Literature DB >> 11858656

CJ-13,981 and CJ-13,982, new squalene synthase inhibitors.

S Watanabe1, H Hirai, T Kambara, Y Kojima, H Nishida, A Sugiura, Y Yamauchi, N Yoshikawa, H J Harwood, L H Huang, N Kojima.   

Abstract

Two new squalene synthase (SSase) inhibitors, CJ-13,981 (I) and CJ-13,982 (II), were isolated from the fermentation broth of an unidentified fungus CL 15036. They inhibited human liver microsomal SSase with IC50s of 2.8 and 1.1 microM, respectively, but showed no inhibitory activity against human brain protein farnesyltransferase (PFTase) at 100 microM. Based on FAB-MS and NMR analyses, the structures of I and II were determined to be 3-hydroxy-3,4-dicarboxy-15-hexadecenoic acid and 3-hydroxy-3,4-dicarboxyhexadecanoic acid, respectively.

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Year:  2001        PMID： 11858656     DOI： 10.7164/antibiotics.54.1025

Source DB:  PubMed          Journal:  J Antibiot (Tokyo)        ISSN： 0021-8820            Impact factor:   2.649


  2 in total

1.  Enantiospecific total synthesis of the squalene synthase inhibitors (-)-CJ-13,982 and its enantiomer from a common intermediate.

Authors:  Dayna Sturgess; Zongjia Chen; Jonathan M White; Mark A Rizzacasa
Journal:  J Antibiot (Tokyo)       Date:  2017-10-25       Impact factor: 2.649

2.  In vitro studies of maleidride-forming enzymes.

Authors:  Sen Yin; Steffen Friedrich; Vjaceslavs Hrupins; Russell J Cox
Journal:  RSC Adv       Date:  2021-04-21       Impact factor: 3.361
  2 in total

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