TABLE 1.
Role of the signal accepting network
In vitro adenylyl cyclase activities, maximal inhibition by serine, and IC50 serine concentrations of mutants in the signal-accepting network of Af1503 HAMP and Tsr are shown. ND, not determined.
| Mutation | AC activity | % of inhibition | IC50 |
|---|---|---|---|
| nmol·mg−1min−1 | by 10 mm serine | μm | |
| Tsr receptor1–215 Af1503 HAMP278–331 Rv3645 CHD331–549 | |||
| WT | 19.1 ± 1.6 | No inhibition | |
| Network from Tsr (Fig. 1C) | 14.6 ± 1.5 | 34 ± 8.8 | 15 ± 40 |
| R308G | 13.1 ± 4.0 | No inhibition | |
| A309S | 9.5 ± 0.6 | No inhibition | |
| R308G/A309S | 9.4 ± 1.2 | No inhibition | |
| Tsr receptor + HAMP1–268 Rv3645 CHD331–549 | |||
| WT | 18.4 ± 0.6 | 82 ± 2.7 | 66 ± 18 |
| Network from Af1503 (Fig. 1C) | 0.7 ± 0.02 | 28 ± 6.6 | 840 ± 247 |
| G245R | 0.4 ± 0.05 | 57 ± 10 | 108 ± 42 |
| S246A | 1.5 ± 0.10 | 84 ± 2.5 | ND |
| G245R/S246A | 0.7 ± 0.03 | 58 ± 2.0 | 111 ± 66 |
| E248K | 0.3 ± 0.02 | No inhibition | |