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Leptin

Metabolic & Circadian Hormones
OB proteinAdipokine

Overview

Leptin, also known as OB protein or Adipokine, is an endogenous hormone predominantly produced by adipose tissue. It belongs to the cytokine family and is classified as a peptide hormone. Leptin plays a crucial role in regulating energy balance and body weight by signaling the brain to reduce appetite and increase energy expenditure. Researchers have extensively studied leptin's role in obesity, metabolic disorders, and its potential therapeutic applications. Leptin's primary physiological roles include the regulation of appetite and energy homeostasis. It acts as a satiety factor, communicating the body's energy status to the hypothalamus in the brain. Research areas include its involvement in obesity, metabolic syndrome, and its potential role in reproductive health and immune function. Leptin's mechanism of action involves binding to the leptin receptor (LEPR), a member of the class I cytokine receptor family, primarily located in the hypothalamus. This binding activates several signaling pathways, including the JAK-STAT pathway, which leads to the regulation of gene expression involved in appetite suppression and energy expenditure. The pharmacokinetic properties of leptin include a circulating half-life of approximately 30 minutes. It is primarily metabolized in the kidneys and liver. Leptin's bioavailability varies depending on the route of administration, with limited data on oral bioavailability due to degradation in the gastrointestinal tract. Clinically, leptin is used in the treatment of leptin deficiency and certain types of lipodystrophy. It is not widely approved for general obesity treatment. Regulatory standing varies by region, with specific approvals for rare metabolic disorders.

Mechanism of Action

Leptin acts on the leptin receptor (LEPR) in the hypothalamus, activating the JAK-STAT signaling pathway. This cascade results in the regulation of genes that suppress appetite and increase energy expenditure.

Molecular Data

FormulaC87H138N22O28S2
Molecular Weight2004.3 g/mol
CAS Number177404-21-6
PubChem CID157010069

Half-Life & Pharmacokinetics

EndogenousCirculating half-life ~30 minutes
OralPoor bioavailability due to first-pass metabolism

Leptin's pharmacokinetics are influenced by its peptide nature, limiting oral bioavailability.

Storage

Temperature

Refrigerate at 2-8°C

Light

Protect from light

Form

Aqueous solution: use within specified time after reconstitution

Notes

Store in a stable environment to maintain efficacy.

Solubility

Leptin is soluble in water, which is relevant for its formulation as an injectable solution.

Legal Status

🇩🇪DE

Data limited

🇺🇸US

FDA approved for specific conditions like leptin deficiency; not a controlled substance.

🇦🇺AU

Data limited

🇬🇧UK

Data limited

Legal status information is provided for general reference only and may not reflect the most current regulatory changes. Always verify with official government sources before making any decisions.

9 Research Publications

Histone deacetylase 6 inhibition restores leptin sensitivity and reduces obesity.

Animal

Nature metabolism · 2022

Researchers found that inhibiting a specific enzyme called HDAC6 in obese mice helped restore their sensitivity to leptin, a hormone that regulates hunger and energy use. This led to reduced food intake and fat mass, suggesting that targeting HDAC6 could be a promising approach for treating obesity.

  • Inhibition of HDAC6 reduces food intake and fat mass in obese mice.
  • HDAC6 inhibitors improve glucose metabolism and reduce liver fat.
  • The effectiveness of HDAC6 inhibitors is linked to their ability to enhance leptin sensitivity.
PubMed

Leptin signaling and cancer chemoresistance: Perspectives.

Unknown

World journal of clinical oncology · 2017

Researchers observed that obesity, particularly through the hormone leptin, may contribute to cancer treatment resistance, especially in breast and pancreatic cancers. They highlighted how leptin promotes cancer growth and survival, complicating the effectiveness of chemotherapy.

  • Obesity increases the risk of several cancers and their resistance to treatment.
  • Leptin is linked to processes that promote cancer growth and survival.
  • Understanding leptin's role may help address drug resistance in cancer therapies.
PubMed

The soluble leptin receptor.

Review

Best practice & research. Clinical endocrinology & metabolism · 2015

Researchers observed that the soluble leptin receptor (sOB-R) plays a crucial role in how leptin, a hormone that helps regulate body weight, functions in the body. They found that levels of sOB-R can vary in conditions like obesity and diabetes, affecting how sensitive the body is to leptin. Additionally, factors like fat toxicity can increase the production of sOB-R, which may inhibit leptin's effects.

  • sOB-R is the main binding protein for leptin in the blood.
  • Levels of sOB-R are altered in metabolic disorders like obesity and diabetes.
  • Increased sOB-R can inhibit leptin's effects, while lower levels may indicate reduced leptin receptor presence.
PubMed

Adipokines and aging.

Review

Journal of atherosclerosis and thrombosis · 2011

Researchers observed that the balance of adipokines, which are molecules produced by fat tissue, plays a crucial role in aging and health. They found that both excess fat and loss of fat with age can lead to insulin resistance and other health issues, while centenarians tend to have better insulin sensitivity and favorable adipokine levels.

  • Dysregulation of adipokines is linked to insulin resistance and metabolic syndrome in obesity.
  • Centenarians have preserved insulin sensitivity and high levels of beneficial adipokines like adiponectin.
  • Age-related loss of fat tissue may contribute to adipose dysfunction and health challenges in older adults.
PubMed

Leptin-based therapeutics.

Unknown

Expert review of endocrinology & metabolism · 2010

Researchers observed that leptin, a hormone involved in regulating energy balance, is produced by various cells and affects many bodily functions. They found that both too much and too little leptin can lead to health issues. The study reviews new therapies targeting leptin receptors, which may offer potential treatments for various diseases beyond obesity.

  • Leptin is produced by cells other than fat cells and influences multiple physiological processes.
  • Both excess and insufficient leptin levels are linked to various health problems.
  • New leptin receptor modifiers show promise as treatments for metabolic, immune, and cancer-related diseases.
PubMed

Leptin in immunology.

Review

Journal of immunology (Baltimore, Md. : 1950) · 2005

Researchers observed that leptin, a hormone related to energy balance, plays a significant role in the immune system. They found that leptin influences immune cell development and function, particularly during energy deficiency. The review highlights recent insights into how leptin affects immune responses and its potential implications for health.

  • Leptin helps regulate energy balance in the body.
  • Leptin influences the development of immune cells.
  • Leptin's role in immune responses is linked to energy deficiency.
PubMed

Cytokines and feeding.

Review

International journal of obesity and related metabolic disorders : journal of the International Association for the Study of Obesity · 2001

Researchers found that certain proteins called cytokines, including interleukins and leptin, play a significant role in controlling food intake. They observed that these cytokines can suppress appetite during various health conditions, such as infections and inflammation, and may also influence eating behaviors in the brain.

  • Cytokines like interleukin-1 and leptin regulate feeding behavior.
  • Appetite suppression occurs during illnesses and cytokine treatments.
  • Cytokines produced in the brain can affect eating and anorexia.
PubMed

The Ob protein (leptin) and the kidney.

Review

Kidney international · 1998

Researchers observed that leptin, a hormone linked to body fat, is not effectively cleared by the kidneys in patients with kidney disease, leading to higher levels in their blood. In patients with end-stage renal disease, leptin levels were found to be four times higher than in healthy individuals. Further studies are needed to understand how leptin affects appetite and kidney function in these patients.

  • Leptin clearance by the kidneys is reduced in patients with kidney disease.
  • Patients with end-stage renal disease have significantly higher leptin levels compared to healthy individuals.
  • The role of leptin in appetite regulation and kidney function needs further investigation.
PubMed

[Leptin].

Review

Ceskoslovenska fysiologie · 1997

Researchers observed that leptin, a protein produced by fat tissue, plays a crucial role in regulating body weight and energy balance by communicating with the brain. They found that obese individuals often become resistant to leptin's effects, which can affect metabolism and feeding behaviors.

  • Leptin acts as a signal between fat tissue and the brain to control body fat and energy.
  • Obese individuals have higher levels of free leptin but may be resistant to its effects.
  • Leptin influences not only weight regulation but also the reproductive endocrine system.
PubMed

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This page is for informational and research purposes only. All information is based on published scientific literature. Nothing on this page constitutes medical advice or replaces consultation with a qualified healthcare professional.