Cited by 298Open Access
National Institutes of Health
ORCID: 0000-0003-2636-2766Publishes on Computational Drug Discovery Methods, Cancer, Hypoxia, and Metabolism, Ubiquitin and proteasome pathways. 321 papers and 2.4k citations.
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This eBook is a comprehensive, crucial resource for investigators optimizing assays to evaluate collections of molecules with the overall goal of developing probes that modulate the activity of biological targets, pathways or cellular phenotypes. Such probes might be candidates for further optimization and investigation in drug discovery and development.Originally written as a guide for therapeutic project teams within a major pharmaceutical company, this manual has been adapted to provide guidelines for scientists in academic, non-profit, government and industrial research laboratories to develop assay formats compatible with High Throughput Screening (HTS) and Structure Activity Relationship (SAR) measurements of new and known molecular entities. Topics addressed in this manual include: Descriptions of assay formats that are compatible with HTS and determination of SAR Selection and development of optimal assay reagents Optimizations and troubleshooting for assay protocols with respect to sensitivity, dynamic range, signal intensity and stability Adaptations of assays for automation and scaling to microtiter plate formats Instrumentation Sources of assay artifacts and interferences Statistical validation of assay performance parameters Secondary assays for chemical probe validation and SAR refinement Data standards for reporting the results of screening and SAR assays In vivo assay development and validation Assay development and validation for siRNA-based high-throughput screens The National Center for Advancing Translational Sciences (NCATS) manages the content of the Assay Guidance Manual with input from industry, academia and government experts. More than 100 authors from around the globe have contributed content to this free resource, which is updated quarterly with contributions by experienced scientists from multiple disciplines working in drug discovery and development worldwide.For more information about the Assay Guidance Manual and related training opportunities, visit https://ncats.nih.gov/expertise/preclinical/agm .
) production via nicotinamide phosphoribosyltransferase (NAMPT) inhibition demonstrated that metabolic catastrophe drives the combination-induced cytotoxicity. This study provides a comprehensive single-agent and combinatorial drug screen for DMG and identifies concomitant HDAC and proteasome inhibition as a promising therapeutic strategy that underscores underrecognized metabolic vulnerabilities in DMG.
The National Center for Advancing Translational Sciences (NCATS) has developed an online open science data portal for its COVID-19 drug repurposing campaign - named OpenData - with the goal of making data across a range of SARS-CoV-2 related assays available in real-time. The assays developed cover a wide spectrum of the SARS-CoV-2 life cycle, including both viral and human (host) targets. In total, over 10,000 compounds are being tested in full concentration-response ranges from across multiple annotated small molecule libraries, including approved drug, repurposing candidates and experimental therapeutics designed to modulate a wide range of cellular targets. The goal is to support research scientists, clinical investigators and public health officials through open data sharing and analysis tools to expedite the development of SARS-CoV-2 interventions, and to prioritize promising compounds and repurposed drugs for further development in treating COVID-19.