Free Fatty Acid 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.
Free fatty acids (FFAs) are metabolic intermediaries that can be generated by the gut microbiota through the fermentation of carbohydrates or through endogenous synthesis. FFAs are known to have a number of both advantageous and harmful impacts on metabolic and inflammatory processes in addition to being a significant source of energy. FFAs act as agonists for a number of GPCRs, including the FFA1-4 family of four receptors. There has been some thought given to alternative therapeutic approaches, specifically by manipulating endogenous FFA concentrations through altering either dietary intake or production by gut microbiota, in addition to the traditional strategy of developing small-molecule therapeutics targeting these receptors.
As a leader in the field of drug discovery, Creative Biolabs can offer high-quality free fatty acid family assays and products to our customers:
Overview of Free Fatty Acid Family
Medium- and long-chain saturated and unsaturated FAs cause FFAR1 to become active. The most effective saturated ligands are pentadecanoic (C15) and palmitic (C16) acids, although chain length and saturation level are not significant factors in determining receptor affinity for unsaturated FAs. The insulin-secreting β cells, the K and L cells of the small and large intestines, splenocytes, and peripheral blood mononuclear cells are the most significant sites for FFAR1 expression. Moreover, FFAR1 is expressed in the α cells of the pancreatic islets, where it controls the release of glucagon in response to unsaturated fatty acids.
Propionate preferentially activates FFAR2, which is connected to Gαi/o and Gαq/11. High levels of FFAR2 expression in leucocytes suggest that this protein may be involved in the activation and differentiation of monocytes and polymorphonuclear cells. Both atherogenesis and the low-grade inflammation that goes along with obesity are controlled by these processes. Moreover, the L cells of the ileum and colon express FFAR2. Peptide YY is created and secreted by these entero-endocrine cells. The release of the latter is known to be accompanied by a decrease in hunger and a decrease in food intake through activities in the central nervous system. The former is known to be elevated in response to shortchain FAs.
Propionate, butyrate, and pentanoate can activate FFAR3, which couples with Gαi/o. Propionate, working through FFAR3, enhanced adipocytes' release of leptin, and giving it to mice boosted levels of circulating leptin. Hence, FFAR3, which is expressed on adipocytes, may be used by short-chain FAs to control appetite and energy homeostasis.
Fig.1 Signaling pathways for free fatty acid receptor (FFAR) family members. (Bartoszek, 2020)
LCFAs cause FFAR4 to be activated. FFAR4 has been found to be highly expressed in a variety of tissues and cell types, including the pancreas, adipose tissue, intestinal tissue, and macrophages. The fact that FFAR4 is found in a variety of tissues suggests that it performs a variety of tasks in the homeostatic control of systemic metabolism and inflammation. Although it was not found in pre-adipocytes, FFAR4 is also expressed in adipocytes.
FA derivatives are the natural ligands for GPR119, and it is possible that receptor agonists will be employed to treat diabetes. Agonists function as insulin secretagogues because the pancreatic β cell of GPR119 has high expression.
Fig.2 The natural ligand of GPR119. (Lee Kennedy, 2010)
References
- Bartoszek, A.; et al. Free fatty acid receptors as new potential therapeutic target in inflammatory bowel diseases. Pharmacological Research. 2020, 152: 104604.
- Lee Kennedy, R.; et al. Free fatty acid receptors: emerging targets for treatment of diabetes and its complications. Therapeutic advances in endocrinology and metabolism. 2010, 1(4): 165-175.
