40 results match your criteria: "University of Zaragoza-CSIC[Affiliation]"

Rational Design of Dual-Domain Binding Inhibitors for -Acetylgalactosamine Transferase 2 with Improved Selectivity over the T1 and T3 Isoforms.

JACS Au

September 2024

Department of Chemistry and Instituto de Investigación en Química de la Universidad de La Rioja, Universidad de La Rioja, Logroño 26006, Spain.

Article Synopsis
  • * Developing inhibitors poses challenges due to similarities among isoenzymes and redundancy among substrates, making specific targeting difficult.
  • * A new GalNAc-T2 inhibitor has been created that shows enhanced potency and selectivity, with a unique design that allows it to effectively bind to different parts of the enzyme, marking a significant advancement in targeting these enzymes for therapeutic purposes.
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[Not Available].

Mater Today Bio

February 2024

Department of Ophthalmology, Miguel Servet University Hospital, Zaragoza, Spain.

Clay minerals have been applied in biomedicine for thousands of years. Laponite is a nanostructured synthetic clay with the capacity to retain and progressively release drugs. In recent years there has been a resurgence of interest in Laponite application in various biomedical areas.

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Towards new fluorometric methodologies based on the in-situ generation of gold nanoclusters.

Talanta

January 2024

Analytical Biosensors Group (GBA), Analytical Chemistry Department, Faculty of Sciences, Instituto de Nanociencia y Materiales de Aragón (INMA), University of Zaragoza-CSIC, C/Pedro Cerbuna 12, 50009, Zaragoza, Spain. Electronic address:

In this manuscript a method for the fluorometric determination of tyramine is described. It is based on the direct reaction between Au(III) and tyramine in a phosphate buffer which produces fluorescent gold nanoclusters (AuNC) (λ = 320 nm, λ = 410 nm) with a diameter of 1.50 ± 0.

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Detailed structural information is essential for understanding the properties of TCNQ and TCNQF compounds (TCNQ = 7,7,8,8-tetracyanoquinodimethane; TCNQF = 2,3,5,6-tetrafluoro-7,7,8,8-tetracyanoquinodimethane). The ineludible requirement of obtaining crystals of a size and quality sufficient to yield a successful X-ray diffraction analysis has been challenging to satisfy because of the instability of many of these compounds in solution. Crystals of two new complexes of TCNQ, [-M(2)(TCNQ)] [M = Ni (), Zn (); 2ampy = 2-aminomethylpyridine], as well as unstable [Li(TCNQF)(CHCN)]·CHCN (), can be prepared in minutes by a horizontal diffusion technique and can be harvested easily for X-ray structural studies.

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Collagen-Laponite Nanoclay Hydrogels for Tumor Spheroid Growth.

Biomacromolecules

June 2023

Multiscale in Mechanical and Biological Engineering, Aragón Institute of Engineering Research (I3A) & Aragón Institute of Healthcare Research (IIS Aragón), Department of Mechanical Engineering, University of Zaragoza, Zaragoza, 50018, Spain.

The extracellular matrix (ECM) plays an important regulatory role in the development and progression of tumoral tissue. Its functions and properties are crucial in determining tumor cell behavior such as invasion, migration, and malignancy development. Our study explores the role of collagen type I in cancer development and spread using engineered tumor models like multicellular spheroids grown in collagen-based hydrogels to simulate early tumor formation.

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Tectomer-Mediated Optical Nanosensors for Tyramine Determination.

Sensors (Basel)

February 2023

Nanosensors and Bioanalytical Systems (N&SB), Analytical Chemistry Department, Faculty of Sciences, Instituto de Nanociencia y Materiales de Aragón (INMA University of Zaragoza-CSIC), 50009 Zaragoza, Spain.

The development of optical sensors for in situ testing has become of great interest in the rapid diagnostics industry. We report here the development of simple, low-cost optical nanosensors for the semi-quantitative detection or naked-eye detection of tyramine (a biogenic amine whose production is commonly associated with food spoilage) when coupled to Au(III)/tectomer films deposited on polylactic acid (PLA) supports. Tectomers are two-dimensional oligoglycine self-assemblies, whose terminal amino groups enable both the immobilization of Au(III) and its adhesion to PLA.

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Intravitreal injection is the gold standard therapeutic option for posterior segment pathologies, and long-lasting release is necessary to avoid reinjections. There is no effective intravitreal treatment for glaucoma or other optic neuropathies in daily practice, nor is there a non-invasive method to monitor drug levels in the vitreous. Here we show that a glaucoma treatment combining a hypotensive and neuroprotective intravitreal formulation (IF) of brimonidine-Laponite (BRI/LAP) can be monitored non-invasively using vitreoretinal interface imaging captured with optical coherence tomography (OCT) over 24 weeks of follow-up.

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Janus Dendrimers to Assess the Anti-HCV Activity of Molecules in Cell-Assays.

Pharmaceutics

November 2020

Instituto de Nanociencia y Materiales de Aragón (INMA), University of Zaragoza-CSIC, Pedro Cerbuna 12, 50009 Zaragoza, Spain.

The use of nanocarriers has been revealed as a valid strategy to facilitate drug bioavailability, and this allows for expanding the drug libraries for the treatment of certain diseases such as viral diseases. In the case of Hepatitis C, the compounds iopanoic acid and 3,3',5-triiodothyroacetic acid (or tiratricol) were identified in a primary screening as bioactive allosteric inhibitors of viral NS3 protease, but they did not exhibit accurate activity inhibiting viral replication in cell-based assays. In this work, dendritic nanocarriers are proposed due to their unique properties as drug delivery systems to rescue the bioactivity of these two drugs.

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Heparin is a promising antimalarial drug due to its activity in inhibiting invasion of red blood cells and to the lack of resistance evolution by the parasite against it, but its potent anticoagulant activity is preventing the advance of heparin along the clinical pipeline. We have determined, in in vitro cultures, the antimalarial activity of heparin-derived structures of different origins and sizes, to obtain formulations having a good balance of in vitro safety (neither cytotoxic nor hemolytic), low anticoagulant activity (≤23 IU/mL according to activated partial thromboplastin time assays), and not too low antimalarial activity (IC50 at least around 100 µg/mL). This led to the selection of five chemically modified heparins according to the parameters explored, i.

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Dissecting the Structural and Chemical Determinants of the "Open-to-Closed" Motion in the Mannosyltransferase PimA from Mycobacteria.

Biochemistry

August 2020

Instituto Biofisika, Centro Mixto Consejo Superior de Investigaciones Científicas-Universidad del País Vasco/Euskal Herriko Unibertsitatea (CSIC, UPV/EHU), Barrio Sarriena s/n, Leioa, Bizkaia 48940, Spain.

The phosphatidyl--inositol mannosyltransferase A (PimA) is an essential peripheral membrane glycosyltransferase that initiates the biosynthetic pathway of phosphatidyl--inositol mannosides (PIMs), key structural elements and virulence factors of . PimA undergoes functionally important conformational changes, including (i) α-helix-to-β-strand and β-strand-to-α-helix transitions and (ii) an "open-to-closed" motion between the two Rossmann-fold domains, a conformational change that is necessary to generate a catalytically competent active site. In previous work, we established that GDP-Man and GDP stabilize the enzyme and facilitate the switch to a more compact active state.

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This paper presents a novel nanoformulation for sustained-release delivery of dexamethasone (DEX) to the ocular posterior segment using a Laponite (LAP) carrier-DEX/LAP 1:10 w w formulation; 10 mg ml. In vivo ocular feasibility and pharmacokinetics after intravitreal (IV) and suprachoroidal (SC) administration in rabbit eyes are compared against IV administration of a DEX solution (1 mg ml). Thirty rabbit eyes were injected with the DEX/LAP formulation (15 suprachoroid/15 intravitreous).

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The self-assembly of the protein clathrin on biological membranes facilitates essential processes of endocytosis and has provided a source of inspiration for materials design by the highly ordered structural appearance. By mimicking the architecture of the protein building blocks and clathrin self-assemblies to coat liposomes with biomaterials, advanced hybrid carriers can be derived. Here, we present a method for fabricating DNA-coated liposomes by hydrophobically anchoring and subsequently connecting DNA-based triskelion structures on the liposome surface inspired by the assembly of the protein clathrin.

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Three new isomorphous complexes [Ni(o-van-en)LnCl(HO)] [H(o-van-en) = N,N'-ethylene-bis(3-methoxysalicylaldiminate; Ln = Ce (1), Gd (2), Dy (3)] were prepared by a stepwise reaction using mild conditions and were structurally characterised as dinuclear molecules in which Ni and Ln are coordinated by the compartmental Schiff base ligand (o-van-en) and doubly bridged by O atoms. While the nickel(ii) centre is diamagnetic within the NO square-planar coordination of the Schiff base ligand, the lanthanide atoms are octa-coordinated to give an {LnClO} chromophore with a fac-arrangement of the chlorido ligands. AC magnetic measurements revealed that all three complexes, including the nominally isotropic Gd(iii) system, show field induced slow magnetic relaxation with two or three relaxation channels: at T = 1.

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Gold as a Possible Alternative to Platinum-Based Chemotherapy for Colon Cancer Treatment.

Cancers (Basel)

June 2019

Deparment of Inorganic Chemistry, University of Zaragoza, Instituto de Síntesis Química y Catálisis Homogénea-ISQCH, University of Zaragoza-CSIC, 50009 Zaragoza, Spain.

Due to the increasing incidence and high mortality associated with colorectal cancer (CRC), novel therapeutic strategies are urgently needed. Classic chemotherapy against CRC is based on oxaliplatin and other cisplatin analogues; however, platinum-based therapy lacks selectivity to cancer cells and leads to deleterious side effects. In addition, tumor resistance to oxaliplatin is related to chemotherapy failure.

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Cobalt(ii) benzoate trihydrate prepared by the reaction of CoCO with benzoic acid (HBz) in boiling water followed by crystallization has been structurally characterized as a chain-like system with the formula unit [Co(Bz)(HO)]Bz·HO where the Co(ii) atoms are triply linked by one bridging syn-syn benzoato (Bz) and two aqua ligands; additional benzoate counter ions and solvate water molecules are present in the crystal structure. DC magnetic measurements reveal a sizable exchange coupling of a ferromagnetic nature between the Co(ii) atoms. At T = 5.

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Crystalline transformers: more within than meets the eye.

Acta Crystallogr B Struct Sci Cryst Eng Mater

October 2018

Department of Inorganic Chemistry and Aragón Materials Science Institute (ICMA), University of Zaragoza - CSIC, Pedro Cerbuna 12, Zaragoza, E-50009, Spain.

Studies of phase transitions in molecular crystals are becoming more commonplace as improvements in instrumentation and technique enable more efficient exploration of the behavior of samples with varying external conditions, usually temperature. This scientific commentary provides contextual background on this type of study, with reference to an article on transformations in a ferrocenyl-acetylide-gold(I) complex [Makal (2018). Acta Cryst.

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Homogeneous polycrystalline Fe O nanoparticles were generated by ablation of iron targets in water by nanosecond laser pulses at 532 nm. In ethanol, crystalline core-shell Fe/Fe O structures with size medians around 20 nm were produced. The ablation of FeW O targets in water resulted in crystalline hollow shells and homogeneous FeW O nanoparticles.

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Infection of orthopedic devices is a major complication in the postsurgical period generating important health issues and economic consequences. Prevention strategies could be based on local release of antibiotics from the orthopedic device itself to avoid adhesion and growth of bacteria. The purpose of this work is to demonstrate the efficiency to prevent these infections by a cefazolin-eluting, perforated stainless steel implant in an in vivo ovine model.

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A phase transition caught in mid-course: independent and concomitant analyses of the monoclinic and triclinic structures of (BuN)[Co(orotate)(bipy)]·3HO.

Acta Crystallogr C Struct Chem

September 2017

Department of Inorganic Chemistry and Instituto de Síntesis Química y Catálisis Homogenea (ISQCH), University of Zaragoza-CSIC, Pedro Cerbuna 12, Zaragoza E-50009, Spain.

The preparation and characterization of the BuN salts of two bis-orotate(2-) complexes of cobalt, namely bis(tetra-n-butylammonium) diaquabis(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-ide-6-carboxylato-κN,O)cobalt(II) 1.8-hydrate, (CHN)[Co(CHNO)(HO)]·1.8HO, (1), and tetra-n-butylammonium (2,2'-bipyridine-κN,N')bis(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-ide-6-carboxylato-κN,O)cobalt(III) trihydrate, (CHN)[Co(CHNO)(CHN)]·3HO, (2), are reported.

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A diphenylalanine (FF) amphiphile blocked at the C terminus with a benzyl ester (OBzl) and stabilized at the N terminus with a trifluoroacetate (TFA) anion was synthetized and characterized. Aggregation of peptide molecules was studied by considering a peptide solution in an organic solvent and adding pure water, a KCl solution, or another organic solvent as co-solvent. The choice of the organic solvent and co-solvent and the solvent/co-solvent ratio allowed the mixture to be tuned by modulating the polarity, the ionic strength, and the peptide concentration.

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A highly sensitive and selective ratiometric sensor for the quantification of cyanide (CN) in aqueous samples has been developed using spherical gold nanoparticles (AuNPs) stabilized by polysorbate 40 (PS-40). Three different AuNP sizes (14, 40 and 80nm mean diameters) were used to evaluate the response of the sensor using both colorimetric and Resonance Rayleigh Scattering (RRS) detection schemes. The best results were obtained for the sensor using 40nm AuNPs, for which the limits of detection (LODs) were found to be 100nmolL in a benchtop instrument and 500nmolL by the naked eye, values well below the maximum acceptable level for drinking water (1.

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Purpose: To develop a simple, specific, and rapid method to determine corticosteroid concentrations in vitreous humor.

Methods: An analytical method based on high-pressure liquid chromatography-tandem mass spectrometry (HPLC-MS) with a simple extraction procedure was developed. New Zealand albino rabbits (n = 54) received a single (0.

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New Ionic bis-MPA and PAMAM Dendrimers: A Study of Their Biocompatibility and DNA-Complexation.

Macromol Biosci

May 2015

Departamento de Química Orgánica-Instituto de Nanociencia de Aragón (INA), University of Zaragoza, C/Pedro Cerbuna 12, 50009, Zaragoza, Spain.

Herein, the synthesis of five novel ionic dendrimers and their evaluation as biological carriers is reported. The compounds include an ionic bis-MPA dendrimer and four PAMAM dendrimers of different generations decorated with negatively charged hydrophilic chains of 2-[2-(2-methoxyethoxy)ethoxy]acetic acid as counter ions in order to increase their biocompatibility. The ionic dendrimers derived from bis-MPA have a low cytotoxicity at 0.

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A bifunctional amorphous polymer exhibiting equal linear and circular photoinduced birefringences.

Macromol Rapid Commun

November 2014

Institute of Materials Science of Aragon (ICMA), University of Zaragoza-CSIC, Faculty of Science, Pedro Cerbuna 12, 50009, Zaragoza, Spain.

The large and reversible photoinduced linear and circular birefringences in azo-compounds are at the basis of the interest in these materials, which are potentially useful for several applications. Since the onset of the linear and circular anisotropies relies on orientational processes, which typically occur on the molecular and supramolecular length scale, respectively, a circular birefringence at least one order of magnitude lower than the linear one is usually observed. Here, the synthesis and characterization of an amorphous polymer with a dimeric repeating unit containing a cyanoazobenzene and a cyanobiphenyl moiety are reported, in which identical optical linear and circular birefringences are induced for proper light dose and ellipticity.

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