ライフサイエンスコーパス: pentamidine

1 iltefosine, paromomycin, amphotericin B, and pentamidine).

2 neumonia prophylaxis (with cotrimoxazole and pentamidine).

3 of 31 [71%]) or 2 doses (31 of 31 [100%]) of pentamidine.

4 ypanosomes often display cross-resistance to pentamidine.

5 ss effective alternatives, often aerosolized pentamidine.

6 nce to existing diamidine therapies, such as pentamidine.

7 t increase was observed with the addition of pentamidine.

8 al and antileishmanial potencies compared to pentamidine.

9 , P. falciparum, and L. donovani compared to pentamidine.

10 rs were more active against L. donovani than pentamidine.

11 vity against L. donovani superior to that of pentamidine.

12 istance to paromomycin, amphothericin B, and pentamidine.

13 in activity compared to the control compound pentamidine.

14 nosomiasis such as melarsoprol (Arsobal) and pentamidine.

15 Pentamidine, a bivalent aromatic diamidine, interacts wi

16 Sixty years after the introduction of pentamidine, a large effort is being made to develop a n

17 n to the (AATT)2 binding site, netropsin and pentamidine acquire 26+/-3 and 34+/-2 additional waters

18 tion, plasma membrane P-type H(+)-ATPases to pentamidine action, and trypanothione and several putati

19 ropane (1) was over 25-fold more potent than pentamidine against the drug-resistant isolate KETRI 243

20 hat has been shown to be more effective than pentamidine against the Pneumocystis carinii pathogen in

21 Pentamidine also significantly reduced the formation of

22 structure illustrates, for the first time, a pentamidine analog capable of binding the "open" form of

23 uded by residue Phe88, but for an asymmetric pentamidine analogue ((Ca)S100B.17), this same channel w

24 For symmetric pentamidine analogues ((Ca)S100B.5a, (Ca)S100B.6b) a cha

25 tudies were therefore completed here with 23 pentamidine analogues, and X-ray structures of (Ca)S100B

26 se data support a model where dual action of pentamidine and chlorpromazine in mitosis results in syn

27 larsoprol and diamidine compounds similar to pentamidine and furamidine are primarily taken up by try

28 bound to two cytotoxic bivalent diamidines, pentamidine and hexamidine.

29 hing was employed to improve the efficacy of pentamidine and Hoechst 33258 ligands that have been sho

30 strate a major role for aquaglyceroporins in pentamidine and melarsoprol cross-resistance.

31 rypanosomal activities comparable to that of pentamidine and melarsoprol.

32 itrypanosomal efficacy comparable to that of pentamidine and melarsoprol.

33 We identified the small molecules pentamidine and neomycin B as compounds that disrupt MBN

34 e uptake that was sensitive to inhibition by pentamidine and proton ionophores.

35 Twenty two compounds were more potent than pentamidine and seven dications were more effective than

36 ders cells sensitive to both melarsoprol and pentamidine and that loss of AQP2 function could explain

37 Diamidine 1 (pentamidine) and 65 analogues (2-66) have been tested fo

38 istic combination of an antiparasitic agent, pentamidine, and a phenothiazine antipsychotic, chlorpro

39 Twenty-six compounds were more active than pentamidine, and seven dications demonstrated increased

40 midino-2-phenylindole (DAPI), netropsin, and pentamidine are minor groove binders that have terminal

41 After protocol implementation, aerosolized pentamidine-associated costs were reduced.

42 l analysis to locate an interaction site for pentamidine at phenylalanine 656, a crucial residue in t

43 how hERG surface expression is disrupted by pentamidine at the cellular and molecular levels.

44 pyl analogue 7 showed toxicity comparable to pentamidine at the dosage of 20 micromol/kg/d.

45 mino)-5'-deoxyadenosine (MDL 73811), but not pentamidine, berenil, or methylglyoxyl bis(guanylhydrazo

46 rs Hoechst 33258, 4'-diamino-2-phenylindole, pentamidine, berenil, spermine, and spermidine, were tes

47 Our data suggest that pentamidine binding to a folding intermediate of hERG ar

48 tween S100B and the drug, and indicates that pentamidine binds into the p53 binding site on S100B def

49 Pentamidine binds QacR in a novel fashion whereby one of

50 An NMR-docked model of one such inhibitor, pentamidine, bound to Ca(2+)-loaded S100B was calculated

51 The leak currents were partially blocked by pentamidine but showed negligible inhibition by NASP.

52 kdown in Caco-2 cells decreased AP uptake of pentamidine by approximately 50% but did not alter BL up

53 OCT1 inhibition decreased AP uptake of pentamidine by approximately 50% in all three systems wi

54 Forty-eight cationically substituted pentamidine congeners possessing benzofuran rings were s

55 onophores revealed that PPT1 may be a proton/pentamidine cotransporter.

56 Although melarsoprol/pentamidine cross-resistance (MPXR) has been an area of

57 ) loss of function was linked to melarsoprol-pentamidine cross-resistance.

58 Pentamidine delays terminal repolarization in human hear

59 , none significantly impaired sensitivity to pentamidine, diminazene or melarsoprol, relative to the

60 rfloxacin, benzalkonium chloride, cetrimide, pentamidine, etc.) was increased 5- to 30-fold in a Stap

61 electrophysiological methods, we found that pentamidine exclusively inhibits hERG export from the en

62 ozoal drug 1,5-bis(4-amidinophenoxy)pentane (pentamidine) has been synthesized and tested for in vitr

63 were more potent against P. falciparum than pentamidine (IC(50) = 58 nM), and eight analogues were m

64 Replacing TMP/SMX with monthly aerosolized pentamidine in cases of ADR further increased life expec

65 Diamidines, and pentamidine in particular, have a long history as valuab

66 The addition of pentamidine in patients who had an ADR to TMP/SMX result

67 approximately 100 times more effective than pentamidine in this animal model.

68 of conformationally restricted congeners of pentamidine in which the flexible pentyl bridge of penta

69 ared with TMP/SMX alone, TMP/SMX followed by pentamidine increased the QALY by 0.07 at an incremental

70 The drug pentamidine inhibits calcium-dependent complex formation

71 Pentamidine is an antiprotozoal compound that clinically

72 Pentamidine is an effective antimicrobial agent against

73 The trypanocidal action of pentamidine is dependent on the rapid, selective accumul

74 We propose that pentamidine is the founding member of a novel pharmacolo

75 r with the development of a new oral form of pentamidine isethionate VLX103, led to investigations of

76 Of the various drugs tested, pentamidine isethionate was most effective against ameba

77 ect of a specific minor groove-binding drug, pentamidine, on hydration dynamics.

78 l lines in vivo more effectively than either pentamidine or chlorpromazine alone.

79 gene affecting resistance to the antibiotic pentamidine, our data support a mitochondrial target for

80 Furthermore, pentamidine partially rescued splicing defects of 2 pre-

81 of an effort to inhibit S100B, structures of pentamidine (Pnt) bound to Ca(2+)-loaded and Zn(2+),Ca(2

82 Both TMP/SMX alone and TMP/SMX followed by pentamidine prophylaxis strategies dominated the no prop

83 At the same time, pentamidine reduces surface expression of the cardiac po

84 Melarsoprol and pentamidine represent the two main classes of drugs, the

85 tional studies using OCT1-specific substrate pentamidine showed transporter-mediated AP but not BL up

86 Institution of pentamidine therapy for patients with a TMP/SMX ADR incr

87 We have investigated pentamidine transport by the bloodstream and procyclic l

88 as characterized, but no adenosine-sensitive pentamidine transport could be detected.

89 The remaining 30 to 50% of [(3)H]pentamidine transport was mediated by a low-capacity hig

90 ne was transported by an adenosine-sensitive pentamidine transporter (ASPT1) that displayed a K(m) va

91 was mediated by a low-capacity high-affinity pentamidine transporter (HAPT1) and a high-capacity low-

92 ter (HAPT1) and a high-capacity low-affinity pentamidine transporter (LAPT1), with K(m) values of 36

93 phonium compounds inhibited the low affinity pentamidine transporter.

94 In procyclics, an HAPT1-analog (procyclic pentamidine transporter; PPT1) was characterized, but no

95 Pentamidine treatment results in chromosomal segregation

96 We show in cell culture that pentamidine was able to reverse the missplicing of 2 pre

97 ts Tdp1 more effectively than berenil, while pentamidine was inactive.

98 idine in which the flexible pentyl bridge of pentamidine was replaced by trans-1,2-bismethylenecyclop

99 In bloodstream forms, 50 to 70% of [(3)H]pentamidine was transported by an adenosine-sensitive pe