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Article

Cancer-Related Somatic Mutations in Transmembrane Helices Alter Adenosine A1 Receptor Pharmacology.

Molecules (Basel, Switzerland) - 10 Jun 2022

Wang Xuesong, Jespers Willem, Wolff Kim A N, Buytelaar Jill, IJzerman Adriaan P, van Westen Gerard J P, Heitman Laura H

Abstract excerpt

Overexpression of the adenosine A1 receptor (A1AR) has been detected in various cancer cell lines. However, the role of A1AR in tumor development is still unclear. Thirteen A1AR mutations were identified in the Cancer Genome Atlas from cancer patient samples. We have investigated the pharmacology of the mutations located at the 7-transmembrane domain using a yeast system. Concentration-growth curves were obtained...

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PMID: 35744872
DOI: 10.3390/molecules27123742
PMCID: PMC9229843

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