ライフサイエンスコーパス: laulimalide

1 t of biologically active natural product (-)-laulimalide.

2 enced in creation of fully active analogs of laulimalide.

3 of peloruside A on the crystal structure of laulimalide.

4 red from the effects of either paclitaxel or laulimalide.

5 r to have a mechanism of action identical to laulimalide.

6 o retain the unique biological activities of laulimalide.

7 , including the anticancer marine polyketide laulimalide.

8 An enantioselective first total synthesis of laulimalide (1) is described.

9 Laulimalide, a natural product from marine sponges, is a

10 Laulimalide, a remarkably potent antitumor macrolide, ha

11 Previous work has shown that laulimalide, a sponge-derived natural product, resembles

12 We also report that a laulimalide analogue lacking the epoxide moiety, while l

13 istant cell lines were less resistant to the laulimalide analogues.

14 most potent analogues, C(16)-C(17)-des-epoxy laulimalide and C(20)-methoxy laulimalide, appear to hav

15 When combined, laulimalide and docetaxel (Taxotere) synergistically inh

16 he most dramatic difference observed between laulimalide and epothilone A was that only laulimalide w

17 paclitaxel and that the polymers formed with laulimalide and epothilone A were more stable at 0 degre

18 In contrast to paclitaxel, both laulimalide and isolaulimalide inhibited the proliferati

19 Laulimalide and isolaulimalide represent a new class of

20 otubule agents from natural products yielded laulimalide and isolaulimalide, two compounds with pacli

21 Because stoichiometric amounts of laulimalide and paclitaxel can cause extensive tubulin a

22 microtubules formed in the presence of both laulimalide and paclitaxel contained near-molar quantiti

23 t study, we searched for differences between laulimalide and paclitaxel in their interactions with tu

24 Nearly equimolar amounts of tubulin, laulimalide, and paclitaxel are recovered from microtubu

25 of epothilone B, ixabepilone (IXEMPRA(TM)), laulimalide, and peloruside A on CET conformation.

26 (17)-des-epoxy laulimalide and C(20)-methoxy laulimalide, appear to have a mechanism of action identi

27 We report here that laulimalide binds at a site on tubulin polymer that is d

28 the uncharacterized biosynthetic pathway for laulimalide can be confidently postulated, the biosynthe

29 In this way, we have identified 15 laulimalide conformations that can be classified into 5

30 The C(16)-C(17)-des-epoxy, C(20)-methoxy laulimalide derivative, which incorporates both chemical

31 In summary, analogues of laulimalide designed to minimize or eliminate its intrin

32 arly strongly stabilized by peloruside A and laulimalide, drugs that bind outside the taxane site.

33 Laulimalide exhibits an activity profile different from

34 Similar to docetaxel, laulimalide had no effect on the VEGF-induced tyrosine p

35 anolides A (1) and B (2), isolaulimalide and laulimalide, have taxol-like microtubule-stabilizing act

36 g the epoxide moiety, while less active than laulimalide in biochemical and cellular systems, is prob

37 rformed an NAMFIS deconvolution analysis for laulimalide in DMSO-d6.

38 logues initiated cellular changes similar to laulimalide, including increased density of interphase m

39 Laulimalide-induced assembly, like paclitaxel-induced as

40 ed paclitaxel-induced polymers, although the laulimalide-induced polymers appeared notably longer.

41 Laulimalide-induced tubulin polymers resembled paclitaxe

42 oruside A was significantly less active than laulimalide, inducing assembly in a manner that was most

43 In the present study, we found that laulimalide inhibited human umbilical vein endothelial c

44 Laulimalide inhibited integrin activation; however, comp

45 In conclusion, although both docetaxel and laulimalide inhibited integrin-associated signaling path

46 Possible mechanism(s) by which laulimalide inhibited VEGF-induced HUVEC migration were

47 Laulimalide is a cytotoxic natural product that stabiliz

48 Laulimalide is a potent inhibitor of cellular proliferat

49 Laulimalide is a potent, structurally unique microtubule

50 Laulimalide is a structurally unique 20-membered marine

51 Laulimalide is also active in P-glycoprotein overexpress

52 thesis of the potent antitumor macrolide (-)-laulimalide is described.

53 Laulimalide is one of the newest naturally occurring mac

54 The compound enhances tubulin assembly, and laulimalide is quantitatively comparable to paclitaxel i

55 Compared with docetaxel, laulimalide more potently caused a reduction in the cons

56 is present in a reaction mixture with either laulimalide or paclitaxel, nucleotide hydrolysis occurs

57 e displaced from microtubules by paclitaxel, laulimalide, or denaturing conditions, suggesting irreve

58 ular oxa-conjugate addition in a macrocyclic laulimalide precursor could be the origin of the 2,6-dih

59 Laulimalide represents a new class of antitumor agents w

60 Treatment of A-10 cells with laulimalide resulted in a dose-dependent reorganization

61 Incubation of MDA-MB-435 cells with laulimalide resulted in mitotic arrest and activation of

62 We found that peloruside A and laulimalide showed no synergism but that both compounds

63 The apparent binding of peloruside A in the laulimalide site led us to attempt construction of a pha

64 ymers suggest that peloruside A binds in the laulimalide site, which is distinct from the taxoid site

65 Laulimalide stimulated tubulin polymerization and, altho

66 Low concentrations of laulimalide substantially blocked subsequent VEGFR-2 dow

67 effects between AJ and either paclitaxel or laulimalide, suggest a distinct binding site.

68 uild the macrocycle enabled us to synthesize laulimalide via an efficient and convergent pathway.

69 n laulimalide and epothilone A was that only laulimalide was able to enhance assembly synergistically

70 Laulimalide was active against cell lines resistant to p

71 Laulimalide was compared with paclitaxel and epothilone

72 the only compound that mimics the action of laulimalide, we examined combinations of microtubule-sta

73 examine the conformational energy surface of laulimalide, we have performed an NAMFIS deconvolution a

74 Five analogues of laulimalide were designed to exhibit enhanced chemical s

75 We found that laulimalide, while as active as paclitaxel, epothilone A

76 he role of the epoxide in the interaction of laulimalide with tubulin is therefore justified.