MCHR1 Membrane Protein Introduction

Introduction of MCHR1

Melanin concentrating hormone receptor 1(MCHR1), also referred to MCH1, is a protein belonging to the G protein-coupled receptor family 1 encoded by MCHR1 gene. Melanin-concentrating hormone (MCH), a cyclic neuropeptide expressed predominantly in the lateral hypothalamus, plays an important role in the control of feeding behavior and energy homeostasis. Melanin-concentrating hormone (MCH) is a hypothalamic neuropeptide that plays an important role in feeding behavior. It activates two G-protein-coupled receptors, MCHR1 and MCHR2. As one of the melanin-concentrating hormone receptors, MCHR1 proteins are found in all mammals. The encoded protein is an integral plasma membrane protein which binds melanin-concentrating hormone.

Function of MCHR1 Membrane Protein

It has been recognized that MCHR1 has a variety of functions such as the regulation of appetite, and in stress, anxiety and depression. MCHR1 can stimulate intracellular calcium flux, and inhibit cAMP accumulation and might be related to the neuronal regulation of food consumption. Through transfected with MCHR1 in mammalian cells, MCH is capable to activate multiple signaling pathways such as calcium mobilization, extracellular signal-regulated kinase activation, and inhibition of cyclic AMP generation through Gi/o- and Gq-coupled pathways. As an important regulator of feeding, this protein is selectively present in neuronal primary cilia in distinct regions of the mouse brain. The molecular mechanism of MCH1 receptor blockade by these antagonists was examined. MCHR1 antagonists have an influence on not only food intake, but also energy expenditure. A new class of potent MCH1 receptor antagonists like AZD1979 and 8-methylquinoline scaffold are considered as anti-obesity agents and bring promise for the treatment of human obesity.

Fig.1 Structure of MCHR1 membrane protein

Application of MCHR1 Membrane Protein in Literature

1. Tomoshige S., et al. Cytoskeleton-related regulation of primary cilia shortening mediated by melanin-concentrating hormone receptor 1. Gen Comp Endocrinol. 2017. 253:44-52. PubMed ID: 28842217.
   
   

   This article reports that MCH progressively has elicited cilia shortening without exclusion of fluorescence-positive material from the tip in live-cell imaging experiments and short cilia phenotypes have been associated with various metabolic disorders. All these findings may contribute to better understanding of how the cytoskeleton take part in the GPCR ligand-triggered cilia shortening with cell mechanical properties.

2. Sherwood A., et al. Deletion of Melanin Concentrating Hormone Receptor-1 disrupts overeating in the presence of food cues. Physiol Behav. 2015, 152(Pt B):402-7. PubMed ID: 26048303
   
   

   This article suggests that disruptions of MCH-1R signaling may be a useful pharmacological tool to inhibit the form of overeating behavior.

3. Otieno M.A, et al. Mechanisms for Hepatobiliary Toxicity in Rats Treated with an Antagonist of Melanin Concentrating Hormone Receptor 1 (MCHR1). Toxicol Sci. 2017, 155(2):379-388. PubMed ID: 28025230
   
   

   This paper shows that thienopyrimidinone MCHR1 antagonists trigger the hepatobiliary injury via a CYP-mediated bioactivation pathway.

4. Geuzaine A., et al. Amphetamine reward in food restricted mice lacking the melanin-concentrating hormone receptor-1. Behav Brain Res. 2014, 1;262:14-20. PubMed ID: 24412349
   
   

   This article indicates that MCH signaling might be associated with the ability of the food restriction (FR) to increase amphetamine-induced the conditioned place preference (CPP).

5. Sakurai T., et al. The MCH (1) receptor, an anti-obesity target, is allosterically inhibited by 8-methylquinoline derivatives possessing subnanomolar binding and long residence times. Br J Pharmacol. 2014, 171(5):1287-98. PubMed ID: 24670150
   
   

   It is the first study which demonstrates that a slowly dissociating negative allosteric modulator of the MCH1 receptor inhibits the numerous signaling pathways of this receptor.

MCHR1 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-MCHR1 antibody development services.

• Magic™ Membrane Protein Production Platform
• Magic™ Anti-Membrane Protein Antibody Discovery Platform

Equipped with world-leading technology platforms and professional scientific staff, Creative Biolabs has successfully generated a variety of functional membrane protein targets for our customers. We are pleased to tailor one-stop, custom-oriented service packages and provide lyophilization or freezing service for long-term storage of membrane proteins from weeks to months. Please feel free to contact us for more information.

All listed services and products are For Research Use Only. Do Not use in any diagnostic or therapeutic applications.