Tachykinin 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.
A class of neuropeptides known as tachykinins (TKs) is broadly dispersed throughout the body of an animal. Substance P (SP), neurokinin A (NKA), and neurokinin B (NKB) are the three main TKs in mammalian species. Other TK peptides, such as neuropeptide K (NPK), neuropeptide (NP), hemokinin-1 (HK-1), and endokinin (EKs), have also been found. The Tac1 gene codes for SP, NKA, NPK, and NP. The N-terminal extensions of NPK and NP, which are variants of NKA, are 26 and 11 amino acids, respectively. While HK-1 and EKs are encoded by the Tac4 gene, NKB and neuropeptide F (NKF) are found in the Tac3 gene. In the mouse and rat, Tac4 encodes HK-1, while in humans, Tac4 is spliced into four variations to create EK-A through EK-D, respectively.
Fig.1. The tachykinins and tachykinin gene-related peptides. (Steinhoff, 2014)
Creative Biolabs provides professional tachykinin family in vitro assays and related tools to facilitate our customers' research of membrane protein drugs:
Overview of Tachykinin Family
- TACR1 (NK1R)
A GPCR with 407 residues was found to be encoded by the NK1R (SP receptor). The clone provided high-affinity binding for SP, which SP, NKA, and NKB replaced. Although NK1Rs from many species share a great deal of similarities, variations at crucial residues can impact how well they interact with antagonists. The short version of the human receptor is preferentially increased in monocytes and macrophages, specific brain areas (cortex, cerebellum), and colonic epithelial cells from patients with colitis-associated malignancy. This differential expression is likely functionally significant since the shortened receptor signals differently from the full-length NK1R.
- TACR2 (NK2R)
The first tachykinin receptor to be cloned was the NK2R (substance K receptor). A GPCR with 384 residues was encoded by the 2,458-nucleotide sequence. The potency ranking of the tachykinin response in oocytes expressing this clone was NKA>NKB>SP.
- TACR3 (NK3R)
A GPCR with 452 residues is encoded by the NK3R (NMB receptor). The rank order of efficacy for NKB, NKA, and SP was determined by ligand-binding assays on membranes from COS cells expressing the NK3R.
Fig.2. Mechanisms of tachykinin receptor signaling. (Steinhoff, 2014)
Tachykinin Family Drug Discovery
It has been obvious that a wide variety of animal taxa from various evolutionary clades have the tachykinin family of peptides well maintained. The signal transduction caused by several TKRPs has been studied using a variety of in vitro cell-based signal transduction studies. Studies have shown that different peptide isoforms can occasionally bind to different receptors and cause or stabilize various receptor conformations, giving rise to various receptor signaling features. Future expansion of these studies and research on the applicability of these in vitro findings to in vivo circumstances would be beneficial. Regardless, all of these characteristics increase the complexity of the invertebrate tachykinin signaling system, which in turn contributes to the variety of physiological functions that TKRPs perform in invertebrates.
Reference
- Steinhoff, M.S.; et al. Tachykinins and their receptors: contributions to physiological control and the mechanisms of disease. Physiological reviews. 2014, 94(1): 265-301.
