Supplementary Materials

Supplementary Materials for:

Identification of a small-molecule ligand that activates the neuropeptide receptor GPR171 and increases food intake

Jonathan H. Wardman, Ivone Gomes, Erin N. Bobeck, Jennifer A. Stockert, Abhijeet Kapoor, Paola Bisignano, Achla Gupta, Mihaly Mezei, Sanjai Kumar, Marta Filizola, Lakshmi A. Devi*

*Corresponding author. Email: lakshmi.devi{at}mssm.edu

This PDF file includes:

  • Fig. S1. Binding of b-LEN–derived peptides and ligands of P2Y12 or P2Y14 to GPR171.
  • Fig. S2. Sequence alignment between mouse GPR171 and P2Y12.
  • Fig. S3. Homology model of GPR171 superimposed with the P2Y12 crystal structure.
  • Fig. S4. Surface receptor abundance of mutant GPR171 constructs expressed in CHO cells.
  • Fig. S5. Selectivity profile MS0015203.
  • Fig. S6. Effect of acute administration of MS0015203 on food intake in mice.
  • Fig. S7. Effect of GPR171 knockdown on receptor abundance in hypothalamus.
  • Table S1. Structures of compounds representative of each cluster.
  • Table S2. Displacement of radiolabeled b-LEN by a compound with chemical similarity to MS0015203.

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Citation: J. H. Wardman, I. Gomes, E. N. Bobeck, J. A. Stockert, A. Kapoor, P. Bisignano, A. Gupta, M. Mezei, S. Kumar, M. Filizola, L. A. Devi, Identification of a small-molecule ligand that activates the neuropeptide receptor GPR171 and increases food intake. Sci. Signal. 9, ra55 (2016).

© 2016 American Association for the Advancement of Science