Biogenic amine-binding GPCRs

Table 6.1 Biogenic amine binding GPCR antitargets and side effects mediated by high-affinity agonists and antagonists of the respective receptor. ...

Antitarget Modeling of Biogenic Amine-Binding GPCRs Common Features and Subtle Differences... 

Klabunde, T., and Evers, A. (2005). GPCR antitarget modeling Pharmacophore models for biogenic amine binding GPCRs to avoid... 

Hamdan et al. (2002) describe another biogenic amine-responsive GPCR in the tegument of S. mansoni, which specifically binds to and is activated by histamine. This cloned receptor shares approximately 30% amino acid sequence homology with other major amine GPCRs, and, when transfected into mammalian cells exhibited the following characteristics ... 

Figure 7. A schematic diagram of the proposed ligand binding domains, shown in light grey, in various GPCRs. The helices are shown as cylinders, the loops, N-termini and C-termini are shown as lines. (A) Biogenic amine receptors, (B) Peptide receptors, (C) Glycoprotein hormone receptors, (D) Thrombin receptor.

More than 100 different GPCRs bind to a variety of ligands encompassing biogenic amines, such as acetylcholine, norepinephrine, and serotonin amino acid neurotransmitlers, such as glutamate and glycine and peptide hormones, such as angiotensin II and somatostatin. 

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