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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). This platform can help identify and optimise pharmacologic properties of new drugs.

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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. PTP-PEST is considered an important drug target owing to its involvement in cancer progression and myocardial injury.

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

Covalent Modifiers

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. Here, we optimized a CHIKV nsP2 protease (nsP2pro) biochemical assay for the screening of a 6,120-compound cysteine-directed covalent fragment library.

Virus 162
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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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Reversible Dual-Covalent Molecular Locking of the 14-3-3/ERR? Protein–Protein Interaction as a Molecular Glue Drug Discovery Approach

Covalent Modifiers

2c12781 Molecules that stabilize protein–protein interactions (PPIs) are invaluable as tool compounds for biophysics and (structural) biology, and as starting points for molecular glue drug discovery. Cossar, and Luc Brunsveld Journal of the American Chemical Society 2023 DOI: 10.1021/jacs.2c12781

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A Guide to DNA Damage Response and Innate Immunity

Drug Target Review

Both are a focus for exciting new small-molecule drug therapeutics that target cancers and autoimmune disorders. The Transcreener HTS Assay platform accelerates these efforts by providing robust and easy-to-use biochemical assays for key enzymes in the pathways.

DNA 104
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The peptide DR3penA exhibits antifibrotic activity in multiple pulmonary fibrosis models induced by particulate and soluble chemical fibrogenic agents [Gastrointestinal, Hepatic, Pulmonary, and Renal]

ASPET

The incidence of ILDs associated with exposure to multiple hazards, such as inhaled particles, fibers, and ingested soluble chemicals, is increasing yearly, and there are no ideal drugs currently available. Further study revealed that DR3penA may mitigate pulmonary fibrosis by negatively regulating the PI3K/AKT pathway and MAPK pathway.