News Release

A new Assay screening method shows therapeutic promise for treating auto-immune disease

The January 2023 issue of SLAS Discovery contains a collection of four full-length articles and one technical brief covering cancer research, high-throughput screening (HTS) assay development and other drug discovery exploration

Peer-Reviewed Publication

SLAS (Society for Laboratory Automation and Screening)

Automated MALDI-TOF MS based high-throughput screening workflow for in vitro enzyme assays

image: Liquid handling devices are used for (1) compound, (2) enzyme, (3) substrate (S), and (4) internal standard (iSt) in quench solution delivery which is interrupted by sensible incubation times (indicated above arrows) to allow compound enzyme alignment and product (P) formation over time. An isotopically labelled internal standard is spiked into the samples to allow quantification. (5) The sample is mixed with matrix and delivered onto the target plate which is acquired by MALDI-TOF MS. (6) Upon laser ionisation, analyte ions are separated in a flight tube according to their mass-to-charge (m/z) ratio before they hit a detector. (7) In the mass spectrum, active and inactive compounds can be distinguished based on the observed product formation. view more 

Credit: Leonie Müller, et al.

Oak Brook, IL (January 27, 2022) – The January 2023 issue of SLAS Discovery contains a collection of four full-length articles and one technical brief covering cancer research, high-throughput screening (HTS) assay development and other drug discovery exploration.

This month's featured article, "A high-throughput MALDI-TOF MS biochemical screen for small molecule inhibitors of the antigen aminopeptidase ERAP1," by Müller, et al, presents a newly developed matrix assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF MS) drug discovery assay for the endoplasmic reticulum aminopeptidase 1 (ERAP1). The dysregulation of ERAP1 has been associated with various auto-immune and auto-inflammatory diseases, making ERAP1 a high-profile target in drug discovery.

The research team behind this study utilized an existing ERAP1 RapidFire MS (RF MS) assay on which to base their MALDI-TOF assay, producing greater assay stability, reproducibility and robustness for the MALDI-TOF platform. When results were compared between the pre-established RF MS and the MALDI-TOF platforms, shorter sample cycle times, reduced reagent consumption and a lower tight-binding limit were all advantages of the MALDI-TOF platform.

Read this original research article to learn how the MALDI-TOF platform may detect other difficult targets, along with more research articles in the January issue of SLAS Discovery.

The January issue of SLAS Discovery includes these additional articles:

Access to the January issue of SLAS Discovery is available at https://www.slas-technology.org/issue/S2472-6303(22)X0007-1

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SLAS Discovery reports how scientists develop and use novel technologies and/or approaches to provide and characterize chemical and biological tools to understand and treat human disease. The journal focuses on drug discovery sciences with a strong record of scientific rigor and impact, reporting on research that:

  • Enables and improves target validation
  • Evaluates current drug discovery technologies
  • Provides novel research tools
  • Incorporates research approaches that enhance depth of knowledge and drug discovery success

SLAS (Society for Laboratory Automation and Screening) is an international professional society of academic, industry and government life sciences researchers and the developers and providers of laboratory automation 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, 2021 Impact Factor 3.341. Editor-in-Chief Robert M. Campbell, Ph.D., Redona Therapeutics, Watertown, MA (USA).

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