Orphan Family Related Drug Discovery Products
Creative Biolabs has the assays you can rely on for high throughput screening, lead optimization, characterizing and discovering targets, and uncovering the complexity of disease pathways. We can offer membrane protein in vitro assay kits that save valuable laboratory time and is ideal for high throughput screening.
Membrane protein stable cell lines are widely used in many areas of biomedical research. Creative Biolabs can offer membrane protein stable cell lines to stablish in vitro models for High Throughput Screening.
Creative Biolabs offers high-quality, innovative tools to help research groups accelerate membrane protein drug discovery. They can be found by targets. If there is no product that meets your needs, please contact us.
Rhodopsin was the first GPCR to be discovered in 1878. It was later established that opsin, a GPCR protein, and retinal, a cofactor that is reversibly covalently attached, make up rhodopsin. The number of human GPCRs expanded to roughly 800 after the human genome sequence was finished in 2004. More than 140 GPCRs, excluding the olfactory receptor family, have not yet been connected to endogenous ligands. These GPCRs are referred to as orphan GPCRs.
Fig.1. The orphan receptors in GPCRs. (Tang, 2012)
Creative Biolabs is an undisputed world-leading provider in membrane protein drug discovery. We offer following orphan family drug discovery tool with the best quality:
Overview of Orphan Family
The orphan receptor has been established as a promising therapeutic target in part thanks to investigations analyzing its distribution and localization. Studies exploring the phenotypic characteristics of targeted KD/KO of orphan GPCRs have been very helpful in understanding their biological roles and in indicating their relevance as prospective therapeutic targets.
Fig.2. Signalling pathways of an orphan GPCR. (Ngo, 2016)
- A study with the orphan receptor GPR88 suggested a function for this receptor in schizophrenia. In situ hybridization was used to identify the presence of GPR88 mRNA in the striatum of WT mice and its absence in GPR88-deficient mice. The increased dopamine sensitivity of GPR88 KO mice indicates that this orphan receptor may be crucial for striatal function and dopamine responsiveness, making it a viable therapeutic target for the treatment of striatum-related psychiatric illnesses.
- A study with the orphan GPR161 suggested that this receptor plays a part in the correct development of the heart's tubes. In this instance, in situ hybridization using growing embryos revealed GPR161 mRNA expression in the precardiac mesoderm, and knock-down of GPR161 led to elevated Ca2+ levels in Kupffer's vesicles in addition to pericardial edema, improper positioning of the ventricle and atrium, and malformation of cardiac loops. The findings of this investigation suggest that the therapeutic target GPR161 may be useful in the management of congenital cardiac abnormalities.
Orphan Family Drug Discovery
The dearth of ligands that have been identified as well as the peculiar architectures of the GPCR themselves have slowed down the advancement of orphan GPCR function research. Understanding the physiological and pathological significance of these new orphan GPCRs requires further study of their signaling networks. For us to fully comprehend the roles of these receptors and the potential pathways they might be a part of, we need to use the knockout strategy for orphan GPCRs. Functional and targeted antibodies can be used to develop therapeutics for cancers and genetic diseases that include orphan GPCRs as well as for the ligands.
References
- Tang, X.L.; et al. Orphan G protein-coupled receptors (GPCRs): biological functions and potential drug targets. Acta Pharmacologica Sinica. 2012, 33(3): 363-371.
- Ngo, T.; et al. Identifying ligands at orphan GPCRs: current status using structure‐based approaches. British journal of pharmacology. 2016, 173(20): 2934-2951.
