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. 2007 May 29;151(6):851–859. doi: 10.1038/sj.bjp.0707293

Figure 2.

Figure 2

Screening of monosubstituted Bpa-Ucn I analogues for receptor binding affinity and maximum stimulation of G-protein activity at HEK-rCRF1 cell membranes obtained from cells expressing Gs- as well as Gi-protein activity. (a) From competition binding curves using 100 pM [125I]-Tyr-sauvagine, fitted according to a one-site model, Ki values were obtained. These represent the resultant of the receptor in all its different states (uncoupled and coupled to Gs/Gi). When more than one screening experiment was performed, data are given as mean±s.e. (b) The sum of Gs and Gi activity was determined by measuring the stimulation of [35S]-GTPγS binding by 1 μM peptides and related to the maximum activity exhibited by 1 μM Ucn. Data are expressed as mean±s.e. of at least three independent experiments, each with triplicate incubations. HEK-rCRF1, HEK293 cells stably transfected with rCRF1.