Introduction of GPR143
Encoded by gene GPR143, GPR143 was originally identified as the protein ocular albinism 1 (OA1), which belongs to G protein-coupled receptor (GPCR). Participation in various neurological processes made GPCR have numerous possibilities for therapeutic applications. GPR143 is targeted to melanosomes in pigment cells. The gene GPR143 consists of 9 exons and is translated into a seven transmembrane protein constituted with α-helix. The third α-helix is considered as the G protein binding domain.
|Basic Information of GPR143|
|Protein Name||G-protein coupled receptor 143|
|Organism||Homo sapiens (Human)|
Function of GPR143 Membrane Protein
GPR143 is mainly expressed in the retinal pigment epithelium and melanocytes with high levels, and it is considered to be involved in intracellular signal transduction mechanisms. GPR143 mutation/defection may cause ocular albinism type 1, also referred to as Nettleship-Falls type ocular albinism, an X-linked visual disorder characterized by the albinism associated with retinal abnormalities. GPR143 was evaluated to bind tyrosine and L-3,4-Dihydroxyphenylalanine (L-DOPA), a traditional therapeutic drug for Parkinson’s disease, to play a role in melanosome biogenesis, organization, and transport. The binding can stimulate Ca2+ influx into the cytoplasm, then enhances secretion of the neurotrophic factor SERPINF1 and relocalizes β-arrestin at the plasma membrane. The signaling transduction relies on a Gq-mediated pathway in melanocytic cells. The binding between GPR143 and L-DOPA in the nucleus tractus solitarii can mediate depressor and bradycardic responses. In addition, GPR143 contributes to the pathogenesis of age-related macular degeneration (AMD). So GPR143 could be developed into a drug target to prevent the Parkinson’s disease, ocular albinism type 1 and AMD.
Fig.1 Model of GPR143. (Pan, 2016)
Application of GPR143 Membrane Protein in Literature
The authors reveal that GPR143 is a candidate receptor for L-3,4-dihydroxyphenylalanine (L-DOPA), which can replenish the depleted brain dopamine in the patients of Parkinson's disease. L-DOPA induces ptosis in a GPR143-independent fashion in mice
This article firstly demonstrates that GPR143 acted as a functional receptor for DOPA to mediate physiological and/or pharmacological responses in the CNS. It mediates the responses of depressor and bradycardic in the nucleus tractus solitarii.
Through the experiment of complete ophthalmologic examinations, including 4 patients, 7 carriers and 17 unaffected individuals in five-generation family, the authors report that the mutation p.Y269X (a substitution of tyrosine for adenine) of GPR143 is responsible for the pathogenesis of familial ocular albinism for the first time.
This article shows the unique distribution pattern of GPR143-immunoreactive neurons and/or cells in the rat CNS. The distribution area includes the hippocampus, cerebral cortex, cerebellum cortex, striatum, substantia nigra, hypothalamic median eminence and supraoptic nucleus, nucleus tractus solitarii and caudal ventrolateral medulla and rostral ventrolateral medulla, medial habenular nucleus and olfactory bulb.
This article verifies the hypothesis that patients taking L-DOPA for movement disorders are protective against AMD due to GPR143-mediated elevation in retinal PEDF.
GPR143 Preparation Options
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