Rene et al., 2010 - Google Patents
Pharmacological chaperones restore function to MC4R mutants responsible for severe early-onset obesityRene et al., 2010
View PDF- Document ID
- 10012945085760866514
- Author
- Rene P
- Le Gouill C
- Pogozheva I
- Lee G
- Mosberg H
- Farooqi I
- Valenzano K
- Bouvier M
- Publication year
- Publication venue
- The Journal of pharmacology and experimental therapeutics
External Links
Snippet
Heterozygous null mutations in the melanocortin-4 receptor (MC4R) cause early-onset obesity in humans, indicating that metabolic homeostasis is sensitive to quantitative variation in MC4R function. Most of the obesity-causing MC4R mutations functionally …
- 230000000144 pharmacologic effect 0 title abstract description 22
Classifications
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by the preceding groups
- G01N33/48—Investigating or analysing materials by specific methods not covered by the preceding groups biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
- G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
- G01N33/502—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics for testing non-proliferative effects
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
- G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
- G01N2333/705—Assays involving receptors, cell surface antigens or cell surface determinants
- G01N2333/72—Assays involving receptors, cell surface antigens or cell surface determinants for hormones
- G01N2333/726—G protein coupled receptor, e.g. TSHR-thyrotropin-receptor, LH/hCG receptor, FSH
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
- C07K14/72—Receptors; Cell surface antigens; Cell surface determinants for hormones
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by the preceding groups
- G01N33/48—Investigating or analysing materials by specific methods not covered by the preceding groups biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
- G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
- G01N33/5044—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics involving specific cell types
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by the preceding groups
- G01N33/48—Investigating or analysing materials by specific methods not covered by the preceding groups biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/68—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
- G01N33/6872—Intracellular protein regulatory factors and their receptors, e.g. including ion channels
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by the preceding groups
- G01N33/48—Investigating or analysing materials by specific methods not covered by the preceding groups biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/53—Immunoassay; Biospecific binding assay
- G01N33/566—Immunoassay; Biospecific binding assay using specific carrier or receptor proteins as ligand binding reagents where possible specific carrier or receptor proteins are classified with their target compounds
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| Rene et al. | Pharmacological chaperones restore function to MC4R mutants responsible for severe early-onset obesity | |
| CA2930810C (en) | Pharmacological chaperones for treating obesity | |
| Ersoy et al. | Mechanism of N-terminal modulation of activity at the melanocortin-4 receptor GPCR | |
| van der Velden et al. | Perspective: implications of ligand–receptor binding kinetics for therapeutic targeting of G protein-coupled receptors | |
| Chen et al. | Identification of serine 348 on the apelin receptor as a novel regulatory phosphorylation site in apelin-13-induced G protein-independent biased signaling | |
| Noorwez et al. | A high-throughput screening method for small-molecule pharmacologic chaperones of misfolded rhodopsin | |
| Deml et al. | Interactions of histamine H1-receptor agonists and antagonists with the human histamine H4-receptor | |
| Sensi et al. | Oxysterols act as promiscuous ligands of class-A GPCRs: in silico molecular modeling and in vitro validation | |
| Wang et al. | Rescue of defective MC4R cell-surface expression and signaling by a novel pharmacoperone Ipsen 17 | |
| Rahman et al. | Evaluation of amide bioisosteres leading to 1, 2, 3-triazole containing compounds as GPR88 agonists: design, synthesis, and structure–activity relationship studies | |
| Bumbak et al. | Conformational changes in tyrosine 11 of neurotensin are required to activate the neurotensin receptor 1 | |
| Han et al. | Characterization of G protein coupling mediated by the conserved D1343. 49 of DRY motif, M2416. 34, and F2516. 44 residues on human CXCR1 | |
| Saitoh et al. | The present and future of synthetic orexin receptor agonists | |
| Peri et al. | A bitter anti-inflammatory drug binds at two distinct sites of a human bitter taste GPCR | |
| Colson et al. | A hydrophobic cluster between transmembrane helices 5 and 6 constrains the thyrotropin-releasing hormone receptor in an inactive conformation | |
| Adams et al. | Development of ProTx-II analogues as highly selective peptide blockers of Nav1. 7 for the treatment of pain | |
| Guan et al. | Indole-containing amidinohydrazones as nonpeptide, dual RXFP3/4 agonists: synthesis, structure–activity relationship, and molecular modeling studies | |
| Hogan et al. | Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3. 28 (125), I3. 32 (129), and I7. 42 (291) is critical for receptor activation | |
| Kaiser et al. | Biased agonists at the human Y1 receptor lead to prolonged membrane residency and extended receptor G protein interaction | |
| Toth et al. | Encoding the β-arrestin trafficking fate of ghrelin receptor GHSR1a: C-tail-independent molecular determinants in GPCRs | |
| Desai et al. | Molecular mechanism of action of triazolobenzodiazepinone agonists of the type 1 cholecystokinin receptor. Possible cooperativity across the receptor homodimeric complex | |
| Manfra et al. | Downregulation of 5-HT7 serotonin receptors by the atypical antipsychotics clozapine and olanzapine. Role of motifs in the C-terminal domain and interaction with GASP-1 | |
| JPH11507518A (en) | Functional bioassay for agonists and antagonists of receptors coupled to G proteins | |
| Heller et al. | Novel probes establish Mas-related G protein-coupled receptor X1 variants as receptors with loss or gain of function | |
| Florén et al. | Multiple interaction sites of galnon trigger its biological effects |