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GPCR

G protein coupled receptors (GPCRs) are a large family of cell surface receptors that have a distinctive structure passing through the plasma membrane seven times. Consequently they are referred to as seven-transmembrane receptors.

Thousands of G-protein coupled receptors are encoded in the human genome, about 350 of which detect hormones, growth factors, and other endogenous ligands. Approximately 150 of the GPCRs found in the human genome have unknown functions.

In all, GPCRs can be grouped into 6 classes based on sequence homology and functional similarity

  • Class A (Rhodopsin-like)
  • Class B (Secretin receptor family)
  • Class C  (Metabotropic glutamate/pheromone)
  • Class D (Fungal mating pheromone receptors)
  • Class E (Cyclic AMP receptors)
  • Class F (Frizzled/Smoothened)

The ligands that bind and activate these receptors include light-sensitive compounds, hormones, neurotransmitters, pheromones and odors.

GPCR’s signal via heterotrimeric G-proteins consisting of an alpha, beta and gamma subunit to two major signaling pathways, the cAMP signalling pathway and the phosphatidylinositol signaling pathway.

GPCRs are involved in a wide variety of physiological and pathological processes including vision, taste, smell, behavioral and mood regulation, autonomic nervous system transmission, immune system, homeostasis modulation, cancer biology and cardiovascular disease.

G protein coupled receptors (GPCRs) are also the target of approximately 40% of all modern medicinal drugs. The most commonly targeted receptors are the following histamine H1, α1A adrenergic, muscarinic M1, dopamine D2, muscarinic M2, 5HT2a, α2A adrenergic, and muscarinic M3.

Synkinase provide a wide range of inhibitors that target GPCRs for research use that have been cited in numerous peer-review publications.

Our GPCRs are available in many formats and compound sizes.

GPCR

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