DRD5 Membrane Protein Introduction

Introduction of DRD5

DRD5 also referred as DBDR, is the D5 subtype of the dopamine receptor that in humans is encoded by the DRD5 gene. Highly homologous to the D1 receptor, DRD5 belongs to the D1-like receptor family together with the D1 receptor subtype. Via activating adenylyl cyclase, the activity of DRD5 is mediated by G proteins. This protein found in the brain functions together with a chemical messenger (neurotransmitter) termed dopamine. Dopamine triggers chemical reactions within nerve cells through perfectly fits into the D5 receptor. Dopamine signaling plays a critical role in the brain, such as the regulation of attention, mood, memory, learning, and movement.

Function of DRD5 Membrane Protein

Dopamine receptors are a subclass of the superfamily of G protein-coupled receptors, that transduce their effects by coupling to specific G proteins. Within the dopamine receptor family, the adenylyl cyclase stimulatory receptors include the D1 and D5 subtypes. The two dopaminergic systems are associated with different receptors for dopamine. The D1 family of dopamine receptors (D1 and D5) is an order of magnitude more abundant in the PFC than D2 family receptors (D2, D3, and D4), while D2 receptors are more prevalent in the striatum than in the cortex3. The DA D1 and D5 receptors are structurally homologous, but the D5 receptor has a higher affinity for DA than the D1 receptor, is more constitutively active in the absence of agonist, has differing affinities for agonists and antagonists, and has a somewhat different regional distribution in the brain. At a functional level, the DA D1 receptor promotes locomotor activity, while the DA D5 receptor appears to inhibit locomotor activity in animals which have been unilaterally lesioned with 6-hydroxydopamine. Dopamine acts mainly through the D1/D5 receptor in the prefrontal cortex (PFC) to modulate neural activity and behaviors associated with working memory.

Fig.1 Structure of DRD5 membrane protein.

Application of DRD5 Membrane Protein in Literature

1. Leng Z. G., et al. Activation of DRD5 (dopamine receptor D5) inhibits tumor growth by autophagic cell death. Autophagy, 2018, 13(8): 1404-1419. PubMed ID: 28613975
   
   

   This article reports that novel mechanisms for the tumor suppressive effects of DRD5 agonists, and suggested a potential use of DRD5 agonists as a novel therapeutic approach in the treatment of different human tumors and cancers.

2. Klein M., et al. Meta-analysis of the DRD5 VNTR in persistent ADHD. Eur Neuropsychopharmacol. 2016, 26(9): 1527-1532. PubMed ID: 27480019
   
   

   This article provides evidence that none of the common DRD5 alleles are associated with Attention-Deficit/Hyperactivity Disorder (ADHD) risk or ADHD symptom counts in adults.

3. Pornour M., et al. Dopamine receptor gene (DRD1-DRD5) expression changes as stress factors associated with breast cancer. Asian Pac J Cancer Prev. 2014, 15(23): 10339-43. PubMed ID: 25556472
   
   

   This article evaluates the expression of five dopamine receptors (DRD1-DRD5) in peripheral blood mononuclear cells (PBMC) as stress factors in breast cancer patients and the human breast cancer cell line (MCF-7).

4. Plouffe B., et al. Functional analysis of human D1 and D5 dopaminergic G protein-coupled receptors: lessons from mutagenesis of a conserved serine residue in the cytosolic end of transmembrane region 6. Methods Mol Biol. 2013, 964: 141-80. PubMed ID: 23296783
   
   

   This article demonstrates how to mutate one conserved residue in the cytosolic end of TM6 of D1R (Ser263) and D5R (Ser287) by modifying two or three nucleotides in the cDNA of human D1-like receptors. In this study, we will test the effect of S263A/G/D and S287A/G/D mutations on ligand binding and DA-dependent activation of D1R and D5R.

5. Seamans J. K., et al. Dopamine D1/D5 receptor modulation of excitatory synaptic inputs to layer V prefrontal cortex neurons. PNAS. 2001, 98 (1): 301-306. PubMed ID: 11134516
   
   

   This article found that the D1/D5 agonists increased depolarization of summating the NMDA component of excitatory postsynaptic potential (EPSP).

DRD5 Preparation Options

To obtain the soluble and functional target protein, the versatile Magic™ membrane protein production platform in Creative Biolabs enables many flexible options, from which you can always find a better match for your particular project. Aided by our versatile Magic™ anti-membrane protein antibody discovery platform, we also provide customized anti-DRD5 antibody development services.

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