title: Leptin-activity blockers: development and potential use in experimental biology and medicine.
abstract: The first adipokine, leptin, discovered almost 20 years ago, is secreted into circulation mainly from adipose tissue and acts both centrally and peripherally. Leptin regulates energy metabolism, reproductive function, bone metabolism, and immune response. However in some physiological or pathological situations such as enhancement of undesired immune responses in autoimmune diseases, tumorigenesis, elevated blood pressure, and certain cardiovascular pathologies, leptin activity may be harmful. In this review we screen different approaches to blocking leptin action, in vitro and in vivo. The recent development of superactive leptin muteins exhibiting antagonistic properties, and other leptin-action-blocking peptides, proteins, monoclonal antibodies, and nanobodies, opens new perspectives for their use in research, and eventually, therapy for cachexia, autoimmune disease, cancer, and other pathologies.
authors.affiliation: The Institute of Biochemistry, Food Science, and Nutrition, The Hebrew University of Jerusalem, P.O. Box 12, Rehovot 76100, Israel.
authors.forename: Arieh
authors.initials: A
authors.lastname: Gertler
authors.forename: Gili
authors.initials: G
authors.lastname: Solomon
mesh_terms: D000273:Adipose Tissue / Q000503:physiopathology; D000818:Animals; D057134:Antibodies, Neutralizing / Q000494:pharmacology; D002162:Camelus; D006801:Humans; D020738:Leptin / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000494:pharmacology / Q000502:physiology; D009765:Obesity / Q000503:physiopathology; D010455:Peptides / Q000138:chemical synthesis / Q000494:pharmacology; D054411:Receptors, Leptin / Q000037:antagonists & inhibitors / Q000235:genetics / Q000502:physiology; D013045:Species Specificity
chemical_list: D057134:Antibodies, Neutralizing; D020738:Leptin; D010455:Peptides; D054411:Receptors, Leptin