Abstract:
The present invention provides novel peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production.
Abstract:
The present invention relates to novel peptide compounds which are effective in modulating one or more melanocortin receptor types, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The compounds of the invention are of particular interest in relation to the treatment of obesity as well as a variety of diseases or conditions associated with obesity.
Abstract:
Small cyclic peptides of the formula X1-X2-X3-X4-X5-X6-X7-R 1 comprising 7-12 amino acid residues are provided. Said peptides are MC4 receptor agonists, and thus useful in the treatment of obesity and related diseases.
Abstract:
Novel peptides with antimicrobial activity are disclosed. The novel peptides are octomeric peptides modifiedfrom a-MSH. The modified a-MSH antimicrobial peptides disclosed herein may have enhanced activity against microbes over a-MSH due to modifications in peptide sequence and chirality of amino acids. Due an identified mechanism of action for antimicrobial activity in which cAMP accumulates in the microbial cell, it may be that microbes will not generate resistance to these modified a-MSH antimicrobial peptides.
Abstract:
Metallopeptides are provided for use in treatment of sexual dysfunction in mammals. The metallopeptides are agonists for at least one of melanocortin-3 or melanocortin-4 receptors. The metallopeptides are conformationally fixed on complexation of a metal ion-binding portion thereof with a metal ion. Also provided are metallopeptides that are antagonists for at least one of melanocortin-3 or melanocortin-4 receptors.
Abstract:
The present invention is concerned with modified biological peptides providing increased potency, prolonged activity and/or increased half-life thereof. The modification is made via coupling through an amide bond with at least one conformationally rigid substituent, either at the N-terminal of the peptide, the C-terminal of the peptide, on a free amino or carboxyl group along the peptide chain, or at a plurality of these sites. Those peptides exhibit clinical usefulness for example in treating states of insulin resistance associated with pathologies such as type II diabetes.
Abstract:
A retroviral vector particle having a modified envelope polypeptide wherein a portion of the receptor binding region of the envelope is replaced with a targeting polypeptide which binds to a ligand or a receptor on the targeted cells. The targeting polypeptide may be a single chain antibody. Such retroviral vector particles are useful in delivering genes encoding therapeutic agents to desired target cells or tissues in vivo.
Abstract:
The present invention provides novel cytokine restraining agents, which limit or control the biological activity of cytokines. The invention also provides pharmaceutical compositions comprising a cytokine restraining peptide and methods of administering the pharmaceutical composition to a subject. The invention further provides methods for using the novel peptides to restrain cytokine activity in a subject.
Abstract:
The subject invention pertains to a modified MCIR peptide ligand comprising a peptide that is a melanocortin 1 receptor (MCIR) ligand and a functionality or linker, such as a click functionality, for conjugation to a surface or agent. The modified MCIR peptide ligand can be coupled, e.g., via a click reaction with a complementary click functionality attached, to a moiety to form an MClR-targeted agent. Drugs, contrast agents, polymers, particles, micelles, surfaces of larger structures, or other moieties can be targeted to the MCIR. The subject invention also pertains to a MCIR 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 MCIR 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.