α-Hexylcinnamaldehyde synergistically increases doxorubicin cytotoxicity towards human cancer cell lines [PDF]
α-Hexylcinnamaldehyde (HCA), a compound derived from cinnamaldehyde, was evaluated for its potential chemosensitizing ...
DI GIACOMO, Silvia +4 more
core
Identification of Trypanosoma cruzi Polyamine Transport Inhibitors by Computational Drug Repurposing [PDF]
Trypanosoma cruzi is the causative agent of Chagas disease, a parasitic infection endemic in Latin America. In T. cruzi the transport of polyamines is essential because this organism is unable to synthesize these compounds de novo.
Martínez Sayé, Melisa Soledad +5 more
core +1 more source
Drug structure–transport relationships [PDF]
Malcolm Rowland has greatly facilitated an understanding of drug structure-pharmacokinetic relationships using a physiological perspective. His view points, covering a wide range of activities, have impacted on my own work and on my appreciation and understanding of our science.
openaire +3 more sources
Exploiting metabolic adaptations to overcome dabrafenib treatment resistance in melanoma cells
We show that dabrafenib‐resistant melanoma cells undergo mitochondrial remodeling, leading to elevated respiration and ROS production balanced by stronger antioxidant defenses. This altered redox state promotes survival despite mitochondrial damage but renders resistant cells highly vulnerable to ROS‐inducing compounds such as PEITC, highlighting redox
Silvia Eller +17 more
wiley +1 more source
Stimulation of glucose utilization in 3T3 adipocytes and rat diaphragm in vitro by the sulphonylureas, glimepiride and glibenclamide, is correlated with modulations of the cAMP regulatory cascade [PDF]
The long-term hypoglycemic activity of sulphonylurea drugs has been attributed, in part at least, to the stimulation of glucose utilization in extra-pancreatic tissues. The novel sulphonylurea, glimepiride, gives rise to a longer lasting reduction in the
Altan +75 more
core +1 more source
Cell surface interactome analysis identifies TSPAN4 as a negative regulator of PD‐L1 in melanoma
Using cell surface proximity biotinylation, we identified tetraspanin TSPAN4 within the PD‐L1 interactome of melanoma cells. TSPAN4 negatively regulates PD‐L1 expression and lateral mobility by limiting its interaction with CMTM6 and promoting PD‐L1 degradation.
Guus A. Franken +7 more
wiley +1 more source
Tae-Eun Kim,1 Na Ha,2 Yunjeong Kim,2 Hyunsook Kim,1 Jae Wook Lee,3 Ji-Young Jeon,2 Min-Gul Kim2,4 1Department of Clinical Pharmacology, Konkuk University Medical Center, Seoul, 2Center for Clinical Pharmacology, Biomedical Research Institute, Chonbuk ...
Kim TE +6 more
doaj
Protein kinase C modulates the activity of a cloned gamma-aminobutyric acid transporter expressed in Xenopus oocytes via regulated subcellular redistribution of the transporter [PDF]
We report that activators and inhibitors of protein kinase C (PKC) and protein phosphatases regulate the activity of a cloned rat brain gamma- aminobutyric acid (GABA) transporter (GAT1) expressed in Xenopus oocytes.
Brecha, Nicholas +4 more
core
Pharmacologic ascorbate (vitamin C) increases ROS, disrupts cellular metabolism, and induces DNA damage in CRPC cells. These effects sensitize tumors to PARP inhibition, producing synergistic growth suppression with olaparib in vitro and significantly delayed tumor progression in vivo. Pyruvate rescue confirms ROS‐dependent activity.
Nicolas Gordon +13 more
wiley +1 more source
Structural basis for the mechanism of ABC transporters. [PDF]
The ATP-binding cassette (ABC) transporters are primary transporters that couple the energy stored in adenosine triphosphate (ATP) to the movement of molecules across the membrane.
Beis, K
core +1 more source

