黑皮质素选择性配体-猫眼课题宝

黑皮质素选择性配体

批准号：

8850437

负责人：

Carrie Haskell-Luevano

金额：

$44.55万

依托单位：

UNIVERSITY OF MINNESOTA

依托单位国家：

美国

项目类别：

财政年份：

2012

资助国家：

美国

项目状态：

已结题

起止时间：

2012-05-01 至 2017-04-30

来源：

https://reporter.nih.gov/project-details/8850437

关键词：

ART protein Adverse effects Agonist Anorexia Nervosa Basic Science Biological Blood Pressure Body mass index Brain Bypass Cachexia Complex Country Coupled Data Developed Countries Diet Disease Eating Evaluation Exercise Fatty acid glycerol esters Feeding behaviors Figs - dietary Food Energy Food Intake Regulation G Protein-Coupled Receptor Genes GTP-Binding Proteins Genes Genetic Goals Heart Diseases Homeostasis Human Hyperphagia Hypertension In Vitro Knockout Mice Knowledge Laboratories Lead Ligands Link Malignant Neoplasms Mediating Melanocortin 3 Receptor Melanocortin 4 Receptor Metabolic Modification Morbidity - disease rate Mus Mutagenesis Neuraxis Neurosecretory Systems Non-Insulin-Dependent Diabetes Mellitus Obesity Obesity associated disease Outcome Pathway interactions Peptides Pharmaceutical Chemistry Pharmacology Phenotype Play Pro-Opiomelanocortin Publications Receptor Activation Regulation Research Research Project Grants Risk Factors Role Satiation Stroke Therapeutic Therapeutic Agents Transcript United States Validation Wasting Syndrome Weight base beta-Defensins candidate selection design drug discovery erection feeding human MC4R protein in vivo innovation male melanocortin receptor novel obesity treatment preprohormone receptor research study small molecule tool tumor growth

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DESCRIPTION (provided by applicant): Obesity (body mass index, BMI >30) afflicts millions of people in the United States and other countries, and is a major risk factor for heart disease, type II diabetes mellitus, stroke, hypertension, and morbidity. The G-protein coupled melanocortin-3 receptor (MC3R) is expressed in the central nervous system (brain) and is part of the melanocortin pathway involved in the regulation of energy homeostasis. The specific role of the MC3R in the regulation of obesity has not been clearly defined due to a lack of receptor specific ligands and a complex metabolic phenotype of the MC3R knockout mouse. This project is focused upon the drug discovery of MC3R selective molecules (peptide and small molecules), in vitro lead candidate selection, and use of wild type and knockout mice for further molecule lead selection and to probe the role of the MC3R in the novel hypothesis of the MC3R directly involved in the regulation of food intake and satiety. It is anticipated that MC3R ligands have the potential to become therapeutic ligands for obesity related diseases that bypass the human melanocortin-4 receptor (MC4R) agonist associated side effects of male erectile activity and hypertension.

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