Molecules, Vol. 25, Pages 725: GPR6 Structural Insights: Homology Model Construction and Docking Studies

Molecules, Vol. 25, Pages 725: GPR6 Structural Insights: Homology Model Construction and Docking Studies Molecules doi: 10.3390/molecules25030725 Authors: Isawi Morales Sotudeh Hurst Lynch Reggio GPR6 is an orphan G protein-coupled receptor that has been associated with the cannabinoid family because of its recognition of a sub-set of cannabinoid ligands. The high abundance of GPR6 in the central nervous system, along with high constitutive activity and a link to several neurodegenerative diseases make GPR6 a promising biological target. In fact, diverse research groups have demonstrated that GPR6 represents a possible target for the treatment of neurodegenerative disorders such as Parkinson’s disease, Alzheimer’s disease, and Huntington’s disease. Several patents have claimed the use of a wide range of pyrazine derivatives as GPR6 inverse agonists for the treatment of Parkinson’s disease symptoms and other dyskinesia syndromes. However, the full pharmacological importance of GPR6 has not yet been fully explored due to the lack of high potency, readily available ligands targeting GPR6. The long-term goal of the present study is to develop such ligands. In this paper, we describe our initial steps towards this goal. A human GPR6 homology model was constructed using a suite of computational techniques. This model permitted the identification of unique GPR6 structural features and the exploration of ...
Source: Molecules - Category: Chemistry Authors: Tags: Article Source Type: research