Search Results - "Rossetti, Thomas"
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On-demand male contraception via acute inhibition of soluble adenylyl cyclase
Published in Nature communications (14-02-2023)“…Nearly half of all pregnancies are unintended; thus, existing family planning options are inadequate. For men, the only choices are condoms and vasectomy, and…”
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Soluble adenylyl cyclase inhibition prevents human sperm functions essential for fertilization
Published in Molecular human reproduction (01-09-2021)“…Abstract Soluble adenylyl cyclase (sAC: ADCY10) has been genetically confirmed to be essential for male fertility in mice and humans. In mice, ex vivo studies…”
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Assessing potency and binding kinetics of soluble adenylyl cyclase (sAC) inhibitors to maximize therapeutic potential
Published in Frontiers in physiology (28-09-2022)“…In mammalian cells, 10 different adenylyl cyclases produce the ubiquitous second messenger, cyclic adenosine monophosphate (cAMP). Amongst these…”
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Corrigendum: Assessing potency and binding kinetics of soluble adenylyl cyclase (sAC) inhibitors to maximize therapeutic potential
Published in Frontiers in physiology (06-03-2023)“…[This corrects the article DOI: 10.3389/fphys.2022.1013845.]…”
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Design, Synthesis, and Pharmacological Evaluation of Second-Generation Soluble Adenylyl Cyclase (sAC, ADCY10) Inhibitors with Slow Dissociation Rates
Published in Journal of medicinal chemistry (24-11-2022)“…Soluble adenylyl cyclase (sAC: ADCY10) is an enzyme involved in intracellular signaling. Inhibition of sAC has potential therapeutic utility in a number of…”
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Optimizing Small Molecule Inhibitors of Soluble Adenylyl Cyclase (sAC) for Use as Male Contraceptives
Published 01-01-2023“…Cyclic adenosine monophosphate (cAMP) is a ubiquitous second messenger that plays an important role in a wide variety of signal transduction pathways. The…”
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Dissertation -
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Scaffold Hopping and Optimization of Small Molecule Soluble Adenyl Cyclase Inhibitors Led by Free Energy Perturbation
Published in Journal of chemical information and modeling (08-05-2023)“…Free energy perturbation is a computational technique that can be used to predict how small changes to an inhibitor structure will affect the binding free…”
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Short-term CaMKII inhibition with tatCN19o does not erase pre-formed memory in mice and is neuroprotective in pigs
Published in The Journal of biological chemistry (01-05-2023)“…The Ca2+/calmodulin-dependent protein kinase II (CaMKII) is a central regulator of learning and memory, which poses a problem for targeting it therapeutically…”
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Discovery of TDI-10229: A Potent and Orally Bioavailable Inhibitor of Soluble Adenylyl Cyclase (sAC, ADCY10)
Published in ACS medicinal chemistry letters (12-08-2021)“…Soluble adenylyl cyclase (sAC) has gained attention as a potential therapeutic target given the role of this enzyme in intracellular signaling. We describe…”
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Journal Article