Search results for "610"
showing 10 items of 1353 documents
Structure‐Activity Relationships of Benzamides and Isoindolines Designed as SARS‐CoV Protease Inhibitors Effective against SARS‐CoV‐2
2020
Abstract Inhibition of coronavirus (CoV)‐encoded papain‐like cysteine proteases (PLpro) represents an attractive strategy to treat infections by these important human pathogens. Herein we report on structure‐activity relationships (SAR) of the noncovalent active‐site directed inhibitor (R)‐5‐amino‐2‐methyl‐N‐(1‐(naphthalen‐1‐yl)ethyl) benzamide (2 b), which is known to bind into the S3 and S4 pockets of the SARS‐CoV PLpro. Moreover, we report the discovery of isoindolines as a new class of potent PLpro inhibitors. The studies also provide a deeper understanding of the binding modes of this inhibitor class. Importantly, the inhibitors were also confirmed to inhibit SARS‐CoV‐2 replication in …
Particle identification algorithms for the PANDA Barrel DIRC
2020
The International Conference Instrumentation for Colliding Beam Physics , INSTR2020, Novosibirsk, Russia, 24 Feb 2020 - 28 Feb 2020; Journal of Instrumentation 15(09), C09057 (2020). doi:10.1088/1748-0221/15/09/C09057
pcaExplorer: an R/Bioconductor package for interacting with RNA-seq principal components
2019
AbstractBackgroundPrincipal component analysis (PCA) is frequently useentirely written ind in genomics applications for quality assessment and exploratory analysis in high-dimensional data, such as RNA sequencing (RNA-seq) gene expression assays. Despite the availability of many software packages developed for this purpose, an interactive and comprehensive interface for performing these operations is lacking.ResultsWe developed the pcaExplorer software package to enhance commonly performed analysis steps with an interactive and user-friendly application, which provides state saving as well as the automated creation of reproducible reports. pcaExplorer is implemented in R using the Shiny fra…
Targeting fibroblast activation protein (FAP): next generation PET radiotracers using squaramide coupled bifunctional DOTA and DATA5m chelators
2020
Abstract Background Fibroblast activation protein (FAP) is a proline selective serine protease that is overexpressed in tumor stroma and in lesions of many other diseases that are characterized by tissue remodeling. In 2014, a most potent FAP-inhibitor (referred to as UAMC1110) with low nanomolar FAP-affinity and high selectivity toward related enzymes such as prolyl oligopeptidase (PREP) and the dipeptidyl-peptidases (DPPs): DPP4, DPP8/9 and DPP2 were developed. This inhibitor has been adopted recently by other groups to create radiopharmaceuticals by coupling bifunctional chelator-linker systems. Here, we report squaric acid containing bifunctional DATA5m and DOTA chelators relied on UAMC…
Association between DRD2/DRD4 interaction and conduct disorder: a potential developmental pathway to alcohol dependence
2013
1 Department of Genetics, Universidade Federal do Rio Grande do Sul, Porto Alegre, Brazil 2 King’s College London, Institute of Psychiatry, MRC Social Genetic and Developmental Psychiatry Centre, London, United Kingdom, UK 3 Department of Child and Adolescent Psychiatry and Psychotherapy, Central Institute of Mental Health, Medical Faculty Mannheim, University of Heidelberg, Mannheim, Germany 4 Department of Cognitive Neuroscience, Donders Institute for Brain, Cognition and Behavior, Radboud University Medical Center, Nijmegen, The Netherlands 5 Psychology Department, National University of Singapore, Singapore, Singapore 6 Department of Psychiatry, Donders Institute for Brain, Cognition an…
¿Proveer justicia u oprimir a los pueblos? La acción de los corregedores de las Azores en el periodo moderno
2020
En Portugal, los corregedores han sido presentados por la historiografía tradicional como uno de los pilares del proceso de centralización política que había tenido lugar en el reino portugués a partir del final de la Edad Media. Esta interpretación ha sido corregida en las últimas décadas por nuevas investigaciones e interpretaciones. En los territorios portu- gueses de ultramar, la distancia amplió algunos de los “obstáculos fácticos” (según Antonio Manuel Hespanha) que hacían difícil, si no imposible, la concreción de cualquier proyecto centralizador. El caso azoriano es de esto un buen ejemplo. En este artículo, además de una síntesis de los poderes de los corregedores…
The Study of Carbamoyl Phosphate Synthetase 1 Deficiency Sheds Light on the Mechanism for Switching On/Off the Urea Cycle
2015
12 páginas, 4 figuras, 2 tablas.
Preventing problematic internet use during the COVID-19 pandemic: Consensus guidance
2020
As a response to the COVID-19 pandemic, many governments have introduced steps such as spatial distancing and “staying at home” to curb its spread and impact. The fear resulting from the disease, the ‘lockdown’ situation, high levels of uncertainty regarding the future, and financial insecurity raise the level of stress, anxiety, and depression experienced by people all around the world. Psychoactive substances and other reinforcing behaviors (e.g., gambling, video gaming, watching pornography) are often used to reduce stress and anxiety and/or to alleviate depressed mood. The tendency to use such substances and engage in such behaviors in an excessive manner as putative coping strategies i…
Medical Student Ultrasound Education, a WFUMB Position Paper, Part II. A consensus statement of ultrasound societies.
2020
Ultrasound is becoming a fundamental first-line diagnostic tool for most medical specialties and an innovative tool to teach anatomy, physiology and pathophysiology to undergraduate and graduate students. However, availability of structured training programs during medical school is lagging behind and many physicians still acquire all their ultrasound skills during postgraduate training.There is wide variation in medical student ultrasound education worldwide. Sharing successful educational strategies from early adopter medical schools and learning from leading education programs should advance the integration of ultrasound into the university medical school curricula. In this overview, we …
The frequent stressor and mental health monitoring-paradigm: a proposal for the operationalization and measurement of resilience and the identificati…
2021
Resilience has been defined as the maintenance or quick recovery of mental health during and after times of adversity. How to operationalize resilience and to determine the factors and processes that lead to good long-term mental health outcomes in stressor-exposed individuals is a matter of ongoing debate and of critical importance for the advancement of the field. One of the biggest challenges for implementing an outcome-based definition of resilience in longitudinal observational study designs lies in the fact that real-life adversity is usually unpredictable and that its substantial qualitative as well as temporal variability between subjects often precludes defining circumscribed time …