Wortmannin, an antibiotic produced by Penicillium wortmanni

Brian, P. W.; Curtis, Peter J.; Hemming, H. G.; Norris, Grace

doi:10.1016/s0007-1536(57)80033-3

Cited by 109 publications

(46 citation statements)

References 2 publications

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“…Two well-known and isoform-unselective PI3K inhibitors are the fungal metabolite wortmannin (compound 1, Figure 2; Brian et al, 1957) and LY294002 (compound 2, Figure 2; Vlahos et al, 1994). These compounds block the enzymatic activity of PI3Ks by different mechanisms.…”

Section: Inhibitors Of the Lipid Kinase Activity Of Pi3kmentioning

confidence: 99%

Drug discovery approaches targeting the PI3K/Akt pathway in cancer

2008

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Section: Inhibitors Of the Lipid Kinase Activity Of Pi3kmentioning

confidence: 99%

Drug discovery approaches targeting the PI3K/Akt pathway in cancer

2008

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“…2) is a toxic steroidal furan that is produced by various fungi including Penicillium wortmanni [54]. The first kinase shown to be targeted by wortmannin was smooth muscle myosin light chain kinase (IC 50 = 0.17 μM).…”

Section: Mtor Kinase Inhibitorsmentioning

confidence: 99%

Rapamycin and mTOR kinase inhibitors

2008

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Mammalian target of rapamycin (mTOR) is a protein kinase that controls cell growth, proliferation, and survival. mTOR signaling is often upregulated in cancer and there is great interest in developing drugs that target this enzyme. Rapamycin and its analogs bind to a domain separate from the catalytic site to block a subset of mTOR functions. These drugs are extremely selective for mTOR and are already in clinical use for treating cancers, but they could potentially activate an mTOR-dependent survival pathway that could lead to treatment failure. By contrast, small molecules that compete with ATP in the catalytic site would inhibit all of the kinase-dependent functions of mTOR without activating the survival pathway. Several non-selective mTOR kinase inhibitors have been described and here we review their chemical and cellular properties. Further development of selective mTOR kinase inhibitors holds the promise of yielding potent anticancer drugs with a novel mechanism of action.

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“…The fungicidal metabolites wortmannin (38) (Brian et al 1957) and 11-desacetoxywortmannin (39) (Haefliger and Hauser 1973) were first obtained from Penicillium species. Chemical and biological properties have recently been reviewed for 38 (Wipf and Halter 2005).…”

Section: Viridinsmentioning

confidence: 99%

Secondary metabolites from species of the biocontrol agent Trichoderma

et al. 2007

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Trichoderma species are free-living fungi that are highly interactive in root, soil and foliar environments and have been used successfully in field trials to control many crop pathogens. Structural and biological studies of the metabolites isolated from Trichoderma species are reviewed. This review, encompassing all the literature in this field up to the present and in which 269 references are cited, also includes a detailed study of the biological activity of the metabolites, especially the role of these metabolites in biological control mechanisms. Some aspects of the biosynthesis of these metabolites and related compounds are likewise discussed.

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Wortmannin, an antibiotic produced by Penicillium wortmanni

Cited by 109 publications

References 2 publications

Drug discovery approaches targeting the PI3K/Akt pathway in cancer

Drug discovery approaches targeting the PI3K/Akt pathway in cancer

Rapamycin and mTOR kinase inhibitors

Secondary metabolites from species of the biocontrol agent Trichoderma

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