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

Covalent Modifiers

Proceedings of the National Academy of Sciences 2024 , 121 (6), e2317756121. 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. Gunaydin, H.; Boezio, A. McLean, T. Watters, J.; Bergstrom, D.

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Electrophilic proximity-inducing synthetic adapters enhance universal T cell function by covalently enforcing immune receptor signaling [@RulloLab]

Covalent Modifiers

Rullo Molecular Therapy 2024 DOI: [link] Proximity-induction of cell-cell interactions via small molecules represents an emerging field in basic and translational sciences. Lake, Galina Denisova,Joanne A. Hammill,Jonathan L. Bramson, Anthony F.

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Peptide–Drug Conjugates: An Emerging Direction for the Next Generation of Peptide Therapeutics

Covalent Modifiers

3c01835 Building on recent advances in peptide science, medicinal chemists have developed a hybrid class of bioconjugates, called peptide–drug conjugates, that demonstrate improved efficacy compared to peptides and small molecules independently. Moore Journal of Medicinal Chemistry 2024 DOI: 10.1021/acs.jmedchem.3c01835

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How to find a drug: the past, present and future of small molecule drug discovery?

DrugBaron

Despite the current hype around so called “advanced therapies”, which range from gene editing to cell therapies, and the inexorable advance of biologic therapeutics such as monoclonal antibodies, even in 2022 the majority of drugs in development and reaching patients are still small organic molecules.

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Covalent Modifiers - Untitled Article

Covalent Modifiers

Rullo, Molecular Therapy: Oncology , 2024 , 200842, [link] Proximity-induction of cell-cell interactions via small molecules represents an emerging field in basic and translational sciences. Lake, Galina Denisova, Joanne A. Hammill, Jonathan L. Bramson, Anthony F.