N-formylpeptide 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.
Formyl-peptide family has three FPRs in humans: FPRs, FPR1, FPR2 and FPR3. The ability of FPR1 and FPR2 to identify N-formyl peptides, which are important proinflammatory byproducts produced in nature by either bacterial or host cell mitochondrial protein degradation, led to their initial identification. Chemotactic agonists that activate FPR1 and FPR2 cause a series of signaling cascades that result in myeloid cell movement, mediator release, enhanced phagocytosis, and novel gene transcription. Although monocytes and dendritic cells (DCs) express FPR3, its overall purpose is yet unknown.
Fig.1. Structural relationship and genomic organization of human FPR-encoding genes. (Migeotte, 2006)
Creative Biolabs can offer high-quality N-formylpeptide family related tools to contribute to the success of drug discovery:
Overview of N-formylpeptide Family
When exposed to the pertussis toxin, FPR, FPRL1 and FPRL2 completely lose their ability to respond to their respective agonists, which is evidence that they are all connected to the Gi family of G proteins. Over the past few years, a thorough examination of the intracellular signal transduction pathways that FPR and FPRL1 activated has been carried out. After the receptor binds to its agonists, the heterotrimeric G protein is activated by the receptor and splits into the α and βγ subunits, activating PLC. Phosphatidylinositol 4,5-biphosphate (PIP2) is hydrolyzed by PLC to produce IP3 and diacylglycerol (DAG), which activate PKC isoforms and release calcium from endoplasmic reticulum storage. Moreover, the phosphoinositide 3-kinase (PI3K)-Akt/PKB pathway is activated, namely PI3Kg, the isoform that is connected to the majority of chemoattractant receptors. Phospholipases A2 and D, mitogen-activated protein kinases ERK1/2, JNK, and p38, and tyrosine kinases like lyn, p125FAK, and others are examples of other intracellular effectors. Phospholipase D activity and the generation of oxidants are mediated by the formyl-peptide receptor and ERK1/2, respectively.
Fig.2. The main signalling pathways initiated by N-formyl peptide receptors. (Rabiet, 2007)
Neurotensin Family Drug Discovery
It is obvious that formyl peptide receptors are crucial for the control of immunological processes. Due to their great promiscuity as well as the fact that activation of the receptors can either stimulate or inhibit the immune response depending on the ligand, its concentration, and the cell type involved, they exhibit complicated functional features. Among G protein-coupled receptors, these receptors have the singular feature of being activated by a very varied range of natural ligands, including endogenous peptides, proteins, and lipids as well as foreign bacterial or viral products. They also react to a wide variety of artificial ligands, which are very helpful for pharmacological research.
References
- Migeotte, I.; et al. Formyl peptide receptors: a promiscuous subfamily of G protein-coupled receptors controlling immune responses. Cytokine & growth factor reviews. 2006, 17(6): 501-519.
- Rabiet, M.J.; et al. The N-formyl peptide receptors and the anaphylatoxin C5a receptors: an overview. Biochimie. 2007, 89(9): 1089-1106.
