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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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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

Based on the druggability of DR3penA, we sought to investigate its effects on respirable particulate silicon dioxide (SiO 2 )- and soluble chemical paraquat (PQ)-induced pulmonary fibrosis in this study by using western blot, RT-qPCR, immunofluorescence, H&E and Masson staining, immunohistochemistry and serum biochemical assays.

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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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Target-directed cancer: protein-ligand interactions  

Drug Target Review

The mission of the CCDD is to discover novel small-molecule therapeutics for the treatment of cancer and progress them to hypothesis testing phase 1 clinical trials. We often screen using a biochemical assay, but we can conduct cell-based screening as well. We need to build the assays that we need for compound screening.

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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

These dual-covalent small molecules reversibly react with a nucleophilic amino acid on each of the partner proteins to dynamically crosslink the protein complex. Based on a focused library of dual-reactive small molecules, a molecular glue tool compound was rapidly developed.

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Accelerating Medicinal Chemistry Cycle Times Through Cloud-Accessible Smart Automated Labs - A Preview of Strateos’ Presentation at SLAS 2022

The Strateos Blog: Drug Discovery

Progress from target ID through to IND submission in conventional workflows can take upwards of 6+ years, where success hinges on iterative cycles of DMTA.