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Ligands for P2 Receptors

Extracellular purine and pyrimidine nucleotides modulate the function of diverse mammalian cell types and tissues under both normal and pathophysiological conditions via corresponding purine and pyrimidine receptors such as the P2 receptor family.

Members of the P2 receptors can be divided into ligand-gated ion channels (P2X receptors) and G-protein-coupled receptors (P2Y receptors), respectively.

Purinergic P2X receptors as ligand-gated cation channels are activated by endogenous ATP and assemble as homo- and hetero-trimers from seven cloned subtypes: P2X1, P2X2, P2X3, P2X4, P2X5, P2X6, and P2X7. From the family of P2Y receptors whose signaling is mediated through coupling to G-proteins, mainly Gqu/11 (P2Y10, P2Y13) and Gi/o (P2Y14), eight mammalian subtypes are known: P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, P2Y13, and P2Y14.

Generally, P2-receptors have been linked to participation in several diseases such as cancer, cardiovascular, inflammatory and neuropathic diseases, including neuropathic pain. Thus, agonist and antagonist ligands for these receptors have a high potential for clinical applications.

We offer different mono- and dinucleotide agonist and antagonist ligands for functional studies of P2X and P2Y subtypes.


Selected References

Jacobson (2013) Structure based approaches to ligands for G-protein-coupled adenosine and P2Y receptors, from small molecules to nanoconjugates. J. Med. Chem. 56:3749.
Jacobson et al. (2009) Development of selective agonists and antagonists of P2Y receptors. Purinergic Signalling 5:75.
Jacobson et al. (2003) Engineering of A3 Adenosine and P2Y Nucleotide Receptors and their ligands. Drug Development Res. 58:330.
Jacobson (2001) Probing adenosine and P2 receptors: design of novel purines and nonpurines as selective ligands. Drug Development Res. 52:178.
Mueller (2002) P2-pyrimidinergic receptors and their ligands. Current Pharmaceutical Design 8:2353.
Volonte et al. (2009) Membrane components and purinergic signalling: the purinome, a complex interplay among ligands, degrading enzymes, receptors and transporters. FEBS J. 276:318.