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Showing 1-30 of 226 results for "V4629" within Papers
Yasuo Uchida et al.
The Journal of pharmacology and experimental therapeutics, 350(3), 578-588 (2014-06-21)
The aim of this study was to investigate whether in vivo drug distribution in brain in monkeys can be reconstructed by integrating four factors: protein expression levels of P-glycoprotein (P-gp)/multidrug resistance protein 1 at the blood-brain barrier (BBB), in vitro
Michaël Lehoux et al.
Methods in molecular biology (Clifton, N.J.), 1249, 67-80 (2014-10-29)
Replication of the human papillomavirus (HPV) double-stranded DNA genome in the nucleus of infected cells relies on the viral proteins E1 and E2 in conjunction with the host DNA replication machinery. This process is tightly linked to the replication of
Lukas Peintner et al.
Autophagy, 17(9), 2384-2400 (2020-09-25)
Mutations in the PKD1 gene result in autosomal dominant polycystic kidney disease (ADPKD), the most common monogenetic cause of end-stage renal disease (ESRD) in humans. Previous reports suggested that PKD1, together with PKD2/polycystin-2, may function as a receptor-cation channel complex
Hasan Salman Siddiqi et al.
Journal of cardiovascular pharmacology, 64(2), 151-163 (2014-04-01)
This study was aimed to offer a possible pharmacological basis regarding the remedial utilization of Wrightia tinctoria in hypertension and dyslipidemia in certain South Asian traditional systems of medicine, using in vivo and in vitro assays. The aqueous methanolic extract
Sisi Feng et al.
Cell reports, 33(10), 108455-108455 (2020-12-10)
The ever-increasing therapeutic and pharmaceutical demand for liver cells calls for systems that enable mass production of hepatic cells. Here we describe a large-scale suspension system that uses human endoderm stem cells (hEnSCs) as precursors to generate functional and transplantable
Lisa Rösch et al.
Molecular oncology, 17(1), 37-58 (2022-10-02)
Chemotherapy resistance is a persistent clinical problem in relapsed high-risk neuroblastomas. We tested a panel of 15 drugs for sensitization of neuroblastoma cells to the conventional chemotherapeutic vincristine, identifying tariquidar, an inhibitor of the transmembrane pump P-glycoprotein (P-gp/ABCB1), and the
Sean Ekins et al.
Drug metabolism and disposition: the biological fate of chemicals, 38(12), 2302-2308 (2010-09-17)
Drug-induced liver injury (DILI) is one of the most important reasons for drug development failure at both preapproval and postapproval stages. There has been increased interest in developing predictive in vivo, in vitro, and in silico models to identify compounds
K Ikeda et al.
Die Pharmazie, 70(7), 471-476 (2015-09-17)
Human choriocarcinoma has been used as a model to study trophoblast transcellular drug transport in the placenta. Previous models had limitations regarding low molecular weight drug transport through the intracellular gap junction. The purpose of this study was to evaluate
Daniel J Greenwood et al.
Science (New York, N.Y.), 364(6447), 1279-1282 (2019-06-30)
Tuberculosis, caused by the intracellular pathogen Mycobacterium tuberculosis, remains the world's deadliest infectious disease. Sterilizing chemotherapy requires at least 6 months of multidrug therapy. Difficulty visualizing the subcellular localization of antibiotics in infected host cells means that it is unclear
Kayoko Ohura et al.
Journal of pharmaceutical sciences, 104(9), 3076-3083 (2015-05-09)
The aim of this study was to develop a suitable prodrug for fexofenadine (FXD), a model parent drug, that is resistant to intestinal esterase but converted to FXD by hepatic esterase. Carboxylesterases (CESs), human carboxylesterase 1 (hCE1) and human carboxylesterase
Gwenola Manic et al.
Cell death and differentiation, 28(7), 2060-2082 (2021-02-04)
Cancer stem cells (CSCs) are tumor subpopulations driving disease development, progression, relapse and therapy resistance, and their targeting ensures tumor eradication. CSCs display heterogeneous replication stress (RS), but the functionality/relevance of the RS response (RSR) centered on the ATR-CHK1 axis
David Cadagan et al.
Anticancer research, 33(10), 4381-4387 (2013-10-15)
Modulating agents are used to circumvent drug resistance in the clinical setting. However achievable serum concentrations are often lower than those which are optimal in vitro. Combination of modulating agents with non-overlapping toxicities may overcome this obstacle. We have investigated
Chunbo Zhang et al.
Epilepsia, 54(7), 1154-1160 (2013-04-05)
Antiepileptic drugs (AEDs) do not effectively treat 30-40% of patients with epilepsy. Export of AEDs by P-glycoprotein (Pgp, ABCB1, or MDR1), which is overexpressed in the blood-brain barrier in drug-resistant patients, may be a mechanism for resistance to AEDs. For
Puspangana Singh et al.
Cell reports, 39(3), 110694-110694 (2022-04-10)
Mutations in the spike protein generated a highly infectious and transmissible D614G variant, which is present in newly evolved fast-spreading variants. The D614G, Alpha, Beta, and Delta spike variants of SARS-CoV-2 appear to expedite membrane fusion process for entry, but
David Balayssac et al.
Chemotherapy, 54(5), 336-342 (2008-08-21)
Cancer patients can be exposed to drug interactions during treatment with toxic anticancer drugs. The peripheral nervous system is a target for neurotoxic anticancer drugs. P-glycoprotein is essential for the functional integrity of blood-tissue barriers, and P-glycoprotein inhibition due to
Balawant Kumar et al.
Cancers, 13(9) (2021-05-06)
Background: Despite recent advances in therapies, resistance to chemotherapy remains a critical problem in the clinical management of colorectal cancer (CRC). Cancer stem cells (CSCs) play a central role in therapy resistance. Thus, elimination of CSCs is crucial for effective
John F Wambaugh et al.
Toxicological sciences : an official journal of the Society of Toxicology, 172(2), 235-251 (2019-09-19)
High(er) throughput toxicokinetics (HTTK) encompasses in vitro measures of key determinants of chemical toxicokinetics and reverse dosimetry approaches for in vitro-in vivo extrapolation (IVIVE). With HTTK, the bioactivity identified by any in vitro assay can be converted to human equivalent
Fangfang Wang et al.
Cell death & disease, 13(2), 136-136 (2022-02-12)
Drug-resistance is a major problem preventing a cure in patients with multiple myeloma (MM). Previously, we demonstrated that activated-leukocyte-cell-adhesion-molecule (ALCAM) is a prognostic factor in MM and inhibits EGF/EGFR-initiated MM clonogenicity. In this study, we further showed that the ALCAM-EGF/EGFR
Nigel Greene et al.
Chemical research in toxicology, 23(7), 1215-1222 (2010-06-18)
Drug-induced liver injury is a major issue of concern and has led to the withdrawal of a significant number of marketed drugs. An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential
Muhammad Waqas Sadiq et al.
PloS one, 10(5), e0118638-e0118638 (2015-05-02)
It is essential to establish a useful validation method for newly generated humanized mouse models. The novel approach of combining our established species-specific protein quantification method combined with in vivo functional studies is evaluated to validate a humanized mouse model
Combination therapy to reduce conjunctival scarring after glaucoma surgery.
Marco A Zarbin
JAMA ophthalmology, 131(9), 1123-1123 (2013-07-13)
Qing Meng et al.
Acta pharmaceutica Sinica. B, 14(5), 2153-2176 (2024-05-27)
Aberrant changes in the gut microbiota are implicated in many diseases, including inflammatory bowel disease (IBD). Gut microbes produce diverse metabolites that can shape the immune system and impact the intestinal barrier integrity, indicating that microbe-mediated modulation may be a
Samantha S Yee et al.
Molecules (Basel, Switzerland), 26(13) (2021-07-20)
Ovarian cancer often has a poor clinical prognosis because of late detection, frequently after metastatic progression, as well as acquired resistance to taxane-based therapy. Herein, we evaluate a novel class of covalent microtubule stabilizers, the C-22,23-epoxytaccalonolides, for their efficacy against
Lei Zhang et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 33(11), 5006-5016 (2013-03-15)
In rodents, adrenergic signaling by norepinephrine (NE) in the hippocampus is required for the retrieval of intermediate-term memory. NE promotes retrieval via the stimulation of β1-adrenergic receptors, the production of cAMP, and the activation of both protein kinase A (PKA)
Chin-Chuan Hung et al.
PloS one, 8(3), e59419-e59419 (2013-03-26)
Methadone is a widely used substitution therapy for opioid addiction. Large inter-individual variability has been observed in methadone maintenance dosages and P-glycoprotein (P-gp) was considered to be one of the major contributors. To investigate the mechanism of P-gp's interaction with
Golam Kibria et al.
Biological & pharmaceutical bulletin, 37(12), 1926-1935 (2014-12-03)
Multi-drug resistance (MDR) of cancers to chemotherapy including doxorubicin (DOX) is mediated by several factors. To design an effective therapy for the treatment of chemotherapy-resistant cancers, it is essential to explore the elements responsible for mediating MDR. However, exploring these
Tuba Incecayir et al.
Molecular pharmaceutics, 10(3), 958-966 (2013-01-19)
The purpose of this study was to investigate labetalol as a potential high permeability reference standard for the application of Biopharmaceutics Classification Systems (BCS). Permeabilities of labetalol and metoprolol were investigated in animal intestinal perfusion models and Caco-2 cell monolayers.
Yong Yu et al.
Die Pharmazie, 68(9), 732-743 (2013-10-24)
Raltitrexed (RTX) has shown clinical activity in a variety of advanced solid tumours. Its oral bioavailability is low and its intestinal absorption mechanism is not clear. In the present study, the absorption mechanism of RTX in the small intestine was
Meng Jiang et al.
Nature communications, 11(1), 19-19 (2020-01-09)
Colorectal cancer (CRC) is the third most commonly diagnosed cancer, which despite recent advances in treatment, remains incurable due to molecular heterogeneity of tumor cells. The B-cell lymphoma 9 (BCL9) oncogene functions as a transcriptional co-activator of the Wnt/β-catenin pathway
Sweat but no gain: inhibiting proliferation of multidrug resistant cancer cells with "ersatzdroges".
Yoonseok Kam et al.
International journal of cancer, 136(4), E188-E196 (2014-08-27)
ATP-binding cassette (ABC) drug transporters consuming ATPs for drug efflux is a common mechanism by which clinical cancers develop multidrug resistance (MDR). We hypothesized that MDR phenotypes could be suppressed by administration of "ersatzdroges," nonchemotherapy drugs that are, nevertheless, ABC
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