A5015525523- Click Chemistry and Applications
- Trypanosoma species research and implications
- Chemical Synthesis and Analysis
- Carbohydrate Chemistry and Synthesis
- Advanced Cellulose Research Studies
- Monoclonal and Polyclonal Antibodies Research
- Glycosylation and Glycoproteins Research
- Synthesis and biological activity
- Cholinesterase and Neurodegenerative Diseases
- Computational Drug Discovery Methods
- Research on Leishmaniasis Studies
- Synthesis and Biological Evaluation
- Enzyme Production and Characterization
- Microbial Metabolites in Food Biotechnology
- Advanced Materials and Mechanics
- Chemical synthesis and alkaloids
- Cancer-related gene regulation
- Quinazolinone synthesis and applications
- Biochemical and Molecular Research
- Psychedelics and Drug Studies
- Enzyme function and inhibition
- Toxin Mechanisms and Immunotoxins
- Plant-derived Lignans Synthesis and Bioactivity
- Biochemical Acid Research Studies
- Peptidase Inhibition and Analysis
Universidade Federal do Rio Grande do Sul
2024
University of Manchester
2020-2024
Universidade de São Paulo
1991-2021
Norwich Research Park
2011-2021
John Innes Centre
2011-2021
University of Cambridge
2014-2019
Universidade de Ribeirão Preto
2017
SUPERA Park of Innovation and Technology of Ribeirão Preto
2010-2011
University of Dundee
2011
Wellcome Trust
2011
A divergent synthetic strategy for generating helical p53 peptides bearing functionalised staple linkages, allowing efficient optimisation of cellular activity.
Trypanosoma cruzi trans-sialidase (TcTS) plays a key role in the recognition and invasion of host cells enabling parasite to escape human immune response. To explore this potential drug target, we have synthesized small library substrate analogues based on 1,4-disubstituted 1,2,3-triazole derivatives galactose modified at either C-1 or C-6 positions. This was achieved by coupling appropriate azido-sugars with panel 23 structurally diverse terminal alkynes using copper(I)-catalyzed...
Abstract Peptide stapling is a method for designing macrocyclic alpha‐helical inhibitors of protein–protein interactions. However, obtaining cell‐active inhibitor can require significant optimization. We report novel technique based on double strain‐promoted azide–alkyne reaction, and exploit its biocompatibility to accelerate the discovery stapled peptides. As proof concept, MDM2‐binding peptides were in parallel, directly cell culture medium 96‐well plates, simultaneously evaluated p53...
Evaluating the influence of staple position, azido amino acid side-chain length and point mutation on activity ‘double-click’ stapled p53 peptides.
Abstract We investigated linear aliphatic dialkynes as a new structural class of i , +7 linkers for the double‐click stapling p53‐based peptides. The optimal combination azido amino acids and dialkynyl linker length MDM2 binding was determined. In direct comparison between aromatic staple scaffolds, staples resulted in superior to vitro p53‐activating capability cells when using diazidopeptide derived from phage display. This work demonstrates that nature scaffold is an important factor can...
Stapled peptides have great potential as modulators of protein–protein interactions (PPIs). However, there is a vast landscape chemical features that can be varied for any given peptide, and identifying set maximizes cellular uptake subsequent target engagement remains key challenge. Herein, we present systematic analysis staple functionality on the peptide bioactivity in assays. Through application "toolbox" diversified dialkynyl linkers to stapling MDM2-binding via double-click approach,...
Understanding the fine details of self-assembly building blocks into complex hierarchical structures represents a major challenge en route to design and preparation soft-matter materials with specific properties. Enzymatically synthesised cellodextrins are known have limited water solubility beyond DP9, point at which they self-assemble particles resembling antiparallel cellulose II crystalline packing. We prepared characterised series site-selectively fluorinated different degrees...
An overview of sialic acid involvement in infection and exploitation diagnostics therapeutics.
Abstract The aim of this work is to present a simple, practical and efficient protocol for drug design, in particular Diabetes, which includes selection the illness, good choice target as well bioactive ligand then usage various computer aided design medicinal chemistry tools novel potential candidates different diseases. We have selected validated dipeptidyl peptidase IV (DPP-IV), whose inhibition contributes reduce glucose levels type 2 diabetes patients. most active inhibitor with complex...
Abstract Peptide stapling is a method for designing macrocyclic alpha‐helical inhibitors of protein–protein interactions. However, obtaining cell‐active inhibitor can require significant optimization. We report novel technique based on double strain‐promoted azide–alkyne reaction, and exploit its biocompatibility to accelerate the discovery stapled peptides. As proof concept, MDM2‐binding peptides were in parallel, directly cell culture medium 96‐well plates, simultaneously evaluated p53...
Chagas, or American trypanosomiasis, remains an important public health problem in developing countries. In the last decade,
Aim: Glioblastoma multiforme (GBM) is an aggressive cancer with very limited clinical therapies. Herein, we have designed novel mercaptobenzimidazole derivatives (1–7) as multitarget antineoplastic drugs and assessed their antiproliferative profiles on experimental model for GBM, the C6 glioma line. Results: The target compounds were synthesized in few steps reasonable yields (33–90%). Compounds 1 (∼18 μM) 4 (∼20 showed dose-dependent effects significantly increased early apoptosis, but only...
Cotton ovule
Abstract The enzymatic synthesis of oligosaccharides depends on the availability suitable enzymes, which remains a limitation. Without recourse to enzyme engineering or evolution approaches, herein we demonstrate ability wild‐type cellodextrin phosphorylase (CDP: β‐1,4‐glucan linkage‐dependent) and laminaridextrin (Pro_7066: β‐1,3‐glucan tolerate number sugar‐1‐ phosphate substrates, albeit with reduced kinetic efficiency. In spite catalytic efficiencies <1 % natural reactions, utility...
The only drugs approved for the treatment of Chagas disease, nifurtimox and benznidazole, present toxic side effects limited efficacy in chronic stage which highlight need new drugs. Amongst different molecular drug targets discovered parasite, Trypanosoma cruzi trans-sialidase (TcTS) has been considered crucial recognition invasion host cells. Hence, we report efficient synthesis biological evaluation (TcTS inhibition antitrypanosomal activities) some galactose-containing...