A5020741580- Reproductive tract infections research
- Urinary Tract Infections Management
- Cannabis and Cannabinoid Research
- Neuroscience and Neuropharmacology Research
- Ubiquitin and proteasome pathways
- Photochromic and Fluorescence Chemistry
- Peptidase Inhibition and Analysis
- Biochemical Analysis and Sensing Techniques
- Tryptophan and brain disorders
- Enzyme Structure and Function
- Microbial Natural Products and Biosynthesis
- Pharmacological Receptor Mechanisms and Effects
- Dermatology and Skin Diseases
- Sexual function and dysfunction studies
- GABA and Rice Research
- Stress Responses and Cortisol
- Toxoplasma gondii Research Studies
- Immunotherapy and Immune Responses
Icesi University
2021-2024
University of Würzburg
2017-2024
Gesellschaft für Klinische Forschung
2022-2023
University of Padua
2022
University of Milan
2022
Instituto de Histología y Embriología de Mendoza
2022
Consejo Nacional de Investigaciones Científicas y Técnicas
2022
Istituto Nazionale Tumori IRCCS "Fondazione G. Pascale"
2022
Obligate intracellular Chlamydia trachomatis replicate in a membrane-bound vacuole called inclusion, which serves as signaling interface with the host cell. Here, we show that chlamydial deubiquitinating enzyme (Cdu) 1 localizes inclusion membrane and faces cytosol active domain. The structure of this domain revealed high similarity to mammalian deubiquitinases unique α-helix close substrate-binding pocket. We identified apoptosis regulator Mcl-1 target interacts Cdu1 is stabilized by...
Human cannabinoid receptor type 1 (hCB1R) plays important roles in the regulation of appetite and development addictive behaviors. Herein, we describe design, synthesis, photocharacterization, molecular docking, vitro characterization "photo-rimonabant", i.e., azo-derivatives selective hCB1R antagonist SR1411716A (rimonabant). By applying azo-extension strategies, yielded compound 16a, which shows marked affinity for CB1R (Ki (cis form) = 29 nM), whose potency increases by illumination with...
Upon infection by an intracellular pathogen, host cells activate apoptotic pathways to limit pathogen replication. Consequently, efficient proliferation of the obligate Chlamydia trachomatis, a major cause trachoma and sexually transmitted diseases, depends on suppression cell apoptosis. C. trachomatis secretes deubiquitinase ChlaDUB1 into cell, leading among other interactions stabilization antiapoptotic proteins and, thus, Targeting bacterial effector protein may, therefore, lead new...
Activation of the human cannabinoid receptor type 1 (hCB1R) with high spatiotemporal control is useful to study processes involved in different pathologies related nociception, metabolic alterations, and neurological disorders. To synthesize new agonist ligands for hCB1R, we have designed classes photoswitchable molecules based on an indole core. The modifications made central core allowed us understand molecular characteristics necessary design optimal pharmacological properties. Compound...
Abstract Based on the similarity between active sites of deubiquitylating and deneddylating enzyme ChlaDub1 (Cdu1) evolutionarily related protease adenain, a target‐hopping screening approach focused set adenain inhibitors was investigated. The cyanopyrimidine‐based identified represent first active‐site‐directed small‐molecule Cdu1. High‐resolution crystal structures Cdu1 in complex with two covalently bound cyanopyrimidines, as well its substrate ubiquitin, were obtained. These structural...
Abstract The cannabinoid receptor subtype 2 (CB R) is rapidly upregulated in neuroinflammatory processes and respective agonists have a high potential to combat several central nervous system disorders related neuroinflammation neurodegeneration. As new strategy for ligand design, dualsteric binding applied by chemically combining positive allosteric modulator with an orthosteric ligand. resulting two sets of (or bitopic) ligands different chain lengths five methylene groups are evaluated [...
Introduction: Cannabis has a historical role for pharmacological analgesia/anaesthesia, as well dental anxiety.Fast-forward to today's scientific literature, there are many considerations regarding the of cannabis in dentistry.We examine endocannabinoid system and its modulation from perspective.Whilst smoking been associated with poor health, tetrahydrocannabinol (THC) intoxication can result tachycardia acute hypertension, (which could cause drug-drug interaction sedation anaesthesia),...
Abstract Introduction Cannabis sativa is a highly versatile plant with long history of cultivation and domestication. It produces multiple compounds that exert distinct valuable therapeutic effects by modulating diverse biological systems, including the endocannabinoid system (ECS). Access to standardized, metabolically diverse, reproducible C. chemotypes chemovars essential for physicians optimize individualized patient treatment industries conduct drug‐discovery campaigns. Objective This...
Abstract Fluoxetine is a safe antidepressant with remarkable anti‐inflammatory actions; therefore, we aimed to investigate its effects on immortalized (HaCaT) as well primary human epidermal keratinocytes in polyinosinic‐polycytidylic acid (p(I:C))‐induced inflammatory model. We found that non‐cytotoxic concentration (MTT‐assay, CyQUANT‐assay) of fluoxetine significantly suppressed p(I:C)‐induced expression and release several pro‐inflammatory cytokines (Q‐PCR, cytokine array, ELISA), it...