Article
Superactive mutants of thromboxane prostanoid receptor: functional and computational analysis of an active form alternative to constitutively active mutants.
Cellular and molecular life sciences : CMLS - 1 Sept 2010
Ambrosio Manuela, Fanelli Francesca, Brocchetti Silvia, Raimondi Francesco, Mauri Mario, Rovati G Enrico, Capra Valérie
Abstract excerpt
In class A GPCRs the E/DRY motif is critical for receptor activation and function. According to experimental and computational data, R3.50 forms a double salt bridge with the adjacent E/D3.49 and E/D6.30 in helix 6, constraining the receptor in an inactive state. The disruption of this network of interactions facilitates conformational transitions that generate a signal or constitutive activity. Here we...
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