Andrew P. Riley

The Human Gut Microbiome Metabolizes Diverse Bioactive Coumarins via α,β-Unsaturated Lactone Reduction

Gabrielle Mingolelli, Rasha M. Bashatwah, Megan J. Jurek, Isabel M. Chauvin et autres

High Resolution Image Download MS PowerPoint Slide The gut microbiome can influence drug efficacy through the direct metabolism of bioactive molecules. Despite numerous high-throughput screens for drug–microbiome interactions, the gut microbial metabolism of many bioactive compounds and its impact on treatment efficacy …

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An accessory orthosteric ligand binding site in the (α3)3(β4)2 nicotinic acetylcholine receptor regulates channel activation

Gauri Kulkarni, Megan J. Jurek, Andrew P. Riley, Christian J. Peters

The α3β4 nicotinic acetylcholine receptor (nAChR) is a heteropentameric ligand-gated channel whose distribution includes reward circuits of the brain, where it regulates expression of drug withdrawal symptoms. α3β4 nAChRs form two stoichiometries in the absence of other subunits, containing orthosteric binding sites …

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Fifteen Years, One Mission: Innovative, Inspirational, and Impactful Discoveries

Simone V. Bigi-Botterill, Chiara Borsari, Amanda W. Dombrowski, Michelle A. Estrada et autres

Recommendations F ifteen years ago, the American Chemical Society (ACS) introduced ACS Medicinal Chemistry Letters as a new means to rapidly report new findings in medicinal chemistry.In the inaugural issue of ACS Medicinal Chemistry Letters, the journal's founding Editor-in-Chief, Dennis Liotta, invited …

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Structural Biology Enabling Drug Discovery

David E. Heppner, Simone V. Bigi-Botterill, Andrew P. Riley, Kelly Chibale et autres

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In This Issue, Volume 16, Issue 9

Andrew P. Riley

Comprehensive pharmacokinetics and ADME evaluation of Akuamma alkaloids

Abhishek Gour, Simone M. Creed, Andrew P. Riley, Abhisheak Sharma

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In This Issue, Volume 16, Issue 4

Andrew P. Riley

Proteolysis-targeting chimeras (PROTACs) are becoming increasingly popular modalities in drug discovery.However, because of their chimeric nature, PROTACs typically fall in Beyond Rule of Five chemical space, which can limit the permeability and bioavailability.Moreover, due in part to their size, highly structurally related …

BPS2025 - Identification and functional characterization of antinociceptive α9α10 nicotinic acetylcholine receptor antagonists

Kyle M. Kremiller, Gauri Kulkarni, Hirushi T. Gunasekara Kalu Arachchige, Yavnika Kashyap et autres

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BPS2025 - Identification and functional characterization of antinociceptive alpha9alpha10 nicotinic acetylcholine receptor antagonists

Kyle M. Kremiller, Gauri Kulkarni, Hirushi T. Gunasekara Kalu Arachchige, Yavnika Kashyap et autres

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BPS2025 - An orthosteric ligand binding site in the accessory subunit of α3β4 nicotinic acetylcholine receptors is revealed by covalent modification

Gauri Kulkarni, Megan J. Jurek, Andrew P. Riley, Christian J. Peters

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Pharmacological characterization of the novel selective kappa opioid receptor agonists 10-Iodo-Akuammicine and 10-Bromo-akuammicine in mice

Kathryn Bland, Chongguang Chen, Peng Huang, Conrad K. Ho et autres

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Semi-synthesis in the exploration of opioid-targeting natural products

Andrew P. Riley

Covering: up to May 2025Since the isolation of morphine from opium, chemists have sought to modify its chemical structure in hopes of developing a safer, less addictive pain killer. At the same time, these novel morphine derivatives have provided new chemical tools …

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