A5037306135- Antibiotic Resistance in Bacteria
- Cancer therapeutics and mechanisms
- Single-cell and spatial transcriptomics
- Biochemical and Molecular Research
- Antibiotics Pharmacokinetics and Efficacy
- Pancreatic function and diabetes
- Cell Image Analysis Techniques
- Diabetes and associated disorders
- Synthesis and pharmacology of benzodiazepine derivatives
- Diabetes Management and Research
- Research on Leishmaniasis Studies
- Antimicrobial Resistance in Staphylococcus
- Cytokine Signaling Pathways and Interactions
- Tuberculosis Research and Epidemiology
- Antimicrobial Peptides and Activities
- Enzyme Structure and Function
- Bacteriophages and microbial interactions
- Drug Transport and Resistance Mechanisms
- Chemical Synthesis and Analysis
- Natural Antidiabetic Agents Studies
- Microbial Natural Products and Biosynthesis
- Fuel Cells and Related Materials
- RNA and protein synthesis mechanisms
- Bioactive Compounds and Antitumor Agents
- Computational Drug Discovery Methods
King's College London
2016-2024
The Francis Crick Institute
2024
Guy's Hospital
2024
Public Health England
2021
Shahid Beheshti University of Medical Sciences
2013-2017
Coventry (United Kingdom)
2016
University of Warwick
2014-2016
Agricultural Biotechnology Research Institute of Iran
2016
Agricultural Research & Education Organization
2016
University of Tehran
1998-2013
Bioactivity-guided fractionation of the ethyl acetate extract obtained from culture endophytic fungus Fusarium solani resulted in isolation one new naphthoquinone, 9-desmethylherbarine (1), and two azaanthraquinone derivatives, 7-desmethylscorpinone (2) 7-desmethyl-6-methylbostrycoidin (3), along with four known compounds. Their structures were elucidated by spectral analysis, as well a direct comparison data those Azaanthraquinones 2 3 showed cytotoxic activity against human tumor cell...
A new class of nontoxic triaryl benzimidazole compounds, derived from existing classes DNA minor groove binders, were designed, synthesized, and evaluated for their antibacterial activity against multidrug resistant (MDR) Gram-positive Gram-negative species. Molecular modeling experiments suggest that the newly synthesized cannot be accommodated within due to a change in shape molecules. Compounds 8, 13, 14 found most active series, with MICs range 0.5–4 μg/mL MDR Staphylococci Enterococci...
Abstract Invasive Candida infections in hospitalized and immunocompromised or critically ill patients have become an important cause of morbidity mortality. There are increasing reports multidrug resistance several species that Candidemia, including C . glabrata C. auris , with limited numbers antifungal agents available to treat invasive infections. Therefore, there is urgent need discover new work against multidrug‐resistant species, particularly which has been identified as emerging...
Increased oxidative stress is a widely accepted factor in the development and progression of diabetes its complications. In this study, we evaluated antioxidative potential Teucrium polium (Family Lamiaceae) aqueous extract for protecting rat pancreatic tissue against streptozotocin (STZ)-induced stress. Diabetes was induced rats by intraperitoneal injections at single dose STZ 40 mg/kg. The crude (equivalent to 0.5 g plant powder/kg body weight) administered orally (intragastrically) group...
Abstract Proteus mirabilis forms extensive crystalline biofilms on indwelling urethral catheters that block urine flow and lead to serious clinical complications. The Bcr/CflA efflux system has previously been identified as important for development of P. biofilms, highlighting the potential pump inhibitors (EPIs) control catheter blockage. Here we evaluate drugs already used in human medicine (fluoxetine thioridazine) act EPIs , biofilm formation. Both fluoxetine thioridazine inhibited...
Abstract The multidrug resistant (MDR) opportunistic pathogen Klebsiella pneumoniae has previously been shown to adapt chlorhexidine by increasing expression of the MFS efflux pump smvA . Here we show that loss regulator SmvR, through adaptation chlorhexidine, results in increased resistance a number cationic biocides K. and other members Enterobacteriaceae. Clinical Enterobacteriaceae isolates which lack smvR also have an susceptibility chlorhexidine. When from Salmonella are expressed...
Abstract Multidrug efflux pumps confer resistance to their bacterial hosts by pumping out a diverse range of compounds, including most antibiotics. Being more familiar with the details functional dynamics and conformations these types could help in discovering approaches stop them functioning properly. Computational approaches, particularly conventional molecular simulations followed post simulation analysis, are powerful methods that researchers opening new window study phenomena not...
Phenylalanine-arginine β-naphthylamide (PAβN) is a broad-spectrum efflux pump inhibitor that has shown to potentiate the activity of antibiotics in Gram-negative bacteria. AdeB part AdeABC tripartite plays pivotal role conferring efflux-mediated resistance Acinetobacter baumannii. To understand molecular mechanism inhibition by PAβN, we investigated interaction PAβN with using different computational methods. We observed does not have specific binding interactions proximal site and interacts...
Antimicrobial resistance has become a major global concern. Development of novel antimicrobial agents for the treatment infections caused by multidrug resistant (MDR) pathogens is an urgent priority. Pyrrolobenzodiazepines (PBDs) are promising class antibacterial initially discovered and isolated from natural sources. Recently, C8-linked PBD biaryl conjugates have been shown to be active against some MDR Gram-positive strains. To explore role building block orientations on activity obtain...
Two new cis-clerodane-type furanoditerpenes, crispenes F and G (1 2), together with seven known compounds, were isolated from the stems of Tinospora crispa. Crispenes 2) inhibited STAT3 dimerization in a cell-free fluorescent polarization assay found to have significant cytotoxicity against STAT3-dependent MDA-MB 231 breast cancer cell line, while being inactive STAT3-null A4 line. These two compounds share structural similarities previously reported inhibitor, crispene E, same plant....
The systematic shortening of the noncovalent element a C8-linked pyrrolobenzodiazepine (PBD) conjugate (13) led to synthesis 19-member library C8-PBD monomers. critical elements 13, which were required render molecule cytotoxic, elucidated by an annexin V assay. effects on transcription factor inhibitory capacity also explored through enzyme-linked immunosorbent assay-based measurement nuclear NF-κB upon exposure JJN-3 cells synthesized molecules. Although interactive 13 had less than...
Combination of four well-established techniques complemented with temperature dependence for probing structural changes and detecting differences between insulin samples.
It is urgent to find new antibiotic classes with activity against multidrug-resistant (MDR) Gram-negative pathogens as the pipeline of antibiotics essentially empty. Modified pyrrolobenzodiazepines a C8-linked aliphatic heterocycle provide class broad-spectrum antibacterial agents MDR bacteria, including WHO priority pathogens. The structure–activity relationship established that third ring was particularly important for activity. Minimum inhibitory concentrations lead compounds ranged from...
Antimicrobial resistance and lack of new antibiotics to treat multidrug-resistant (MDR) bacteria is a significant public health problem. There discovery void the pipeline classes in clinical development almost empty. Therefore, it important understand structure activity relationships (SAR) current chemical as that can help drug community their efforts develop by modifying existing antibiotic classes. We studied SAR C5-acylaminomethyl moiety linezolid, an oxazolidinone antibiotic,...
The aim of the study was to use in silico and vitro techniques evaluate whether a triple formulation antiretroviral drugs (tenofovir, darunavir, dapivirine) interacted with P-glycoprotein (P-gp) or exhibited any other permeability-altering drug-drug interactions colorectal mucosa. Potential drug P-gp were screened initially using molecular docking, followed by dynamics simulations analyze identified drug-transporter interaction more mechanistically. transport tenofovir, dapivirine...