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Wyniki wyszukiwania dla: MURAMYL DIPEPTIDE, MURAMYL DIPEPTIDE ANALOGS, ANTICANCER COMPOUNDS, ANTICANCER ACTIVITY, NOD2 RECEPTOR, ADJUVANT THERAPY
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Texture or Linker? Competitive Patterning of Receptor Assembly toward Ultra-Sensitive Impedimetric Detection of Viral Species at Gold-Nanotextured Titanium Surfaces
PublikacjaIn this work, we study the electrodes with a periodic matrix of gold particles pattered by titanium dimples and modified by 3-mercaptopropionic acid (MPA) followed by CD147 receptor grafting for specific impedimetric detection of SARS-CoV-2 viral spike proteins. The synergistic DFT and MM/MD modeling revealed that MPA adsorption geometries on the Au–Ti surface have preferential and stronger binding patterns through the carboxyl...
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Modification of Bacterial Cellulose with Quaternary Ammonium Compounds Based on Fatty Acids and Amino Acids and the Effect on Antimicrobial Activity
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Quantitative Structure–Activity Relationships in Two-Electron Reduction of Nitroaromatic Compounds by Enterobacter cloacae NAD(P)H:Nitroreductase
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Profile of phenolic compounds and antioxidant activity of organically and conventionally grown black-grain barley genotypes treated with biostimulant
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Olfactory receptor-based biosensors as potential future tools in medical diagnosis
PublikacjaThe detection of biomarkers is the future of non-invasive medical diagnosis and screening. Discovery and identification of reliable disease specific volatile organic compounds is dependent on repeatable, accurate analysis of trace level gaseous analytes mainly in breath samples. Natural variety of the olfactory systems and the compounds capable of gas molecules binding creates wide possibilities of acquisition and implementation...
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Tinnitus Therapy Based on High-Frequency Linearization Principles - Preliminary Results
PublikacjaThe aim of this work is to present problems related to tinnitus symptoms, its pathogenesis, hypotheses on tinnitus causes, and therapy treatment to reduce or mask the phantom noise. In addition, the hypothesis on the existence of parasitic quantization that accompanies hearing loss has been recalled. Moreover, the paper describes a study carried out by the Authors with the application of high-frequency dither having specially formed...
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Inhibiting activity of HIV-1: protease, reverse transcriptase and integrase all together by novel compounds using computational approaches (flexible and rigid docking)
PublikacjaAcquired immunodeficiency syndrome (AIDS), caused by human immunodeficiency virus type 1 (HIV-1) infection, is one of the most challenging diseases in recent decades. Nevertheless the shortcomings of chemical drugs such as toxicity, lack of curative effects, the search for more potent anti-HIV agents have been focused in our study. In current study, novel scaffold was designed having a benzyl and imidazole in it which are very...
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NUTRITIONAL AND PHARMACEUTICAL APPLICATIONS OF BIOACTIVE COMPOUNDS IN TROPICAL FRUITS
PublikacjaDuring the past two decades our international scientific group investigated in vitro the physicochemical and nutritional characteristics of some cultivars of durian at various stages of ripening, mangosteen and new cultivars of snake fruit in comparison with widely used avocado, kiwifruit and mango, and in vivo their influence on laboratory animals. The main objective of the present study was to screen and compare the properties...
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Mind, Culture, and Activity
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Physical Activity Review
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Physiotherapy and Health Activity
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Physical Activity and Health
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Polyacrylamide substrate viscosity impact on temozolomide activity in glioblastoma cells by flow cytometry and rheological measurements
Dane BadawczeDataset includes raw data on cell lines LN-229 and LN-18 treated with temozolomide measured by flow cytometry, rheometry and cell projections. It also includes calculations necessary for creation of figures and conclusions based on those figures in the publication titiled: "Substrate viscosity impairs temozolomide-mediated inhibition of glioblastoma...
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Solid Phase Synthesis and Biological Activity of Tuftsin Conjugates
PublikacjaNew tuftsin/retro-tuftsin conjugates were designed and synthesized using a classical fluorenylmethoxycarbonyl (Fmoc) solid phase procedure. All the peptide conjugates were divided into three series: 1,4-dihydroxyanthraquinone (type A), 1-nitroacridine (type B), and 4-carboxyacridone (type C) derivatives. In type A conjugates, the N-terminal group of the peptide chain is directly connected to the anthraquinone ring at C1 (Scheme...
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Tetrahydroquinolinone derivatives exert antiproliferative effect on lung cancer cells through apoptosis induction
PublikacjaThe anticancer properties of quinolones is a topic of interest among researchers in the scientific world. Because these compounds do not cause side effects, unlike the commonly used cytostatics, they are considered a promising source of new anticancer drugs. In this work, we designed a brief synthetic pathway and obtained a series of novel 8-phenyltetrahydroquinolinone derivatives functionalized with benzyl-type moieties at position...
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Bioactive Compounds in Health and Disease
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JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
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New Materials Compounds and Applications
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Interaction of antitumor triazoloacridone C-1305 and its analogs with telomeric DNA
PublikacjaBadaliśmy oddziaływanie pochodnej triazoloakrydonu C-1305 i jego bliskich analogów strukturalnych z oligonukleotydami zawierającycmi sekwencje telomerowe TTAGGG oraz oligonukleotydami sfałdowanymi w strukturę G-kwadrupleksu. Wykazaliśmy, że spośród badanych związków pochodna C-1305 wykazała największą specyficzność w stosunku do telomerowego DNA. Związek ten stabilizował także strukturę G-kwadrupleksu, podczas gdy jego analogi...
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Metallochromic crown ether analogs bearing aromatic residues and azo groupings
PublikacjaPraca zawiera przegląd syntezowanych, różnych chromogenicznych związków koronowych, zawierających oprócz dwóch grup azowych i łańcucha polieterowego fragmenty heterocykliczne. Porównano właściwości otrzymanych związków w zależności od obecności heteroatomów w pierścieniu makrocyklicznym oraz różnego podstawienia cząsteczki heterocykliczej.
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Novel approaches in the synthesis of batracylin and its analogs: rebirth of an old player?
PublikacjaW pracy opisano batracylinę (BAT), jej syntezę i aktywność biologiczną oraz otrzymane analogi. BAT została wyselekcjonowana przez NCI (Bethesda, USA) w programie poszukiwań nowych potencjalnych leków przeciwnowotworowych. Związek ten w badaniach in vivo na myszach okazał się bardzo aktywny przeciw nowotworowi okrężnicy 38 (Colon 38), trudnemu do wyleczenia przez dotychczas znane leki przeciwnowotworowe. Jest ona skuteczna również...
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Recent breakthroughs in the stability testing of pharmaceutical compounds
PublikacjaPharmaceutical development is mostly focused on the research leading to approval of a new and viable active substance. However, there is a number of old generation compounds that are still being used in contemporary medicinal practice. So that new analytical developments should cover not only the safety of newly developed drug substances, which is obvious, but should also be directed into the search of individual stability issues...
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Guidelines regarding ineffective maintenance of organ functions (futile therapy) in paediatric intensive care units
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Are the short cationic lipopeptides bacterial membrane disruptors? Structure-Activity Relationship and molecular dynamic evaluation
PublikacjaShort cationic lipopeptides are amphiphilic molecules that exhibit antimicrobial activity mainly against Grampositives. These compounds bind to bacterial membranes and disrupt their integrity. Here we examine the structure-activity relation (SAR) of lysine-based lipopeptides, with a prospect to rationally design more active compounds. The presented study aims to explain how antimicrobial activity of lipopeptides is affected by...
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Structural Factors Affecting Cytotoxic Activity of (E)-1-(Benzo[d ][1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-one Derivatives
PublikacjaDerivatives of (E)-1-(5-alkoxybenzo[d][1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-one (1) demonstrated exceptionally high in vitro cytotoxic activity, with IC50 values of the most active derivatives in the nanomolar range. To identify structural fragments necessary for the activity, several analogs deprived of selected fragments were prepared, and their cytotoxic activity was tested. It was found that the activity depends on combined effects...
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Endocrine Disrupting Compounds – Problems and Challenges
PublikacjaIn this chapter, information about some of the estrogenic compounds and their environmental fate and biological influence can be found. Special attention is paid to the review of the analytical approaches used at the stages of detection and determination of Endocrine Disrupting Compounds (EDCs) in the environmental samples. Also, a brief characterization of both cellular and non-cellular bioassays is presented. The discovery of...
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Analysis and characterization of coordination compounds by resonance Raman spectroscopy
PublikacjaResonance Raman spectroscopy has become a powerful tool to study excited-state geometries, excited-state charge distributions and photoinduced reaction dynamics in coordination compounds. Due to their rich photophysical properties coordination compounds are utilized for a variety of applications ranging from DNA sensing to photocatalysis. This review features recent applications of various resonance Raman scattering techniques...
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Inhibiting Activity of HIV-1: Protease, Reverse Transcriptase and Integrase All Together by Novel Compounds Using Computational Approaches
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The Application of Lamiaceae Lindl. Promotes Aroma Compounds Formation, Sensory Properties, and Antioxidant Activity of Oat and Buckwheat-Based Cookies
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Anti-Inflammatory Therapy of Infections
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Antihypertensive therapy and cancer risks?
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HPV16 E6 Gene Transcripts in Primary Type II Endometrial Carcinomas
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Antifungal dipeptides incorporating an inhibitor of homoserine dehydrogenase
PublikacjaThe antifungal activity of 5‐hydroxy‐4‐oxo‐L‐norvaline (HONV), exhibited under conditions mimicking human serum, may be improved upon incorporation of this amino acid into a dipeptide structure. Several HONV‐containing dipeptides inhibited growth of human pathogenic yeasts of the Candida genus in the RPMI‐1640 medium, with minimal inhibitory concentration values in the 32 to 64 μg mL−1 range. This activity was not affected by multidrug...
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Xanthone synthetic derivatives with high anticandidal activity and positive mycostatic selectivity index values
PublikacjaWith the current massive increases in drug-resistant microbial infection as well as the significant role of fungal infections in the death toll of COVID-19, discovering new antifungals is extremely important. Natural and synthetic xanthones are promising derivatives, although only few reports have demonstrated their antifungal mechanism of action in detail. Newly synthetized by us xanthone derivative 44 exhibited strong antifungal...
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918 The role of patients and doctors in making decisions about the choice of the kind of adjuvant treatment in early breast cancer
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260. The role of patients and doctors in making decisions about the choice of the kind of adjuvant treatment in early brest cancer
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Molecular docking studies towards development of novel Gly-Phe analogs for potential inhibition of Cathepsin C (dipeptidyl peptidase I).
PublikacjaCathepsin C is a cysteine protease required for activation of various pro-inflammatory serine proteases and, essentially, is of interest as a therapeutic target. Cathepsin C coordinate system was employed as a model to study the interaction of some already available inhibitors of Cathepsin C. Compounds containing Gly-Phe fragment with functional groups at its ends were designed by knowledge based approach. Using AutoDock and...
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Mutagenic and Carcinogenic Compounds in Food
PublikacjaFood is a major environmental human cancer risk factor. One of the reasons for this is that food products contain substances that exhibit mutagenic and carcinogenic potential which may induce the transformation of normal somatic cells into cancerous cells. These compounds occur in food as a result of microbial contaminations (mycotoxins produced by molds), are generated from natural food components upon processing (e.g. heterocyclic...
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Molecular Modeling of the Neurohypophyseal Receptor/Atosiban Complexes
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Estrogen receptor 2 polymorphism in idiopathic scoliosis
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Affinity of fentanyl and its derivatives for the σ1-receptor
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Synthesis and biological evaluation of novel analogues of batracylin with synthetic amino acids and adenosine: an unexpected effect on centromere segregation in tumor cells through a dual inhibition of topoisomerase IIa and Aurora B
PublikacjaIn the search for new anticancer agents we designed and synthesized batracylin derivatives with linking synthetic amino acid side chains of different lengths and adenosine. Unexpectedly, we have found that in water and the culture media adenosine–amino acid–BAT conjugates form supramolecular structures and this prevents these compounds from entering cells. Consequently, these compounds exerted no biological activity when tested...
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Artificial intelligence models in prediction of response to cardiac resynchronization therapy: a systematic review
PublikacjaThe aim of the presented review is to summarize the literature data on the accuracy and clinical applicability of artificial intelligence (AI) models as a valuable alternative to the current guidelines in predicting cardiac resynchronization therapy (CRT) response and phenotyping of patients eligible for CRT implantation. This systematic review was performed...
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Phytochemical screening and effect of Viscum album L. on monoamine oxidase A and B activity and serotonin, dopamine and serotonin receptor 5-HTR1A levels in Galleria mellonealla (Lepidoptera)
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The influence of cultivation conditions on the myrosinase activity and glucosinolate content in white cabbage
PublikacjaIn the process of biofumigation typically natural compounds present in Brassicaceae family are used to combat pests and protect crops. Glucosinolates, sulfur-containing secondary metabolites found in Brassica plants, are hydrolized by the enzyme myrosinase (β-thioglucosidase, EC 3.2.3.1) with the liberation of degradation products such as isothiocyanates, nitriles, thiocyanates and epithionitriles. Isothiocyanates are the most...
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Paweł Możejko dr hab.
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A convenient and efficient alfa-sulfenylation of carbonyl compounds
PublikacjaA method for alfa-sulfenylation of carbonyl compounds by a 5,5-dimethyl-2-thioxo-1,3,2-dioxaphosphorinane-2-disulfanyl derivatives has been developed. Readily available reagents, mild reaction conditions, and excellent yields with high selectivity makes this method quite simple, convenient and practical.
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Moving out of CF3‐Land: Synthesis, Receptor Affinity, and in silico Studies of NK1 Receptor Ligands Containing a Pentafluorosulfanyl (SF5) Group
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Numerical model of human head phantom to ensure dosimetry of dose components for boron neutron capture therapy
PublikacjaExtremely important aspects of the boron neutron capture therapy are, first of all, administering to the patient a boron compound that selectively reaches the neoplastic cells, and in the second step, the verification of the irradiation process. This paper focuses on the latter aspect, which is the detailed dosimetry of the processes occurring after the reaction of thermal neutrons with the boron-10 isotope. The results of computer...
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Antiproliferative, Antiangiogenic, and Antimetastatic Therapy Response by Mangiferin in a Syngeneic Immunocompetent Colorectal Cancer Mouse Model Involves Changes in Mitochondrial Energy Metabolism
PublikacjaIn spite of the current advances and achievements in cancer treatments, colorectal cancer (CRC) persists as one of the most prevalent and deadly tumor types in both men and women worldwide. Drug resistance, adverse side effects and high rate of angiogenesis, metastasis and tumor relapse remain one of the greatest challenges in long-term management of CRC and urges need for new leads of anticancer drugs. We demonstrate that CRC...