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Single Stabilizing Point Mutation Enables High-Resolution Co-Crystal Structures of the Adenosine A_2A Receptor with Preladenant Conjugates.

ABSTRACT: The G protein-coupled adenosine A_2A receptor (A_2A AR) is an important new (potential) drug target in immuno-oncology, and for neurodegenerative diseases. Preladenant and its derivatives belong to the most potent A_2A AR antagonists displaying exceptional selectivity. While crystal structures of the human A_2A AR have been solved, mostly using the A_2A -StaR2 protein that bears 9 point mutations, co-crystallization with Preladenant derivatives has so far been elusive. We developed a new A_2A AR construct harboring a single point mutation (S91^3.39 K) which renders it extremely thermostable. This allowed the co-crystallization of two novel Preladenant derivatives, the polyethylene glycol-conjugated (PEGylated) PSB-2113,

SUBMITTER: Claff T

PROVIDER: S-EPMC9310709 | biostudies-literature | 2022 May

REPOSITORIES: biostudies-literature

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Single Stabilizing Point Mutation Enables High-Resolution Co-Crystal Structures of the Adenosine A_2A Receptor with Preladenant Conjugates.

OmicsDI is part of the ELIXIR infrastructure

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Dataset Information

Single Stabilizing Point Mutation Enables High-Resolution Co-Crystal Structures of the Adenosine A2A Receptor with Preladenant Conjugates.

OmicsDI is part of the ELIXIR infrastructure

Tweets

Single Stabilizing Point Mutation Enables High-Resolution Co-Crystal Structures of the Adenosine A_2A Receptor with Preladenant Conjugates.