February's SLAS Discovery Special Issue, "Advances in Cellular Target Engagement and Target Deconvolution" Now Available

Oak Brook, IL (USA) The February special issue of SLAS Discovery, “Advances in Cellular Target Engagement and Target Deconvolution,” features 13 articles focused on multiple aspects and technologies of cellular target engagement. Special issue editors Martin Main, Ph.D., (Medicines Discovery Catapult, UK) and Andrew Zhang, Ph.D., (AstraZeneca, USA) selected articles that span a variety of relevant topics, from the direct measurement of compound-target interaction using BRET technologies to the measurement of compound-induced changes in protein stability and localization.

Proof of target engagement is a crucial element of drug discovery. In addition, target engagement in biochemical settings provides critical insights around binding modes and avenues to rapidly identify hit series, yet findings are not guaranteed to translate into desired effects. When applied in combination, the methods highlighted in this issue can build a strong platform of evidence linking compound to target to biological response, in turn, impacting project attrition and drug discovery success.

February’s SLAS Discovery includes the following reviews and perspectives:

• NanoBRET – A Novel BRET Platform for the Analysis of Protein-Protein Interactions
• High-Throughput Implementation of the NanoBRET® Target Engagement Intracellular Kinase Assay to Reveal Differential Compound Engagement by SIK2/3 Isoforms
• A High-Throughput BRET Cellular Target Engagement Assay Links Biochemical-to-Cellular Activity for Bruton's Tyrosine Kinase
• Cellular Target Engagement Approaches to Monitor Epigenetic Reader Domain Interactions
• NanoBiT Complementation to Monitor Agonist-Induced Adenosine A1 Receptor Internalization
• Medium-Throughput Detection of Hsp90/Cdc37 Protein–Protein Interaction Inhibitors Using a Split Renilla Luciferase-Based Assay
• Perspective on CETSA Literature – Towards More Quantitative Data Interpretation
• Drug Target Engagement Using Coupled Cellular Thermal Shift AssayAcoustic Reverse Phase Protein Array
• High-Throughput Cellular Thermal Shift Assays in Research and Drug Discovery
• Horizontal Cell Biology: Monitoring Global Changes of Protein Interaction States with the Proteome-Wide Cellular Thermal Shift Assay (CETSA)
• Over-Expression of Comprehensive Libraries of Human Proteins in a Cellular System Provides a Biologically Relevant Platform for Target Deconvolution
• Bioorthogonal Reporters for Detecting and Profiling Protein Acetylation and Acylation
• The Opportunities and Use of Imaging to Measure Target Engagement

Access to this special issue of SLAS Discovery is available at https://journals.sagepub.com/toc/jbxb/25/2 through February 20. For more information about SLAS and its journals, visit www.slas.org/publications/slas-discovery/.

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SLAS (Society for Laboratory Automation and Screening) is an international community of 16,000 professionals and students dedicated to life sciences discovery and technology. The SLAS mission is to bring together researchers in academia, industry and government to advance life sciences discovery and technology via education, knowledge exchange and global community building.

SLAS Discovery: Advancing the Science of Drug Discovery, 2018 Impact Factor 2.192. Editor-in-Chief Robert M. Campbell, Ph.D., Eli Lilly and Company, Indianapolis, IN (USA).

SLAS Technology: Translating Life Sciences Innovation, 2018 Impact Factor 2.048. Editor-in-Chief Edward Kai-Hua Chow, Ph.D., National University of Singapore (Singapore).

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