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New review article in Nature Reviews Drug Discovery on Functional Dynamics of GPCRs, based on discussions from a great CECAM GPCR meeting. Congrats to Vittorio, Paolo, and all the other coauthors! #NMR #NMRchat nature.com/articles/s4157…

Excited to share our work on GPCR antagonism: Contrary to popular belief, inverse agonists can bind to and act via GPCR:G protein complexes. We show this at kappa-opioid receptors by cellular, radioligand binding and cryoEM studies. A 🧵: USC USC Dornsife College of Letters, Arts & Sciences nature.com/articles/s4158…

Molecular mechanisms of inverse agonism via κ-opioid receptor–G protein complexes nature.com/articles/s4158… the canonical model of receptor antagonism and offers crucial insights into GPCR pharmacology.

Cornelius Gati USC USC Dornsife College of Letters, Arts & Sciences Congratulations Gati! and team, wonderful work and amazing structures!

Molecular mechanisms of inverse agonism via κ-opioid receptor–G protein complexes GPCRの定常活性を抑え込むインバースアゴニスト、これまで不活性型フォームでGタンパク結合を抑え込むと考えられてきたけど、実はそうではなかった と言う、お話 nature.com/articles/s4158…

A new paper uncovers that certain κ-opioid receptor inverse agonists form receptor-G protein complexes, even in inactive states, challenging the classic GPCR activation model nature.com/articles/s4158…

Molecular mechanisms of inverse agonism via κ-opioid receptor–G protein complexes | Nat Chem Biol doi.org/10.1038/s41589…

A platform for the continuous selection of protein aggregation inhibitors from genetically encoded cyclic peptide libraries in E. coli is developed, here used to develop inhibitors against amyloid-β42 and human islet amyloid polypeptide aggregation nature.com/articles/s4158…

Molecular mechanisms of inverse agonism via κ-opioid receptor–G protein complexes. Nature Chemical Biology Check the #cryoEM #structure of this #membrane #protein in the UniTmp database: pdbtm.unitmp.org/entry/8vvf nature.com/articles/s4158…

Really looking forward to hosting Dr. Derek Abbott for tomorrow's Raiziss seminar. Don't miss it! BBCB Graduate Group Penn Microbiology Penn Medicine

Great review from @RenataMarchette Leandro Vendruscolo and George Koob on Dynorphin/KOR system in substance use disorders and hyperkatifeia Give it a read 👇 link.springer.com/epdf/10.1007/s…

A cannabinoid bitopic, biased and peripheral agonist analgesic with limited tolerance and tetrad in Nature. Work led by Vipin Rangari with Rob Gereau Dror Lab kaavya Krishna Kumar Center for Clinical Pharmacology WashU Medicine Anesthesiology A short thread nature.com/articles/s4158…

Excited to share work led by Preston Anderson and Peng Xiao in collaboration with Jinpeng Sun (just like old times when we were postdocs in Lefko lab). We find that beta-arrestins form biomolecular condensates to regulate GPCR function - biorxiv.org/content/10.110…

We have innovated design of templates for CRISPR/Cas9 editing which allows efficient introduction of epitope tags in vivo. It is a simple hack which we hope to be broadly useful. Work by talented graduate student Chuanping Zhao. nature.com/articles/s4146…

Excited to share the final version of our paper! In this study, we demonstrate that the mu opioid receptor increases G protein activity on endosomes in a manner that doesn’t require receptor internalization. Check it out! pnas.org/doi/10.1073/pn…

Excited to present our preprint on the structure-function relationship of anaphylatoxin complement receptors. A casual number of 19 structures deciphering ligand recognition mechanisms, G protein/arrestin and species specific signaling. Check it out! biorxiv.org/content/biorxi…

New preprint from Daniel X. Du Fitzpatrick Laboratory shows #femtosecond light pulses can lens electron beams, promising higher contrast in #cryoET and better aberration correction in #cryoEM biorxiv.org/content/10.110… Experiments made possible by support from CZI Science #ImagingTheFuture