TY - JOUR
T1 - Leptin-activity blockers
T2 - Development and potential use in experimental biology and medicine1
AU - Gertler, Arieh
AU - Solomon, Gili
PY - 2013/6
Y1 - 2013/6
N2 - 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.
AB - 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.
KW - Antagonist
KW - Anti-autoimmune diseases
KW - Blood pressure
KW - Cancer
KW - Inflammatory disease
KW - Leptin
KW - Metabolic syndrome
KW - T2DM model
KW - Uremic cachexia
UR - http://www.scopus.com/inward/record.url?scp=84885457523&partnerID=8YFLogxK
U2 - 10.1139/cjpp-2013-0012
DO - 10.1139/cjpp-2013-0012
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C2 - 24117254
AN - SCOPUS:84885457523
SN - 0008-4212
VL - 91
SP - 873
EP - 882
JO - Canadian Journal of Physiology and Pharmacology
JF - Canadian Journal of Physiology and Pharmacology
IS - 11
ER -