Constitutive activity of neural melanocortin receptors.

[1]  Y. Tao.  The melanocortin-4 receptor: physiology, pharmacology, and pathophysiology. , 2010, Endocrine reviews.

[2]  G. Nikiforovich,et al.  Computational modeling of constitutively active mutants of GPCRs C5a receptor. , 2010, Methods in enzymology.

[3]  L. Pennacchio,et al.  Association of functionally significant Melanocortin-4 but not Melanocortin-3 receptor mutations with severe adult obesity in a large North American case-control study. , 2009, Human molecular genetics.

[4]  Zhen‐Chuan Fan,et al.  Functional characterization and pharmacological rescue of melanocortin-4 receptor mutations identified from obese patients , 2009, Journal of cellular and molecular medicine.

[5]  H. Biebermann,et al.  A novel melanocortin-4 receptor gene mutation in a female patient with severe childhood obesity , 2009, Endocrine.

[6]  Y. Tao.  Mutations in melanocortin-4 receptor and human obesity. , 2009, Progress in molecular biology and translational science.

[7]  Ya-Xiong Tao,et al.  Constitutive activation of G protein-coupled receptors and diseases: insights into mechanisms of activation and therapeutics. , 2008, Pharmacology & therapeutics.

[8]  Oliver P. Ernst,et al.  Crystal structure of opsin in its G-protein-interacting conformation , 2008, Nature.

[9]  Zhen‐Chuan Fan,et al.  Pharmacological analyses of two naturally occurring porcine melanocortin-4 receptor mutations in domestic pigs. , 2008, Domestic animal endocrinology.

[10]  M. Petroni,et al.  Sporadic mutations in melanocortin receptor 3 in morbid obese individuals , 2008, European Journal of Human Genetics.

[11]  Zhen‐Chuan Fan,et al.  Molecular cloning and pharmacological characterization of porcine melanocortin-3 receptor. , 2007, The Journal of endocrinology.

[12]  R. Stevens,et al.  High-Resolution Crystal Structure of an Engineered Human β2-Adrenergic G Protein–Coupled Receptor , 2007, Science.

[13]  Y. Lee,et al.  The role of melanocortin 3 receptor gene in childhood obesity. , 2007, Diabetes.

[14]  Y. Tao.  Functional characterization of novel melanocortin-3 receptor mutations identified from obese subjects. , 2007, Biochimica et biophysica acta.

[15]  P. Plas,et al.  Identification of a novel series of benzimidazoles as potent and selective antagonists of the human melanocortin-4 receptor. , 2007, Bioorganic & medicinal chemistry letters.

[16]  B. Cheung,et al.  Identification and functional characterization of three novel human melanocortin‐4 receptor gene variants in an obese Chinese population , 2006, Clinical endocrinology.

[17]  Zhimin Xiang,et al.  Pharmacological characterization of 40 human melanocortin-4 receptor polymorphisms with the endogenous proopiomelanocortin-derived agonists and the agouti-related protein (AGRP) antagonist. , 2006, Biochemistry.

[18]  R. Cone.  Studies on the physiological functions of the melanocortin system. , 2006, Endocrine reviews.

[19]  T. Meitinger,et al.  Prevalence, spectrum, and functional characterization of melanocortin-4 receptor gene mutations in a representative population-based sample and obese adults from Germany. , 2006, The Journal of clinical endocrinology and metabolism.

[20]  W. Millard,et al.  Molecular Mechanism of the Constitutive Activation of the L250Q Human Melanocortin‐4 Receptor Polymorphism ‡ , 2006, Chemical biology & drug design.

[21]  Robert A. McGovern,et al.  Divergence of Melanocortin Pathways in the Control of Food Intake and Energy Expenditure , 2005, Cell.

[22]  D. Segaloff,et al.  Functional analyses of melanocortin-4 receptor mutations identified from patients with binge eating disorder and nonobese or obese subjects. , 2005, The Journal of clinical endocrinology and metabolism.

[23]  J. Yanovski,et al.  Co-occurrence of two partially inactivating polymorphisms of MC3R is associated with pediatric-onset obesity. , 2005, Diabetes.

[24]  Y. Tao.  Molecular mechanisms of the neural melanocortin receptor dysfunction in severe early onset obesity , 2005, Molecular and Cellular Endocrinology.

[25]  R. Cone.  Anatomy and regulation of the central melanocortin system , 2005, Nature Neuroscience.

[26]  B. Conklin,et al.  Constitutive activity of the melanocortin-4 receptor is maintained by its N-terminal domain and plays a role in energy homeostasis in humans. , 2004, The Journal of clinical investigation.

[27]  D. Segaloff,et al.  Functional characterization of melanocortin-3 receptor variants identify a loss-of-function mutation involving an amino acid critical for G protein-coupled receptor activation. , 2004, The Journal of clinical endocrinology and metabolism.

[28]  Ping Li,et al.  Identification of 2-[2-[2-(5-bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole (ML00253764), a small molecule melanocortin 4 receptor antagonist that effectively reduces tumor-induced weight loss in a mouse model. , 2004, Journal of medicinal chemistry.

[29]  D. Segaloff,et al.  Functional characterization of melanocortin-4 receptor mutations associated with childhood obesity. , 2003, Endocrinology.

[30]  Richard R. Neubig,et al.  Inverse agonist activity of agouti and agouti-related protein , 2003, Peptides.

[31]  Tim Cheetham,et al.  Clinical spectrum of obesity and mutations in the melanocortin 4 receptor gene. , 2003, The New England journal of medicine.

[32]  Y. Lee,et al.  A novel melanocortin 3 receptor gene (MC3R) mutation associated with severe obesity. , 2002, The Journal of clinical endocrinology and metabolism.

[33]  C. Haskell-Luevano,et al.  Agouti-related protein functions as an inverse agonist at a constitutively active brain melanocortin-4 receptor , 2001, Regulatory Peptides.

[34]  R. Adan,et al.  AgRP(83-132) acts as an inverse agonist on the human-melanocortin-4 receptor. , 2001, Molecular endocrinology.

[35]  R. Cone,et al.  A Unique Metalolic Sysdrone Causes Obesity in the Melanocortin-3 Receptor-Deficient Mouse. , 2000, Endocrinology.

[36]  Yue Feng,et al.  Inactivation of the mouse melanocortin-3 receptor results in increased fat mass and reduced lean body mass , 2000, Nature Genetics.

[37]  A. Abell,et al.  Constitutive activation of G protein-coupled receptors as a result of selective substitution of a conserved leucine residue in transmembrane helix III. , 2000, Molecular endocrinology.

[38]  K. Clément,et al.  Melanocortin-4 receptor mutations are a frequent and heterogeneous cause of morbid obesity. , 2000, The Journal of clinical investigation.

[39]  K. Clément,et al.  A frameshift mutation in human MC4R is associated with a dominant form of obesity , 1998, Nature Genetics.

[40]  S. O’Rahilly,et al.  A frameshift mutation in MC4R associated with dominantly inherited human obesity , 1998, Nature Genetics.

[41]  R. Cone,et al.  Targeted Disruption of the Melanocortin-4 Receptor Results in Obesity in Mice , 1997, Cell.

[42]  H. Okayama,et al.  High-efficiency transformation of mammalian cells by plasmid DNA. , 1987, Molecular and cellular biology.

[43]  D. Kipnis,et al.  Radioimmunoassay for the measurement of adenosine 3',5'-cyclic phosphate. , 1969, Proceedings of the National Academy of Sciences of the United States of America.