38 results about "Melanocortin" patented technology

Multiple agent therapy for treatment of sexual dysfunction, including male erectile dysfunction, with sequential administration a type V phosphodiesterase inhibitor (PDE-5), such as sildenafil, preferably wherein the PDE-5 inhibitor is administered by oral dose means, and a melanocortin 3 and/or 4 receptor agonist, such as Ac-Nle-cyclo(-Asp-His-D-Phe-Arg-Trp-Lys)-OH (PT-141) preferably wherein the PT-141 is formulated for and administered by intranasal means, and further preferably wherein the PDE-5 inhibitor is administered prior to PT-141.

A process for detecting pig melanocortin-3 receptor (MC3R) gene and its single nucleotide polymorphism (SNP) includes extracting DNA from pig blood genom, designing primer based on human and mouse MC3R gene conservative region, PCR amplification, directly sequencing the PCR product, comparing sequence, analyzing and detecting SNP.

Multiple agent therapy for treatment of sexual dysfunction, including male erectile dysfunction, with sequential administration a type V phosphodiesterase inhibitor (PDE-5), such as sildenafil, preferably wherein the PDE-5 inhibitor is administered by oral dose means, and a melanocortin 3 and/or 4 receptor agonist, such as Ac-Nle-cyclo(-Asp-His-D-Phe-Arg-Trp-Lys)-OH (PT-141) preferably wherein the PT-141 is formulated for and administered by intranasal means, and further preferably wherein the PDE-5 inhibitor is administered prior to PT-141.

The present invention relates to methods of using GPR101 G protein-coupled receptor (GPCR) to screen candidate compounds as modulators of hypothalamic proopiomelanocortin (POMC)-derived biologically active peptide secretion. Modulators of GPR101 receptor modulate hypothalamic POMC-derived biologically active peptide secretion and are useful in the treatment of POMC-derived biologically active peptide-related disorders. POMC-derived biologically active peptides include, but are not limited to, α-melanocyte stimulating hormone (α-MSH), β-melanocyte stimulating hormone (β-MSH) and γ-melanocyte stimulating hormone (γ-MSH). Agonists and partial agonists of GPR101 receptor stimulate hypothalamic α-MSH, β-MSH and γ-MSH secretion and are useful, for example, in the treatment and prevention of obesity and conditions related thereto (including but not limited to Type 2 diabetes, insulin resistance, and metabolic syndrome), inflammation-associated disorders, and pyrexia. Inverse agonists and antagonists of GPR101 receptor inhibit α-MSH, β-MSH and γ-MSH secretion and are useful, for example, in the treatment and prevention of disorders such as cachexia.

The present invention provides compounds of Formula (I) that are useful for modulating the biological activity of the melanocortin-5 receptor (MC5R). Compounds of this invention can be used to treat diseases and/or conditions in which downregulation of MC5R is beneficial. Such diseases and/or conditions include, but are not limited to, acne, seborrhea, seborrheic dermatitis, cancer, and inflammatory diseases.

Certain embodiments of the invention provide a compound of formula (I):

R¹—C(═O)—W—X—Y—Z—N(R²)₂   (I)

or a salt thereof, wherein R¹, R², W, X, Y and Z are as defined herein, as well as methods of use thereof.

The invention provides compounds having the general formula I:

and salts thereof, wherein the variables Pro, DPro, DPhe, Arg, Trp, X¹, X², X³ and X⁴ have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

Disclosed are methods for the use of pro-opiomelanocortin-encoding polynucleotides in the creation of transformed host cells and transgenic animals. In particular, the use of recombinant adeno-associated viral (rAAV) vector compositions, virions, and pluralities of virus particles that comprise a nucleic acid segment that expresses one or more mammalian pro-opiomelanocortin polypeptides in suitably transformed host cells is described. Also disclosed are methods for the treatment and amelioration of symptoms of a variety of conditions and disorders in an animal, including hyperinsulinemia, obesity, adiposity, overeating, and related eating disorders.

The present invention provides compounds of Formula (I) that are useful for modulating the biological activity of the melanocortin-5 receptor (MC5R). Compounds of this invention can be used to treat diseases and/or conditions in which downregulation of MC5R is beneficial. Such diseases and/or conditions include, but are not limited to, acne, seborrhea, seborrheic dermatitis, cancer, and inflammatory diseases.

The present invention provides compounds of Formula (I) that are useful for modulating the biological activity of the melanocortin-5 receptor (MC5R). Compounds of this invention can be used to treat diseases and/or conditions in which downregulation of MC5R is beneficial. Such diseases and/or conditions include, but are not limited to, acne, seborrhea, seborrheic dermatitis, cancer, and inflammatory diseases.

Disclosed are chelating agent-conjugated α-MSH peptide derivatives, preparation methods thereof, and compositions for use in a diagnosis or treatment of a melanoma tumor containing the same as an active ingredient. The novel α-MSH peptide derivatives conjugated with chelating agent according to the present invention are highly selective to the melanocortin-1 receptor which is α-MSH receptor expressing in melanoma tumor and their labeling rate of a radioactive isotope is high. Also, they remain in kidney shortly and have high taking rate of the melanoma tumor. Therefore, with the aforesaid reasons, they may be effectively used for early diagnosis or treatment of melanoma tumor.

The invention relates to an application of Ipsen17 in preparing medicaments for treating obesity caused by melanocortin-4 receptor. Obesity means early-onset morbid obesity. 10 different kinds of cell membrane expression deficient human melanocortin-4 receptors can be rescued by functions of the Ipsen17 in human embryonic kidney cell HEK293, the EC 50 (effective concentration 50) expressed by the cell membrane of the melanocortin-4 receptor mutant rescued by the micro-molecular pharmaceutical molecular chaperone is less than 10-7M, wherein the EC50 of two mutants achieves the level of less than 10-8M. The EC50 of the signal molecule producing ability of the rescued melanocortin-4 receptor mutant is less than 10-7M, wherein the EC50 of a mutation receptor achieves the level less than 10-8M.

The invention provides compounds having the general formula I:

and salts thereof, wherein the variables R¹, R², R³ and R⁴ have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

There are provided herein transgenic non-human animals and cells comprising a transgene encoding either a mutated human melanocortin type-4 receptor (hMC4R) protein, wherein the mutated protein is misfolded and retained intracellularly, or a wild-type human melanocortin type-4 receptor (hMC4R) protein. Transgenes and targeting constructs used to produce such transgenic animals and cells are also provided, as well as methods for using the transgenic animals in pharmaceutical screening and as commercial research animals for modeling obesity.