Polyketide derivatives

Polyketides are a diverse class of compounds that are the source of many biologically active molecules such as tetracycline, erythromycin, epothilone, narbomycin, picromycin, rapamycin, spinocyn, and tylosin. Other important examples include naturally occurring immunosuppressants FK-506 (also known...

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Bibliographic Details
Main Authors Chu, Daniel, Fardis, Maria, Khosla, Chaitan, Reeves, Christopher, Santi, Daniel, Schirmer, Andreas
Format Patent
LanguageEnglish
Published 27.05.2003
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Summary:Polyketides are a diverse class of compounds that are the source of many biologically active molecules such as tetracycline, erythromycin, epothilone, narbomycin, picromycin, rapamycin, spinocyn, and tylosin. Other important examples include naturally occurring immunosuppressants FK-506 (also known as tacrolimus) and FK-520 (also known as ascomycin). The present invention relates to novel polyketides, host cells that produce the novel compounds, and methods fort their use. The compounds of the present invention are cyclic polyketides (also referred to as a "macrolides" or "macrolactones") that include as part of their structure and bind to a FK binding protein wherein Rand Rare each selected from the group consisting of hydrogen, methyl, ethyl, and methoxy, provided that at least one of Rand Ris hydrogen, methyl, or ethyl. As will be explained in greater detail below, the compounds of the present invention have properties such as favorable P450 enzyme activity profiles that are desirable for use of these compounds as drugs.