A5025568973- Venomous Animal Envenomation and Studies
- Ion channel regulation and function
- Nicotinic Acetylcholine Receptors Study
- Healthcare and Venom Research
- Marine Invertebrate Physiology and Ecology
- Biochemical and Structural Characterization
- Cardiac electrophysiology and arrhythmias
- Marine Sponges and Natural Products
- Insect and Pesticide Research
- Neurobiology and Insect Physiology Research
- Toxin Mechanisms and Immunotoxins
- Receptor Mechanisms and Signaling
- Antimicrobial Peptides and Activities
- Phosphodiesterase function and regulation
- Marine Toxins and Detection Methods
- Phytochemical compounds biological activities
- Connexins and lens biology
- Pharmacological Effects of Natural Compounds
- Ion Transport and Channel Regulation
- Computational Drug Discovery Methods
- Cardiac Arrhythmias and Treatments
- Enzyme function and inhibition
- Calpain Protease Function and Regulation
- Chemical Synthesis and Analysis
- bioluminescence and chemiluminescence research
KU Leuven
2020-2024
Universidade de São Paulo
2014-2024
Universidade Vila Velha
2020
Universidade Estadual Paulista (Unesp)
2020
Universidade Federal de Roraima
2020
Universidade Federal de Uberlândia
2020
Universidade de Ribeirão Preto
2014-2019
SUPERA Park of Innovation and Technology of Ribeirão Preto
2019
Apamin is often cited as one of the few substances selectively acting on small-conductance Ca2+-activated potassium channels (KCa2). However, published pharmacological and structural data remain controversial. Here, we investigated molecular pharmacology apamin by two-electrode voltage-clamp in Xenopus laevis oocytes patch-clamp HEK293, COS7, CHO cells expressing studied ion channels, well isolated rat brain neurons. The microtitre broth dilution method was used for antimicrobial activity...
Abstract Snake venom serine proteases (SVSPs) are complex and multifunctional enzymes, acting primarily on hemostasis. In this work, we report the hitherto unknown inhibitory effect of a SVSP, named collinein-1, isolated from Crotalus durissus collilineatus , cancer-relevant voltage-gated potassium channel (hEAG1). Among 12 ion channels tested, collinein-1 selectively inhibited hEAG1 currents, with mechanism independent its enzymatic activity. Corroboratively, demonstrated that reduced...
The Kunitz/BPTI peptide family includes unique representatives demonstrating various biological activities. Electrophysiological screening of peptides HCRG1 and HCRG2 from the sea anemone Heteractis crispa on six Kv1.x channel isoforms insect Shaker IR expressed in Xenopus laevis oocytes revealed their potassium channels blocking activity. appear to be first Kunitz-type anemones Kv1.3 with IC50 40.7 29.7 nM, respectively. In addition, mainly vary binding affinity Kv1.2 channels. It was...
The role of insulin and insulin-like peptides (ILPs) in vertebrate animals is well studied. Numerous ILPs are also found invertebrates, although there uncertainty as to the function many these peptides. We have identified transcripts with similarity family tentacle transcriptomes sea anemone Oulactis sp. (Actiniaria: Actiniidae). translated showed that highly conserved A- B-chains among individuals this species, other Anthozoa. An ILP sequence (IlO1_i1) was synthesized using Fmoc solid-phase...
Background: The prevalent class of snake venom serine proteases (SVSP) in Viperidae venoms is the thrombin-like enzymes, which, similarly to human thrombin, convert fibrinogen into insoluble fibrin monomers. However, differ from thrombin by being unable activate factor XIII, thus leading formation loose clots and consumption. We report functional biological characterization a recombinant protease Crotalus durissus collilineatus, named rCollinein-1. Methods: Heterologous expression...
Sea anemones are a rich source of biologically active compounds. Among approximately 1100 species described so far, Heteractis crispa species, also known as sebae anemone, is native to the Indo-Pacific area. As part its venom components, Hcr 1b-2 peptide was first an ASIC1a and ASIC3 inhibitor. Using Xenopus laevis oocytes two-electrode voltage-clamp technique, in present work we describe remarkable lack selectivity this toxin. Besides acid-sensing ion channels previously described,...
The nicotinic acetylcholine receptors (nAChRs) are prototypical ligand-gated ion channels, provide cholinergic signaling, and modulated by various venom toxins drugs in addition to neurotransmitters. Here, four APETx-like toxins, including two new named Hmg 1b-2 Metox 1b-5, were isolated from the sea anemone Heteractis magnifica characterized as novel nAChR ligands acid-sensing channel (ASIC) modulators. All peptides competed with radiolabeled α-bungarotoxin for binding Torpedo californica...
The voltage-gated potassium channel KV1.3 has been recognized as a tumor marker and represents promising new target for the discovery of anticancer drugs. We designed novel structural class inhibitors through optimization benzamide-based hit compounds structure-activity relationship studies. potency selectivity were investigated using whole-cell patch- voltage-clamp experiments. 2D 3D cell models used to determine antiproliferative activity. Structural resulted in most potent selective...
Nicotine binds to nicotinic acetylcholine receptors (nAChRs) that are overexpressed in different cancer cells, promoting tumor growth and resistance chemotherapy. In this study, we aimed investigate the potential of APS7-2 APS8-2, synthetic analogs a marine sponge toxin, inhibit nicotine-mediated effects on A549 human lung cells. Our electrophysiological measurements confirmed APS8-2 act as α7 nAChR antagonists. showed no cytotoxicity while concentration-dependent The cytotoxic responses...
Abstract Background The identification of novel toxins from overlooked and taxonomically exceptional species bears potential for various pharmacological applications. remipede Xibalbanus tulumensis , an underwater cave-dwelling crustacean, is the only crustacean which a venom system has been described. Its contains several xibalbin peptides that have inhibitor cysteine knot (ICK) scaffold. Results Our screenings revealed all tested variants particularly inhibit potassium channels. Xib 1 xib...
Voltage-gated potassium channels (KVs) perform vital physiological functions and are targets in different disorders ranging from ataxia arrhythmia to autoimmune diseases. An important issue is the search for production of selective ligands these channels. Peptide toxins found scorpion venom named KTx excel both potency selectivity with respect some channel isoforms, which may present only minute differences their structure. Despite several decades research molecular determinants still poorly...
Scorpionism is responsible for most accidents involving venomous animals in Brazil, which leads to severe symptoms that can evolve death. Scorpion venoms consist of complexes cocktails, including peptides, proteins, and nonprotein compounds, making separation purification procedures extremely difficult time-consuming. toxins target different biological systems be used basic science, clinical, biotechnological applications. This study the first explore venom content unexplored scorpion...
(1) Background: G protein-coupled inward-rectifier potassium (GIRK) channels, especially neuronal GIRK1/2 have been the focus of intense research interest for developing drugs against brain diseases. In this context, venom peptides that selectively activate GIRK channels can be seen as a new source drug development. Here, we report on identification and electrophysiological characterization novel activator AsKC11, found in sea anemone Anemonia sulcata. (2) Methods: AsKC11 was purified from...
Expression of the voltage-gated potassium channel KV10.1 (Eag1) has been detected in over 70% human cancers, making a promising new target for anticancer drug discovery. A structural class inhibitors was prepared by optimisation and exploration structure–activity relationship previously published hit compound ZVS-08 (1) its optimised analogue 2. The potency selectivity between hERG were investigated using whole-cell patch-clamp experiments. We obtained two inhibitors, 17a 18b, with improved...
Coral snake venoms from the Micrurus genus are a natural library of components with multiple targets, yet poorly explored. In Brazil, 34 species currently described, and just few have been investigated for their venom activities. composed mainly phospholipases A2 three-finger toxins, which responsible neuromuscular blockade—the main envenomation outcome in humans. Beyond these two major toxin families, minor also important global activity, including Kunitz-peptides, serine proteases, 5′...