Magic™ In Vitro Cell-based Tachykinin Receptor Functional Assay Service

The Importance of Tachykinin Receptors

The tachykinin receptor family consists of three members (NK1~3) and is a subfamily of class A GPCRs. Activation of these receptors facilitates their fast endocytosis and internalization, which means the receptor signaling is terminated. Functionally, tachykinin receptors are related to the occurrence of numerous illnesses like stress-related disorders. Despite several tachykinin receptor agonists and antagonists have been developed, our knowledge of these receptors is still limited. As a result, learning more about the tachykinin receptors is critically important for the treatment of diseases.

Fig.1 The expression of NK1R and substance P (SP) in the cells related to neurovascular unit (NVU).¹

The Principle of Magic™ In Vitro Cell-Based Tachykinin Receptor Functional Assay Service

Creative Biolabs was successful in establishing a cost-effective Magic™ in vitro cell-based tachykinin receptor functional assay service as a valuable tool to help global customers progress their projects and contribute to drug development.

Our Magic™ in vitro cell-based tachykinin receptor functional assay service is based on the cells and carried out with the principle of the accumulation of second messengers caused by tachykinin receptors binding to ligands. With the assistance of this assay, you can analyze the candidate samples or their functions. Throughout the whole process, we will develop the most appropriate experiment designs and provide comprehensive services to satisfy global customers' diverse needs. At Creative Biolabs, you can achieve your projects and attain high-quality results in a short period.

Fig.2 Pathways of chemoresistance-related NK-1R signaling.²

Our Advantages

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

Representative Data

Representative data 1: In the treatment of inoperable glioblastoma, the neuropeptide Substance P (SP) analog 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-[Thi8, Met(O2)11]-SP (DOTA-[Thi8, Met(O2)11]SP) has demonstrated encouraging clinical effects. The therapeutic potential of SP may be impaired due to the alterations that reduce the analog's selectivity for the targeted target (NK1R). Here, HEK293-T cells expressing NK1R, NK2R, NK3R, or MRGPRX2 were subjected to an inositol phosphate accumulation test to determine the analog's receptor selectivity. The findings reveal that the analog is highly selective for NK1R and has excellent efficacy, suggesting it may find use as a targeted theranostic in the treatment of NK1R-overexpressing diseases such as glioblastoma multiforme.

Fig.4 The results of inositol phosphate accumulation test.³

Representative data 2: Evidence from various preclinical studies suggests that NK-1R antagonists may be useful as antitumor agents against a wide range of human malignancies, lending credence to the SP/NK-1R system as an essential indicator in cancer. These results also support the use of NK-1R and NK-2R antagonists as a possible therapeutic strategy for treating metastatic illness.

Fig.5 The findings from relevant preclinical investigations.²

Work with Creative Biolabs

Creative Biolabs is perpetually refining services and technologies in an effort to increase its competitiveness and contribute to the growth of the industry. We consistently prioritize providing each customer with results of the utmost quality.

For more information about our Magic™ in vitro cell-based tachykinin receptor functional assay service, feel free to contact us at your convenience.

References

1. Turner, Renée J., and Alan J. Nimmo. "Evidence for the involvement of the Tachykinin NK1 Receptor in Acute Inflammation of the Central Nervous System." Receptors 2.4 (2023): 232-250.
   Distributed under Open Access License CC BY 4.0, without modification.
2. Téllez, Teresa, et al. "Neurokinin-1 Receptor (NK-1R) Antagonists as a New Strategy to Overcome Cancer Resistance." Cancers 14.9 (2021): 2255.
   Distributed under Open Access License CC BY 4.0. The original image Figure 2 was not modified. The original Table 2 was modified by extracting and using a part, and the title was changed to "The findings from relevant preclinical investigations".
3. Suthiram, Janine, et al. "Tachykinin Receptor-Selectivity of the Potential Glioblastoma-Targeted Therapy, DOTA-[Thi8, Met (O2) 11]-Substance P." International Journal of Molecular Sciences 24.3 (2023): 2134.
   Distributed under Open Access License CC BY 4.0, without modification.

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