Filters
total: 1402
-
Catalog
displaying 1000 best results Help
Search results for: EPIGENETIC DRUGS
-
The phenomenology, socio-demographic, and clinical profile of substance abusers admitted to drug de-addiction unit at eradah and mental health hospital, taif, Saudi Arabia
Publication -
Drug affinity to human serum albumin prediction by retention of cetyltrimethylammonium bromide pseudostationary phase in micellar electrokinetic chromatography and chemically advanced template search descriptors
Publication -
Systemy ekspresyjne białek cytochromu P450 w badaniach in vitro metabolizmu leków = Expression systems of cytochrome P450 proteins in studies of drug metabolism in vitro
PublicationBiałka cytochromu P450 to najważniejsze enzymy biorące udział w metabolizmie większości stosowanych w klinice leków, odpowiedzialne za ich aktywację lub detoksykację. Niektóre z dróg metabolizmu leku mogą być jednak odpowiedzialne za jego podwyższoną toksyczność. Nowe systemy ekspresyjne białek cytochromu P450 w komórkach ssaków, w tym człowieka, projektowane są w celu poznania roli metabolizmu w mechanizmie działania potencjalnych,...
-
The Effect of Millisecond Pulsed Electric Fields (msPEF) on Intracellular Drug Transport with Negatively Charged Large Nanocarriers Made of Solid Lipid Nanoparticles (SLN): In Vitro Study
Publication -
Successive cytotoxicity control by evolutionary surface decorated electronic push-pull green ZnCr-LDH nanostructures: Drug delivery enlargement for targeted breast cancer chemotherapy
PublicationThe reason for the increasing bioavailability and biocompatibility of the porous nanomaterials in the presence of different (bio)molecules is still unknown. The role of difference functional groups and their interactions with the potential bioavailability and biocompatibility is of great importance. To investigate the potential contribution of the electronic effects (especially on the surface of the porous nanomaterials) on their...
-
Development of novel (BiO)2OHCl/BiOBr enriched with boron doped-carbon nanowalls for photocatalytic cytostatic drug degradation: Assessing photocatalytic process utilization in environmental condition
PublicationIn this work, a series of novel (BiO)2OHCl/BiOBr-x%B:DGNW (x = 0%, 1%, 1.5%, 2%) composites with different content of boron-doped diamond/graphene nanowalls (B:DGNW) were fabricated by simple solvothermal synthesis. A boron-doped diamond/graphene nanowalls (B:DGNW) were prepared by CVD method. A series of analyses: XRD, XPS, SEM, and TEM showed that the photocatalyst (BiO)2OHCl/BiOBr-x%B:DGNW with a “flower-like” morphology was...
-
Analytical procedures for determination of cocaine and its metabolites in biological samples
PublicationThe dangerous effects and increased usage of illicit drugs have inspired the development of analytical methodologies. We based our review of analytical procedures for determination of cocaine (COC) and its metabolites on literature from the past two decades. Our main aim was to compare the capabilities of different analytical techniques. The diversity of matrices from which COC is determined (e.g., blood, hair, saliva, plasma,...
-
World Research Journal of Computer-Aided Drug Design
Journals -
Recent Patents on Endocrine Metabolic & Immune Drug Discovery
Journals -
Javed Ather Siddiqui DR.
PeopleI AM PSYCHATRIST,WANTS TO BRING SMILE ON THE FACES OF MENTALLY ILL PATIENTS. I LOVE MY PROFESSION AND WANT TO FACE CHALLENGES FOR SAKE OF THE PATIENTS. I EARNED POST GRADUATE DEGREE FROM MUMBAI UNIVERSITY AT G S SRTH MEDICAL COLLEGE AND KEM HOSPITAL, MUMBAI, INDIA. I HAVE OVER 20 YEARS OF MENTAL HEALTH EXPERIENCE. I HAVE WORKED IN VARIETY OF CLINICAL SETTINGS THAT HAVE INCLUDED DRUG DEADDICTION, CHILD, ADOLESCENT, GERIATRIC AND...
-
Stable nanoconjugates of transferrin with alloyed quaternary nanocrystals Ag–In–Zn–S as a biological entity for tumor recognition
PublicationOne way to limit the negative effects of anti-tumor drugs on healthy cells is targeted therapy employing functionalized drug carriers. Here we present a biocompatible and stable nanoconjugate of transferrin anchored to Ag-In-Zn-S quantum dots modified with 11-mercaptoundecanoic acid (Tf-QD) as a drug carrier versus typical anticancer drug, doxorubicin. Detailed investigations of Tf-QD nanoconjugates without and with doxorubicin...
-
Krzysztof Gierłowski dr inż.
PeopleKrzysztof Gierłowski received his Ph.D. degree in telecommunications from the Faculty of Electronics, Gdańsk University of Technology (GUT), Poland, in 2018. He is author or co-author of more than 80 scientific papers and reviewer for a number of conferences and journals. Krzysztof Gierłowski took part in major IT-oriented projects, including: EU-funded Polish Future Internet Engineering initiative, PL-LAB2020 Infrastructural...
-
Increased cytotoxicity of an unusual DNA topoisomerase II inhibitor compound C-1305 toward HeLa cells with downregulated PARP-1 activity results from re-activation of the p53 pathway and modulation of mitotic checkpoints
PublicationOur previous studies have shown that murine fibroblast cells, in which PARP-1 gene was inactivated by gene disruption, are extremely sensitive to triazoloacridone compound C-1305, an inhibitor of DNA topoisomerase II with unusual properties. Here, we show that pharmacological inhibition of PARP-1 activity by its inhibitor compound NU1025, sensitizes human cervical carcinoma HeLa cells to compound C-1305 compared to treatment with...
-
Genome-Wide DNA Methylation and Gene Expression in Patients with Indolent Systemic Mastocytosis
PublicationMastocytosis is a clinically heterogenous, usually acquired disease of the mast cells with a survival time that depends on the time of onset. It ranges from skin-limited to systemic disease, including indolent and more aggressive variants. The presence of the oncogenic KIT p. D816V gene somatic mutation is a crucial element in the pathogenesis. However, further epigenetic regulation may also affect the expression of genes that...
-
Predicting Value of Binding Constants of Organic Ligands to Beta-Cyclodextrin: Application of MARSplines and Descriptors Encoded in SMILES String
PublicationThe quantitative structure–activity relationship (QSPR) model was formulated to quantify values of the binding constant (lnK) of a series of ligands to beta–cyclodextrin (β-CD). For this purpose, the multivariate adaptive regression splines (MARSplines) methodology was adopted with molecular descriptors derived from the simplified molecular input line entry specification (SMILES) strings. This approach allows discovery of regression...
-
Anna Toruńska-Sitarz
PeopleAnna Toruńska-Sitarz, Msc in Oceanography, PhD in Earth Sciences. She is a cyanobacteriologist and academic teacher, working in the Division of Marine Biotechnology, University of Gdańsk. Her main scientific interests concern antibacterial compounds from marine organisms, regulation of cyanometabolites production in cyanobacteria and cyanobacterial molecular diversity. Further information
-
Jacek Oskarbski dr hab. inż.
PeopleAssociate professor (D.SC.Eng.) in the Department of Civil Engineering at the Gdansk University of Technology. Main research areas are traffic modeling and forecasting, transport planning, intelligent transport systems, traffic engineering, and mobility management. A graduate of the University (1994). He worked as road planner in BPBK and Transprojekt Gdański Office (1993-1996). Pposition of assistant in the Highway Engineering...
-
Occurrence and seasonal variations of 25 pharmaceutical residues in wastewater and drinking water treatment plants
PublicationThousands of tons of pharmaceuticals are introduced into the aqueous environment due to their incomplete elimination during treatment process in wastewater treatment plants (WWTPs) and water treat- ment plants (WTPs). The presence of pharmacologically active compounds in the environment is of a great interest because of their potential to cause negative effects. Furthermore, drugs can undergo different pro- cesses leading to the...
-
Thermodynamics aspects of interactions between acridine derivatives and DNA
PublicationDNA is a molecular target for many anticancer and antiviral drugs. Therefore, a clear understanding of the interaction of small molecules with DNA is important in the rational design of ligands that can bind to DNA with high affinity and selectivity. There are several methods to investigate interactions between drug and DNA. Some of them measure changing into DNA structures, such as lengthening and untwisting of helix of DNA. Other...
-
Low frequency of itraconazole resistance found among avian Aspergillus fumigatus isolates
PublicationAspergillus fumigatus is the most frequent etiological factor of invasive aspergillosis in human as well as animals, including birds. Aspergillosis caused by drug-resistant strains poses a significant therapeutic issue, especially if resistance pattern includes insensitivity to triazoles, i.e. drugs recommended for the primary therapy purposes. Majority of resistant isolates hold the TR34/L98H...
-
RNS reverse high-speed converter with quasi-regular structure based on the Chinese Remainder Theorem
PublicationPrzedstawiono dwie nowe architektury szybkiego konwertera z systemuresztowego do systemu binarnego oparte o chińskie tw. o resztach. Zastosowano nowe struktury 4-operandowych sumatorów modulo 2M. Pierwsza ze struktur oparta jest o wstępne sumowanie najstarszych bitów wektorów sumy i przeniesienia na wyjściu sumatora CSA, natomiast druga o bezpośrednie wykrywanie przekroczenia 2M. Konwerter wykorzystujący drugą ze struktur charakteryzuje...
-
Electrochemical simulation of enzymatic transformations studied for the selected antitumor acridine derivatives
PublicationThe elucidation of the metabolic pathways and the biotransformation mechanisms of potential drugs is a crucial point in drug development. It allows to know the activation routes of the new biologically active compounds, especially in respect to their possible toxicity. Generally, in vivo or in vitro experiments with liver microsomes or hepatocytes are performed. However, these testing schemes are tedious, time consuming and of...
-
Detection of some volatile degradation products released during photoexposition of ranitidine in a solid state
PublicationRanitidine (RAN) is on top of the list of prescribed drugs, due to its popularity as a selective H2-receptor antagonist, which efficiently decreases the amount of acid produced in the stomach. RAN is not stable both in a solid state and in a solution, which creates manufacturing problems, requires appropriate storage conditions, and results in a short drug shelf-life. The aim of this work was to study the emission of volatile...
-
C-1311 (Symadex), a potential anti-cancer drug, intercalates into DNA between A and G moieties. NMR-derived and MD-refined stereostructure of the d(GAGGCCTC) 2 :C-1311 complex
PublicationImidazoacridinone C-1311 (Symadex®) is an antitumor agent which has been recommended for Phase II clinical trials a few years ago. Previously, it was shown experimentally that during the initial stage of its action C-1311 forms stable intercalation complexes with DNA duplexes. Herein, a NMR-derived stereostructure of d(GAGGCCTC)2:C-1311 complex was reported. The ligand was found locating itself between A and G moieties, forming...
-
Future of medicine: personalized oncology
PublicationUnderstanding genetic and epigenetic mechanisms of tumorigenesis allows identifying many vital mutations affected the formation of various malignancies. This led to the discovery of a new therapeutic approach, based on molecular mechanisms in the world of medicine, which is called personalized medicine (PM). This review aims to outline the state of the art of the personalized medicine in treatment, taking into account anti-cancer...
-
Electrochemistry/mass spectrometry (EC/MS) for fast generation and identification of novel reactive metabolites of two unsymmetrical bisacridines with anticancer activity.
PublicationThe development of a new drug requires knowledge about its metabolic fate in a living organism, regarding the comprehensive assessment of both drug therapeutic activity and toxicity profiles. Electrochemistry (EC) coupled with mass spectrometry (MS) is an efficient tool for predicting the phase I metabolism of redox-sensitive drugs. In particular, EC/MS represents a clear advantage for the generation of reactive drug transformation...
-
Joanna Wolszczak-Derlacz dr hab.
PeopleI am an Associate Professor at Gdańsk University of Technology, Faculty of Management and Economics. I gained my PhD in July 2006 for which I received the Polish Prime Ministry’s Award for the outstanding doctoral thesis. Between 2007 and 2008, I was a beneficiary of the Max Weber Fellowship at the European University Institute in Florence, Italy. I conducted part of my research at the Katholieke Universiteit Leuven, Belgium...
-
Otwarte Dni Drewna - druga edycja
e-Learning CoursesDruga Edycja Otwartych Dni Drewna na PG - tym razem ze względu na panującą sytuacje spotykamy sie online!
-
Paweł Sachadyn prof. dr hab. inż.
People -
CURRENT DRUG TARGETS
Journals -
DRUG AND ALCOHOL DEPENDENCE
Journals -
Current Drug Delivery
Journals -
Infection and Drug Resistance
Journals -
Inhibitors of glucosamine-6-phosphate synthase as potential antimicrobials or antidiabetics – synthesis and properties
PublicationGlucosamine-6-phosphate synthase (GlcN-6-P synthase) is known as a promising target for antimicrobial agents and antidiabetics. Several compounds of natural or synthetic origin have been identified as inhibitors of this enzyme. This set comprises highly selective L-glutamine, amino sugar phosphate or transition state intermediate cis-enolamine analogues. Relatively low antimicrobial activity of these inhibitors, poorly penetrating...
-
Mechanism-based inactivation of human cytochrome P450 1A2 and 3A4 isoenzymes by antitumor triazoloacridinone C-1305.
Publication5-Dimethylaminopropylamino-8-hydroxytriazoloacridinone, C-1305, is a promising antitumor therapeutic agent with high activity against several experimental tumors. It was determined to be a potent and selective inhibitor of liver microsomal and human recombinant cytochrome P450 (CYP) 1A2 and 3A4 isoenzymes. Therefore, C-1305 might modulate the effectiveness of other drugs used in multidrug therapy. The objective of this study was...
-
Investigating the disease- modifying properties of sclerotiorin in Alzheimer's therapy using acetylcholinesterase inhibition
PublicationAlzheimer's disease (AD) is a progressive neurodegenerative disorder caused due to the damage and loss of neurons in specific brain regions. It is the most common form of dementia observed in older people. The symptoms start with memory loss and gradually cause the inability to speak and do day-to-day activities. The cost of caring for those affected individuals is huge and is probably beyond most developing countries capability....
-
Ramp and chain-lift-launched lifeboats - radical concepts for evacuating cruise ships
PublicationW artykule przedstawiono dwie oryginalne koncepcje systemów ewakuacyjnych statków pasażerskich. Pierwsza z nich polega na zastosowaniu otwieranej rampy i pochylni z rolkami, na których umieszczone są w rzędzie łodzie ratunkowe, zaczepione do elementów wyciągu łańcuchowego. Druga koncepcja polega na umieszczeniu łodzi, jedna nad drugą, na wyciągu łańcuchowym. W obu systemach w trakcie ewakuacji łodzie opuszczane są grawitacyjnie...
-
Sulfonamides with hydroxyphenyl moiety: Synthesis, structure, physicochemical properties, and ability to form complexes with Rh(III) ion
PublicationSulfonamides are the first successfully synthesized antimicrobial drugs. The mechanism of sulfonamides’ antimicrobial action involves competitive inhibition of folic acid synthesis and prevention of the growth and reproduction of bacteria. Even though they have been applied in therapy for more than 75 years, sulfonamides are still the drugs of choice for the treatment of various diseases. The aim of this work was to synthesize...
-
Quantum dots conjugates with unsymmetrical bisacridines enhance cytotoxicity of these antitumor compounds in lung cancer cells and have protecting effects on normal cells
PublicationBackground: In recent years, with the rapid development of nanotechnology and its extensive applications in the medicine, nanocarriers for anticancer drug delivery have gained a great importance. Spherical semiconductor nanocrystals, frequently called quantum dots (QDs) are very attractive nanomaterials for bioimaging applications and they possess properties as potential candidates for drug carrier. Unsymmetrical bisacridines (UAs),...
-
Nanoparticles: Taking a Unique Position in Medicine
PublicationThe human nature of curiosity, wonder, and ingenuity date back to the age of humankind. In parallel with our history of civilization, interest in scientific approaches to unravel mechanisms underlying natural phenomena has been developing. Recent years have witnessed unprecedented growth in research in the area of pharmaceuticals and medicine. The optimism that nanotechnology (NT) applied to medicine and drugs is taking serious...
-
Antifungal Activity of Capridine β as a Consequence of Its Biotransformation into Metabolite Affecting Yeast Topoisomerase II Activity
PublicationIn the last few years,increasing importance is attached to problems caused by fungal pathogens. Current methods of preventing fungal infections remain unsatisfactory. There are several antifungal compounds whichare highly effective in some cases, however, they have limitations in usage: Nephrotoxicity and other adverse effects. In addition, the frequent use of available fungistatic drugs promotes drug resistance....
-
Electrochemistry meets enzymes: Investigation of the biotransformation pathway of C-1311 based on electrochemical simulation in comparison to in vitro methods.
PublicationThe knowledge of the metabolic pathways and the biotransformation of new drugs is one of the major challenges in pharmaceutical research. It is crucial for elucidation of degradation routes of the new biologically active compounds, especially in the area of possible toxicity. Conventional in vitro drug metabolism studies are based on incubating drug candidate with e.g. hepatocytes or, most importantly, liver cell microsomes and...
-
Detailed results of shaping personnel risk factors in enterprise A
Open Research DataThe data presents the shape of all the researched personnel risk factors in the A enterprise (which was tested by the author). Further considerations should be started with the presentation of the synthesis of the obtained results, which is presented in this research data.
-
Results of modeling of pharmaceuticals mixtures toxicity with deviation ratio and best-fit functions models using Saccharomyces cerevisiae yeast as model organism
Open Research DataThe research was concerned with verifying the impact of binary mixtures of nine pharmaceuticals against a selected organism, i.e., the yeast Saccharomyces cerevisiae. S cerevisiae is used as a model organism in the monitoring of endocrine disruptors in environmental and reference samples in Xenometrix® systems - XenoScreen®. Tested pharmaceuticals,...
-
Problem of aggregation in dye-DNA interaction, calorimetry studies
PublicationNucleic acids are the biological target for many antimicrobial, antitumor and antiviral drugs. Ligand-DNA interactions can be classified into two major categories: 1. covalent binding, which can provide to intermolecular adducts, 2. physico-chemical interactions, which can be divided into intercalation (e.g. adriamycin) or groove binding (e.g. dystamycin). There are several methods to investigate interactions between drug and DNA....
-
Results of pharmaceuticals mixtures toxicity on inhibition of bioluminescence of Vibrio fischeri (Microtox)
Open Research DataThe research was concerned with verifying the impact of mixtures of nine pharmaceuticals against a selected organism, i.e., the bacterium Aliivibrio fischeri. A. fisheri is used as a model organism in the monitoring of acute toxicity in environmental and reference samples in Microtox® systems. Tested pharmaceuticals, namely: diclofenac (sodium salt),...
-
Modulation of UDP-glucuronidation by acridinone antitumor agents C-1305 and C-1311 in HepG2 and HT29 cell lines, despite slight impact in noncellular systems.
PublicationBackground Among the studied antitumor acridinone derivatives developed in our laboratory, 5-dimethylaminopropylamino-8-hydroxytriazoloacridinone (C-1305) and 5-diethylaminoethylamino-8-hydroxyimidazoacridinone (C-1311) exhibited cytotoxic and antitumor properties against several cancer types and were selected to be evaluated in preclinical and early-phase clinical trials. In the present work, we investigated the impact of C-1305...
-
Fluconazole resistant Candida auris clinical isolates have increased levels of cell wall chitin and increased susceptibility to a glucosamine-6-phosphate synthase inhibitor
PublicationIn 2009 Candida auris was first isolated as fungal pathogen of human disease from ear canal of a patient in Japan. In less than a decade, this pathogen has rapidly spread around the world and has now become a major health challenge that is of particular concern because many strains are resistant to multiple class of antifungal drugs. The lack of available antifungals and rapid increase of this fungal pathogen provides an incentive...
-
The effect of anthraquinone derivatives (C1-C9) on telomerase activity
Open Research DataThe data set contains images of the PCR products obtained from the Telomerase Repeated Amplification Protocol (TRAP). The effect of anthraquinone derivatives (C-C9) on telomerase activity was analyzed using lysates from drug-treatedcancer cell line.
-
Alcoholism and Drug Addiction
Journals