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Small Molecules Evolve

Drug Hunter

Small molecule drugs make up most of the drugs we take conveniently as pills, including painkillers like ibuprofen (Advil), antibiotics like penicillin and amoxicillin, or cholesterol-lowering drugs like atorvastatin (Lipitor). The small molecules drugs of today look nothing like the molecules of the 1970s.

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Bayer partners with RNA drugmaker to develop new cancer therapies

BioPharma Drive: Drug Pricing

Under a collaboration with NextRNA Therapeutics, Bayer will access the biotech’s platform to target long, non-coding RNA interactions with small molecule drugs.

RNA 293
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Synthesis and Investigation of Peptide–Drug Conjugates Comprising Camptothecin and a Human Protein‐Derived Cell‐Penetrating Peptide

Chemical Biology and Drug Design

ABSTRACT Drug targeting strategies, such as peptidedrug conjugates (PDCs), have arisen to combat the issue of off-target toxicity that is commonly associated with chemotherapeutic small molecule drugs.

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Lost brain function restored in mice after stroke

Science Daily: Pharmacology News

Researchers have succeeded in restoring lost brain function in mouse models of stroke using small molecules that in the future could potentially be developed into a stroke recovery therapy.

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Development of a Covalent Small Molecule Downmodulator for the Transcription Factor Brachyury

Covalent Modifiers

Herein, we use afatinib as a lead to undertake a structure-based drug design approach, aided by mass-spectrometry and x-ray crystallography, to develop DHC-156, a small molecule that more selectively binds brachyury and downmodulates it as potently as afatinib.

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Discovery of lirafugratinib (RLY-4008), a highly selective irreversible small-molecule inhibitor of FGFR2

Covalent Modifiers

The most common adverse effects are hyperphosphatemia caused by FGFR1 inhibition and diarrhea due to FGFR4 inhibition, as current therapies are not selective among the FGFRs.

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Chemoselective Covalent Modification of K-Ras(G12R) with a Small Molecule Electrophile

Covalent Modifiers

While small molecule inhibitors for the G12C mutant have been successfully developed, allele-specific inhibition for other KRAS hotspot mutants remains challenging. Shokat Journal of the American Chemical Society 2022 144 (35), 15916-15921 DOI: 10.1021/jacs.2c05377