Results 91 to 100 of about 158,142 (288)

A novel quinazolinone insulin receptor inhibitor and its synergy with an EGFR inhibitor in glucose‐driven glioblastoma

Molecular Oncology, EarlyView.
The novel styrylquinazolinone‐based molecule W1B effectively suppresses glioblastoma by inhibiting IGF1R and EGFR. In high‐glucose microenvironments driving tumor resistance, W1B acts synergistically with the EGFR inhibitor dacomitinib. This combination safely blocks compensatory survival signaling in zebrafish xenograft models. Showcasing promising in
Patryk Rurka, Wioleta Cieślik, Wojciech Płaziński, Katarzyna Stępnik, Anna Boguszewska‐Czubara, Elżbieta Kot, Robert Musioł, Mateusz Jasica, Anna Mrozek‐Wilczkiewicz, Katarzyna Malarz   +9 more
wiley   +1 more source

The role of mitochondrial and plasma membrane nucleoside transporters in drug toxicity

, 2007
Many anticancer and antiviral drugs are nucleoside analogues, which interfere with nucleotide metabolism and DNA replication to produce pharmacological effects.
George PH Leung, Leung, GPH, Chung-Ming Tse, Tse, CM   +3 more
core   +1 more source

The Role of ABCB1, ABCG2, and SLC Transporters in Pharmacokinetic Parameters of Selected Drugs and Their Involvement in Drug–Drug Interactions

Membranes
Membrane transporters are expressed in a wide range of tissues in the human organism. These proteins regulate the penetration of various substances such as simple ions, xenobiotics, and an extensive number of therapeutics.
Kajetan Kiełbowski, Małgorzata Król, Estera Bakinowska, Andrzej Pawlik   +3 more
doaj   +1 more source

Mycobacterial cell division arrest and smooth‐to‐rough envelope transition using CRISPRi‐mediated genetic repression systems

FEBS Open Bio, EarlyView.
CRISPRI‐mediated gene silencing and phenotypic exploration in nontuberculous mycobacteria. In this Research Protocol, we describe approaches to control, monitor, and quantitatively assess CRISPRI‐mediated gene silencing in M. smegmatis and M. abscessus model organisms.
Vanessa Point, Wafaa Achache, Janïs Laudouze, Eliana Sepulveda Ramos, Mickaël Maziero, Céline Crauste, Stéphane Canaan, Pierre Santucci   +7 more
wiley   +1 more source

Suppression of lung adenocarcinoma migration through organelle alkalization by human lactoferrin – albumin fusion

FEBS Open Bio, EarlyView.
This paper reveals how human lactoferrin–albumin fusion (hLF‐HSA) potently suppresses lung adenocarcinoma cell migration. hLF‐HSA upregulates NHE7, leading to Golgi alkalization, disruption of the Golgi secretome, downregulation of MMP1, and reversal of EMT. These findings suggest a novel Golgi‐targeting strategy to suppress cancer cell migration.
Hana Nopia, Masahiro Kimura, Daisuke Kurimoto, Atsushi Sato   +3 more
wiley   +1 more source

Diurnal Rhythmicity in the Transcription of Jejunal Drug Transporters†

Journal of Pharmacological Sciences, 2008
Intestinal drug efflux proteins play a major role in the pharmacokinetics of many drugs. We assessed diurnal rhythmicity in the expression of ten major drug transporters.
Adam T. Stearns, Anita Balakrishnan, David B. Rhoads, Stanley W. Ashley, Ali Tavakkolizadeh   +4 more
doaj   +1 more source

Identifying transcription factors controlling the basal expression of human MRP4 highlights a substantial role for Sp1

FEBS Open Bio, EarlyView.
The MRP4 transporter exports several drugs and signaling molecules. Here, we identified key promoter elements regulating basal MRP4 expression. Using reporter assays, we defined a conserved region with essential Sp1 and contributory Ets sites, which controlled basal MRP4 expression.
Debora Singer, Angelique Kragl, Katrin Ziems, Juliane Glaubitz, Sophie Grammbauer, Susanne Hildebrandt, Mladen V. Tzvetkov, Gabriele Jedlitschky   +7 more
wiley   +1 more source

Entecavir interacts with influx transporters hOAT1, hCNT2, hCNT3, but not with hOCT2: the potential for renal transporter-mediated cytotoxicity and drug-drug interactions

Frontiers in Pharmacology, 2016
Entecavir (ETV) is one of the most potent agents for the treatment of the hepatitis B viral infection. The drug is principally eliminated by the kidney.
František eTrejtnar, Jana eMandíková, Marie eVolková, Petr ePávek, Lucie eNavrátilová, Lucie eHyršová, Zlatko eJaneba, Jan ePavlík, Pavel eBárta   +8 more
doaj   +1 more source

Lipopolysaccharide uptake is augmented in lipopolysaccharide‐tolerant mouse macrophage‐like cells via increased CD14 expression

FEBS Open Bio, EarlyView.
In normal (nontolerant) cells, CD14 is crucial for both LPS uptake and LPS signaling. In LPS‐tolerant cells, in which LPS‐induced TNF‐α and IFN‐β production is suppressed, there is a dramatic increase in surface CD14 expression. The overexpressed CD14 in LPS‐tolerant cells is responsible for the enhanced LPS uptake without inducing pro‐inflammatory ...
Saeka Nishihara, Takayuki Manabe, Mika Jouta, Kiyoshi Kawasaki   +3 more
wiley   +1 more source

Transporters and Renal Drug Elimination

, 2004
Carrier-mediated processes, often referred to as transporters, play key roles in the reabsorption and secretion of many endogenous and xenobiotic compounds by the kidney.
Lee, Wooin, Kim, Richard B.
core   +1 more source