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Figure 1.

Bombykol receptor expressed in the Xenopus oocyte recording system.

Robust currents from BmorOR1•BmorOrco-expressing oocytes when perfused with bombykol, and dose-dependent responses. n = 3–5, error bars in all figures represent SEM.

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Figure 1 Expand

Figure 2.

Activation by bombykal.

(A) Current responses and (B) dose-dependent relationships obtained by challenging BmorOR1•BmorOrco-expressing oocytes with increasing concentrations of bombykol and bombykal. n = 6.

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Figure 2 Expand

Figure 3.

Chemical analysis of synthetic pheromone components.

GC-MS traces obtained from bombykol (upper trace) and bombykal (lower trace) samples freshly prepared to challenge BmorOR1•BmorOrco-expressing oocytes. Arrow indicates trace amounts of bombykal (1.3%) in the bombykol sample, whereas a dotted arrow shows traces of bombykol (0.9%) in bombykal sample. The ratio of bombykol (retention time, 16.06 min) to bombykal (15.42 min) in the two samples was 1.015±0.02, n = 3.

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Figure 4.

Synthetic pheromone components trapped by PBP.

(A) Traces and (B) quantification of current responses obtained from the BmorOR1•BmorOrco-expressing oocytes when presented with bombykol and bombykal solubilized either by DMSO or BmorPBP1. n = 3. *Significantly different (t-test, P<0.05).

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Figure 4 Expand

Figure 5.

Chemical structures.

Structures of the silkworm moth sex pheromone (1) and bombykol-related compounds, which were used to challenge BmorOR1•BmorOrco-expressing oocytes.

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Figure 6.

Stereochemical selectivity.

(A) Traces and (B) quantification of current responses from BmorOR1•BmorOrco-expressing oocytes perfused with four isomers of bombykol at 0.1 µM. n = 5. Bars with the same letter arwe not significantly different (One-way ANOVA, P<0.01).

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Figure 7.

Effect of altering unsaturation on receptor response.

(A) Traces and (B) quantification of current responses elicited by (8E,10Z)-hexadecadien-1-ol (9) and 10,12-hexadecadiyn-1-ol (6) presented at 1 mM. n = 3. Bars with the same letter are not significantly different (One-way ANOVA, P<0.01).

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Figure 8.

Effect of number of carbons distal to unsaturation.

(A) Current responses obtained by challenging BmorOR1•BmorOrco-expressing oocytes with bombykol (lower trace, positive control), (10E,12Z)-octadecadien-1-ol (7), and (10E,12Z)-tetradecadien-1-ol (8), robust response at 10 µM. (B) Dose-dependent relationships; n = 4.

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Figure 9.

Reducing responses by adding rigidity to the C1–C9 moiety.

(A) Current responses elicited by (10E,12Z)-hexadecadien-4-yn-1-ol (10), (4Z,10E,12Z)-hexadecatrien-1-ol (11), and bombykol (1) from BmorOR1•BmorOrco-expressing oocytes (ligands presented at 10 µM). EC50s 1.7×10−5M, 1.3×10−5M, and 5.9×10−6M, respectively. (B) Dose-dependent relationships, n = 3–4.

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Figure 10.

Schemes A–C.

Synthetic sequence for preparation of analogues 711 containing the (E,Z)-dienyl moiety.

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Figure 11.

Schemes D–G.

Synthetic sequence for preparation of analogues 36 differing in unsaturation.

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