40 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.

Compositions and methods are disclosed for a non-naturally occurring melanocortin ligand comprised of a melanocortin analog coupled to a degradation-resistant C-terminal extension and, optionally, an N-terminal extension, to produce a stable melanocortin ligand having diminished or abolished cardiovascular activity while retaining desired melanocortin regulatory activity.

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 methods of treating overproduction of cortisol in a subject by administering to the subject a peptide that antagonizes adrenocorticotropin hormone (ACTH) to block the activation of melanocortin 2 receptors.

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.

The subject invention pertains to a modified MC1R peptide ligand comprising a peptide that is a melanocortin 1 receptor (MC1R) ligand and a functionality or linker, such as a click functionality, for conjugation to a surface or agent. The modified MC1R peptide ligand can be coupled, e.g., via a click reaction with a complementary click functionality attached, to a moiety to form an MC1R-targeted agent. Drugs, contrast agents, polymers, particles, micelles, surfaces of larger structures, or other moieties can be targeted to the MC1R. The subject invention also pertains to a MC1R peptide ligand-micelle complex comprising a peptide that is a melanocortin 1 receptor ligand connected via a click reaction product to a micelle. The micelle is stable in vivo and can target melanoma tumor cells by association of the peptide ligand with the MC1R or the tumor and selectively provide a detectable and / or therapeutic agent (such as an imageable contrast agent and / or anti-cancer agent) selectively to the tumor cell.

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.

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.

The subject invention pertains to a modified MC1R peptide ligand comprising a peptide that is a melanocortin 1 receptor (MC1R) ligand and a functionality or linker, such as a click functionality, for conjugation to a surface or agent. The modified MC1R peptide ligand can be coupled, e.g., via a click reaction with a complementary click functionality attached, to a moiety to form an MC1R-targeted agent. Drugs, contrast agents, polymers, particles, micelles, surfaces of larger structures, or other moieties can be targeted to the MC1R. The subject invention also pertains to a MC1R peptide ligand-micelle complex comprising a peptide that is a melanocortin 1 receptor ligand connected via a click reaction product to a micelle. The micelle is stable in vivo and can target melanoma tumor cells by association of the peptide ligand with the MC1R or the tumor and selectively provide a detectable and / or therapeutic agent (such as an imageable contrast agent and / or anti-cancer agent) selectively to the tumor cell.