March 2022 Crinetics Pharmaceuticals Expands Executive Team With Appointment Of James Hassard As Chief therapeutics for rare endocrine diseases and endocrine-related tumors, today announced the appointment of James

, Vlaams Instituut Biotechnologie , at the Vrije Universiteit Brusle, Brussels, Belgium, has been named

September 2022 "Morphine, the most widely used analgesic, relieves severe pain by activating the μ-opioid receptor (MOR), whereas naloxone, with only slight structural changes compared to morphine, exhibits inhibitory effect, and is used to treat opioid abuse. The mechanism by which the MOR distinguishes between the two is unclear. Molecular dynamics (MD) simulations on a 1-μs time scale and metadynamics-enhanced conformational sampling are used here to determine the different interactions of these two ligands with MOR: morphine adjusted its pose by continuously flipping deeper into the pocket, whereas naloxone failed to penetrate deeper because its allyl group conflicts with several residues of MOR. The endogenous peptide ligand endomorphin-1 (EM-1) underwent almost no significant conformational changes during the MD simulations. To validate these processes, we employed GIRK4S143T, a MOR-activated Gβγ-protein effector, in combination with mutagenesis and electrophysiological recordings. We verified the role of some key residues in the dynamic recognition of naloxone and morphine and identified the key residue I322, which leads to differential recognition of morphine and naloxone while assisting EM-1 in activating MOR. Reducing the side chain size of I322 (MORI322A) transformed naloxone from an inhibitor directly into an agonist of MOR, and I322A also significantly attenuated the potency of MOR on EM-1, confirming that binding deep in the pocket is critical for the agonistic effect of MOR. This finding reveals a dynamic mechanism for the response of MOR to different ligands and provides a basis for the discovery of new ligands for MOR at the atomic level." Read more at the source #DrGPCR #GPCR #IndustryNews

signaling.[19–23] The 1988 Nobel Prize in Physiology or Medicine went to George Herbert Hitchings, Sir James Nobel Prize: Three Named for Medicine, Physiology Award. Sir James W. Sir James W. Sir James Whyte Black OM. 14 June 192422 March 2010.

time, the neurexins, another family of adhesion molecules that also happened to be targeted by the same The excitement I felt when I first attended back in Boston is the same one I feel now that I am the organizer Of course, there is the famous parade popularized by the James Bond movie Spectre.

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December 2021 " Dame Carol Robinson DBE, FRS, FRSC, FMedSci, Oxford University’s first female Professor

While early evidence for the role of oligomerization in receptor signaling came from ensemble biochemical

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