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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

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

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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). Our approach is to treat cancer in fundamentally new ways based on emergent data to optimise therapeutic outcomes.

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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

Our previous research showed that the novel and low-toxicity peptide DR3penA had a strong antifibrotic effect on a bleomycin-induced murine model. The results showed that DR3penA alleviated the extent of fibrosis by inhibiting the expression of fibronectin and collagen I and suppressed oxidative stress and EMT in vitro and in vivo.

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Target-directed cancer: protein-ligand interactions  

Drug Target Review

Could you provide an overview of your research on target directed cancer drug discovery, particularly your focus on protein lagging interactions. How do structural biology and biochemical methods play a role in your world? We often screen using a biochemical assay, but we can conduct cell-based screening as well.

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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

SLAS 2022 is set to be an exciting conference where scientists can come together to learn about the innovative technologies transforming the way life sciences research is executed. 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.

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Top 10 Drug Discovery Trends at the Top 20 Pharma

PerkinElmer

Small screens are better than large ones. Biochemical assays have the highest success rate. Small molecules are making a comeback. These simple, stable compounds, used to treat various conditions, are the focus for 78% of preclinical research. Biologics are booming. Think again.

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On quality criteria for covalent and degrader probes

Molecular Design

In any case, it needed to be made clear that the quality criteria proposed by the authors for covalently acting small-molecule probes only apply to probes that act irreversibly. Carefully designed biochemical assays used in determining IC50 values can be well-suited as surrogates for k.inact/K.i measurements. (