Fig. 15 | Signal Transduction and Targeted Therapy

Fig. 15

From: G protein-coupled receptors (GPCRs): advances in structures, mechanisms and drug discovery

Fig. 15The alternative text for this image may have been generated using AI.

a Schematic representation of PAM LSN3160440 and orthosteric GLP-1 bound to GLP-1R (PDB: 6VCB). GLP-1 is indicated in pink. b Detailed binding modes of GLP-1R bound to LSN3160440; π–π stacking is indicated in gray dashes. c 2D structure of small-molecule allosteric ligand LSN3160440 presented for clarity. d Superposition of orthosteric small-molecule agonists Boc5 (displayed with purple sticks), TT-OAD2 (displayed with salmon sticks), LY3502970 (displayed with yellow sticks), and CHU-128 (displayed with blue sticks) to LSN3160440–GLP-1–GLP-1R structure reveals a partial overlap in the TM1-TM2 cleft. The conserved residue Tyr1451.40 is highlighted

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