Journal Papers

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5-HT1B receptor activation produces rapid antidepressant-like effects in rodents
5-HT1B receptor activation produces rapid antidepressant-like effects in rodents
Ketamine is noted for its rapid onset antidepressant response and effectiveness in patients with treatment resistant depression. While most research has focused on glutamatergic mechanisms, recent studies show that antidepressant-like effects in rodents are dependent upon the serotonergic (5-HT) system and suggest a potential contribution of the 5-HT1B receptor.
Journal Papers

December 16, 2024

Novel Macrocyclic NLRP3 Inhibitors
Novel Macrocyclic NLRP3 Inhibitors
Stefanie Mesch, Jonathan Shannon, David Miller, Angus MacLeod, Léa Bouché, Heather J. Johnston, Kim…
Journal Papers

November 25, 2024

To homeostasis and beyond! Recent advances in the medicinal chemistry of heterobifunctional derivatives
To homeostasis and beyond! Recent advances in the medicinal chemistry of heterobifunctional derivatives
Diana Castagna, Benoit Gourdet, Roland Hjerpe, Philip MacFaul, Andrew Novak, Guillaume Revol, Etienne Rochette, Allan Jordan Abstract The field…
Journal Papers

September 19, 2024

A decentralized solid compound storage facility managed by a centralized electronic platform at a growing drug discovery company
A decentralized solid compound storage facility managed by a centralized electronic platform at a growing drug discovery company
Ting Qin, Sergio Ernesto Ruiz Hernandez, Jason Shiers, Matthew Crittall, Andrew Novak, Colin Sambrook Smith Abstract Within a growing drug discovery company, scientists acquire (either…
Journal Papers

May 11, 2024

Breaking Bad Proteins—Discovery Approaches and the Road to Clinic for Degraders
Breaking Bad Proteins—Discovery Approaches and the Road to Clinic for Degraders
Corentin Bouvier, Rachel Lawrence, Francesca Cavallo, Wendy Xolalpa, Allan Jordan, Roland Hjerpe, Manuel S.
Journal Papers

March 26, 2024

Discovery of the Potent and Selective ATR Inhibitor Camonsertib (RP-3500)
Discovery of the Potent and Selective ATR Inhibitor Camonsertib (RP-3500)
W Cameron Black, Abbas Abdoli, Xiuli An, Anick Auger, Patrick Beaulieu, Michel Bernatchez, Cathy Caron, Amandine Chefson, Sheldon Crane, Mohamed Diallo, Stéphane Dorich, Lee D…
Journal Papers

February 22, 2024

Structure–activity relationships for the G-quadruplex-targeting experimental drug QN-302 and two analogues probed with comparative transcriptome profiling and molecular modeling
Structure–activity relationships for the G-quadruplex-targeting experimental drug QN-302 and two analogues probed with comparative transcriptome profiling and molecular modeling
Ahmed Abdullah Ahmed, Shuang Chen, Maria Roman-Escorza, Richard Angell, Sally Oxenford, Matthew McConville, Naomi Barton, Mihiro Sunose, Dan Neidle, Shozeb Haider, Tariq Arshad & Stephen Neidle …
Journal Papers

February 11, 2024

Key aspects of modern GPCR drug discovery
Key aspects of modern GPCR drug discovery
Phil Addis, Utsav Bali, Frank Baron, Adrian Campbell, Steven Harborne, Liz Jagger, Gavin Milne, Martin Pearce, Elizabeth M Rosethorne, Rupert Satchell, Denise Swift, Barbara Young, John…
Journal Papers

January 29, 2024

TAAR1 agonists improve glycemic control, reduce body weight and modulate neurocircuits governing energy balance and feeding
TAAR1 agonists improve glycemic control, reduce body weight and modulate neurocircuits governing energy balance and feeding
Nina Dedic, Lien Wang, Eva Hajos-Korcsok, Jacob Hecksher-Sørensen, Urmas Roostalu, Steven P Vickers, Serena Wu, Christoph Anacker, Colleen Synan, Philip G Jones, Snezana Milanovic, Seth…
Journal Papers

January 16, 2024

Discovery of Five SOS2 Fragment Hits with Binding Modes Determined by SOS2 X-Ray Cocrystallography
Discovery of Five SOS2 Fragment Hits with Binding Modes Determined by SOS2 X-Ray Cocrystallography
Christopher R. Smith, Dan Chen,James G. Christensen, René Coulombe, James Féthière, Robin J. Gunn,…
Journal Papers

December 29, 2023

Melatonin and Its Metabolites Can Serve as Agonists on the Aryl Hydrocarbon Receptor and Peroxisome Proliferator-Activated Receptor Gamma
Melatonin and Its Metabolites Can Serve as Agonists on the Aryl Hydrocarbon Receptor and Peroxisome Proliferator-Activated Receptor Gamma
Andrzej T Slominski, Tae-Kang Kim, Radomir M Slominski, Yuwei Song, Shariq Qayyum, Wojciech Placha, Zorica Janjetovic, Konrad Kleszczyński, Venkatram Atigadda, Yuhua Song, Chander Raman, Cornelis…
Journal Papers

October 23, 2023

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