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

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

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

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

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

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

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

24 complex with the methyltransferase inhibitor sinefungin at 1.7 A.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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