GPR142 is highly expressed in the pancreas and immune system and shares 33% homology with GPR139. Endogenous agonists identified to date include aromatic amino acids such as tryptophan and phenylalanine. CLP-3094 was identified as a potent and selective GPR142 antagonist with an IC50=2.3 μM...
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GPR142 is highly expressed in the pancreas and immune system and shares 33% homology with GPR139. Endogenous agonists identified to date include aromatic amino acids such as tryptophan and phenylalanine. CLP-3094 was identified as a potent and selective GPR142 antagonist with an IC50=2.3 μM against 1 mM L-tryptophan. It inhibited insulin secretion from islets induced by L-tryptophan and other agonists and displayed anti-inflammatory activity in a mouse arthritis model
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