ライフサイエンスコーパス: Bestatin

1 ty in HepG2 cells in presence and absence of bestatin.

2 the toxicity of the aminopeptidase inhibitor bestatin.

3 nt metal ions in AAP are involved in binding bestatin.

4 erved for 4 hours in the presence of 0.05 mM bestatin.

5 itors including the aminopeptidase inhibitor bestatin.

6 inhibitors and the aminopeptidase inhibitor bestatin.

7 he alpha-hydroxy-beta-amino acid scaffold of bestatin.

8 the peptidomimetic inhibitors, amastatin and bestatin.

9 dium containing 50 mM glucose, both E-64 and bestatin (0.05 mM each) significantly reduced the extent

10 Thiorphan (10 muM), captopril (1 muM), or bestatin (10 muM) were used to inhibit the activity of n

11 g of the competitive, slow-binding inhibitor bestatin ([(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoy]-le

12 substantially enhanced by the CD13 inhibitor bestatin (-5.9 +/- 0.6 degrees C) and by CD13 deficiency

13 ngiotensin IV, one of IRAP substrates, or by bestatin a pan aminopeptidase inhibitor, have been discl

14 ive was to evaluate antimicrobial effects of bestatin, a potential CP drug candidate.

15 This activity was inhibited by bestatin, an aminopeptidase inhibitor.

16 relatively stronger inhibitory effects than bestatin, an established inhibitor of LTA(4)H activity,

17 In this study, we investigated whether bestatin, an LTA4H inhibitor, could suppress skin acute

18 57 nM exceeding that of the natural product bestatin and approaching that of amastatin.

19 Activity was potently inhibited by bestatin and apstatin in a slow binding competitive fash

20 so significantly potentiated the efficacy of bestatin and cisplatin even at low concentrations (25 mu

21 In contrast, the protease inhibitors bestatin and lysine CMK, previously shown to block LF ac

22 proximately 3-4 mM), inhibited by amastatin, bestatin and tyrosine.

23 cs delta-aminolevulinic acid (delta-ALA) and bestatin, and the neuropeptide N-acetyl-Asp-Glu (NAAG),

24 e-directed mutagenesis and identification of bestatin as a potent inhibitor of the enzyme.

25 Inhibition of FCGAP by bestatin attenuates Ca(2+)-induced globulization of the

26 We evaluated bestatin bacteriostatic efficiency against periodontopat

27 In the case of the bestatin-based inhibitor, His79 interacts with atoms in

28 viously for the complex of the enzyme with a bestatin-based inhibitor.

29 tides and structurally similar drugs such as bestatin, beta-lactam antibiotics, and angiotensin-conve

30 The alkoxide oxygen of bestatin bridges between the two Zn(II) ions in the acti

31 and inhibited by several di/tripeptides and bestatin, but it remained unaffected by glycine and tetr

32 Cleavage can be blocked with bestatin, but not with other protease inhibitors tested,

33 rs of APA, amastatin has higher potency than bestatin by fitting better in the S1 pocket and interact

34 The M-M distances observed in the AAP-bestatin complex and native AAP are identical (3.5 A) wi

35 resonance (EPR) spectrum of the [CoCo(AAP)]-bestatin complex exhibited no observable perpendicular-

36 dent loop ordering, which in the case of the bestatin complex suggests a new route to inhibitor desig

37 e X-ray crystal structure of the [ZnZn(AAP)]-bestatin complex was solved to 2.0 A resolution.

38 More importantly, topical administration of bestatin cream dramatically inhibited BLT1 expression in

39 Importantly, bestatin does not aggravate anaphylaxis in CD13-deficien

40 Bestatin exhibited bacteriostatic activity against both

41 ity of hPEPT1 is: Gly-Sar > NAAG, delta-ALA, bestatin > cefadroxil, cephalexin > ampicillin, amoxicil

42 Of note, actinonin and bestatin had no effect on TNFRII expression under restin

43 Finally, we found that providing bestatin in the animal feed prevented alveolar bone reso

44 ted by the specific aminopeptidase inhibitor bestatin, indicating that FCGAP could be an aminopeptida

45 Mechanistic studies showed that bestatin inhibited skin carcinogenesis by suppressing ce

46 for [CoZn(AAP)] and [ZnCo(AAP)] confirm that bestatin interacts with both metal ions.

47 Taken together, these results suggest that bestatin is a promising drug choice for the treatment an

48 tingly, the backbone carbonyl oxygen atom of bestatin is coordinated to Znl at a distance of 2.3 A.

49 ocktail of protease inhibitors that includes bestatin, leupeptin, E64, AEBSF, and aprotinin.

50 opical application of novel cream containing bestatin might open a helpful avenue for SSL-induced ski

51 We show that in a murine model of CP bestatin not only shifted the biofilm species compositio

52 Both side chains of bestatin occupy a well-defined hydrophobic pocket that i

53 e effect of the protease inhibitors E-64 and bestatin on the prevention of hyperglycemic cataract, th

54 face aminopeptidase N (APN) using actinonin, bestatin, or inhibitory peptides significantly enhanced

55 We demonstrated that bestatin promotes the phagocytosis of periodontopathogen

56 Co(AAP)] enzymes recorded in the presence of bestatin revealed that both of the divalent metal ions i

57 These studies show that a bestatin-sensitive aminopeptidase may be critical for th

58 Upon extract fractionation, three bestatin-sensitive aminopeptidase peaks were detected.

59 , was rapidly destroyed in the extracts by a bestatin-sensitive exopeptidase, apparently by the purom

60 n and therapeutic studies, which showed that bestatin significantly attenuated SSL-induced skin carci

61 ing aminopeptidase inhibitors (amastatin and bestatin) strongly inhibited activities of all three LAP

62 able displacement of NPA by the AP inhibitor bestatin suggest that PM APs may be involved in both low

63 ases in the cell extract were inhibited with bestatin, the 9-17 residue proteasome products were also

64 The ability of bestatin to block parasite replication was only slightly

65 ssed in acute SSL-induced Lta4h-knockout and bestatin-treated mice skin tissues.

66 We have synthesized this bestatin-type MetAP2 inhibitor with the aid of crystal s

67 fficacy and the immunomodulatory function of bestatin was assessed in a murine model of CP.

68 based on the general MAP inhibitor scaffold, bestatin, we generated specific ABPs for these two enzym

69 In addition, the NH(2) group of bestatin, which mimics the N-terminal amine group of an