Melanocortin receptor-specific cyclic peptide

##STR00001##

or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions or formulations and methods of preventing, ameliorating or treating melanocortin receptor-medicated diseases, indications, conditions and syndromes, including ocular indications, utilizing the cyclic peptide of the foregoing formula.

Melanocortin receptor-specific cyclic peptide

##STR00001##

or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions or formulations and methods of preventing, ameliorating or treating melanocortin receptor-medicated diseases, indications, conditions and syndromes, including ocular indications, utilizing the cyclic peptide of the foregoing formula.

Provided are cyclic peptidomimetics that can, e.g., antagonize the extracellular domain of EGFR, and methods of use thereof.

Provided are cyclic peptidomimetics that can, e.g., antagonize the extracellular domain of EGFR, and methods of use thereof.

The present invention provides a new type of alpha-helix nucleating cross-link (“staple”) formed by olefin metathesis of a proline derivative with an alkenyl side chain and another amino acid derivative with an alkenyl side chain. The proline derivatives as described herein have been found to be strong nucleators of alpha-helix formation. The invention also provides moieties for shielding the free amide N—H's at the N-terminus of an alpha-helix, thereby further stabilizing the helix. The proline derivatives, precursors prior to cross-linking, and the cross-linked peptides are provided as well as methods of using and preparing these compounds and peptides.

The present invention provides a new type of alpha-helix nucleating cross-link (“staple”) formed by olefin metathesis of a proline derivative with an alkenyl side chain and another amino acid derivative with an alkenyl side chain. The proline derivatives as described herein have been found to be strong nucleators of alpha-helix formation. The invention also provides moieties for shielding the free amide N—H's at the N-terminus of an alpha-helix, thereby further stabilizing the helix. The proline derivatives, precursors prior to cross-linking, and the cross-linked peptides are provided as well as methods of using and preparing these compounds and peptides.

A probe for imaging EGFR expressing cells includes an EGFR targeting moiety, a reporter moiety, and a hydrophilic linker that links the EGFR targeting moiety to the reporter moiety. The hydrophilic linker enhances solubility of the probe in an aqueous media as well as binding affinity of the probe to EGFR expressing cells.

Disclosed in the present invention are an immobilized cycloaliphatic peptide acyltransferase and a preparation method and use thereof. The cycloaliphatic peptide acyltransferase is immobilized on a carrier; the cycloaliphatic peptide acyltransferase is derived from natural or artificial mutants or variants thereof, or can be obtained by introducing a foreign cyclic acyltransferase gene and transforming thereafter; the material of the carrier is selected from an inorganic carrier or a polypropylene resin carrier. Also disclosed in the present invention are the preparation method for the immobilized cycloaliphatic peptide acyltransferase and uses thereof.

Disclosed in the present invention are an immobilized cycloaliphatic peptide acyltransferase and a preparation method and use thereof. The cycloaliphatic peptide acyltransferase is immobilized on a carrier; the cycloaliphatic peptide acyltransferase is derived from natural or artificial mutants or variants thereof, or can be obtained by introducing a foreign cyclic acyltransferase gene and transforming thereafter; the material of the carrier is selected from an inorganic carrier or a polypropylene resin carrier. Also disclosed in the present invention are the preparation method for the immobilized cycloaliphatic peptide acyltransferase and uses thereof.

Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of lipoprotein signal peptidase II (LspA), a key protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.