Melanocortin Receptors: Why They Matter

MC1R, MC2R, MC3R, MC4R, and MC5R are the five subtypes of the melanocortin receptor, a family of G-protein coupled receptors. They play a variety of important roles, including eating behavior, energy balance, stress response, etc. Regarding this context, many significant degenerative illnesses involve them, such as obesity and other food disorders, cancer, diabetes, and plenty more. Nevertheless, after many years of work, there are just a few drugs targeting this family of receptors and their inherent ligands, the melanotropins.

MCR in the hypothalamic control of food intake and energy homeostasisFig.1 MCR in the hypothalamic control of food intake and energy homeostasis.1

Our Magic™ In Vitro Cell-based Melanocortin Receptor Functional Assay Service

Through the integration of our experience and expertise, Creative Biolabs has innovatively developed a Magic™ in vitro cell-based melanocortin receptor functional assay service and welcomes global customers to inquire and order.

Our Magic™ in vitro cell-based melanocortin receptor functional assay service incorporates the advantages of cell-based assay with melanocortin receptors functional assay, which is capable of being applied to efficiently measure the receptor activation/inhibition and assay compounds. The principle of this assay is to examine the accumulation of the second messengers triggered by the reaction of melanocortin receptors with ligands. Throughout this entire procedure, we provide comprehensive, customized, top-notch services that cater to the diverse requirements of global customers.

Melanocortin receptors mediating anti-inflammatory effectsFig.2 Melanocortin receptors mediating anti-inflammatory effects.2

Benefits for You

Constantly listening to our customers' suggestions, Creative Biolabs strives tirelessly to improve and optimize technological innovations. Simultaneously, our Magic™ in vitro cell-based melanocortin receptor functional assay service will benefit global customers with:

Advantages of our Magic™ in vitro cell-based melanocortin receptor functional assay service.Fig.3 Advantages of our Magic™ in vitro cell-based melanocortin receptor functional assay service.

Representative Data

DATA 1: The pituitary gland produces an α-melanocyte-stimulating hormone (α-MSH). And pituitary-derived-MSH inhibits antitumor immunity by increasing myelopoiesis. To explore the mechanism by which α-MSH stimulates myelopoiesis, the expression of these receptors in BM cells was investigated and it was discovered that only MC5R was substantially expressed in Lin BM cells, particularly LSK cells.

The findings demonstrate that α-MSH induced myelopoiesis, myeloid cell accumulation, immunosuppression, and tumor growth by acting on bone marrow progenitors via its melanocortin receptor MC5R. The MC5R peptide antagonist improved anticancer immunity.

MC5R is involved in tumor-induced myelopoiesis and immunosuppressionFig.4 MC5R is involved in tumor-induced myelopoiesis and immunosuppression.3

MC5R antagonism enhances antitumor immunityFig.5 MC5R antagonism enhances antitumor immunity.3

DATA 2: The results uncovered the therapeutic potential of restoring loss-of-function MC1R in MC1R RHC-variants by activating MC1R protein palmitoylation. Palmitoylation of the melanocortin 1 receptor (MC1R) is necessary for the activation of MC1R signaling, which in turn increases pigmentation, induces a G1-like cell cycle arrest in response to ultraviolet light (UVB), and controls senescence and melanogenesis in vitro and in vivo.

MC1R palmitoylation in cells infected with shZDHHC13 and/or WT HA-ZDHHC13 virusFig.6 MC1R palmitoylation in cells infected with shZDHHC13 and/or WT HA-ZDHHC13 virus.4

Work with Creative Biolabs

Constantly listening to our customers' suggestions, Creative Biolabs strives tirelessly to improve and optimize technological innovations. For more details about our Magic™ in vitro cell-based melanocortin receptor functional assay service, please don't hesitate to contact us. We are sincerely looking forward to being partners with global customers.

References

  1. Domingo, Pere, et al. "Potential role of the melanocortin signaling system interference in the excess weight gain associated to some antiretroviral drugs in people living with HIV." International Journal of Obesity 44.9 (2020): 1970-1973.
  2. Markov, Dmitrii D., et al. "The melanocortin system: A promising target for the development of new antidepressant drugs." International Journal of Molecular Sciences 24.7 (2023): 6664.
  3. Xu, Yueli, et al. "Pituitary hormone α-MSH promotes tumor-induced myelopoiesis and immunosuppression." Science 337.6610 (2022): 1085-1091.
  4. Chen, Shuyang, et al. "Palmitoylation-dependent activation of MC1R prevents melanomagenesis." Nature 549.7672 (2017): 399-403.

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