Compounds with reduced ring size for use in diagnosing and treating melanoma, including metastatic melanoma and methods related to same
US-9493537-B2 · Nov 15, 2016 · US
US9624270B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9624270-B2 |
| Application number | US-201314090679-A |
| Country | US |
| Kind code | B2 |
| Filing date | Nov 26, 2013 |
| Priority date | Nov 29, 2012 |
| Publication date | Apr 18, 2017 |
| Grant date | Apr 18, 2017 |
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Occidiofungin is a cyclic nonribosomally synthesized antifungal peptide with submicromolar activity. This invention is directed to compositions enriched for particular occidiofungin diastereomers/conformers, methods of making compositions enriched for particular diastereomers/conformers and microorganisms suitable for producing enriched compositions of particular diastereomers/conformers. Methods of treating fungal infections or plants infected by fungi are also provided.
Opening claim text (preview).
We claim: 1. A method of increasing production of occidiofungin diastereomers/conformers corresponding to the diastereomers/conformers having the total correlation spectroscopy (TOCSY) fingerprint set forth in FIG. 5C as the green NH correlations in a microorganism producing occidiofungin comprising: decreasing the thioesterase activity of an occidiofungin gene D (ocfD) product (OcfD) in said microorganism, wherein said OcfD thioesterase activity is decreased by the introduction of a point mutation at the serine in position 2954 of the amino acid sequence of SEQ ID NO: 4, said point mutation replaces said serine with an alanine, glycine or proline, and culturing said microorganism under conditions to produce said occidiofungin diastereomers/conformers, wherein said increase in production of occidiofungin diastereomers/conformers is as compared to a reference microorganism without said decrease in OcfD thioesterase activity cultured under the same conditions.
Antibacterial agents · CPC title
the cyclisation not occurring through 2,4-diamino-butanoic acid · CPC title
Cyclic peptides {, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C (A61K38/043 - A61K38/046 take precedence)} · CPC title
having rings with four or more nitrogen atoms as the only ring hetero atoms · CPC title
acting on ester bonds (3.1) · CPC title
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