A5077150194- Natural product bioactivities and synthesis
- Chemical Synthesis and Analysis
- Analytical Chemistry and Chromatography
- Glycosylation and Glycoproteins Research
- Tuberculosis Research and Epidemiology
- Carbohydrate Chemistry and Synthesis
- Cancer therapeutics and mechanisms
- Antimicrobial Peptides and Activities
- Nerve injury and regeneration
- Crystallization and Solubility Studies
- Advanced Chemical Sensor Technologies
- Biochemical Analysis and Sensing Techniques
- X-ray Diffraction in Crystallography
- Biochemical and Structural Characterization
- Pancreatic function and diabetes
- Mesenchymal stem cell research
- Lung Cancer Treatments and Mutations
- Neurogenesis and neuroplasticity mechanisms
- Metabolomics and Mass Spectrometry Studies
- Pneumonia and Respiratory Infections
- Mycobacterium research and diagnosis
- Antibiotic Resistance in Bacteria
- Venomous Animal Envenomation and Studies
- Plant-based Medicinal Research
- Phytochemistry and Biological Activities
University College London
2017-2025
University of London
2022
Spider venom toxins, such as Protoxin-II (ProTx-II), have recently received much attention selective Nav1.7 channel blockers, with potential to be developed leads for the treatment of chronic nocioceptive pain. ProTx-II is a 30-amino acid peptide three disulfide bonds that has been reported adopt well-defined inhibitory cystine knot (ICK) scaffold structure. Potential drawbacks peptides include poor pharmacodynamics and scrambling in vivo. In order address these issues, present study we...
Parkinson’s disease is a neurodegenerative condition associated with the progressive loss of dopaminergic neurons. This leads to neurological impairments heightening severity and globally increasing in prevalence due to...
In response to the growing threat posed by antibiotic-resistant bacterial strains, extensive research is currently focused on developing antimicrobial agents that target lipid II, a vital precursor in biosynthesis of cell walls. The lantibiotic nisin and related peptides display unique highly selective binding II. A key feature nisin–lipid II interaction formation cage-like complex between pyrophosphate moiety two thioether-bridged rings, rings B, at N-terminus nisin. To understand important...
In this study, we have designed and synthesized pyrazoline analogues that partially mimic the structure of mycobactin, to address requirement novel therapeutics tackle emerging global challenge antimicrobial resistance (AMR). Our investigation resulted in identification lead compounds 44 49 as potential mycobactin biosynthesis inhibitors against mycobacteria. Moreover, candidates efficiently eradicated intracellularly surviving Thermofluorimetric analysis molecular dynamics simulations...
Abstract Natural products that target lipid II, such as the lantibiotic nisin, are strategically important in development of new antibacterial agents to combat rise antimicrobial resistance. Understanding structural factors govern highly selective molecular recognition II by N‐terminal region nisin(1–12), is a crucial step exploiting potential compounds. In order elucidate relationships between amino acid sequence and conformation this bicyclic peptide fragment, we have used solid‐phase...
New designs of antimicrobial peptides are urgently needed in order to combat the threat posed by recent increase resistance antibiotics. In this paper, we present a new series peptides, based on key structural features lantibiotic nisin. We have simplified structure nisin conjugating lipid II-binding motif at N-terminus cationic and peptoids with known antibacterial action pore-forming properties. Hybrid where hydrophilic PEG4 linker was used, showed good activity against Micrococcus luteus.
Identification and validation of novel therapeutic targets is imperative to tackle the rise drug resistance in tuberculosis. An essential Mur ligase-like gene (Rv3712), expected be involved cell-wall peptidoglycan (PG) biogenesis conserved across mycobacteria, including genetically depleted Mycobacterium leprae, was primary focus this study.Biochemical analysis Rv3712 performed using inorganic phosphate release assays. The operon structure identified reverse-transcriptase PCR a...
Class A serine β-lactamases (SBLs) have a conserved non-active site structural domain called the omega loop (Ω-loop), in which glutamic acid residue is believed to be directly involved hydrolysis of β-lactam antibiotics by providing water molecule during catalysis. We aimed design and characterise potential pentapeptides mask function Ω-loop reduce their efficacy, along with potentiating eventually decreasing resistance. Considering sequence as template, group pentapeptide models were...
Lipid II recognition: Analogues of the bicyclic N-terminal region lantibiotic nisin, residues 1–12, were synthesised. In order to analyse how this peptide binds its target, pyrophosphate moiety lipid II, NMR ensemble analysis wild-type and one synthetic analogues was carried out. This revealed that two rings are pre-organised an extent for binding group. A high degree flexibility exhibited in central amide bond joining enables switch between “open” structure a “cage” capable pyrophosphate....