Radioiodination of Two Carborane-Based Dual Cyclooxygenase-2/5-Lipoxygenase Inhibitors and Their In Vitro and In Vivo Evaluation. [PDF]
Two dicarbadodecaborane(12)‐based dual cyclooxygenase‐2/5‐lipoxygenase (COX‐2/5‐LO) inhibitors were 123I‐labeled. Refinement of labeling and formulation conditions and extensive in vitro characterization are presented. Cell uptake studies in COX‐2‐ and 5‐LO‐overexpressing cell lines showed COX‐2‐independent and partly 5‐LO‐dependent uptake.
Schädlich J +11 more
europepmc +2 more sources
Targeting EZH2 reverses thyroid cell dedifferentiation and enhances iodide uptake in anaplastic thyroid cancer. [PDF]
Anaplastic thyroid cancer (ATC) lacks iodide uptake ability due to MAPK activation increasing the expression of the histone methyltransferase EZH2, which represses thyroid differentiation genes (TDGs) such as the sodium iodide symporter (NIS). Dual inhibition of MAPK (U0126) and EZH2 (EPZ6438/Tazemetostat) reverses this mechanism, thus restoring TDG ...
de Mello DC +6 more
europepmc +2 more sources
Modeling, substrate docking, and mutational analysis identify residues essential for the function and specificity of a eukaryotic purine-cytosine NCS1 transporter [PDF]
Background: The purine-cytosine FcyB transporter is a prototype member of the NCS1 family. Results: Using homology modeling, substrate docking, and rational mutational analysis, we identify residues critical for function and specificity.
Amillis, Sotiris +5 more
core +1 more source
Glycine transporters GlyT1 and GlyT2 are differentially modulated by glycogen synthase kinase 3β [PDF]
© 2014 Elsevier Ltd. All rights reserved. Inhibitory glycinergic neurotransmission is terminated by the specific glycine transporters GlyT1 and GlyT2 which actively reuptake glycine from the synaptic cleft.
Giménez, C. +4 more
core +1 more source
Trypanosoma brucei methylthioadenosine phosphorylase protects the parasite from the antitrypanosomal effect of deoxyadenosine [PDF]
Trypanosoma brucei causes African sleeping sickness for which no vaccine exists and available treatments are of limited use due to their high toxicity or lack of efficacy. T.
de Koning, Harry P. +4 more
core +1 more source
The elements of life and medicines [PDF]
Which elements are essential for human life? Here we make an element-by-element journey through the periodic table and attempt to assess whether elements are essential or not, and if they are, whether there is a relevant code for them in the human genome.
Chellan , Prinessa, Sadler, P. J.
core +1 more source
Substrate binding and translocation of the serotonin transporter studied by docking and molecular dynamics simulations [PDF]
The serotonin (5-HT) transporter (SERT) plays an important role in the termination of 5-HT-mediated neurotransmission by transporting 5-HT away from the synaptic cleft and into the presynaptic neuron.
Mari Gabrielsen +3 more
core +2 more sources
Lactate Regulates Metabolic and Proinflammatory Circuits in Control of T Cell Migration and Effector Functions [PDF]
Licensed by the Creative Commons Attribution ...
A Ene-Obong +62 more
core +5 more sources
Evidence for the Existence of a Channel in the Glucose-Specific Carrier EIIGlc of the Salmonella typhimurium Phosphoenolpyruvate-Dependent Phosphotransferase System [PDF]
The effect of membrane-impermeable sulfhydryl reagents on glucose-specific enzyme II (EIIGlc) activity has been studied in Salmonella typhimurium whole cells and in properly sealed inverted cytoplasmic membrane vesicles.
Beechey, R.B., Robillard, G.T.
core +4 more sources
Molecular theranostics: principles, challenges and controversies
Molecular theranostics offers a powerful tool to drive precision medicine in nuclear oncology. While theranostics is not a new principle in nuclear medicine, recent advances in instrumentation and radiopharmacy have driven a reinvigoration and a broader suite of applications.
Geoffrey Currie
wiley +1 more source

