Abstract: Compositions and methods for treating a depressive disorder or an anxiety disorder in a subject in need of such treatment are described herein. A therapeutically effective amount of a composition comprising a melanocortin 5 receptor (MC5R) peptide ligand according to the following: in a pharmaceutically acceptable carrier is administered to the subject. Xaa can be Cha or Pro. The MC5R peptide is a selective MC5R antagonist, and administration thereof to the subject can treat the depressive or anxiety disorder with clinical improvement observed in a relatively short time.

Abstract: Ligand-drug conjugates for targeted melanoma therapies are disclosed herein. A ligand is conjugated to a cytotoxic cancer drug through a cleavage linker. The ligand can bind to an overexpressed receptor on a cancer cell, resulting in selectivity. This allows the drug to enter a cancer cell selectively and release the drug within that specific cancer cell. Such therapies provide selectivity to melanoma through a ligand that targets the MC1R receptor, which is highly expressed in 80% of malignant melanomas. The ligand-drug conjugates can be used to deliver a wide range of cytotoxic cancer drugs selective to melanoma cells which may solve the drug resistance problem of melanoma in current therapies.

Abstract: Modulators of melanocortin receptors (MCR) are provided herein. An MC5R peptide ligand is represented by to Formula 1: R1-Nle4-c[Xaa5-Yaa6-(NMe)D-Nal(2?)7-Arg8-Trp9-(NMe)Zaa10]-R2. R1 can be an acetyl, a glycosylated amino acid, —CO—(CH2)nCH3, or —CO—(CH2)nCF3 with n ranging from 1 to 6. R2 can be an —CONH2, —COOH, or —CH2OH. Xaa, Yaa, and Zaa can each be a natural amino acid or an unnatural amino acid.

Abstract: Compositions and methods for treating a depressive disorder or an anxiety disorder in a subject in need of such treatment are described herein. A therapeutically effective amount of a composition comprising a melanocortin 5 receptor (MC5R) peptide ligand according to the following: in a pharmaceutically acceptable carrier is administered to the subject. Xaa can be Cha or Pro. The MC5R peptide is a selective MC5R antagonist, and administration thereof to the subject can treat the depressive or anxiety disorder with clinical improvement observed in a relatively short time.

Abstract: Compositions and methods for treating a depressive disorder or an anxiety disorder in a subject in need of such treatment are described. A therapeutically effective amount of a composition comprising compound PG-20N in a pharmaceutically acceptable carrier is described. According to another embodiment, the subject disclosure features method of treating a depressive disorder or an anxiety disorder in a subject in need of such treatment. The method may comprise administering to the subject a therapeutically effective amount of a composition comprising PG-20N.

Abstract: Compositions and methods of treating a central nervous system (CNS) disorder or mood disorder in a subject in need of such treatment are described. A therapeutically effective amount of a composition comprising a melanocortin 5 receptor (MC5R) peptide ligand in a pharmaceutically acceptable carrier is administered to the subject. The MCSR peptide ligand is a selective MCSR antagonist, in which administration thereof to the subject can treat the CNS disorder or mood disorder with clinical improvement observed in a relatively short time.

Abstract: Modulators of melanocortin receptors (MCR) are provided herein. An MC5R peptide ligand is represented by to Formula 1: R1-Nle4-c[Xaa5-Yaa6-(NMe)D-Nal(2?)7-Arg8-Trp9-(NMe)Zaa10]-R2. R1 can be an acetyl, a glycosylated amino acid, —CO—(CH2)nCH3, or —CO—(CH2)nCF3 with n ranging from 1 to 6. R2 can be an —CONH2, —COON, or —CH2OH. Xaa, Yaa, and Zaa can each be a natural amino acid or an unnatural amino acid.

Abstract: Compositions and methods for treating a depressive disorder or an anxiety disorder in a subject in need of such treatment are described. A therapeutically effective amount of a composition comprising a melanocortin 5 receptor (MC5R) peptide ligand according to SEQ NO. 1: in a pharmaceutically acceptable carrier is administered to the subject. Xaa can be Cha or Pro. The MC5R peptide is a selective MC5R antagonist, and administration thereof to the subject can treat the depressive or anxiety disorder with clinical improvement observed in a relatively short time.

Abstract: A backbone N-methylation approach on SHU9119, a non-selective cyclic peptide antagonist at hMC3R and hMC4R. Systematic N-methylated derivatives of SHU9119, with all possible backbone N-methylation combinations have been synthesized and examined for their binding and functional activities towards melanocortin receptor subtypes 1, 3, 4 and 5 (hMCRs). Several N-methylated analogues, which have selective and potent agonists or antagonists activity for the hMC1R or hMC5R or selective antagonist activity for the hMC3R, are discovered from the library. The selective hMC1R ligands show strong binding for human melanoma cells. The first universal antagonist for all subtypes of hMCRs will be of critical importance to modulate the melanocortin system with endogenous agonists.

Abstract: A gamma-melanocyte stimulating hormone (?-MSH) derivative having improved stability, selectivity and bioavailabilty. The ?-MSH derivative is selective for the melanocortin-1 receptor (MC1 R) and is deliverable to skin cells via topical or transdermal delivery. The ?-MSH derivative is made up of naturally occurring amino acids for stimulating melanin from within for photoprotection of human skin against ultraviolet radiation damage.

Abstract: Compositions and methods of treating a central nervous system (CNS) disorder or mood disorder in a subject in need of such treatment are described. A therapeutically effective amount of a composition comprising a melanocortsn 5 receptor (MC5R) peptide ligand in a pharmaceutically acceptable carrier is administered to the subject. The MCSR peptide ligand is a selective MCSR antagonist, in which administration thereof to the subject can treat the CNS disorder or mood disorder with clinical improvement observed in a relatively short time.

Abstract: Compositions and methods for treating a depressive disorder or an anxiety disorder in a subject in need of such treatment are described. A therapeutically effective amount of a composition comprising compound PG-20N in a pharmaceutically acceptable carrier is described. According to another embodiment, the subject disclosure features method of treating a depressive disorder or an anxiety disorder in a subject in need of such treatment. The method may comprise administering to the subject a therapeutically effective amount of a composition comprising PG-20N.

Abstract: A gamma-melanocyte stimulating hormone (?-MSH) derivative having improved stability, selectivity and bioavailabilty. The ?-MSH derivative is selective for the melanocortin-1 receptor (MC1 R) and is deliverable to skin cells via topical or transdermal delivery. The ?-MSH derivative is made up of naturally occurring amino acids for stimulating melanin from within for photoprotection of human skin against ultraviolet radiation damage.

Abstract: Methods of treating a central nervous system (CNS) disorder or mood disorder in a subject in need of such treatment are described. A therapeutically effective amount of a composition comprising a melanocortin 5 receptor (MC5R) peptide ligand in a pharmaceutically acceptable carrier is administered to the subject. The MC5R peptide ligand is a selective MC5R antagonist, in which administration thereof to the subject can treat the CNS disorder or mood disorder with clinical improvement observed in a relatively short time.

Abstract: Methods of treating a depressive disorder or an anxiety disorder in a subject in need of such treatment are described. A therapeutically effective amount of a composition comprising Ac-Nle4-c[Asp5-His6-(NMe)D-Nal(2?)7-Arg8-Trp9-(NMe)Lys10]-NH2 (PEPTIDE 9), in a pharmaceutically acceptable carrier is administered to the subject. PEPTIDE 9 is a selective MC5R antagonist, in which administration thereof to the subject can treat the depressive or generalized anxiety disorder with clinical improvement observed in a relatively short time.

Abstract: Modulators of melanocortin receptors (MCR) are provided herein. An MC5R peptide ligand is represented by to Formula 1: R1-Nle4-c[Xaa5-Yaa6-(NMe)D-Nal(2?)7-Arg8-Trp9-(NMe)Zaa10]-R2. R1 can be an acetyl, a glycosylated amino acid, —CO—(CH2)n—CH3, or ?CO—(CH2)nCF3 with n ranging from 1 to 6. R2 can be an —CONH2, —COOH, or —CH2OH. Xaa, Yaa, and Zaa can each be a natural amino acid or an unnatural amino acid.

Abstract: Methods of treating a depressive disorder or an anxiety disorder in a subject in need of such treatment are described. A therapeutically effective amount of a composition comprising Ac-Nle4-c[Asp5-His6-(NMe)D-Nal(2?)7-Arg8-Trp9-(NMe)Lys10]-NH2 (PEPTIDE 9), in a pharmaceutically acceptable carrier is administered to the subject. PEPTIDE 9 is a selective MC5R antagonist, in which administration thereof to the subject can treat the depressive or generalized anxiety disorder with clinical improvement observed in a relatively short time.

Abstract: Methods of treating a central nervous system (CNS) disorder or mood disorder in a subject in need of such treatment are described. A therapeutically effective amount of a composition comprising a melanocortin 5 receptor (MC5R) peptide ligand in a pharmaceutically acceptable carrier is administered to the subject. The MC5R peptide ligand is a selective MC5R antagonist, in which administration thereof to the subject can treat the CNS disorder or mood disorder with clinical improvement observed in a relatively short time.

Abstract: A melanocortin 1 receptor (MC1R) peptide ligand-elastic vesicle complex. The MC1R peptide ligand is modified by coupling the MC1R ligand to 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, elastic vesicles, surfaces of larger structures, or other moieties can be targeted to the MC1R. The MC1R peptide ligand-elastic vesicle complex is prepared as a topical formulation.

Abstract: A melanocortin 1 receptor (MC1R) peptide ligand-elastic vesicle complex. The MC1R peptide ligand is modified by coupling the MC1R ligand to 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, elastic vesicles, surfaces of larger structures, or other moieties can be targeted to the MC1R. The MC1R peptide ligand-elastic vesicle complex is prepared as a topical formulation.