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).