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Small Molecule of the Year – 2022

Drug Hunter

We asked the global drug discovery community to nominate and vote on their favorite molecule from 2022, and the results are in. The 2022 winner, with the most overall votes across the ten finalist molecules , is BMS’ oral, deuterated allosteric TYK2 inhibitor, deucravacitinib, the first new treatment for plaque psoriasis in nearly a decade.

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Reviewing the IDH1 Mutation‐Mediated Mechanism of Drug Resistance and Revisiting Its Overcoming Strategies

Chemical Biology and Drug Design

At present, there are few studies on the drug resistance of mIDH1 inhibitors. Currently, the FDA has granted approval for the use of the small molecule inhibitor Ivosidenib (AG-120) in the treatment of IDH1-mutated AML and cholangiocarcinoma. Representative mIDH1 inhibitors and their binding modes were also discussed.

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Interactions of small molecule inhibitors with secreted phospholipase A2: A review of the structural data

Chemical Biology and Drug Design

sPLA 2 inhibitors have been developed for the treatment of inflammatory and other conditions such as cardiovascular disease, arteriosclerosis and rheumatoid arthritis. The three-dimensional structures presented in this review have been published by various research groups and have been deposited in the Protein Data Bank.

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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.

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Differential Efficacy of Small Molecules Dynasore and Mdivi-1 for the Treatment of Dry Eye Epitheliopathy or as a Countermeasure for Nitrogen Mustard Exposure of the Ocular Surface [Cellular and Molecular]

ASPET

Dynasore and dyngo-4a, small molecules developed to inhibit the GTPase activity of classic dynamins DNM1, DNM2 and DNM3, but not mdivi-1, a specific inhibitor of DNM1L, protect corneal epithelial cells exposed to the oxidant tert-butyl hydroperoxide (tBHP).

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How GPCR-targeting therapies are advancing the fight against inflammatory disease

Drug Target Review

In this article, Stephan Schann, Chief Scientific Officer at Domain Therapeutics , explains why this class of drug target is so useful despite the challenges they present. Despite this, the therapeutic potential of targeting most GPCRs remains untapped, as only 10 percent of GPCRs have been drugged.

Disease 59
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Bristol Myers Squibb Highlights Targeted Protein Degradation Data, Including CELMoD Agents, at EHA 2025

The Pharma Data

The presentations highlight the ongoing progress and growing promise of the company’s innovative therapeutic platform, featuring its investigational oral CELMoD™ (Cereblon E3 Ligase Modulating Drugs) agents mezigdomide, iberdomide, and golcadomide, alongside its first-in-class, oral BCL6 (B-Cell lymphoma 6) ligand-directed degrader (LDD) BMS-986458.