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Small Molecule of the Year – 2022

Drug Hunter

. #2: MRTX1133 (Mirati Therapeutics/Array BioPharma, 21%) The 2nd place runner-up is MRTX1133 , the non-covalent KRAS(G12D) inhibitor and is the first reported inhibitor specific for G12D, which makes up as much as 33% of all KRAS mutations and carries a 2 to 3-fold higher disease burden than G12C. LP0200 has completed a Ph.

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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. Due to their roles in inflammation, the sPLA 2 enzymes are of much medicinal interest.

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Researchers devise new way to target and correct disease-related proteins

Broad Institute

Related groups Xavier lab Over the past two decades, large genetic studies have linked tens of thousands of DNA variants to thousands of human traits and diseases. Yet, correcting the effects of those variants to treat disease has been hampered in part by the lack of precise molecular tools to do so.

Disease 139
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Selective Covalent Inhibiting JNK3 by Small Molecules for Parkinson's Diseases

Covalent Modifiers

Wherein JNK3 is specifically expressed in brain and emerges as therapeutic target, especially for neurodegenerative diseases. However, developing JNK3 selective inhibitors as chemical probes to investigate its therapeutic potential in diseases remains challenging.

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More LRRK2 On-Target Toxicity?

Drug Hunter

LRRK2 has been a hotly pursued drug target for Parkinson’s Disease based on human genetics.

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New avenues for rare disease treatment

Drug Target Review

Almost every one of us will know someone with a neurodegenerative disease such as Alzheimer’s or Parkinson’s. It is less common to know someone with a rare genetic disease; but while individually rare, collectively they have an enormous impact. This will, in turn, slow the progression of, or even halt, the disease.

Disease 113
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RNA processing in health and disease: challenges and opportunities of the field

Drug Target Review

In this article Drug Target Review’s Izzy Wood spoke to Sam Hasson, Director of Target Biology at Rgenta Therapeutics, a biotech firm in Massachusetts, US, that aims to develop small molecule therapeutics to target RNA processing.

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