RPR113228, a Novel Farnesyl Protein Transferase Inhibitor Produced by Chrysosporium lobatum.

Pyl, Didier Van Der; Cans, Pierre; Debernard, Jean Jacques; Herman, Frédéric; Lelièvre, Yves; Tahraoui, L.; Vuilhorgne, Marc; Leboul, J.

doi:10.7164/antibiotics.48.736

Cited by 19 publications

(4 citation statements)

References 5 publications

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“…multifidum . The literature describes several chemical prospecting works carried out on species of the Chrysosporium genus, which led to the discovery of groups of compounds such as adenopeptines [27], nucleosides [28], zearalenone derivatives [29], benzoquinones [30], naphthoquinones [31], anthraquinones [32], benzolactones [33], naphthopyrones [34], naphthalenes [35], phenyl-2(1H)-pyridinones [36], alkylphenols [37], bisdechlorogeodins [38], sterols [39,40], and caryophillenes [41]. However, there is no prior record of any α-pyrone derivatives, so this would be the first report of these compounds within the genus.…”

Section: Resultsmentioning

confidence: 99%

Identification and characterization of compounds from Chrysosporium multifidum, a fungus with moderate antimicrobial activity isolated from Hermetia illucens gut microbiota

et al. 2019

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The gut microbiota of insects is composed of a wide range of microorganisms which produce bioactive compounds that protect their host from pathogenic attack. In the present study, we isolate and identify the fungus Chrysosporium multifidum from the gut of Hermetia illucens larvae. Extract from C. multifidum culture broth supernatant showed moderate activity against a strain of methicillin-resistant Staphylococcus aureus (MRSA). Bioguided isolation of the extract resulted in the characterization of six α-pyrone derivatives (1–6) and one diketopiperazine (7). Of these compounds, 5,6-dihydro-4-methoxy-6-(1-oxopentyl)-2H-pyran-2-one (4) showed the greatest activity (IC50 = 11.4 ± 0.7 μg/mL and MIC = 62.5 μg/mL) against MRSA.

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Section: Resultsmentioning

confidence: 99%

Identification and characterization of compounds from Chrysosporium multifidum, a fungus with moderate antimicrobial activity isolated from Hermetia illucens gut microbiota

et al. 2019

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“…This study is the first published chemical characterization of Chrysosporium multifidum. The literature describes several chemical prospecting works carried out on species of the Chrysosporium genus, which led to the discovery of groups of compounds such as: adenopeptines [35], nucleosides [36], zearalenone derivatives, benzoquinones [38], naphthaquinones [39], anthraquinones [40], benzolactones [41], naphthopyrones [42], naphthalenes [43], phenyl-2(1H)-pyridinones [44], alkylphenols [45], bisdechlorogeodins [46], sterols [47, 48], and caryophillenes [49]. However, there is no prior record of any α-pyrones derivatives, so this would be the first report of these compounds within the genus.…”

Section: Resultsmentioning

confidence: 99%

Bioactive compounds from Chrysosporium multifidum, a fungus isolated from Hermetia illucens gut microbiota

Correa

Cabanillas

Jullian

et al. 2019

Preprint

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The gut microbiota of insects contains a wide range of organisms that protect them against the attack of pathogens by releasing various types of bioactive compounds. In the present study, we report the isolation and identification of the fungus Chrysosporium multifidum as a component of the microbiota from the larval gut of Hermetia illucens. Extract from the broth culture of C. multifidum showed moderate activity on a strain of methicillin-resistant Staphylococcus aureus (MRSA). The bioguided isolation of the extract resulted in the characterization of six α-pyrone derivatives (1-6) and one diketopiperazines (7), among them 5,6-dihydro-4-methoxy-6-(1-oxopentyl)-2H-pyran-2-one (4) showed the best activity (IC50 = 11.4 ± 0.7 µg/ml and MIC = 62.5 μg/ml).

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“…Inhibitor RPR-113228 has a hydroIn the search for potent farnesyltransferase inhibitors, a series of natural products with novel chemical philic region that contains a phosphate and three adjacent hydroxyl groups. 113 The hydrophobic stestructures has been discovered from random screening. Unlike inhibitors from rational chemical design, roid skeleton of this compound probably binds to large hydrophobic pockets in the enzyme.…”

Section: Natural Product Inhibitors Of Ras Farnesyltransferasementioning

confidence: 99%

Farnesyltransferase as a target for anticancer drug design

1997

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This study aims to design some dual-target anticancer candidates, capable to act as an alkylating agent as well as a thymidylate synthase (TS) inhibitor. The designed scaffold is a combination of nucleobase, amino acid and aziridine structures. The candidates are docked into TS and three DNA double strand structures and evaluated based on their binding interaction energies and ligand efficiencies, compared to several reference drugs. The ADME properties of the alkylating agents are also predicted. The designed ligands exhibit improved interaction energies and lower ligand efficiencies with respect to the reference drugs. Among the ligands, L4 is the best DNA binding agent and L2, L5 and L6 are the best TS inhibitors. In addition, the thioTEPA based Ser and Met analogues are the strongest and poorest alkylating agents, respectively. Further, molecular dynamics simulations on the best ligand-target complexes, i.e. L4-4AWL and L6-TS systems, provide evidences for the potential L6 and L4 anti-proliferation activities.

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RPR113228, a Novel Farnesyl Protein Transferase Inhibitor Produced by Chrysosporium lobatum.

Cited by 19 publications

References 5 publications

Identification and characterization of compounds from Chrysosporium multifidum, a fungus with moderate antimicrobial activity isolated from Hermetia illucens gut microbiota

Identification and characterization of compounds from Chrysosporium multifidum, a fungus with moderate antimicrobial activity isolated from Hermetia illucens gut microbiota

Bioactive compounds from Chrysosporium multifidum, a fungus isolated from Hermetia illucens gut microbiota

Farnesyltransferase as a target for anticancer drug design

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