ライフサイエンスコーパス: sinefungin

1 ubstrate and an S-adenosylmethionine analog (Sinefungin).

2 ne (SAM) and the methyltransferase inhibitor sinefungin.

3 ional changes upon binding of the SAM-analog sinefungin.

4 e based peptide substrate to homocysteine or sinefungin.

5 sensitivity of yeast to growth inhibition by sinefungin.

6 incipal target of the antifungal activity of sinefungin.

7 y was stimulated by adding SAM or its analog sinefungin.

8 s inhibited by S-adenosyl-L-homocysteine and sinefungin.

9 otic and general methyltransferase inhibitor sinefungin (2.25 A resolution).

10 tensions toward the synthesis of carbocyclic sinefungin 7 document the importance of realizing the su

11 nformationally stabilized by the presence of sinefungin, a consistent increase in backbone mobility i

12 y, inhibition of endogenous oocyte PIMT with sinefungin, a nonhydrolyzable analog of S-adenosylhomocy

13 tected from cleavage only in the presence of sinefungin, a potent AdoMet analogue.

14 rget DNA duplexes (25 bp) in the presence of sinefungin, a potent inhibitory analog of AdoMet.

15 copy to describe the consequences of binding sinefungin, a SAM analogue, on the structure and dynamic

16 The IC(50) values for miltefosine, sinefungin, amodiaquine, diphenhydramine, and tacrine su

17 Finally, we demonstrate that sinefungin, an MTase inhibitor that binds the catalytic

18 Interestingly, we found two compounds, sinefungin and 5'-amino-5'-deoxyadenosine, that increase

19 omplexed to S-adenosylhomocysteine (SAH) and sinefungin and by measuring the affinity of SAM and SAH

20 ues of 133 +/- 18 and 4.6 +/- 0.5 microM for sinefungin and S-adenosylhomocysteine, respectively.

21 Additionally, an antifungal (Sinefungin) and several anti-viral drugs (e.g. Maraviroc

22 active analogs Aza-adenosyl-L-methionine and Sinefungin, and characterized the binding of these ligan

23 ffect occurs when S-adenosyl homocysteine or sinefungin are substituted for S-adenosyl methionine, an

24 nosyl-l-homocysteine (AdoHcy), the inhibitor sinefungin, as well as a mutant apo-enzyme have been det

25 complex with the methyltransferase inhibitor sinefungin at 1.7 A.

26 th SmyD1 in complex with the cofactor analog sinefungin at 2.3 A.

27 The crystal structure of an Ecm1-sinefungin binary complex reveals sinefungin-specific po

28 SAH and sinefungin bind to Nep1 at a preformed binding site that

29 product AdoHcy and the competitive inhibitor sinefungin bind with a straight conformation in which th

30 e yeast cap methyltransferase Abd1, to which sinefungin binds 900-fold more avidly than AdoHcy or Ado

31 he structural and dynamic effects of binding sinefungin for the catalytic mechanism of the enzyme and

32 finities of different ligands (SAM, SAH, and sinefungin) for M.BceJIV, as a step towards developing s

33 bstrate analogues S-adenosylhomocysteine and sinefungin gave competitive inhibition patterns against

34 y (IC(50) 4 microm) and by substrate analogs sinefungin (IC(50) 1.5 microm), aza-AdoMet (IC(50) 100 m

35 tion or inhibition by the natural nucleoside sinefungin impairs telomerase recruitment to telomeres l

36 h pEA (substrate), phosphocholine (product), sinefungin (inhibitor), and both pEA and S-adenosylhomoc

37 The S-adenosylmethionine (AdoMet) analog sinefungin is a natural product antibiotic that inhibits

38 The natural product antibiotic sinefungin is an AdoMet analog that inhibits Ecm1 with m

39 In contrast, sinefungin is an extremely potent inhibitor of the yeast

40 haromyces cerevisiae to growth inhibition by sinefungin is diminished when Abd1 is overexpressed.

41 ticular sensitivity of fungi and protozoa to sinefungin is not known.

42 structures bound either to the SAM analogue sinefungin or to 7-keto-8-aminopelargonic acid (KAPA) al

43 Thus, Sam3 is a tunable determinant of sinefungin potency.

44 N-propyl sinefungin (Pr-SNF) was shown to interact preferentially

45 In all cases, sinefungin resistance was attributable to a loss-of-func

46 solation and characterization of spontaneous sinefungin-resistant mutants of the budding yeast Saccha

47 cysteine and the methyltransferase inhibitor Sinefungin, respectively, show that the enzyme undergoes

48 n parasites to import AdoMet might determine sinefungin's anti-infective spectrum.

49 RNA cap methylation is a principal target of sinefungin's bioactivity.

50 Privileged sinefungin scaffolds are expected to have broad use as s

51 The antibiotic sinefungin (SFG) is a SAM analog in which the S-CH3 sulf

52 hibitors S-adenosyl-l-homocysteine (SAH) and sinefungin (SFG), we identified new synthetic inhibitors

53 denosylhomocysteine (SAH), or the SAH analog sinefungin (SFG).

54 C bound to SAM cofactor (2.54 angstroms) and sinefungin (SIN) inhibitor (1.72 angstroms).

55 Sinefungin (SIN), a natural S-adenosyl-L-methionine anal

56 We report here that sinefungin (SIN), an AdoMet analog, inhibits several fla

57 of an Ecm1-sinefungin binary complex reveals sinefungin-specific polar contacts with main-chain and s

58 Insights to the intracellular action of sinefungin stem from the finding that increased gene dos

59 sine, methylthioadenosine, homocysteine, and sinefungin suggest that potent and selective bisubstrate

60 e present crystal structures of M.BceJIV/DNA/sinefungin ternary complex and allied biochemical, compu

61 yltransferase afforded greater resistance to sinefungin than either enzyme alone.

62 chemical shift mapping experiments localize sinefungin to a highly conserved site in classical methy

63 Their Ki values for AVG and sinefungin vary from 0.019 to 0.80 microm and 0.15 to 12

64 plain the 3-fold higher affinity of Ecm1 for sinefungin versus AdoMet or S-adenosylhomocysteine (AdoH

65 issociation constants for AdoMet, AdoHcy and sinefungin were determined using an intrinsic tryptophan

66 nsfer, such as S-adenosyl-L-homocysteine and sinefungin, were shown to inhibit this reaction but had

67 y indirect conformational changes induced by sinefungin, which may play a role in substrate recogniti

68 SR:I bound DNA substrates in the presence of sinefungin with decreasing affinities: hemimethylated >