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Showing 1-30 of 214 results for "V4629" within Papers
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
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
Mohammed Sedeeq et al.
Molecular neurobiology, 59(5), 2932-2945 (2022-03-05)
Medulloblastoma (MB) is the most common malignant paediatric brain tumour. In our previous studies, we developed a novel 3D assay for MB cells that was used to screen a panel of plasma membrane calcium channel modulators for their effect on
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
Hiroki Shimizu et al.
ChemMedChem, 17(16), e202200204-e202200204 (2022-06-14)
We synthesized and experimentally tested the passive permeability of more than thirty tetrapeptides mimicking the N-terminus of the pro-apoptotic protein Smac (Second mitochondria-derived activator of caspases). Each peptide bore one or two unnatural Hydrogen Bond Acceptor-bearing Amino Acid (HBA-AA) residues
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
Seema Saksena et al.
American journal of physiology. Gastrointestinal and liver physiology, 304(6), G615-G622 (2013-01-19)
Intestinal P-glycoprotein (Pgp/multidrug resistance 1), encoded by the ATP-binding cassette B1 gene, is primarily involved in the transepithelial efflux of toxic metabolites and xenobiotics from the mucosa into the gut lumen. Reduced Pgp function and expression has been shown to
Timo Smit et al.
Cells, 10(10) (2021-10-24)
The heart tissue is a potential target of various noxae contributing to the onset of cardiovascular diseases. However, underlying pathophysiological mechanisms are largely unknown. Human stem cell-derived models are promising, but a major concern is cell immaturity when estimating risks
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
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
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
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
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
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
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
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)
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
Margaret Elizabeth Eng et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 36(4), e22245-e22245 (2022-03-10)
Antenatal synthetic glucocorticoids (sGCs) are a life-saving treatment in managing pre-term birth. However, off-target effects of sGCs can impact blood-brain barrier (BBB) drug transporters essential for fetal brain protection, including P-glycoprotein (P-gp/Abcb1) and breast cancer resistance protein (BCRP/Abcg2). We hypothesized
Shipeng Dang et al.
Annals of translational medicine, 8(4), 127-127 (2020-03-17)
Heart failure (HF) is an end-stage syndrome of all structural heart diseases which accompanies the loss of myocardium and cardiac fibrosis. Although the role of inflammasome in cardiac fibrosis has recently been a point of focus, the mechanism of inflammasome
Kowit Yu Chong et al.
Cancer biology & therapy, 16(1), 149-159 (2015-01-16)
Multiple drug resistance (MDR) is a major obstacle to attenuating the effectiveness of chemotherapy to many human malignancies. Proteasome inhibition induces apoptosis in a variety of cancer cells and is recognized as a novel anticancer therapy approach. Despite its success
Dasha Palmer et al.
Colloids and surfaces. B, Biointerfaces, 104, 174-180 (2013-01-15)
The ability of anionic polymer sodium carboxymethylcellulose to influence the release of four model cationic drugs (chlorpheniramine maleate, venlafaxine hydrochloride, propranolol hydrochloride and verapamil hydrochloride) from extended release (ER) hydrophilic matrices based on non-ionic polymer polyethylene oxide was investigated by
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
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
Lian Duan et al.
International journal of pharmaceutics, 445(1-2), 134-140 (2013-02-14)
The aim of the study was to observe the characteristic of permeation of capsaicin across jejunum, ileum and colon in the rat, and to investigate the role of transient receptor potential cation channel (TRPV1). The interaction of capsaicin with P-glycoprotein
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.
Yankun Lyu et al.
iScience, 25(1), 103624-103624 (2022-01-11)
The mammalian heart beats incessantly with rhythmic mechanical activities generating acids that need to be buffered to maintain a stable intracellular pH (pHi) for normal cardiac function. Even though spatial pHi non-uniformity in cardiomyocytes has been documented, it remains unknown
Jiu Wang et al.
Zhong yao cai = Zhongyaocai = Journal of Chinese medicinal materials, 35(9), 1500-1507 (2013-03-05)
The aim of this study was to load Verapamil Hydrochloride to carboxylated multi-walled carbon nanotubes( c-CNTs) and discuss the mechanism of drug release which could act as an effective basis for c-MWNTs used as drug carriers of controlled and sustained
Meng Zhao et al.
Journal of visualized experiments : JoVE, (149) (2019-07-30)
A crucial factor in improving cellular therapy effectiveness for myocardial regeneration is to safely and efficiently increase the cell engraftment rate. Y-27632 is a highly potent inhibitor of Rho-associated, coiled-coil-containing protein kinase (RhoA/ROCK) and is used to prevent dissociation-induced cell
Seyoum Ayehunie et al.
Pharmaceutical research, 35(4), 72-72 (2018-02-25)
The study evaluates the use of new in vitro primary human cell-based organotypic small intestinal (SMI) microtissues for predicting intestinal drug absorption and drug-drug interaction. The SMI microtissues were reconstructed using human intestinal fibroblasts and enterocytes cultured on a permeable
Yiqun Zhang et al.
Bioorganic & medicinal chemistry, 18(7), 2756-2766 (2010-03-09)
Malaria is endemic in tropical and subtropical regions of Africa, Asia, and the Americas. The increasing prevalence of multi-drug-resistant Plasmodium falciparum drives the ongoing need for the development of new antimalarial drugs. In this light, novel scaffolds to which the
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