G protein-coupled receptors (GPCRs) are a large and crucial protein family involved in cell signaling, responding to various ligands such as hormones and neurotransmitters. They are key drug targets, with ~30% of prescription drugs acting on GPCRs. However, discovering new compounds targeting GPCRs is challenging due to their instability outside the cell membrane, particularly for wild-type receptors. Fragment screening has emerged as an effective strategy for identifying high-quality chemical scaffolds for drug development.
In this poster, researchers tested 704 fragments on the human A2A receptor (hA2AR) using a kinetic-based screening approach as a proof of principle.
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G protein-coupled receptors (GPCRs) are a large and crucial protein family involved in cell signaling, responding to various ligands such as hormones and neurotransmitters. They are key drug targets, with ~30% of prescription drugs acting on GPCRs. However, discovering new compounds targeting GPCRs is challenging due to their instability outside the cell membrane, particularly for wild-type receptors. Fragment screening has emerged as an effective strategy for identifying high-quality chemical scaffolds for drug development.
In this poster, researchers tested 704 fragments on the human A2A receptor (hA2AR) using a kinetic-based screening approach as a proof of principle.
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