Article
A point mutation that confers constitutive activity to CXCR4 reveals that T140 is an inverse agonist and that AMD3100 and ALX40-4C are weak partial agonists.
The Journal of biological chemistry - 5 Jul 2002
Zhang Wen-Bo, Navenot Jean-Marc, Haribabu Bodduluri, Tamamura Hirokazu, Hiramatu Kenichi, Omagari Akane, Pei Gang, Manfredi John P, Fujii Nobutaka, Broach James R, Peiper Stephen C
Abstract excerpt
CXCR4 is a G protein-coupled receptor for stromal-derived factor 1 (SDF-1) that plays a critical role in leukocyte trafficking, metastasis of mammary carcinoma, and human immunodeficiency virus type-1 infection. To elucidate the mechanism for CXCR4 activation, a constitutively active mutant (CAM) was derived by coupling the receptor to the pheromone response pathway in yeast. Conversion of Asn-119 to Ser or Ala,...
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