André Luiz Lourenço
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View article: Large library docking and biophysical analysis of small molecule TMPRSS2 inhibitors
Large library docking and biophysical analysis of small molecule TMPRSS2 inhibitors Open
Transmembrane protease, serine -2 (TMPRSS2) is an essential host entry factor in human airways for SARS-CoV-2 and influenza A/B and has presented as a target for antiviral drug development; however, no clinically viable, oral small molecul…
View article: Editorial: Mapping enzyme activity: from novel diagnostics to target-based therapeutics, how activity-based probes are improving our understanding of biological catalysts
Editorial: Mapping enzyme activity: from novel diagnostics to target-based therapeutics, how activity-based probes are improving our understanding of biological catalysts Open
EDITORIAL article Front. Pharmacol., 22 August 2023Sec. Experimental Pharmacology and Drug Discovery Volume 14 - 2023 | https://doi.org/10.3389/fphar.2023.1271247
View article: Perturbations in podocyte transcriptome and biological pathways induced by FSGS associated circulating factors
Perturbations in podocyte transcriptome and biological pathways induced by FSGS associated circulating factors Open
We identified several novel and previously described genes associated with FSGS progression. Targeted blockade of suPAR and CD40 pathways with novel human antibodies showed inhibition of podocyte injury in FSGS.
View article: Adversarial Robustness and Feature Impact Analysis for Driver Drowsiness Detection
Adversarial Robustness and Feature Impact Analysis for Driver Drowsiness Detection Open
Drowsy driving is a major cause of road accidents, but drivers are dismissive of the impact that fatigue can have on their reaction times. To detect drowsiness before any impairment occurs, a promising strategy is using Machine Learning (M…
View article: High-throughput optofluidic screening of single B cells identifies novel cross-reactive antibodies as inhibitors of uPAR with antibody-dependent effector functions
High-throughput optofluidic screening of single B cells identifies novel cross-reactive antibodies as inhibitors of uPAR with antibody-dependent effector functions Open
The urokinase-type plasminogen activator receptor (uPAR) is an essential regulator for cell signaling in tumor cell proliferation, adhesion, and metastasis. The ubiquitous nature of uPAR in many aggressive cancer types makes uPAR an attrac…
View article: Anxolotl, an Anxiety Companion App -- Stress Detection
Anxolotl, an Anxiety Companion App -- Stress Detection Open
Stress has a great effect on people's lives that can not be understated. While it can be good, since it helps humans to adapt to new and different situations, it can also be harmful when not dealt with properly, leading to chronic stress. …
View article: Perturbations in podocyte transcriptome and biological pathways induced by FSGS associated circulating factors
Perturbations in podocyte transcriptome and biological pathways induced by FSGS associated circulating factors Open
Focal segmental glomerulosclerosis (FSGS) is frequently associated with heavy proteinuria and progressive renal failure requiring dialysis or kidney transplantation. However, primary FSGS also has 40-80% risk of recurrence of disease in th…
View article: Structure-based identification of naphthoquinones and derivatives as novel inhibitors of main protease Mpro and papain-like protease PLpro of SARS-CoV-2
Structure-based identification of naphthoquinones and derivatives as novel inhibitors of main protease Mpro and papain-like protease PLpro of SARS-CoV-2 Open
The worldwide COVID-19 pandemic caused by the coronavirus SARS-CoV-2 urgently demands novel direct antiviral treatments. The main protease (Mpro) and papain-like protease (PLpro) are attractive drug targets among coronaviruses due to their…
View article: A novel class of TMPRSS2 inhibitors potently block SARS-CoV-2 and MERS-CoV viral entry and protect human epithelial lung cells
A novel class of TMPRSS2 inhibitors potently block SARS-CoV-2 and MERS-CoV viral entry and protect human epithelial lung cells Open
Significance MM3122 represents an advanced lead candidate for clinical development as a novel antiviral drug for COVID-19. In addition to being novel drugs, these selective TMRSS2 inhibitors can be used as valuable chemical probes to help …
View article: In Vivo Measurement of Granzyme Proteolysis from Activated Immune Cells with PET
In Vivo Measurement of Granzyme Proteolysis from Activated Immune Cells with PET Open
The biology of human granzymes remains enigmatic in part due to our inability to probe their functions outside of in vitro assays or animal models with divergent granzyme species. We hypothesize that the biology of human granzymes could be…
View article: COVID-19 in chronic myeloid leukemia patients in Latin America
COVID-19 in chronic myeloid leukemia patients in Latin America Open
This observational, multicenter study aimed to report the clinical evolution of COVID-19 in patients with chronic myeloid leukemia in Latin America. A total of 92 patients presented with COVID-19 between March and December 2020, 26% of who…
View article: Identification of recombinant Fabs for structural and functional characterization of HIV-host factor complexes
Identification of recombinant Fabs for structural and functional characterization of HIV-host factor complexes Open
Viral infection and pathogenesis is mediated by host protein—viral protein complexes that are important targets for therapeutic intervention as they are potentially less prone to development of drug resistance. We have identified human, re…
View article: A novel class of TMPRSS2 inhibitors potently block SARS-CoV-2 and MERS-CoV viral entry and protect human epithelial lung cells
A novel class of TMPRSS2 inhibitors potently block SARS-CoV-2 and MERS-CoV viral entry and protect human epithelial lung cells Open
The host cell serine protease TMPRSS2 is an attractive therapeutic target for COVID-19 drug discovery. This protease activates the Spike protein of Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) and of other coronaviruses and…
View article: COVID-19 IN CHRONIC MYELOID LEUKEMIA PATIENTS – BRAZILIAN EXPERIENCE
COVID-19 IN CHRONIC MYELOID LEUKEMIA PATIENTS – BRAZILIAN EXPERIENCE Open
View article: 4532 Pancreatic Cyst Risk Stratification for Early Detection of Pancreatic Cancer Using Quantitative Radiomics and Activity-Based Biomarkers
4532 Pancreatic Cyst Risk Stratification for Early Detection of Pancreatic Cancer Using Quantitative Radiomics and Activity-Based Biomarkers Open
OBJECTIVES/GOALS: Pancreatic cysts are comprised of both precancerous mucinous lesions and non-mucinous lesions with minimal malignant potential. Our goal is to improve our ability to classify the type of cyst using a combination of novel …
View article: Antibody-Drug Conjugates Targeting the Urokinase Receptor (uPAR) as a Possible Treatment of Aggressive Breast Cancer
Antibody-Drug Conjugates Targeting the Urokinase Receptor (uPAR) as a Possible Treatment of Aggressive Breast Cancer Open
A promising molecular target for aggressive cancers is the urokinase receptor (uPAR). A fully human, recombinant antibody that binds uPAR to form a stable complex that blocks uPA-uPAR interactions (2G10) and is internalized primarily throu…
View article: Semantic Navigation Mapping from Aerial Multispectral Imagery
Semantic Navigation Mapping from Aerial Multispectral Imagery Open
The emergence of Unmanned Aerial Vehicles (UAV) in the Precision Agriculture (PA) domain allowed decision support systems to have access to aerial images of the terrain surface. By exploiting multispectral aerial imagery, crop health analy…
View article: IL-1β Blockade Attenuates Thrombosis in a Neutrophil Extracellular Trap-Dependent Breast Cancer Model
IL-1β Blockade Attenuates Thrombosis in a Neutrophil Extracellular Trap-Dependent Breast Cancer Model Open
Cancer patients are at increased risk of developing thrombosis, comorbidity that has been associated with increased neutrophil counts and the formation of neutrophil extracellular traps (NETs). Interleukin-1β (IL-1β) modulates the expressi…
View article: Pyrazolyl-Tetrazoles and Imidazolyl-Pyrazoles as Potential Anticoagulants and their Integrated Multiplex Analysis Virtual Screening
Pyrazolyl-Tetrazoles and Imidazolyl-Pyrazoles as Potential Anticoagulants and their Integrated Multiplex Analysis Virtual Screening Open
This article reports a novel virtual screening algorithm seeking the rational identification of novel lead anticoagulants.Seven 5-(3-methyl-1-aryl-1H-pyrazol-4-yl)-1H-tetrazoles and seven novel 1-aryl-4-(4,5-dihydro-1H-imidazol-2-yl)-3-met…
View article: Synthesis and mechanistic evaluation of novel N ’-benzylidene-carbohydrazide-1 H -pyrazolo[3,4 -b ]pyridine derivatives as non-anionic antiplatelet agents
Synthesis and mechanistic evaluation of novel N ’-benzylidene-carbohydrazide-1 H -pyrazolo[3,4 -b ]pyridine derivatives as non-anionic antiplatelet agents Open
View article: Marine Diterpenes: Molecular Modeling of Thrombin Inhibitors with Potential Biotechnological Application as an Antithrombotic
Marine Diterpenes: Molecular Modeling of Thrombin Inhibitors with Potential Biotechnological Application as an Antithrombotic Open
Thrombosis related diseases are among the main causes of death and incapacity in the world. Despite the existence of antithrombotic agents available for therapy, they still present adverse effects like hemorrhagic risks which justify the s…
View article: New approaches in tail‐bleeding assay in mice: improving an important method for designing new anti‐thrombotic agents
New approaches in tail‐bleeding assay in mice: improving an important method for designing new anti‐thrombotic agents Open
Summary This report describes a modified, simple, low‐cost and more sensitive method to determine bleeding patterns and haemoglobin concentration in a tail‐bleeding assay using BALB /c mice and tail tip amputation. The cut tail was immerse…
View article: Antiplatelet pyrazolopyridines derivatives: pharmacological, biochemical and toxicological characterization
Antiplatelet pyrazolopyridines derivatives: pharmacological, biochemical and toxicological characterization Open
Platelet aggregation is one of the main events involved in vascular thrombus formation. Recently, N'-substituted-phenylmethylene-3-methyl-1,6-diphenyl-1H-pyrazolo[3,4-b]pyridine-4-carbohydrazides were described as antiplatelet derivatives.…
View article: The antihemostatic profile of vitamin C: Mechanisms that underlie the technical application of a physiological molecule
The antihemostatic profile of vitamin C: Mechanisms that underlie the technical application of a physiological molecule Open
The potential of antioxidants as tools for lowering the incidence of diseases, including cardiovascular events, is of growing interest. Some antioxidants (e.g. vitamin E and acetyl-salicylic acid) have been described as effective on cardio…
View article: Non-invasive imaging and cellular tracking of pulmonary emboli by near-infrared fluorescence and positron-emission tomography
Non-invasive imaging and cellular tracking of pulmonary emboli by near-infrared fluorescence and positron-emission tomography Open
View article: Synthesis and Antiplatelet Activity of Antithrombotic Thiourea Compounds: Biological and Structure-Activity Relationship Studies
Synthesis and Antiplatelet Activity of Antithrombotic Thiourea Compounds: Biological and Structure-Activity Relationship Studies Open
The incidence of hematological disorders has increased steadily in Western countries despite the advances in drug development. The high expression of the multi-resistance protein 4 in patients with transitory aspirin resistance, points to …