Structural basis of allosteric modulation of metabotropic glutamate receptor activation and desensitization.

Alexa Strauss,Alberto J Gonzalez-Hernandez,Joon Lee,Nohely Abreu,Purushotham Selvakumar,Leslie Salas-Estrada,Melanie Kristt,Dagan C Marx,Kristen Gilliland,Bruce J Melancon,Marta Filizola,Joel Meyerson,Joshua Levitz

bioRxiv : the preprint server for biology（2023）

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摘要

-Agonists and PAMs drive mGluR activation, desensitization, and endocytosis-PAMs are desensitization-biased and synergistic with agonists-Four combinatorial ligand conditions reveal an ensemble of full-length mGluR structures with novel interfaces-Activation and desensitization involve rolling TMD interfaces which are re-shaped by PAM.

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关键词

metabotropic glutamate receptor activation,allosteric modulation

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