A high-throughput screening assay for small molecule inhibitors of the antigen aminopeptidase ERAP1

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January 2023 issue SLAS Discovery contains four full articles and one technical brief on cancer research, high-throughput screening (HTS) assay development, and other drug discovery.

This month’s feature article, “A high-throughput MALDI-TOF MS biochemical screening for small-molecule inhibitors 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 against endoplasmic reticulum aminopeptidase 1 (ERAP1). Associated with various autoimmune and autoinflammatory diseases, ERAP1 has become an attractive target for drug discovery.

The research team behind this study leveraged the existing ERAP1 RapidFire MS (RF MS) assay underlying the MALDI-TOF assay to improve assay stability, reproducibility, and robustness of the MALDI-TOF platform. I was allowed to. Comparing results between pre-established RF MS and MALDI-TOF platforms, shorter sample cycle times, reduced reagent consumption, and lower tight binding limits were all advantages of the MALDI-TOF platform.

Read this original research article to learn how the MALDI-TOF platform detects other challenging targets, along with other research articles in the January issue. SLAS Discovery.

January issue of SLAS Discovery Includes the following additional articles:

  • of SLAS Discovery Top 10 Editors of 2022
  • Identifying Decreased Serum EPA and DHA Levels in Non-Small Cell Lung Cancer Patients Using a New, Validated Rapid LC-MS/MS Method
  • DNA methylation-induced ablation of miR-133a accelerates glioma cancer aggressiveness via upregulation of peroxisome proliferator-activated receptor γ
  • Optimizing Cell-Based Bioassays with Integrated Design of Experiments (ixDoE) – A Practical Guide
  • Development of a high-throughput TR-FRET screening assay for fast-cycling KRAS mutants
  • An errata for DNA methylation-induced removal of miR-133a accelerates cancer aggressiveness in gliomas via upregulation of peroxisome proliferator-activated receptor-γ [SLAS Discov. 2022 Sep 5;S2472-5552(22)13691-9. doi: 10.1016/j.slasd.2022.08.004.]


Journal reference:

Müller, L., and others. (2022) High throughput MALDI-TOF MS biochemical screen for small molecule inhibitors of the antigenic aminopeptidase ERAP1. SLAS Discovery. doi.org/10.1016/j.slasd.2022.11.002.

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