Topical TrkA Kinase Inhibitor CT327 is an Effective, Novel Therapy for the Treatment of Pruritus due to Psoriasis: Results from Experimental Studies, and Efficacy and Safety of CT327 in a Phase 2b Clinical Trial in Patients with Psoriasis.

Pruritus is an important symptom in psoriasis with no targeted treatment. Tropomyosin-receptor kinase A (TrkA) is associated with pruritus and psoriatic plaque formation. We report the efficacy of a TrkA inhibitor, CT327, on pruritus in psoriasis.

Water exchange across the erythrocyte plasma membrane studied by HR-MAS NMR spectroscopy.

Water exchange across the plasma membrane of erythrocytes (red blood cells (RBCs)) was studied by means of high-resolution magic angle spinning (HR-MAS) NMR spectroscopy. Under HR-MAS conditions, the centrifugal force causes the splitting of RBC suspensions into a two-phase system composed of a central core of cell free water and an outer layer of tightly packed cells. Water belonging to each of these phases gives rise to two separated resonances.

HR-MAS of cells: A "cellular water shift" due to water-protein interactions?

Under HR-MAS conditions, cells are subjected to high centrifugal forces that may cause irreversible cell damage. First, conditions have been defined to monitor and keep to a minimum unwanted effects in HR-MAS spectra arising from the loss of cell integrity. Then, the HR-MAS spectra of reasonably intact cells have been analyzed.

Magnetic resonance imaging visualization of targeted cells by the internalization of supramolecular adducts formed between avidin and biotinylated Gd3+ chelates.

The high binding affinity between avidin and biotin has been exploited to develop a procedure for magnetic resonance imaging (MRI) visualization of target cells. SHIN3 and PANC1 tumor cell lines have been used as target cells because they possess on their membranes galactosyl receptors able to bind avidin molecules. Avidin-Gd chelate adducts have been built by using two Gd complexes containing one (Gd-I) and two (Gd-II) biotin residues, respectively.

Synthesis of a bifunctional monophosphinic acid DOTA analogue ligand and its lanthanide(III) complexes. A gadolinium(III) complex endowed with an optimal water exchange rate for MRI applications.

A new bifunctional octa-coordinating ligand containing an aminobenzyl moiety, DO3APABn (H4DO3APABn = 1,4,7,10-tetraazacyclododecane-4,7,10-triacetic-1-{methyl[(4-aminophenyl)methyl]phosphinic acid}), has been synthesized. Its lanthanide(III) complexes contain one water molecule in the first coordination sphere. The high-resolution 1H and 31P spectra of [Eu(H2O) (DO3APABn)]- show that the twisted square-antiprismatic form of the complexes is more abundant in respect to the corresponding Eu(III)-DOTA complex.

Modulation of the antioxidant activity of HO* scavengers by albumin binding: a 19F-NMR study.

The interaction between different HO(z.rad;) radical scavengers in a three-component antioxidant system has been investigated by means of 19F-NMR spectroscopy. This system is composed of bovine serum albumin (BSA), trolox, and N-(4-hydroxyphenyl)-trifluoroacetamide (CF(3)PAF).

Innovative magnetic resonance imaging diagnostic agents based on paramagnetic Gd(III) complexes.

Gd(III) complexes are under intense scrutiny as contrast agents for magnetic resonance imaging (MRI). They act by enhancing tissutal proton relaxation rates. Much has already been done in order to get an in-depth understanding of the relationships between structure, dynamics, and contrastographic ability of these paramagnetic complexes.

Separation of intra- and extracellular lactate NMR signals using a lanthanide shift reagent.

This work describes the use of [Pr-DO3A] as a shift reagent for differentiating intra- and extracellular L-lactate resonance in (1)H- and (13)C-NMR spectra. DO3A acts as heptadentate ligand towards lanthanide(III) ions, leaving two coordination vacancies for the coordination of the L-lactate ion. The exchange between free and [Pr-DO3A]-bound L-lactate is fast on the NMR timescale, thus yielding a paramagnetically shifted L-lactate signal for the substrate in the compartment containing the paramagnetic chelate.