Figure 9: Comparison of BETP and 2-sulfonyl pyrimidines covalently bound to active-state GLP-1Rs:
Model of BETP’s (purple sticks, left panel) binding pocket, adapted from ref. [19], illustrating covalent modification of Cys347 in TM6 at the GLP-1R (cyan) in active conformation and additional putative influences of surrounding residues, such as van-der Waals interactions with hydrophobic residues or halogen attraction of Lys346; model was modified for A1-like (green sticks, middle panel) and A3-like (pale blue sticks, right panel) 2-sulfonyl pyrimidine analogs; illustrations generated using Chimera 1.13.1.