ライフサイエンスコーパス: O6-benzylguanine

1 mbination with 2 daily doses of 120 mg/m2 of O6-benzylguanine.

2 ylfolate (7) are far more water soluble than O6-benzylguanine.

3 sferase that is resistant to inactivation by O6-benzylguanine.

4 d) of reduction in the rate of reaction with O6-benzylguanine.

5 er from P140A in reaction with the free base O6-benzylguanine.

6 th the low molecular weight pseudosubstrate, O6-benzylguanine.

7 .2- and 12- to 29-fold greater than those of O6-Benzylguanine.

8 tide without altering the reaction with free O6-benzylguanine.

9 kyltransferase, Ada-C, is not inactivated by O6-benzylguanine.

10 hich would have an AGT activity sensitive to O6-benzylguanine.

11 ity and provide a form that was resistant to O6-benzylguanine.

12 Topical carmustine and intravenous O6-benzylguanine.

13 nsferase (MGMT[P140K]) gene transduction and O6-benzylguanine/1,3-bis(2-chloroethyl)-1-nitrosourea (B

14 pharmacological depletion of tumor MGMT with O6-benzylguanine (6-BG) and protection of sensitive tiss

15 plus 2 subsequent daily doses of intravenous O6-benzylguanine, administered every 2 weeks for up to 2

16 ause it is roughly 30 times more active than O6-benzylguanine against the wild-type alkyltransferase

17 There was no toxicity attributable to O6-Benzylguanine alone at all doses tested.

18 sistance could be overcome by treatment with O6-benzylguanine, an AGT inhibitor.

19 Compared with single-dose O6-benzylguanine and carmustine, dual-dose O6-benzylguan

20 possibility that resistance to therapy with O6-benzylguanine and chloroethylating agents may arise b

21 rine samples were collected and analyzed for O6-Benzylguanine and O6-Benzyl-8-oxoguanine concentratio

22 ubpopulation of patients may be resistant to O6-benzylguanine and that higher doses or additional alk

23 er oligodeoxyribonucleotides, one containing O6-benzylguanine and the other, O6-methylguanine.

24 rendered the expressed AGT less sensitive to O6-benzylguanine, and O6-benzylguanine was therefore muc

25 provided the greater amount of resistance to O6-benzylguanine, and the CHO cells expressing this muta

26 hich suggests it may prove to be superior to O6-benzylguanine as a chemotherapy adjuvant.

27 wenty-five cancer patients were treated with O6-Benzylguanine at a dose level of 10, 20, 40, and 80 m

28 gene-marked lymphoid and myeloid cells after O6-benzylguanine (BG) and temozolomide (TMZ) administrat

29 Pretreatment with O6-benzylguanine (BG) depleted tumor AGT activity for at

30 O6-Benzylguanine (BG) inactivates the MGMT protein and t

31 O6-Benzylguanine (BG) is a potent inactivator of AGT, re

32 O6-Benzylguanine (BG) is a potent inactivator of human A

33 1-nitrosourea (BCNU), a stem cell toxin, and O6-benzylguanine (BG), an inhibitor of a key BCNU resist

34 O6-benzylguanine (BG), an inhibitor of O6-alkylguanine-D

35 Recently, an AGT inhibitor, O6-benzylguanine (BG), entered clinical trials.

36 ion conditioning with temozolomide (TMZ) and O6-benzylguanine (BG).

37 n clinical trial for the AGT-depleting agent O6-benzylguanine (BG).

38 40A (ED50, 5 microM) render AGT resistant to O6-benzylguanine (BG).

39 rosoguanidine (MNNG), and the AGT inhibitor, O6-benzylguanine (BG).

40 lanine slightly increased the sensitivity to O6-benzylguanine (by up to 4-fold).

41 AGT mutants resistant to O6-benzylguanine can be made by converting Pro140 to an

42 In addition, O6-benzylguanine depleted alkyltransferase activity in B

43 AGT is strongly inhibited by O6-benzylguanine (ED50, 0.2 microM), and this drug is pr

44 retreated with MGMT-specific inhibitors (eg, O6 benzylguanine) has raised the possibility that tumor

45 The Ada-C protein was able to repair O6-benzylguanine in a 16-mer oligodeoxyribonucleotide.

46 e the pharmacokinetics and metabolic fate of O6-Benzylguanine in humans and its effect on AGT activit

47 s321 is buried and thus permit access of the O6-benzylguanine inhibitor.

48 O6-Benzylguanine is a potent inactivator of the DNA-repa

49 methylating and chloroethylating agents, and O6-benzylguanine is currently undergoing clinical trials

50 The effects of treatment of mice with O6-benzylguanine (O6-BeG) on the levels of O6-alkylguani

51 al was designed to (1) establish the dose of O6-benzylguanine (O6-BG) administered intravenously as a

52 O6-benzylguanine (O6-BG) is an AGT substrate that inhibi

53 O6-benzylguanine (O6-BG), a potent inhibitor of the DNA

54 llowing pretreatment with the MGMT inhibitor O6-benzylguanine (O6-BG).

55 CEM cells with MGMT-inactivating compounds, O6-benzylguanine (O6-BG, 20 microM) or 1,3-bis(chloroeth

56 Treatment consisting of both O6-benzylguanine (O6BG) and N,N'-bis(2-chloroethyl)-N-ni

57 This pediatric phase I trial of O6-benzylguanine (O6BG) and temozolomide (TMZ) on a dail

58 Coadministration of O6-benzylguanine (O6BG) can restore TMZ sensitivity, but

59 We show that O6-benzylguanine (O6BG), a nontoxic inhibitor of AGT, ca

60 utant AGT were not effectively killed by the O6-benzylguanine plus BCNU combination.

61 dose-limiting toxicity of the combination of O6-benzylguanine plus BCNU in clinical trials.

62 The MTD for dual-dose O6-benzylguanine plus carmustine was also ascertained.

63 O6-benzylguanine pretreatment markedly sensitized hemato

64 ltransferase is inactivated by the free base O6-benzylguanine, raising the possibility that substanti

65 O6-Benzylguanine rapidly disappeared from plasma and was

66 n of O6-alkylguanine-DNA alkyltransferase by O6-benzylguanine renders tumor cells more sensitive to k

67 -alkylguanine-DNA alkyltransferase (AGT), by O6-benzylguanine renders tumor cells susceptible to kill

68 e O6-benzylguanine and carmustine, dual-dose O6-benzylguanine resulted in higher overall response rat

69 transferase (alkyltransferase) in vitro than O6-benzylguanine, the prototype alkyltransferase inactiv

70 is study demonstrates that administration of O6-Benzylguanine to humans results in a rapid conversion

71 of carmustine in combination with dual-dose O6-benzylguanine to prolong alkyltransferase inhibition

72 tial responses to combination carmustine and O6-benzylguanine treatment.

73 e interaction of human alkyltransferase with O6-benzylguanine using direct determination of the amoun

74 eaction of the mutant A316P/W336A-Ada-C with O6-benzylguanine was greatly stimulated by the presence

75 AGT less sensitive to O6-benzylguanine, and O6-benzylguanine was therefore much less effective in re

76 P140A and G156A preferentially reacted with O6-benzylguanine when incubated with a mixture of two 16

77 d a much smaller effect on the reaction with O6-benzylguanine when it was incorporated into a short s

78 than an order of magnitude more active than O6-benzylguanine, which is currently in clinical trials

79 nine drastically reduced the inactivation by O6-benzylguanine with at least a 20-fold increase in the

80 In a phase 1 trial, single-dose O6-benzylguanine with topical carmustine for patients wi