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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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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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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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Synthesis Methods and Therapeutic Journey of Carprofen and Its Derivatives: A Review

Chemical Biology and Drug Design

Although it is currently only used in veterinary therapy, carprofen proves to be a molecule with a versatile therapeutic potential for human pharmacotherapy. Moreover, the molecule is a target in the drug discovery process for the development of new bioactive compounds.

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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 GPCR agonists, including antibodies, are shaping the future of metabolic care

Drug Target Review

Confo Therapeutics , led by CEO Dr Cedric Ververken, is at the forefront of developing innovative GPCR-targeted therapies using its proprietary ConfoBody ® platform. In addition to generating agonistic antibodies, Confo is also successfully applying the ConfoBody/ConfoChimer technology to drugging GPCR with small molecules.