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Literature summary for 2.5.1.59 extracted from

  • Sun, Q.; Xiong, K.; Yuan, Y.; Yu, J.; Yang, L.; Shen, C.; Su, C.; Lu, Y.
    Inhibiting fungal echinocandin resistance by small-molecule disruption of geranylgeranyltransferase type i activity (2020), Antimicrob. Agents Chemother., 64, e02046-19 .
    View publication on PubMedView publication on EuropePMC
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Inhibitors

Inhibitors Comment Organism Structure
1-[2-[(Z)-[[4-(8-chloro-10,11-dihydrodibenzo[b,f]thiepin-10-yl)piperazin-1-yl]imino]methyl]phenoxy]-N,N-dimethylmethanamine i.e L-269289, selective chemical inhibition of GGTase I by L-269289 potentiates echinocandin activity and renders echinocandin-resistant Candida albicans responsive to treatment in vitro and in animal models for disseminated infection Candida albicans
L-269289 inhibitor L-269289 is active on its own to kill Candida glabrata, and its fungicidal activity is enhanced when combined with caspofungin [Candida] glabrata
L-269289 inhibitor L-269289 and echinocandins act in a synergistic manner for the treatment of Candida parapilosis Candida parapsilosis
L-269289 inhibitor L-269289 and echinocandins act in a synergistic manner for the treatment of Candida tropicalis Candida tropicalis

Organism

Organism UniProt Comment Textmining
Candida albicans Q9Y764 Q9Y764 i.e. beta-subunit CDC43
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Candida parapsilosis
-
-
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Candida tropicalis
-
-
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[Candida] glabrata
-
-
-

Synonyms

Synonyms Comment Organism
CDC43
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 Candida tropicalis
CDC43
-
 Candida parapsilosis
CDC43
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 [Candida] glabrata
CDC43
-
 Candida albicans

General Information

General Information Comment Organism
physiological function deleting beta-subunit CDC43 of geranylgeranyltransferase type I confers hypersensitivity to echinocandins. The membrane localization of Rho is disrupted in the CDC43 mutant, resulting in decreased amounts of glucans in the cell wall, thereby exacerbating the cell wall stress upon caspofungin addition Candida albicans
physiological function deletion of CDC43 is lethal in Candida glabrata [Candida] glabrata