학술논문
Zaragozic acids D and D2: potent inhibitors of squalene synthase and of Ras farnesyl-protein transferase.
Document Type
Academic Journal
Author
Dufresne C; Merck Research Laboratories, Rahway, New Jersey.; Wilson KE; Singh SB; Zink DL; Bergstrom JD; Rew D; Polishook JD; Meinz M; Huang L; Silverman KC; et. al.
Source
Publisher: American Society of Pharmacognosy Country of Publication: United States NLM ID: 7906882 Publication Model: Print Cited Medium: Print ISSN: 0163-3864 (Print) Linking ISSN: 01633864 NLM ISO Abbreviation: J Nat Prod Subsets: MEDLINE
Subject
Language
English
ISSN
0163-3864
Abstract
Two new zaragozic acids, D and D2, have been isolated from the keratinophilic fungus Amauroascus niger. Zaragozic acids D [4] and D2 [5] are related to the previously described zaragozic acids A [1], B [2], and C [3] and are potent inhibitors of squalene synthase. Furthermore, all the zaragozic acids (A, B, C, D, and D2) are also active against farnesyl transferase. Zaragozic acids D and D2 inhibit farnesyl transferase with IC50 values of 100 nM, while zaragozic acids A and B are less potent.