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showing 10 items of 6731 documents
Development of an Easily Bioconjugatable Water-Soluble Single-Photon Emission-Computed Tomography/Optical Imaging Bimodal Imaging Probe Based on the …
2021
A water-soluble fluorescent aza-BODIPY platform (Wazaby) was prepared and functionalized by a polyazamacrocycle agent and a bioconjugable arm. The resulting fluorescent derivative was characterized and bioconjugated onto a trastuzumab monoclonal antibody as a vector. After bioconjugation, the imaging agent appeared to be stable in serum (>72 h at 37 °C) and specifically labeled HER-2-positive breast tumors slices. The bioconjugate was radiolabeled with [111In] indium and studied in vivo. The developed monomolecular multimodal imaging probe (MOMIP) is water-soluble and chemically and photochemically stable, emits in the near infrared (NIR) region (734 nm in aqueous media), and displays a goo…
3-D image analysis of fluorescent drug binding
2004
Fluorescent ligands provide the means of studying receptors in whole tissues using confocal laser scanning microscopy and have advantages over antibody- or non-fluorescence-based method. Confocal microscopy provides large volumes of images to be measured. Histogram analysis of 3-D image volumes is proposed as a method of graphically displaying large amounts of volumetric image data to be quickly analyzed and compared. The fluorescent ligand BODIPY FL-prazosin (QAPB) was used in mouse aorta. Histogram analysis reports the amount of ligand-receptor binding under different conditions and the technique is sensitive enough to detect changes in receptor availability after antagonist incubation or…
Development of peptidomimetic boronates as proteasome inhibitors.
2013
Abstract Proteasome inhibition has emerged over the past decade as an effective therapeutic approach for the treatment of hematologic malignancies. It is a multicatalytic complex, whose proteolytic activity relies in three types of subunits: chymotrypsin-like (β5), trypsin-like (β2) and caspase-like (β1). Most important for the development of effective antitumor agents is the inhibition of the β5 subunits. In this context, the dipeptide boronate bortezomib (Velcade ® ) represents the first proteasome inhibitor approved by the FDA and the lead compound in drug discovery. This paper describes the synthesis and biological evaluation of a series of conformationally constrained pseudopeptide bor…
Near-infrared emitting fluorescent homobimetallic gold(I) complexes displaying promising in vitro and in vivo therapeutic properties
2021
International audience; Boron neutron capture therapy (BNCT) has the potential to specifically destroy tumor cells without damaging the tissues infiltrated by the tumor. BNCT is a binary treatment method based on the combination of two agents that have no effect when applied individually: 10B and thermal neutrons. Exclusively, the combination of both produces an effect, whose extent depends on the amount of 10B in the tumor but also on the organs at risk. It is not yet possible to determine the 10B concentration in a specific tissue using non-invasive methods. At present, it is only possible to measure the 10B concentration in blood and to estimate the boron concentration in tissues based o…
Il confine come luogo educativo nell'era planetaria. In dialogo con Ernesto Balducci
2016
In questo articolo viene affrontato il confine come risorsa educativa nell’era planetaria attraverso la prospettiva del nuovo umanesimo planetario proposta nel secondo Novecento da padre Ernesto Balducci. Dopo avere descritto la natura effimera e mutevole che i confini hanno assunto nell’attuale momento storico, in ragione di alcuni fenomeni che, espressione di «una globalizzazione negativa», diffondono incertezza, insicurezza, paura e negano il valore dell’alterità, viene avviato un dialogo con il pensiero di Balducci, partendo dalla critica che egli muoveva alla rimozione dell’Altro operata dall’Occidente e sostando sulla sua profezia di una cultura dialogica che avrebbe reso il confine, …
Über spezialisierte Verbreitungseinrichtungen anatolischer Galieae
1971
Summary Some annual species of the Rubiaceae native in Anatolia are specialized in their methods of seed dispersal. Contrary to other members of the genus, the frucitficence of Cruriata articulata with its persisting bracts falls to pieces which act as ‘surface:rollers’ transported by the wind. Valantia hispida and Callipeltis cucullaria are heterodissmeniate. Some of the mericarps arc dispersed by different agents, the other ones stay attached to the plant, showing a form of atelechory, a common phenomenon in arid regions. Other aberrant forms of dissemination are studied.
Mildronate treatment improves functional recovery following middle cerebral artery occlusion in rats
2011
Mildronate (3-(2,2,2-trimethylhydrazinium) propionate) is an inhibitor of l-carnitine biosynthesis and an anti-ischemic drug. In the present study, we investigated the effects of mildronate in rats following focal cerebral ischemia. Male Wistar rats were subjected to transient occlusion of the middle cerebral artery (MCAO) for 90min, followed by the intraperitoneal administration of mildronate at doses of 100 and 200mg/kg 2h after reperfusion and then daily for an additional 14days. The beam-walking, rota-rod and cylinder tests were used to assess sensorimotor function, and vibrissae-evoked forelimb-placing and limb-placing tests examined responses to tactile and proprioceptive stimulation.…
A Neuroprotective Function for the Hematopoietic Protein Granulocyte-Macrophage Colony Stimulating Factor (GM-CSF)
2007
Granulocyte-macrophage colony-stimulating factor (GM-CSF) is a hematopoietic cytokine responsible for the proliferation, differentiation, and maturation of cells of the myeloid lineage, which was cloned more than 20 years ago. Here we uncovered a novel function of GM-CSF in the central nervous system (CNS). We identified the GM-CSF α-receptor as an upregulated gene in a screen for ischemia-induced genes in the cortex. This receptor is broadly expressed on neurons throughout the brain together with its ligand and induced by ischemic insults. In primary cortical neurons and human neuroblastoma cells, GM-CSF counteracts programmed cell death and induces BCL-2 and BCL-Xl expression in a dose- a…
Strengths and Weaknesses of Cancer Pain Management in Italy: Findings from a Nationwide SIAARTI Survey
2022
Objectives: Despite guidelines, a large percentage of cancer patients continue to suffer from ineffectively treated pain. The authors undertook this survey to assess the strengths and weaknesses of cancer pain management in Italy. Design: This was a prospectively administered survey. Participants: The participants were anesthesiologists of the Italian Society of Anesthesia, Analgesia, Resuscitation and Intensive Care (SIAARTI). Intervention: A 58-item questionnaire covered the demographics and features of cancer pain management in the Italian context. Results: The authors received responses from 611 pain therapists of 279 centers. Only 22% of physicians are exclusively pain therapists. Seve…
Social Bricolage as the Path to Social Entrepreneurship
2021
In the present chapter, the concept of social bricolage is applied to the particular case of Dr. Mateo. A contextualization of her environment is exposed, for the reader to understand the intrinsic and extrinsic motivators explained in Part I. These influences represent the starting point of her professional career. Dr. Mateo’s interests have always been placed in advancing local solutions for local problems. In Pilar’s case, the phenomenon of entrepreneurship began as an act of seeking economic solvency and survival through her ingenuity, creativity, and innovation. Similarly, the phenomenon of causation-related bricolage predominates, in which the process of incessant experimentation fost…