Leptin is a hormone predominantly made by adipose cells and enterocytes in the small intestine that helps to regulate energy balance by inhibiting hunger. Leptin acts on cell receptors in the arcuate nucleus of the hypothalamus. In recent years, researchers have developed various leptin antagonists to study and potentially treat conditions related to leptin signaling, such as obesity and metabolic disorders.
The Leptin Antagonist Triple Mutant Ovine Recombinant, often referred to as Leptin tA Ovine, is a specially engineered protein designed to inhibit the action of leptin. This antagonist is a single non-glycosylated polypeptide chain containing 146 amino acids, with an additional alanine at the N-terminus. The molecular mass of this protein is approximately 16 kDa .
The Leptin Antagonist Triple Mutant is characterized by three specific mutations: L39A, D40A, and F41A. These mutations are introduced to disrupt the normal binding of leptin to its receptor, thereby inhibiting its biological activity. The protein is produced using recombinant DNA technology in Escherichia coli (E. coli) and is purified through proprietary chromatographic techniques .
The Leptin Antagonist Triple Mutant Ovine Recombinant is typically supplied as a white lyophilized (freeze-dried) powder. It is recommended to reconstitute the lyophilized protein in sterile water or sterile 0.4% NaHCO3 adjusted to pH 8, at a concentration of not less than 100 µg/ml. The protein is stable at room temperature for several weeks when lyophilized, but should be stored desiccated below -18°C for long-term storage .
This leptin antagonist is capable of inhibiting leptin-induced proliferation of BAF/3 cells that are stably transfected with the long form of the mouse leptin receptor. It also inhibits various leptin effects in several in vitro bioassays. This makes it a valuable tool for studying leptin signaling pathways and for potential therapeutic applications in conditions where leptin activity needs to be modulated .
Leptin antagonists, including the Leptin Antagonist Triple Mutant Ovine Recombinant, are used extensively in research to understand the role of leptin in energy homeostasis, obesity, and metabolic disorders. They are also being explored for their potential therapeutic applications in treating conditions such as obesity, diabetes, and other metabolic diseases .