Apelin 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.
Apelin and its G protein-coupled receptor (APLNR) have become important cardiovascular system signaling pathways. The peptide is an effective vasodilator and inotrope. Heart failure and pulmonary arterial hypertension both cause apelin to be downregulated. In order to fill in for the missing endogenous peptide, "selective" apelin agonists that preferentially activate G protein pathways have been developed. These agonists minimize receptor internalization and β-arrestin recruitment while also attenuating harmful β-arrestin signaling. Apelian receptor biased agonists have clinical potential.
Creative Biolabs recently has developed high-quality drug discovery tools for apelin receptor, advancing breakthrough science on drug discovery in research and therapeutic industries:
Overview of Apelin Receptor
Due to the apelin receptor's sequence resemblance to that of the angiotensin AT1 receptor (also known as APJ, APLNR, or AGTRL1), it is classified as a class A GPCR. Numerous species, including the mouse, rat, Western clawed frog, and zebrafish, have been found to express and conserve the human apelin receptor, which has 380 amino acids. The fact that some apelin responses are sensitive to pertussis toxin is consistent with coupling via Gai, and there is also evidence that Gaq-linked activation of phospholipase C (PLC) and protein kinase C is also involved (PKC). Ga13-activated myocyte enhancer factor 2 has a potential role in heart development. Through the involvement of β-arrestin, a protein that initiates receptor internalization as well as downstream signaling, the apelin receptor may function as a mechanosensor for stretch in the heart in a way that is apelin- and G protein-independent.
Fig.1 Mechanisms of apelin receptor.1,2
Apelin Receptor Drug Discovery
- Pulmonary arterial hypertension (PAH)
Right ventricular hypertrophy and finally death from right ventricular failure are the results of right ventricular failure in PAH, a deadly condition characterized by complicated remodeling of the pulmonary vasculature. Bone morphogenic protein receptor type II (BMPR-II) expression and function are diminished in patients with PAH, whether or not there are associated BMPR-II mutations. Even though apelin expression is downregulated in PAH, the receptor is still there and has a therapeutic target.
- Left ventricular HF
Enhancing apelin receptor signaling may be helpful in treating left ventricular hypertrophy in addition to right ventricular failure in PAH. Plasma apelin levels in people with HF are either unaffected or elevated in the early stages, but they decline as the disease progresses. These findings imply that apelin initially increases compensatorily to enhance cardiac contractility, but as the disease advances, apelin decreases or disappears.
References
- Yang, Peiran, Janet J. Maguire, and Anthony P. Davenport. "Apelin, Elabela/Toddler, and biased agonists as novel therapeutic agents in the cardiovascular system." Trends in pharmacological sciences 36.9 (2015): 560-567.
- Image retrieved from Figure 3 " Proposed mechanisms of apelin-induced positive inotropy and apelin-independent stretch-induced hypertrophy. " Yang, et al. 2015, used under CC BY 4.0. The original image was modified by extracting and the title was changed to " Mechanisms of apelin receptor.".
