In a groundbreaking study, a multinational research team led by Dr. Adnan Sljoka (RIKEN) and Prof. Akio Kitao (Tokyo Tech), in collaboration with Prof.
Tokyo Institute of Technology Aug 1 2024 In a groundbreaking study, a multinational research team led by Dr. Adnan Sljoka and Prof. Akio Kitao , in collaboration with Prof. Scott Prosser , has carried out experimental and computational studies to elucidate the mechanisms behind G protein selectivity and efficacy in the human adenosine A2A receptor .
However, GPCRs activation is related to dynamic events, key intermediate states, and activation states that arise between the time a ligand binds and when the G protein is activated. Furthermore, many GPCRs are promiscuous as they selectively interact with different G proteins, each influencing a unique cellular response. In fact, G protein selectivity is one of the least understood aspects of GPCR biology.
The researchers focused on studying key conformational states and dynamics of A2AR by complexing it with both cognate Gs and non-cognate Go G-proteins with same agonist ligand. 19F NMR revealed several functional activation states of A2AR when it is coupled to Gs and Go G-proteins. When A2AR is engages with its preferred Gs partner, the receptor adapts long-lived and highly populated activation states.
Related StoriesTo probe allostery in the receptor, the researchers utilized rigidity theory techniques developed by Dr. Sljoka. Rigidity theory analysis validated the presence of multiple adaptive allosteric networks which were distinct when receptor engages with Gs and Go. The allosteric mechanisms directly control the dynamics differences and transitions between distinct functional states, playing a major role in G protein selectivity and G-protein-receptor coupling.
Adenosine Brain Cancer Cell Cell Signaling Drug Discovery Drugs Efficacy Heart Inflammation Ligand Pharmacology Protein Receptor Research Technology
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