Document Detail

TMC-86A, B and TMC-96, new proteasome inhibitors from Streptomyces sp. TC 1084 and Saccharothrix sp. TC 1094. I. Taxonomy, fermentation, isolation, and biological activities.
MedLine Citation:
PMID:  10695669     Owner:  NLM     Status:  MEDLINE    
TMC-86A, B and TMC-96, new 20S proteasome inhibitors with an epoxy-beta-aminoketone moiety, were isolated from the fermentation broth of Streptomyces sp. TC 1084 and Saccharothrix sp. TC 1094, respectively. TMC-86A, B and TMC-96 inhibited the chymotrypsin-like and peptidylglutamyl-peptide hydrolyzing activities of 20S proteasome with the following IC50 values: TMC-86A, 5.1 microM and 3.7microM; TMC-86B, 1.1 microM and 31 microM; TMC-96, 2.9 microM and 3.5 microM, respectively. TMC-86A, B and TMC-96 exhibited the weak inhibitory activity against the trypsin-like activity of 20S proteasome with IC50 values of 51 microM, 250 microM, and 36 microM, respectively. They did not inhibit m-calpain, cathepsin L, and trypsin at 100 microM, suggesting their high specificity for proteasome. Taxonomy of the producing strains is also described.
Y Koguchi; J Kohno; S Suzuki; M Nishio; K Takahashi; T Ohnuki; S Komatsubara
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  The Journal of antibiotics     Volume:  52     ISSN:  0021-8820     ISO Abbreviation:  J. Antibiot.     Publication Date:  1999 Dec 
Date Detail:
Created Date:  2000-03-16     Completed Date:  2000-03-16     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0151115     Medline TA:  J Antibiot (Tokyo)     Country:  JAPAN    
Other Details:
Languages:  eng     Pagination:  1069-76     Citation Subset:  IM    
Basic Technology Department, TAnabe Seiyaku Co., Ltd., Toda-shi, Saitama, Japan.
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MeSH Terms
Actinomycetales / metabolism*
Cysteine Endopeptidases / drug effects*
Dipeptides / isolation & purification*,  pharmacology
Multienzyme Complexes / drug effects*
Protease Inhibitors / isolation & purification*,  pharmacology
Proteasome Endopeptidase Complex
Streptomyces / classification,  metabolism*
Reg. No./Substance:
0/Dipeptides; 0/Multienzyme Complexes; 0/Protease Inhibitors; 0/TMC 86A; 0/TMC 86B; 0/TMC 96; EC 3.4.22.-/Cysteine Endopeptidases; EC Endopeptidase Complex

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