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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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Betulinic acid reduces inflammation in rats with sepsis?induced myocardial dysfunction by inhibiting TLR4/MyD88/NF??B signaling pathway

Chemical Biology and Drug Design

Betulinic acid (BA) improved cardiac function, reduced myocardial injury, and attenuated inflammation in the cecal ligation and puncture (CLP) rats, indicating BA as a potential drug for sepsis-induced myocardial dysfunction.

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Variability in biological activity measurements reported in the drug discovery literature

Molecular Design

In the Compatibility Issues section the authors state: Looking beyond laboratory-to-laboratory variability of assays that are nominally the same, there are numerous reasons why literature results for different assays measured against the same “target” may not be comparable.

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SARS-CoV-2 main protease. Crowdsourcing, peptidomimetics and fragments

Molecular Design

Satchel Paige (1906-1982) The COVID Moonshot and OSC19 are examples of what are sometimes called crowdsourced or open source approaches to drug discovery. Open source drug discovery originated with OSDD in India and it should be noted that the approach has also been pioneered for malaria by OSM.

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On quality criteria for covalent and degrader probes

Molecular Design

I’ll be taking a look at H2023 (Expanding Chemical Probe Space: Quality Criteria for Covalent and Degrader Probes) in this post and this article has also been discussed In The Pipeline. This Perspective is intended to jumpstart this important scientific discussion. Subscripting doesn't work well in blogger and so I'll use K.i

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Unique self-activating proteins for drug discovery

Drug Target Review

fowleri cases 3 suggest that combinations of antibiotic and antifungal drugs, including azithromycin, amphotericin B, fluconazole, rifampin and miltefosine (the latter originally formulated for leishmaniasis and cancer chemotherapy 4 ), have a minimal impact on survival. The activity of Z#1334 in inhibiting Nf Ga7 GTPase assay (IC 50 of 2.4

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Article FDA Thank You Draft guidance on potency assays for CGT products garners extensive stakeholder input

Agency IQ

Assays are tests designed to assess various properties (like potency) of chemical or biological samples. In addition to assessing binding capabilities, assays can also be used to characterize the activity elicited by a product, whether bound or unbound to the target of interest. Code in order to have their products approved by the FDA.