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Biochemical assays and deep cyclic inhibition in cancer treatment

Drug Target Review

Molecular-level biochemical assays like transcriptomics, genomics and proteomics have emerged as valuable tools for identifying potential targets in cancer treatment through deep cyclic inhibition (DCI).

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Structural Dynamics of the Ubiquitin Specific Protease USP30 in Complex with a Cyanopyrrolidine-Containing Covalent Inhibitor

Covalent Modifiers

We have integrated structural and quantitative proteomics with biochemical assays to decipher the mode of action of covalent USP30 inhibition by a small molecule containing a cyanopyrrolidine reactive group, USP30-I-1. The inhibitor demonstrated high potency and selectivity for endogenous USP30 in neuroblastoma cells.

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Positive Impact of Dragonfly™ Discovery in Biochemical Assay

Zobio

Biochemical assays are commonly used to assess how organic compounds impact the activity of a protein of interest (POI). Het bericht Positive Impact of Dragonfly™ Discovery in Biochemical Assay verscheen eerst op ZoBio - Drug Discovery Technology.

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Identification of a cell-active chikungunya virus nsP2 protease inhibitor using a covalent fragment-based screening approach

Covalent Modifiers

Here, we optimized a CHIKV nsP2 protease (nsP2pro) biochemical assay for the screening of a 6,120-compound cysteine-directed covalent fragment library. CHIKV nonstructural protein 2 (nsP2), which contains a cysteine protease domain, is essential for viral replication, making it an attractive target for a drug discovery campaign.

Virus 162
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A Guide to DNA Damage Response and Innate Immunity

Drug Target Review

The Transcreener HTS Assay platform accelerates these efforts by providing robust and easy-to-use biochemical assays for key enzymes in the pathways. In this guide, we provide an overview of the DDR and innate immune pathways and describe assay systems for key therapeutic targets.

DNA 104
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Reversible Dual-Covalent Molecular Locking of the 14-3-3/ERR? Protein–Protein Interaction as a Molecular Glue Drug Discovery Approach

Covalent Modifiers

Biochemical assays and X-ray crystallographic studies validated the ternary covalent complex formation and overall PPI stabilization via dynamic covalent crosslinking. The PPI between the hub protein 14-3-3 and estrogen-related receptor γ (ERRγ) was used as a pharmacologically relevant case study.

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Biochemical and Structural Studies of Protein Tyrosine Phosphatase PTP‐PEST (PTPN12) in Search of Small Molecule Inhibitors

Chemical Biology and Drug Design

The invitro biochemical assays validated that J1-65 inhibits PTP-PEST activity competitively and the inhibitor binding stabilizes the protein-ligand complex. An in-house molecule library was screened using in silico molecular docking, and a myo-inositol derivative was identified as a potent hit molecule.