Fig. 3: Structure-based protein engineering improves the affinity of AdTx1 to α1AAR.
From: Molecular mechanism of human α1A-adrenoceptor inhibition by Mamba snake toxin AdTx1
a H29 and K34 are chosen for mutation to increase their interactions with E3057.32 and D1063.32. S54 is chosen to be mutated to either N or Q to bridge the interaction between R28 and D172ECl2. b The AdTx1-3mut (H29R, K34R and S54Q) show higher affinity than AdTx1 in a 3H prazosin competition binding assay. Data are given as means ± SEM of 8 independent samples. c The AdTx1-3mut shows increased activity in an α1AAR-Gsq cAMP accumulation assay compared to AdTx1. Data as given as means ± SEM of 4 independent samples.
