ライフサイエンスコーパス: Bestatin

1 the toxicity of the aminopeptidase inhibitor bestatin.

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

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

4 itors including the aminopeptidase inhibitor bestatin.

5 inhibitors and the aminopeptidase inhibitor bestatin.

6 the peptidomimetic inhibitors, amastatin and bestatin.

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

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

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

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

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

12 57 nM exceeding that of the natural product bestatin and approaching that of amastatin.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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