1 er, the smaller ring size represented by the
didemnin analogue, tamandarin A, is equipotent to didemn
2 e binding by the unrelated natural products,
didemnin and cytotrienin.
3 fications exhibit a parallel effect for both
didemnins and tamandarins.
4 Synthetic and naturally occurring
didemnins are potent and specific inhibitors of protein
5 two natural products similar in structure to
didemnin B (3), were recently isolated from a Brazilian
6 The antineoplastic cyclic depsipeptide
didemnin B (DB) inhibits protein synthesis in cells and
7 The total synthesis of a
didemnin B analogue containing a conformationally constr
8 wo conformationally constrained analogues of
didemnin B are described.
9 ic analysis of this inhibition revealed that
didemnin B inhibits PPT1 uncompetitively.
10 As the first described inhibitor of PPT1,
didemnin B may prove to be a useful tool in the investig
11 the protein synthesis inhibitory activity of
didemnin B observed at intermediate concentrations.
12 ding site of 1 with the anti-cancer compound
didemnin B on EF-1alpha.
13 Our initial investigation of
didemnin B resulted in the discovery of its GTP-dependen
14 of the antiproliferative cyclic depsipeptide
didemnin B to PPT1.
15 a indicating that MCF-7 cells can accumulate
didemnin B up to 2-3 orders of magnitude compared to the
16 The [N,O-Me(2)Tyr(5)]residue of
didemnin B was replaced with L-1,2,3,4-tetrahydroisoquin
17 Didemnin B was shown to inhibit recombinant human PPT1 w
18 The marine natural product
didemnin B, currently in clinical trials as an antitumor
19 tostatic and immunosuppressive activities of
didemnin B, observed at low concentrations, additional d
20 nin analogue, tamandarin A, is equipotent to
didemnin B.
21 es and shown to be slightly more potent than
didemnin B.
22 in vitro and in vivo activities compared to
didemnin B.
23 rt the purification of a 36-kDa glycosylated
didemnin-
binding protein from bovine brain lysate.
24 , observed at low concentrations, additional
didemnin-
binding proteins were sought.
25 Bioactivities of 42
didemnin congeners, either isolated from the marine tuni
26 uirement for most of the bioactivites of the
didemnins,
especially for cytotoxicities and antiviral a
27 bition, in vitro binding studies of PPT1 and
didemnin indicate that the natural product binds prefere
28 s and in in vivo studies in mice, as well as
didemnin M, tested for the mixed lymphocyte reaction and
29 is observation supports tamandarins' role as
didemnins'
mimic.
30 Immunosuppressive activity of the
didemnins was determined using a mixed lymphocyte reacti