Angiotensin 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' membrane preparations are useful for membrane protein research. We offer membrane preparations to study the role of membrane proteins in diseases. Membrane preparations from Creative Biolabs are quality-assured frozen membranes from cells expressing recombinant or natural receptors.
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.
Blood pressure (BP), plasma volume, cardiac, renal, and neuronal functioning, as well as thirst responses, are all regulated by the multifunctional peptide hormone angiotensin II (Ang II). The primary effector molecule of the renin-angiotensin system, this peptide is crucial for hypertension and cardiac remodeling (RAS). Pathological effects appear in RAS that is ill or dysfunctional. The type 1 receptors (AT1Rs) and type 2 receptors (AT2Rs), two membrane receptors that mediate tissue-specific activities, are primarily responsible for the classical actions of Ang II on its target organs.
Fig.1 Angiotensin II receptors. (Dasgupta & Zhang, 2011)
Creative Biolabs is an undisputed leader in drug discovery and development, we can offer angiotensin family drug discovery tools to help scientists accelerate drug discovery and development projects:
Overview of Angiotensin Receptors
All organs, including the heart, kidney, liver, adrenals, brain, lung, and vasculature, express AT1Rs. In contrast to the fact that there is only one AT1R gene in humans, rats and mice have the AT1a receptor (AT1aR) and AT1b receptor (AT1bR) gene subtypes. These receptors have 359 amino acids, a denatured molecular weight of 40-41 kDa, and seven transmembrane domains. Multiple signaling pathways can be activated by AT1 receptor activation. Traditional G-protein-dependent signaling mechanisms predominantly act through AT1R to mediate Ang II's acute vasoconstrictor action. Ang II activated AT1 receptors have the ability to block adenylate cyclase and activate at least four separate effector pathways, including voltage-gated Ca2+ channels, phospholipase C, phospholipase D (PLD), and phospholipase A-2 (PLA-2).
Comparisons of the structural features of AT1 and AT2 receptors reveal some significant discrepancies. The N-terminus of AT2R has five possible sites for glycosylation. AT2R has a possible PKC phosphorylation site in its second intracellular loop, three consensus PKC phosphorylation sites in its cytoplasmic tail, and a site for cyclic AMP-dependent protein kinase phosphorylation. The fetal heart and aorta, as well as the kidney, lung, and liver, all have low levels of AT2R expression. Although AT2R expression rapidly diminishes after birth, suggesting that it may be crucial for fetal development, it can still be stimulated later in adulthood under pathological circumstances. For AT2R signaling, three main routes have been identified: the protein phosphatase pathway, which results in protein dephosphorylation, the activation of the NO/cGMP system, and the stimulation of PLA-2 with arachidonic acid release.
Angiotensin Receptors Drug Discovery
Hypertension, cardiac arrhythmia, stroke, diabetic nephropathy, and metabolic diseases are all brought on by an imbalance in AT1R signaling, and these conditions are being successfully treated with AT1R-blockers. As a result, AT1R antagonists, also known as AT1R-blockers (ARBs), are now considered to be a significant class of medications for the treatment of hypertension and heart failure, as well as the prevention of diabetic nephropathy.
Reference
- Dasgupta, C.; Zhang, L. Angiotensin II receptors and drug discovery in cardiovascular disease. Drug discovery today. 2011, 16(1-2): 22-34.
