ライフサイエンスコーパス: bisubstrate

1 f the complexes with oxaloacetate and with a bisubstrate adduct indicate that each of the oxaloacetat

2 intermediate and by the observation that the bisubstrate analog adenosine 5'-tetraphosphoryl-3-O-(1,2

3 hibition suggest that the CoA portion of the bisubstrate analog can bind to the enzyme-aminoglycoside

4 The bisubstrate analog forces PGK to assume a novel, "inhibi

5 tion of a brominated CoA-S-acetyl-tryptamine-bisubstrate analog inhibitor and the MAD method permitte

6 The potent bisubstrate analog inhibitor H3-CoA-20 was competitive v

7 -acetyltransferase; AANAT) bound to a potent bisubstrate analog inhibitor has been determined at 2.0

8 late formats and was validated using a known bisubstrate analog inhibitor of carboxyltransferase.

9 crystal structure of Y168F AANAT bound to a bisubstrate analog inhibitor showed no significant struc

10 ion X-ray structure of the enzyme bound to a bisubstrate analog inhibitor, with a longer tether betwe

11 sulting in the production of a tight-binding bisubstrate analog inhibitor.

12 of novel, hydroxamic acid-based, collective bisubstrate analog inhibitors of farnesyl protein transf

13 was realized with 16 (I50 = 42.5 microM), a bisubstrate analog involving anchorage of farnesyl and t

14 lase (OTCase, EC 2.1.3.3) complexed with the bisubstrate analog N-(phosphonacetyl)-L-ornithine (PALO)

15 re of the complex of the holoenzyme with the bisubstrate analog N-phosphonacetyl-L-aspartate (PALA).

16 nithine transcarbamoylase complexed with the bisubstrate analog N-phosphonacetyl-L-ornithine has been

17 ation in the scattering pattern, whereas the bisubstrate analog N-phosphonoacetyl-L-aspartate induced

18 s possible that the two conformations of the bisubstrate analog observed crystallographically corresp

19 racterization of GO-CoA-Tat, a peptide-based bisubstrate analog that antagonizes GOAT.

20 However, at the high concentrations of bisubstrate analog used in crystallization experiments,

21 rypanosoma brucei PGK in the presence of the bisubstrate analog, adenylyl 1,1,5,5-tetrafluoropentane-

22 substrate-free enzyme and the complex with a bisubstrate analog, coenzyme A-S-acetyltryptamine, demon

23 ak inhibition of the coupled reaction by the bisubstrate analog, N-(phosphonacetyl)-L-aspartate (PALA

24 ugs to generate a tight, noncovalently bound bisubstrate analog.

25 tween the active C trimer and the holoenzyme:bisubstrate-analog complex call into question the view t

26 in the T state enzyme than in the holoenzyme:bisubstrate-analog complex, which has been considered as

27 Unlike the C trimer in either the T state or bisubstrate-analog-bound holoenzyme, the isolated C trim

28 transferase, we demonstrate that a series of bisubstrate analogs are only micromolar inhibitors.

29 1.35 A TAT cocrystal structures with bisubstrate analogs constrain TAT action to the microtub

30 Bisubstrate analogs for the aminoglycoside N-acetyltrans

31 evious studies of the interaction of similar bisubstrate analogs with other aminoglycoside N-acetyltr

32 the bisubstrate analogues indicate that the bisubstrate analogue approach can produce more potent in

33 herein is the synthesis and evaluation of a bisubstrate analogue designed to inhibit estrogen sulfot

34 in PCAF(Wloop), binding of the high-affinity bisubstrate analogue H3-CoA-20 led to a 2-fold fluoresce

35 ammonium hydrochloride (AAI), to generate a bisubstrate analogue inhibitor of PRMT1.

36 sinefungin suggest that potent and selective bisubstrate analogue inhibitor(s) for PRMT1 can be devel

37 PPK and the minimum length of the link for a bisubstrate analogue is approximately 7 A.

38 e of wild-type AOTCase in a complex with the bisubstrate analogue N(delta)-(phosphonoacetyl)-N(alpha)

39 The binding of the bisubstrate analogue N-(phosphonoacetyl)-l-aspartate (PA

40 The concentration of the bisubstrate analogue N-phosphonacetyl-L-aspartate (PALA)

41 ATCase substrate carbamoyl phosphate or the bisubstrate analogue N-phosphonacetyl-L-aspartate unexpe

42 A bisubstrate analogue of the riboflavin synthase-catalyze

43 ture of MshC in complex with a tight binding bisubstrate analogue, 5'-O-[N-(L-cysteinyl)sulfamonyl]ad

44 A stable bisubstrate analogue, 5'-O-[N-(l-cysteinyl)sulfamonyl]ad

45 The bisubstrate analogue, N1-spermine-acetyl-coenzyme A, exh

46 As further test, the PALA, a bisubstrate analogue, was displaced by citrate and phosp

47 unication, it should be possible to generate bisubstrate analogue-based inhibitors of PRMT isozymes t

48 The key features of the synthesis of bisubstrate analogues 3-OPP and 4-OPP are a regioselecti

49 OPP, and 5-OPP/OPP and bis-thiolodiphosphate bisubstrate analogues 3-SPP/SPP, 4-SPP/SPP, and 5-SPP/SP

50 All three bisubstrate analogues consist of a pterin, an adenosine

51 Bisubstrate analogues containing the allylic and homoall

52 Three bisubstrate analogues have been synthesized for HPPK and

53 he biochemical and structural studies of the bisubstrate analogues indicate that the bisubstrate anal

54 The bisubstrate analogues were substrates for FPP synthase,

55 Four bisubstrate analogues, compounds 1-4, were designed and

56 Here we designed bisubstrate analogues-based inhibitors, by mimicking eac

57 ntity of the aminoglycoside component of the bisubstrate and the number of carbon atoms that are used

58 ibitors by being non-sulfhydryl and by being bisubstrate based rather than peptide or FPP derived inh

59 The high inhibition potency and apparent bisubstrate behavior of 3-phenyl-1,5-bisthioglutarimide

60 k are consistent with the observed ping-pong bisubstrate--biproduct reaction kinetics.

61 large subunit methyltransferase in a pseudo-bisubstrate complex with S-adenosylhomocysteine and a HE

62 tants are not constrained covalently as in a bisubstrate complex, so it is possible to measure how pr

63 he three-dimensional structure of the enzyme-bisubstrate complex.

64 ctures of yeast Esa1 (yEsa1/KAT5) bound to a bisubstrate H4K16CoA inhibitor and human MOF (hMOF/KAT8/

65 The bisubstrate inhibitor binds with its phosphate and phosp

66 Structural analysis of a bisubstrate inhibitor bound to the enzyme suggests that

67 the structure-activity relationships of the bisubstrate inhibitor glycosyl domain resulting in the i

68 Bisubstrate inhibitor kinetics is a powerful diagnostic

69 bound trifluoromethylketal, shikimate-based bisubstrate inhibitor of 5-enolpyruvylshikimate-3-phosph

70 '-O-[N-(Salicyl)sulfamoyl]adenosine (1) is a bisubstrate inhibitor of MbtA and exhibits exceptionally

71 We previously demonstrated that a bisubstrate inhibitor of the adenylation enzyme MbtA, wh

72 protein in complex with the adenylate kinase bisubstrate inhibitor P(1),P(5)-di(adenosine-5') pentaph

73 decreased by 12.1 A upon the binding of the bisubstrate inhibitor P1, P5-bis(5'-adenosyl) pentaphosp

74 EP) and ribose 5-phosphate (R5P), and with a bisubstrate inhibitor that mimics the postulated linear

75 We fluorescently labeled a bisubstrate inhibitor to generate a fluorescent probe/tr

76 thymidine kinase (TmTK) in complex with the bisubstrate inhibitor TP4A.

77 nsional crystal structure of SSAT with bound bisubstrate inhibitor was determined at 2.3 A resolution

78 mechanisms and provide two examples in which bisubstrate inhibitors allow the kinetic mechanism to be

79 Structures of rationally designed bisubstrate inhibitors are also presented.

80 of 5-phenyl-2-thiooxazolidone were apparent bisubstrate inhibitors for DbetaM with respect to tyrami

81 dict the binding affinities of aryl acid-AMP bisubstrate inhibitors of MbtA.

82 Bisubstrate inhibitors represent a potentially powerful

83 PBMCs suggest that these compounds could be bisubstrate inhibitors that occupy both the phosphate an

84 nds from this class are predicted to bind as bisubstrate inhibitors through interactions with the AcC

85 Conversion of KAT bisubstrate inhibitors to clickable photoaffinity probes

86 suggest the intriguing possibility that the bisubstrate inhibitors utilize a transporter for entry a

87 e site were studied using a series of chiral bisubstrate inhibitors.

88 edict the existence of a noncovalently bound bisubstrate intermediate, not previously anticipated, wh

89 Bisubstrate kinetic analysis indicates that Sir2 enzymes

90 monstrated by using it to conduct a complete bisubstrate kinetic analysis of rat heart SKase.

91 e synthase as explored by the combination of bisubstrate kinetic analysis, product inhibition studies

92 In this study, we used NMR spectroscopy, bisubstrate kinetic assays, and product inhibition exper

93 Using steady-state, pre-steady-state, bisubstrate kinetic studies, and high-resolution electro

94 Steady-state bisubstrate kinetics, inhibition kinetics, isotope parti

95 ct of steric and heteroatom substitutions on bisubstrate ligand binding and to predict second generat

96 and farnesyl subunits is suggestive of their bisubstrate nature.

97 SA) and 4,7-dioxosebacic acid (4,7-DOSA) are bisubstrate reaction intermediate analogs for PBGS.

98 The bisubstrate reaction that it catalyzes between retinol a

99 c reaction with kinetics that approximates a bisubstrate-substituted enzyme mechanism in which millim

100 orientation of the two substrates within the bisubstrate system could be used to maximize enzyme inhi

101 bamoyl phosphate, and in the presence of the bisubstrate/transition state analog N-phosphonacetyl-L-a

102 sted that these derivatives behave as pseudo bisubstrates with respect to ascorbic acid and the amine