Search results for "anticancer"
showing 10 items of 171 documents
Characteristics of advanced cancer patients who were readmitted to an acute palliative/supportive care unit
2017
Objectives: The aim of this study was to assess the characteristics of patients readmitted to an acute supportive/palliative care unit (ASPCU), the reasons for readmission, and the outcome after receiving specialistic assessment and treatment. Methods: A consecutive sample of patients was assessed for a period of 10Â months. Epidemiological characteristics, including age, gender, Karnofsky level, diagnosis, caregivers, education, disease awareness, kind of admission, and anticancer treatment in the previous 30Â days, were recorded, as well as hospital stay, death, and discharge at home. The principal reasons for admission were recorded. Symptom intensity and opioid doses, expressed as oral …
Selective targeting of PARP-1 zinc finger recognition domains with Au(III) organometallics
2018
The binding of Au(iii) complexes to the zinc finger domain of the anticancer drug target PARP-1 was studied using a hyphenated mass spectrometry approach combined with quantum mechanics/molecular mechanics (QM/MM) studies. Competition experiments were carried out, whereby each Au complex was exposed to two types of zinc fingers. Notably, the cyclometallated Au-C^N complex was identified as the most selective candidate to disrupt the PARP-1 zinc finger domain, forming distinct adducts compared to the coordination compound Auphen.
Ultralow-intensity near-infrared light induces drug delivery by upconverting nanoparticles
2014
Mesoporous silica coated upconverting nanoparticles are loaded with the anticancer drug doxorubicin and grafted with ruthenium complexes as photoactive molecular valves. Drug release was triggered by 974 nm light with 0.35 W cm(-2). Such low light intensity minimized overheating problems and prevented photodamage to biological samples.
Fluorescence spectroscopy for estimation of anticancer drug sonodestruction in vitro
2013
The effect of ultrasound exposure on bleomycin fluorescence and pharmacological properties is studied. Bleomycin was treated by ultrasound for 7 min. Bleomycin fluorescence was measured during ultrasound exposure by means of fiber-optic spectrometry. Cell colony test was used to evaluate blemycin cytotoxity before and after ultrasound exposure.
Metal drugs and the anticancer immune response
2018
The immune system deploys a multitude of innate and adaptive mechanisms not only to ward off pathogens but also to prevent malignant transformation ("immune surveillance"). Hence, a clinically apparent tumor already reflects selection for those malignant cell clones capable of evading immune recognition ("immune evasion"). Metal drugs, besides their well-investigated cytotoxic anticancer effects, massively interact with the cancer-immune interface and can reverse important aspects of immune evasion. This topic has recently gained intense attention based on combination approaches with anticancer immunotherapy (e.g., immune checkpoint inhibitors), a strategy recently delivering first exciting…
Multinuclear Cytotoxic Metallodrugs: Physicochemical Characterization and Biological Properties of Novel Heteronuclear Gold-Titanium Complexes
2011
An unprecedented series of titanocene-gold bi- and trimetallic complexes of the general formula [[(η(5)-C(5)H(5))(μ-η(5):κ(1)-C(5)H(4)(CH(2))(n)PPh(2))TiCl(2)](m)AuCl(x)](q+) (n = 0, 2, or 4; m = 1, x = 1, q = 0 or m = 2, x = 0, q = 1) have been prepared and characterized spectroscopically. The luminescence spectroscopy and photophysics of one of the compounds, [[(η(5)-C(5)H(5))(μ-η(5):κ(1)-C(5)H(4)PPh(2))TiCl(2)](2)Au]PF(6), have been investigated in 2MeTHF solution and in the solid state at 77 and 298 K. Evidence for interfragment interactions based on the comparison of electronic band positions and emission lifetimes, namely, triplet energy transfer (ET) from the Au- to the Ti-containing…
On the Mechanism of Gold/NHC Compounds Binding to DNA G-Quadruplexes: Combined Metadynamics and Biophysical Methods
2018
The binding modes and free-energy landscape of two AuI /N-heterocyclic carbene complexes interacting with G-quadruplexes, namely a human telomeric (hTelo) and a promoter sequence (C-KIT1), are studied here for the first time by metadynamics. The theoretical results are validated by FRET DNA melting assays and provide an accurate estimate of the absolute gold complex/DNA binding free energy. This advanced in silico approach is valuable to achieve rational drug design of selective G4 binders.
Identification of 2-(thiophen-2-yl)acetic Acid-Based Lead Compound for mPGES-1 Inhibition.
2021
We report the implementation of our in silico/synthesis pipeline by targeting the glutathione-dependent enzyme mPGES-1, a valuable macromolecular target in both cancer therapy and inflammation therapy. Specifically, by using a virtual fragment screening approach of aromatic bromides, straightforwardly modifiable by the Suzuki-Miyaura reaction, we identified 3-phenylpropanoic acid and 2-(thiophen-2-yl)acetic acid to be suitable chemical platforms to develop tighter mPGES-1 inhibitors. Among these, compounds 1c and 2c showed selective inhibitory activity against mPGES-1 in the low micromolar range in accordance with molecular modeling calculations. Moreover, 1c and 2c exhibited interesting IC…
Conjugados poliméricos y su utilización como nanomedicinas anticancerígenas
2009
Independientemente del descubrimiento de nuevos fármacos para dianas farmacológicas bien establecidas, el compromiso de la ciencia con la sociedad demanda del desarrollo de análogos macromoleculares que mejoren las posibilidades terapéuticas de los fármacos existentes aportando una mayor actividad biológica y una mayor especificidad. Se postula, cada vez con más fuerza, que la aplicación de la nanotecnología a la medicina es la clave para conseguir las mejoras necesarias tanto en diagnosis como en terapia anticancerígeno [1]. Para poder distinguirlos de otros productos biotecnológicos como proteínas y anticuerpos, los nanofármacos han sido definidos como “... sistemas complejos de escala na…
Endocrine side-effects of new anticancer therapies: Overall monitoring and conclusions
2018
IF 0.795 (2017); International audience; The present final consensus statement of the French Society of Endocrinology lays out the assessments that are to be systematically performed before and during anticancer treatment by immunotherapy, tyrosine kinase inhibitors or mTOR inhibitors, even without onset of any endocrinopathy. It also discusses the CTCAE adverse event grading system in oncology and the difficulty of implementing it for endocrine side-effects of these anticancer treatments. Notably, this is why certain treatment steps applied in other side-effects (e.g., high-dose corticosteroids, contraindications to immunotherapy, etc.) need to be discussed before implementation for endocr…