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1994-08-27
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34 lines
Document 0752
DOCN M9480752
TI Novel retrovirus protease inhibitors, RPI-856 A, B, C and D, produced by
Streptomyces sp. AL-322.
DT 9410
AU Asano T; Matsuoka K; Hida T; Kobayashi M; Kitamura Y; Hayakawa T; Iinuma
S; Kakinuma A; Kato K; Discovery Research Division, Takeda Chemical
Industries, Ltd.,; Osaka, Japan.
SO J Antibiot (Tokyo). 1994 May;47(5):557-65. Unique Identifier : AIDSLINE
MED/94314632
AB Four kinds of retrovirus protease inhibitors (RPI-856 A, B, C and D)
were isolated as white powder from the culture filtrate of a soil
isolate, Streptomyces sp. AL-322 by column chromatography using Diaion
HP-20, Sephadex LH-20, ODS reversed phase HPLC and SP-2SW ion exchange
HPLC. The structures of these inhibitors were elucidated by
physico-chemical properties, chemical reactions and spectral analyses,
as valyl-ADPAA-leucyl-AOPBA-valyl-valyl-aspartic acid (RPI-856 A and B)
and valyl-ADPAA-leucyl-AOPBA-valyl-valine (RPI-856 C and D) [ADPAA =
2-amino-2-(3,5-dihydroxyphenyl)acetic acid, AOPBA =
3-amino-2-oxo-4-phenylbutyric acid]. RPI-856 A and B, and RPI-856 C and
D were both determined to be diasteromers each other on the asymmetric
carbon in AOPBA. These four inhibitors strongly inhibited in vitro HIV-1
protease and HTLV-I protease both derived from recombinant Escherichia
coli with IC50 of 10(-7) approximately 10(-8) M.
DE Amino Acid Sequence Fermentation HIV-1/ENZYMOLOGY HTLV-I/ENZYMOLOGY
Molecular Sequence Data Molecular Structure
Oligopeptides/CHEMISTRY/ISOLATION & PURIF/PHARMACOLOGY Protease
Inhibitors/*CHEMISTRY/*ISOLATION & PURIF/PHARMACOLOGY Spectrophotometry
Streptomyces/*CHEMISTRY/CLASSIFICATION JOURNAL ARTICLE
SOURCE: National Library of Medicine. NOTICE: This material may be
protected by Copyright Law (Title 17, U.S.Code).