EI-1507-1 and -2, novel interleukin-1 beta converting enzyme inhibitors produced by Streptomyces sp. E-1507.
EI-1507-1 and -2, novel interleukin-1 beta converting enzyme (ICE) inhibitors, were isolated from the culture broths of Streptomyces sp. E-1507. EI-1507-1 and EI-1507-2 selectively inhibited the recombinant human ICE activity with IC50 values of 0.23 and 0.42 microM, respectively. EI-1507-1 and EI-1507-2 also inhibited mature interleukin-1 beta secretion from THP-1 cells with IC50 values of 1.1 and 1.4 microM, respectively.
Tsukuda
E
E
Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., Japan.
Tanaka
T
T
Ochiai
K
K
Kondo
H
H
Yoshida
M
M
Agatsuma
T
T
Saitoh
Y
Y
Teshiba
S
S
Matsuda
Y
Y
D000595:Amino Acid Sequence; D000880:Anthraquinones / Q000737:chemistry* / Q000145:classification / Q000494:pharmacology; D001551:Benz(a)Anthracenes / Q000737:chemistry* / Q000145:classification / Q000494:pharmacology; D020170:Caspase 1; D002470:Cell Survival / Q000187:drug effects; D003546:Cysteine Endopeptidases / Q000096:biosynthesis*; D015853:Cysteine Proteinase Inhibitors / Q000737:chemistry* / Q000145:classification / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D008969:Molecular Sequence Data; D015394:Molecular Structure; D009000:Monocytes / Q000187:drug effects / Q000378:metabolism; D013302:Streptomyces / Q000254:growth & development / Q000378:metabolism* / Q000502:physiology
D000880:Anthraquinones; D001551:Benz(a)Anthracenes; D015853:Cysteine Proteinase Inhibitors; C099661:EI 1507-1; C099662:EI 1507-2; D003546:Cysteine Endopeptidases; D020170:Caspase 1