ライフサイエンスコーパス: gossypol

1 o pan-Bcl-2 family inhibitors, obatoclax and gossypol.

2 t hydrocarbon of cotton phytoalexins such as gossypol.

3 y reduced the apoptosis induced by TRAIL and gossypol.

4 ses of apogossypol 2- to 4-times higher than gossypol.

5 eins, with binding potency comparable to (-)-gossypol.

6 group of Ala-1 by stoichiometric amounts of gossypol.

7 nd arachidonic acid) mimicked treatment with gossypol.

8 may exist for tirilazad and the antioxidant gossypol.

9 lipophilic antioxidants such as tirilazad or gossypol.

10 ms of actions of certain polyphenols such as Gossypol (a compound from cotton seed extracts) and Purp

11 We investigated whether gossypol, a BH3 mimetic that is currently in the clinic,

12 Gossypol, a cottonseed extract derivative, acts as a BH3

13 first committed step of the biosynthesis of gossypol, a phytoalexin that defends the plant from bact

14 The combination of the STAT3 decoy and gossypol, a small molecule targeting Bcl-X(L), also yiel

15 on-approved natural compounds and identified gossypol acetic acid (GAA) as a potent inhibitor of oxid

16 Gossypol also down-regulated cell survival proteins (Bcl

17 re increased substantially by treatment with gossypol and its expression was critical for the gossypo

18 city and efficacy in mice of natural product gossypol and its semisynthetic derivative apo-gossypol,

19 ignificantly (capsaicin) or insignificantly (gossypol and nicotine) induced L-ACY-1 expression in H.

20 the systemic absence of glands that contain gossypol and other protective terpenoids.

21 Most relevant, the levels of gossypol and related terpenoids in the foliage and flora

22 l molecules (e.g. oblimersen, obatoclax, and gossypol), antifols (e.g. pralatrexate), proteasome inhi

23 Gossypol appears to prevent or delay the observed cell i

24 gent), cyclopamine (hedgehog inhibitor), and gossypol (Bcl-2 inhibitor).

25 We have successfully used RNAi to disrupt gossypol biosynthesis in cottonseed tissue by interferin

26 ace promotes only the noncovalent binding of gossypol, but not the covalent modification.

27 d culture of P. falciparum trophozoites with gossypol caused induction in expression of Pf MDH, while

28 ossypol and its semisynthetic derivative apo-gossypol, compounds that bind and inhibit antiapoptotic

29 Overall, our results show that gossypol enhances TRAIL-induced apoptosis through the do

30 We demonstrated previously that gossypol failed to directly inhibit BCL2 in cells or ind

31 In vivo, using the maximum tolerated dose of gossypol for sequential daily dosing, apogossypol displa

32 Therefore, elimination of gossypol from cottonseed has been a long-standing goal o

33 e combination of erlotinib, STAT3 decoy, and gossypol further enhanced cell growth inhibition and apo

34 Gossypol, however, did not exhibit this property.

35 We report here that AT-101, a derivative of gossypol in clinical trials, overcomes stroma-mediated r

36 , apogossypol displayed superior activity to gossypol in terms of reducing splenomegaly and reducing

37 ence the kinetics of modification of PLA2 by gossypol in the aqueous phase, and the enzyme at the int

38 Gossypol, in conjunction with spectroscopic and kinetic

39 anolamines, phosphatidic acids, sterols, and gossypol, indicating the broad range of metabolites and

40 Gossypol induced cell death in a concentration- and time

41 ROS); however, antioxidants did not abrogate gossypol-induced cell death.

42 , and thus, gene silencing of CHOP abolished gossypol-induced DR5 expression and associated potentiat

43 Calcium chelation also abrogated the gossypol-induced increase in calcium, ER stress, and NOX

44 Gossypol-induced receptor induction was not cell type-sp

45 APK or JNK) activation was also required for gossypol-induced TRAIL receptor induction; gene silencin

46 iescent lymphocytes, we investigated whether gossypol induces apoptosis in these cells and what mecha

47 Gossypol induction of the death receptor required the in

48 Gossypol is a putative BH3 mimetic proposed to inhibit B

49 A rapid initial noncovalent binding of gossypol is followed by a slow covalent modification of

50 Gossypol is shown to covalently modify secreted phosphol

51 possible to significantly reduce cottonseed-gossypol levels in a stable and heritable manner.

52 NOXA and Mcl-1 are critical determinants for gossypol-mediated cell death in ABT-737-resistant cells.

53 poptosis, suggesting that AIF contributes to gossypol-mediated cytotoxicity in CLL lymphocytes.

54 in these cells and what mechanism underlies gossypol-mediated cytotoxicity.

55 Residual activity of the gossypol-modified PLA2 from several different sources is

56 but insignificantly inhibited (capsaicin and gossypol) or induced (nicotine) it in H. assulta.

57 ation of sesquiterpene synthase genes in the gossypol pathway exemplifies the chemical diversity of l

58 -8, -9, and -3 activity assays revealed that gossypol potentiated TRAIL-induced apoptosis in human co

59 Gossypol promotes binding of PLA2 to the interface, and

60 Here, we demonstrate that gossypol rapidly increased activity of phospholipase A2

61 ypol and its expression was critical for the gossypol response.

62 nt manner; 24-hour incubation with 30 microM gossypol resulted in 50% cell death (median; range, 10%-

63 drug delivery of paclitaxel, cyclopamine and gossypol, resulting in tumor growth inhibition and prolo

64 und that reactive oxygen species produced by gossypol treatment was critical for TRAIL receptor induc

65 Although gossypol was effective only in resistant cells, obatocla

66 Oxamic acid did not inhibit Pf MDH, while gossypol, which interacts at the nucleotide binding site

67 t apogossypol is superior to parent compound gossypol with respect to toxicology and efficacy, sugges

68 represented the major adverse activities of gossypol, with apogossypol far less toxic.

69 to cytotoxicity induced by apogossypol than gossypol, with LD50 values of 3 to 5 microM and 7.5 to 1

70 derutilized because of the presence of toxic gossypol within seed glands.