ライフサイエンスコーパス: taxoid

1 potent taxoids were termed "third-generation taxoids".

2 nsitivity to Taxol and Taxotere, a synthetic taxoid.

3 tubulin at a site distinct from that of the taxoids.

4 3 (DW-2), which consist of a next-generation taxoid, 1 (SB-T-1214), and camptothecin as two warheads,

5 Moreover, taxoid 19 exhibited excellent in vivo efficacy against h

6 Taxoids 19 and 14g also showed excellent cytotoxicity ag

7 We formulated 3rd generation taxoids, able to avoid common drug resistance mechanisms

8 Competition studies versus a fluorescent taxoid across a temperature range, in comparison with pa

9 of 0.42 mM and 0.40 mM for the N-deacylated taxoid and benzoyl-CoA, respectively.

10 These data suggest that taxoids and camptothecin analogs could have activity in

11 Taxoids and other microtubule-damaging drugs are known t

12 earing methyldisulfanyl(alkanoyl) groups for taxoid-antibody immunoconjugates were designed, synthesi

13 say, i.e., the IC50 values of almost all the taxoids are in the subnanomolar level.

14 Several new nonaromatic taxoids are synthesized by means of the beta-lactam synt

15 bulin poisons (maytansinoids auristatins and taxoids) are undergoing clinical evaluation or are in pr

16 Taxoids bearing methyldisulfanyl(alkanoyl) groups for ta

17 tropic profile as compared with those of the taxoid binding reactions, which are characterized more b

18 es that have a Phe270-to-Val mutation in the taxoid binding site of beta-tubulin.

19 , which has a 3-fold higher affinity for the taxoid binding site than paclitaxel, indicated that 6-ep

20 ived from Taxus cuspidata cells (induced for taxoid biosynthesis with methyl jasmonate) was undertake

21 at cyclostreptin formed a pharmacophore with taxoids but formed hydrogen bonds only with the S9-S10 a

22 A cDNA clone (designated TAX7) encoding a taxoid C-13 O-phenylpropanoyltransferase was isolated wh

23 lear cooperative effect was observed for the taxoid-camptothecin combination when two drugs were deli

24 y conjugating a specific microtubule-binding taxoid core to the tetrazole/alkene prefluorophores, rob

25 A series of new taxoids derived from 14 beta-hydroxy-10-deacetylbaccatin

26 ts, we assessed the in vitro activity of the taxoid docetaxel (Taxotere; Rhone-Poulenc Rorer, Antony,

27 nd interaction partner with C19ORF5, and the taxoid drug family.

28 A number of the new taxoids exhibit remarkable activity (IC50 = 2.1-9.1 nM)

29 A number of these taxoids exhibited exceptionally high potency against mul

30 multidrug-resistant cell lines, and several taxoids exhibited virtually no difference in potency aga

31 products with minimal structural analogy to taxoids, have effects similar to those of paclitaxel (Ta

32 o previously uncharacterized cytochrome P450 taxoid hydroxylases, and provided candidate genes for al

33 t solubilization of different 3rd generation taxoids irrespective of the drug's chemical structures w

34 The observed exceptional activity of these taxoids may well be ascribed to an effective inhibition

35 the oxygenation steps of taxane diterpenoid (taxoid) metabolism.

36 toxy-14 beta-(2-methyl)butyrate (7), a major taxoid metabolite isolated from Japanese yew heart wood.

37 This strategy yielded a family of taxoid-metabolizing enzymes and revealed the taxane 10 b

38 These include taxoids modified with 3-methylbut-2-enoate, 3-methylbuta

39 by peloruside, which targets a distinct, non-taxoid pocket on beta-tubulin.

40 All but one of these new taxoids possess better activity than paclitaxel and doce

41 Two of the fully aliphatic taxoids possess similar or stronger activity than paclit

42 means of attaching modified aroyl groups to taxoid precursors for the purpose of improving drug effi

43 The new taxoid SB-T-1213 (4a) shows an excellent activity (T/C =

44 Moreover, a selected formulation with the taxoid SB-T-1214 is about one to two orders of magnitude

45 Among these, three new taxoids, SB-T-1213 (4a), SB-T-1214 (4b), and SB-T-1102 (

46 F-7) cancer cell lines, and several of these taxoids show subnanomolar IC50 values which are severalf

47 s could act synergistically with a number of taxoid site agents [paclitaxel, epothilones A/B, discode

48 None of the taxoid site compounds showed any synergism with each oth

49 laulimalide site, which is distinct from the taxoid site.

50 onds only with the S9-S10 and M loops in the taxoid site.

51 on tubulin polymer that is distinct from the taxoid site.

52 , K(m) values of 0.64 mM and 0.30 mM for the taxoid substrate and benzoyl-CoA, respectively, and is a

53 o screening of oxygenase activity by feeding taxoid substrates.

54 ated with a long-wavelength photoactivatable taxoid-tetrazole probe.

55 Highly efficient photoactivation of the taxoid-tetrazoles inside the mammalian cells was also ob

56 Most of the new taxoids thus synthesized possess excellent cytotoxicity

57 The new taxoids thus synthesized show excellent cytotoxicity aga

58 ctive inhibition of the binding of these new taxoids to P-glycoprotein that is responsible for MDR.

59 hly cytotoxic C-10 methyldisulfanylpropanoyl taxoid was conjugated to monoclonal antibodies recognizi

60 These taxoids were found to possess exceptional activity in pr

61 These exceptionally potent taxoids were termed "third-generation taxoids".

62 n of prodrug modules of an anticancer agent (taxoid with a cleavable linker) that is activated to its

63 11(12)-diene has been utilized to prepare a taxoid with oxygenation in the B and C rings.

64 In addition, taxoids with 2-methylprop-1-enyl, 2-methylpropyl, (E)-pr

65 ppropriate alkyl and alkenyl groups provides taxoids with equivalent or superior activity.

66 2-methyl-1-propenyl) and 3'-(2-methylpropyl) taxoids with modifications at C-10 was synthesized by me

67 Novel second-generation taxoids with systematic modifications at the C2, C10, an