SAR study of a novel triene-ansamycin group compound, quinotrierixin, and related compounds, as inhibitors of ER stress-induced XBP1 activation.
Four novel triene-ansamycin group compounds, quinotrierixin, demethyltrienomycin A, demethyltrienomycin B and demethyltrienomycinol, were isolated from the culture broth of Streptomyces sp. PAE37 as inhibitors of ER stress-induced XBP1 activation. The structures of quinotrierixin, demethyltrienomycin A, demethyltrienomycin B and demethyltrienomycinol were determined on the basis of their spectroscopical and chemical properties. All of four possessed 21-membered macrocyclic lactams including triene moieties.
Kawamura
Tatsuro
T
Department of Biosciences and Informatics, Faculty of Science and Technology, Keio University, Yokohama, Japan.
Tashiro
Etsu
E
Shindo
Kazutoshi
K
Imoto
Masaya
M
D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004268:DNA-Binding Proteins / Q000378:metabolism*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008968:Molecular Conformation; D009904:Optical Rotation; D000071701:Regulatory Factor X Transcription Factors; D017828:Rifabutin / Q000031:analogs & derivatives* / Q000737:chemistry* / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared; D013056:Spectrophotometry, Ultraviolet; D013302:Streptomyces / Q000737:chemistry / Q000378:metabolism*; D013312:Stress, Physiological / Q000378:metabolism; D013329:Structure-Activity Relationship; D014157:Transcription Factors / Q000378:metabolism*; D000071717:X-Box Binding Protein 1
D000900:Anti-Bacterial Agents; D004268:DNA-Binding Proteins; D000071701:Regulatory Factor X Transcription Factors; D014157:Transcription Factors; D000071717:X-Box Binding Protein 1; C000605543:XBP1 protein, human; C532275:quinotrierixin; D017828:Rifabutin