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A covalent compound selectively inhibits RNA demethylase ALKBH5 rather than FTO

Covalent Modifiers

Herein, we used a targeted covalent inhibition strategy and identified a covalent inhibitor, TD19, which selectively inhibits ALKBH5 compared with FTO demethylase in protein-based and tumor cell-based assays. TD19 irreversibly modifies the residues C100 and C267, preventing ALKBH5 from binding to m6A-containing RNA.

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Gamcemetinib

New Drug Approvals

nM) and cell based assays ( EC 50 =89 nM). Gamcemetinib CAS 1887069-10-4 CC-99677 , OS2IR8TV1O Molecular Weight 469.94 Gamcemetinib is extracted from patent WO2020236636, compound 1.

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Generation and characterization of mirikizumab, a humanized monoclonal antibody targeting the p19 subunit of IL-23 [Drug Discovery and Translational Medicine]

ASPET

Mirikizumab effectively inhibits the interaction of IL-23 with its receptor, and potently blocks IL-23-induced IL-17 production in cell-based assays while preserving the function of IL-12. In both local and systemic in vivo mouse models, mirikizumab blocked IL-23-induced keratin mRNA or IL-17 production, respectively.

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The Novel GlycoPEGylated FGF21 Analog Pegozafermin Activates Human FGF Receptors and Improves Metabolic and Liver Outcomes in Diabetic Monkeys and Healthy Human Volunteers [Drug Discovery and Translational Medicine]

ASPET

In cell-based assays, pegozafermin had a similar receptor engagement profile as native FGF21, with approximately 8-fold higher potency at FGF receptor 1 (FGFR1).

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Time for change: non-human primates in drug research

Drug Target Review

7 This initiative forms part of a broader effort to modernise drug development and align regulatory expectations with emerging new approach methodologies (NAMs), including human cell-based assays, artificial intelligence models and organ-on-chip platforms.

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Expanding Your Assay Specificity: Cisbio Joins PerkinElmer

PerkinElmer

The structure of HTRF reagents also makes assays highly resistant to most experimental conditions, and particularly well suited for cell-based assays.

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Genetic variant identification: unveiling the power of STING-seq

Drug Target Review

The perennial challenge with STING-seq (and all cell-based assays) is finding the right cell type for the disease or trait. This encompasses many common diseases and we are optimistic that STING-seq will be a useful platform to rapidly understand which variants and genes are key players in these diseases.