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Milka Kostic
Every month the editors of Cell Chemical Biology bring you highlights of the most recent chemical biology literature. Our September 2016 selection includes the discovery of PZM21, a μOR biased agonist with minimal side effects, and the role of cholesterol in Hedgehog signaling pathway.
September 22, 2016: Cell Chemical Biology
Aashish Manglik, Henry Lin, Dipendra K Aryal, John D McCorvy, Daniela Dengler, Gregory Corder, Anat Levit, Ralf C Kling, Viachaslau Bernat, Harald Hübner, Xi-Ping Huang, Maria F Sassano, Patrick M Giguère, Stefan Löber, Da Duan, Grégory Scherrer, Brian K Kobilka, Peter Gmeiner, Bryan L Roth, Brian K Shoichet
Morphine is an alkaloid from the opium poppy used to treat pain. The potentially lethal side effects of morphine and related opioids-which include fatal respiratory depression-are thought to be mediated by μ-opioid-receptor (μOR) signalling through the β-arrestin pathway or by actions at other receptors. Conversely, G-protein μOR signalling is thought to confer analgesia. Here we computationally dock over 3 million molecules against the μOR structure and identify new scaffolds unrelated to known opioids...
August 17, 2016: Nature
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