Skip to main content
. 2017 Nov;10(4):334–344. doi: 10.2174/1874467210666170110114727

Fig. (1).

Fig. (1)

Overview of the CRF1R crystal structures solved in complex with CP-376395. A - Left) Crystals grown in lipidic cubic phase of CRF1R-#76 – hexagonal setting. B) The overall structure of CRF1R-#76 solved with three copies in the asymmetric unit. CRF1R-T4L fusion is shown in ribbon representation and coloured by chain, pink, blue and green. The CP-376395 small-molecule is depicted in space fill representation with carbon, nitrogen and oxygen atoms coloured yellow, blue and red respectively. CRF1R-TMD and T4L fusions are denoted. C) Crystal packing of CRF1R in the hexagonal setting – view down unique c axis. Receptor copies coloured as in (B). D - Right) Crystals grown in lipidic cubic phase of CRF1R-#105 – orthorhombic setting. E) The overall structure of CRF1R-#105 solved with three copies in the asymmetric unit. CRF1R-T4L fusion is shown in ribbon representation and coloured by chain, pink, blue and green. The CP-376395 small-molecule is depicted in space fill representation coloured as in (B), CRF1R-TMD and T4L fusions are denoted. F) Crystal packing of CRF1R in the orthorhombic setting – view down a axis. Receptor copies coloured as in (B). G - Centre) Superposition of all 6 CRF1R-TMD copies in ribbon representation coloured in varying shades of cyan as viewed from a plane parallel to the membrane. TM helices are labeled. CP-376395 is labeled and shown in stick representation coloured as in B. H) Close-up view of the induced-fit small-molecule allosteric site in CRF1R – receptor copies coloured as in (G). Important receptor residues are labeled and shown in stick representation with carbon, nitrogen and oxygen atoms coloured white, blue and red respectively. CP-376395 is labeled and shown in stick representation coloured as in B. Hydrogen bonds depicted as dashed red lines. I) Superposition of all 6 CRF1R-TMD copies as in (G) shown in sausage representation coloured using a relative B-factor spectrum, blue=low; red=high. J) Representation as in (I) rotated to view from extracellular space. (The color version of the figure is available in the electronic copy of the article).