Universal allosteric mechanism for Gα activation by GPCRs

T Flock, CNJ Ravarani, D Sun, AJ Venkatakrishnan… - Nature, 2015 - nature.com
G protein-coupled receptors (GPCRs) allosterically activate heterotrimeric G proteins and
trigger GDP release. Given that there are∼ 800 human GPCRs and 16 different Gα genes,
this raises the question of whether a universal allosteric mechanism governs Gα activation.
Here we show that different GPCRs interact with and activate Gα proteins through a highly
conserved mechanism. Comparison of Gα with the small G protein Ras reveals how the
evolution of short segments that undergo disorder-to-order transitions can decouple regions …

[PDF][PDF] Universal allosteric mechanism for Ga activation by GPCRs

DB Veprintsev, MM Babu - mrc-lmb.cam.ac.uk
G protein-coupled receptors (GPCRs) allosterically activate heterotrimeric G proteins and
trigger GDP release. Given that there are 800 human GPCRs and 16 different Ga genes, this
raises the question of whether a universal allosteric mechanism governs Ga activation. Here
we show that different GPCRs interact with and activate Ga proteins through a highly
conserved mechanism. Comparison of Ga with the small G protein Ras reveals how the
evolution of short segments that undergo disorder-to-order transitions can decouple regions …
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