{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"omics_type":["Unknown"],"volume":["5(6)"],"submitter":["Finger JN"],"pubmed_abstract":["Therapies that suppress RIPK1 kinase activity are emerging as promising therapeutic agents for the treatment of multiple inflammatory disorders. The ability to directly measure drug binding of a RIPK1 inhibitor to its target is critical for providing insight into pharmacokinetics, pharmacodynamics, safety and clinical efficacy, especially for a first-in-class small-molecule inhibitor where the mechanism has yet to be explored. Here, we report a novel method for measuring drug binding to RIPK1 protein in cells and tissues. This TEAR1 (Target Engagement Assessment for RIPK1) assay is a pair of immunoassays developed on the principle of competition, whereby a first molecule (ie, drug) prevents the binding of a second molecule (ie, antibody) to the target protein. Using the TEAR1 assay, we hav"],"journal":["Pharmacology research & perspectives"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC5723705"],"repository":["biostudies-literature"],"pubmed_title":["Identification of an antibody-based immunoassay for measuring direct target binding of RIPK1 inhibitors in cells and tissues."],"pmcid":["PMC5723705"],"pubmed_authors":["Maguire S","Nagilla R","Campobasso N","Cook MN","Rivera EJ","Brusq JM","Gough PJ","Haag H","Bertin J","Joglekar D","Deutsch J","Lich JD","Harris PA","Jenkins EL","Votta BJ","Sun H","Finger JN"],"additional_accession":[]},"is_claimable":false,"name":"Identification of an antibody-based immunoassay for measuring direct target binding of RIPK1 inhibitors in cells and tissues.","description":"Therapies that suppress RIPK1 kinase activity are emerging as promising therapeutic agents for the treatment of multiple inflammatory disorders. The ability to directly measure drug binding of a RIPK1 inhibitor to its target is critical for providing insight into pharmacokinetics, pharmacodynamics, safety and clinical efficacy, especially for a first-in-class small-molecule inhibitor where the mechanism has yet to be explored. Here, we report a novel method for measuring drug binding to RIPK1 protein in cells and tissues. This TEAR1 (Target Engagement Assessment for RIPK1) assay is a pair of immunoassays developed on the principle of competition, whereby a first molecule (ie, drug) prevents the binding of a second molecule (ie, antibody) to the target protein. Using the TEAR1 assay, we hav","dates":{"release":"2017-01-01T00:00:00Z","publication":"2017 Dec","modification":"2025-04-21T16:17:22.881Z","creation":"2019-03-27T03:04:22Z"},"accession":"S-EPMC5723705","cross_references":{"pubmed":["29226625"],"doi":["10.1002/prp2.377"]}}