up-regulates P-glycoprotein via the vitamin D receptor and not farnesoid X receptor in both fxr (−/−) and fxr (+/+) mice and increased renal …

ECY Chow, MR Durk, CL Cummins, KS Pang - Journal of Pharmacology and …, 2011 - ASPET
Secondary farnesoid X receptor (FXR) effects, in addition to vitamin D receptor (VDR) effects,
were observed in the rat liver after treatment with 1α,25-dihydroxyvitamin D 3 [1,25(OH) 2 D …

Complex DDI by fenebrutinib and the use of transporter endogenous biomarkers to elucidate the mechanism of DDI

…, L Salphati, JR Kenny, MR Durk… - Clinical …, 2020 - Wiley Online Library
Mechanistic understanding of complex clinical drug–drug interactions ( DDI s) with potential
involvement of multiple elimination pathways has been challenging, especially given the …

[HTML][HTML] Inhaled JAK inhibitor GDC-0214 reduces exhaled nitric oxide in patients with mild asthma: a randomized, controlled, proof-of-activity trial

…, M Williams, AG McGregor, A Eliahu, MR Durk… - Journal of Allergy and …, 2021 - Elsevier
… In preclinical species, GDC-0214 is retained in the lung and is rapidly cleared in the
circulation (MR Durk, unpublished data, 2015-2016). In rodent ovalbumin challenge models of …

Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3H)-quinazolinone Aryl Urea pan-RAF Kinase Inhibitor

…, D Dela Cruz, AG DiPasquale, MR Durk… - Journal of Medicinal …, 2021 - ACS Publications
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 hinge-binding motif. By …