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 The structurally unrelated cyclic peptides
didemnin B and ternatin-4 bind to the eEF1A(GTP)-aa-tRNA
9 We also show that
didemnin B and ternatin-4 exhibit distinct effects on th
10 By binding to a common site on eEF1A,
didemnin B and ternatin-4 trap eEF1A in an intermediate
11 wo conformationally constrained analogues of
didemnin B are described.
12 Both 2E2 cells and HepG2 cells treated with
didemnin B exhibited increased neutral lipid content, wh
13 ic analysis of this inhibition revealed that
didemnin B inhibits PPT1 uncompetitively.
14 As the first described inhibitor of PPT1,
didemnin B may prove to be a useful tool in the investig
15 the protein synthesis inhibitory activity of
didemnin B observed at intermediate concentrations.
16 ding site of 1 with the anti-cancer compound
didemnin B on EF-1alpha.
17 Our initial investigation of
didemnin B resulted in the discovery of its GTP-dependen
18 of the antiproliferative cyclic depsipeptide
didemnin B to PPT1.
19 a indicating that MCF-7 cells can accumulate
didemnin B up to 2-3 orders of magnitude compared to the
20 The [N,O-Me(2)Tyr(5)]residue of
didemnin B was replaced with L-1,2,3,4-tetrahydroisoquin
21 Didemnin B was shown to inhibit recombinant human PPT1 w
22 tivities, and some, such as griselimycin and
didemnin B, are membrane permeable and have intracellula
23 The marine natural product
didemnin B, currently in clinical trials as an antitumor
24 tostatic and immunosuppressive activities of
didemnin B, observed at low concentrations, additional d
25 lls treated with selective EEF1A inhibitors,
didemnin B, or plitidepsin.
26 nin analogue, tamandarin A, is equipotent to
didemnin B.
27 es and shown to be slightly more potent than
didemnin B.
28 in vitro and in vivo activities compared to
didemnin B.
29 rt the purification of a 36-kDa glycosylated
didemnin-
binding protein from bovine brain lysate.
30 , observed at low concentrations, additional
didemnin-
binding proteins were sought.
31 Bioactivities of 42
didemnin congeners, either isolated from the marine tuni
32 uirement for most of the bioactivites of the
didemnins,
especially for cytotoxicities and antiviral a
33 bition, in vitro binding studies of PPT1 and
didemnin indicate that the natural product binds prefere
34 s and in in vivo studies in mice, as well as
didemnin M, tested for the mixed lymphocyte reaction and
35 is observation supports tamandarins' role as
didemnins'
mimic.
36 Immunosuppressive activity of the
didemnins was determined using a mixed lymphocyte reacti