The University of Arizona

The Texas A&M University System

Minying Cai

Victor J Hruby

Horst Kessler

Sean Shelby

Caurnel Morgan

Yang Zhou

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.

Conjugation of MCR1 ligand with cytotoxic drugs for treating skin cancer

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.

Modulators of melanocortin receptors for the treatment of depression and anxiety

Modulators of melanocortin receptors (MCR) are provided herein. An MC5R peptide ligand is represented by to Formula 1:R-Nle-[Xaa-Yaa-(NMe)D-Nal(2')-Arg-Trp-(NMe)Zaa]-R.Rcan be an acetyl, a glycosylated amino acid, &#x2014;CO&#x2014;(CH)CH, or &#x2014;CO&#x2014;(CH)CFwith n ranging from 1 to 6. Rcan be an &#x2014;CONH, &#x2014;COOH, or &#x2014;CHOH. Xaa, Yaa, and Zaa can each be a natural amino acid or an unnatural amino acid.

Modulators of melanocortin receptors

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. 

Methods for the treatment of depression and anxiety by a melanocortin 5 receptor antagonist, PG-20N

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.

Compositions and methods for treating central nervous system (CNS) disorders and mood disorders

A gamma-melanocyte stimulating hormone (&#x3b3;-MSH) derivative having improved stability, selectivity and bioavailabilty. The &#x3b3;-MSH derivative is selective for the melanocortin-1 receptor (MC1 R) and is deliverable to skin cells via topical or transdermal delivery. The &#x3b3;-MSH derivative is made up of naturally occurring amino acids for stimulating melanin from within for photoprotection of human skin against ultraviolet radiation damage.

Enhanced melanoma cancer prevention by novel melanotropins

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.

Methods for the treatment of central nervous system (CNS) disorders and mood disorders

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-Nle-c[Asp-His-(NMe)D-Nal(2')-Arg-Trp-(NMe)Lys]-NH(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.

Methods for the treatment of depression and anxiety

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.

Melanotropin ligands for skin care

A MC1R peptide ligand-elastic vesicle complex for preventing skin maladies. The MC1R peptide ligand is modified by coupling the melanocortin 1 receptor (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 patch or viscous emulsion that can be applied to human skin.

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Tucson, AZ, United States of America

Minying Cai