Fig. 1: Sequence and agonistic effect on IR phosphorylation of IR-A62 monomer and IR-A62 dimers.
From: Structural mechanism of insulin receptor activation by a dimeric aptamer agonist
a Sequence comparison between the IR-A62 monomer and IR-A62 dimers linked by the 8 T linker. For clarity, only IR-A62D-8T is shown. Z and P represent the benzyl modified- and naphthyl modified-dU, respectively. Red- and green-colored nucleotides represent 2′-fluoro ribose and 2′-O-methyl ribose, respectively. The linker between the two A62M aptamers is underlined. b Activity comparison of the IR-A62 monomer and IR-A62 dimers. Rat-1/hIR cells were stimulated with 50 nM insulin for 10 min, 400 nM A62M for 1 h or 200 nM A62 dimers for 1 h. Bar graphs are presented as the mean ± s.d. of three independent replicates and normalized by A62D-8T stimulated samples. c, d Phosphorylation of IR (c) and downstream signaling (d) were analyzed using specific phospho-antibodies. Rat-1/hIR cells were stimulated with 50 nM insulin for 10 min, 400 nM A62M for 1 h or 200 nM A62M-8T. Bar graphs are presented as the mean ± s.d. of three independent replicates and normalized by 50 nM insulin-stimulated samples.
