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Chimeric deubiquitinase engineering reveals structural basis for specific inhibition of the mitophagy regulator USP30

Covalent Modifiers

Whether enhanced mitochondrial quality control through inhibition of USP30 can protect dopaminergic neurons is currently being explored in a clinical trial for Parkinsons disease. However, the molecular basis for specific inhibition of USP30 by small molecules has remained elusive.

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ALS drug effectively treats Alzheimer's disease in new animal study

Science Daily: Pharmacology News

Experimental drug NU-9 -- a small molecule compound approved by the U.S. Food and Drug Administration (FDA) for clinical trials for the treatment of amyotrophic lateral sclerosis (ALS) -- improves neuron health in animal models of Alzheimer's disease, according to a new study.

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Small Molecule of the Year – 2022

Drug Hunter

The molecule was the first allosteric TYK2 inhibitor to enter clinical trials, is the first JAK-family kinase inhibitor approved for psoriasis, and is also the first approved drug targeting a pseudokinase domain. Emraclidine was developed by rational design and is the only selective M4 PAM in clinical trials.

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Redefining Acceleration of the Drug Development Journey

PPD

Accelerate your drug development and clinical trial goals and benefit from our 360° CDMO and CRO solutions and expertise. Partner with us The post Redefining Acceleration of the Drug Development Journey appeared first on PPD.

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Molecules on the Move: April ’23

Drug Hunter

This article compiles 20+ recent small molecules of general interest in the news in April 2023, with structures where they are available.

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Antibody Drug Conjugates: windows of opportunity

Drug Target Review

These therapies have broadened treatment options for patients to expand beyond the more traditional small molecule drug alternatives. 2 However, when dosed at the MTD, ADCs display improved efficacy over small molecules in oncology trials. 3D rendering of Antibody Drug Conjugate Molecules.

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Mutate and Conjugate: A Method to Enable Rapid In-Cell Target Validation

Covalent Modifiers

[link] Target validation remains a challenge in drug discovery, which leads to a high attrition rate in the drug discovery process, particularly in Phase II clinical trials. Consequently, new approaches to enhance target validation are valuable tools to improve the drug discovery process.