Article

Crystal structure of adenosine A2A receptor in complex with clinical candidate Etrumadenant reveals novel antagonist interaction

2023-02-27

Abstract excerpt

<title>Abstract</title>The Gs-protein-coupled adenosine A2Areceptor (A2AAR) represents an emerging drug target for cancer immunotherapy. The clinical candidate Etrumadenant was developed as an A2AAR antagonist with ancillary blockade of the A2BAR subtype. It constitutes a novel chemotype featuring a poly-substituted 2-amino-4-phenyl-6-triazolylpyrimidine co...

Topics

Open a Topic to create a Post that cites this publication.

Identifiers and source

Literature Corpus work: b2d13f11-629b-5dcf-84cf-d3df96f4ef09
DOI: 10.21203/rs.3.rs-2602909/v1

Open publication

Related research

Semantic proximity does not establish scientific evidence.

Click a neighbor to travelStep 1 · 12 closest

Crystal structure of adenosine A2A receptor in complex with clinical candidate Etrumadenant reveals novel antagonist interactionDOI 10.21203/rs.3.rs-2602909/v1Read

A2A and A2B adenosine receptors: The extracellular loop 2 determines high (A2A) or low affinity (A2B) for adenosine.Semantic proximity Read

Cancer-Associated Mutations of the Adenosine A2A Receptor Have Diverse Influences on Ligand Binding and Receptor Functions.Semantic proximity Read

Structure-Based Design of Potent and Selective Ligands at the Four Adenosine Receptors.Semantic proximity Read

The second extracellular loop of GPCRs determines subtype-selectivity and controls efficacy as evidenced by loop exchange study at A2 adenosine receptors.Semantic proximity Read

Characterization of cancer-related somatic mutations in the adenosine A2B receptor.Semantic proximity Read

Off-target-free chemogenetic platform that decodes physiological roles of target GPCRsSemantic proximity Read

Why are A(2B) receptors low-affinity adenosine receptors? Mutation of Asn273 to Tyr increases affinity of human A(2B) receptor for 2-(1-Hexynyl)adenosine.Semantic proximity Read

Synthesis of 3'-ureidoadenosines and their high binding affinity at the mutant A3 adenosine receptor.Semantic proximity Read

Structure of a lasso peptide bound ETB receptor provides insights into the mechanism of GPCR inverse agonismSemantic proximity Read

Structural Mapping of Adenosine Receptor Mutations: Ligand Binding and Signaling Mechanisms.Semantic proximity Read

Thermostabilisation of an agonist-bound conformation of the human adenosine A(2A) receptor.Semantic proximity Read