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1 des are detected in the reaction mixtures of bisubstrate.
2 f the complexes with oxaloacetate and with a bisubstrate adduct indicate that each of the oxaloacetat
3 intermediate and by the observation that the bisubstrate analog adenosine 5'-tetraphosphoryl-3-O-(1,2
4 hibition suggest that the CoA portion of the bisubstrate analog can bind to the enzyme-aminoglycoside
5                                          The bisubstrate analog forces PGK to assume a novel, "inhibi
6 tion of a brominated CoA-S-acetyl-tryptamine-bisubstrate analog inhibitor and the MAD method permitte
7                                   The potent bisubstrate analog inhibitor H3-CoA-20 was competitive v
8 -acetyltransferase; AANAT) bound to a potent bisubstrate analog inhibitor has been determined at 2.0
9 late formats and was validated using a known bisubstrate analog inhibitor of carboxyltransferase.
10  crystal structure of Y168F AANAT bound to a bisubstrate analog inhibitor showed no significant struc
11 ion X-ray structure of the enzyme bound to a bisubstrate analog inhibitor, with a longer tether betwe
12 sulting in the production of a tight-binding bisubstrate analog inhibitor.
13  of novel, hydroxamic acid-based, collective bisubstrate analog inhibitors of farnesyl protein transf
14  was realized with 16 (I50 = 42.5 microM), a bisubstrate analog involving anchorage of farnesyl and t
15 lase (OTCase, EC 2.1.3.3) complexed with the bisubstrate analog N-(phosphonacetyl)-L-ornithine (PALO)
16 re of the complex of the holoenzyme with the bisubstrate analog N-phosphonacetyl-L-aspartate (PALA).
17 nithine transcarbamoylase complexed with the bisubstrate analog N-phosphonacetyl-L-ornithine has been
18 ation in the scattering pattern, whereas the bisubstrate analog N-phosphonoacetyl-L-aspartate induced
19 s possible that the two conformations of the bisubstrate analog observed crystallographically corresp
20 racterization of GO-CoA-Tat, a peptide-based bisubstrate analog that antagonizes GOAT.
21       However, at the high concentrations of bisubstrate analog used in crystallization experiments,
22 rypanosoma brucei PGK in the presence of the bisubstrate analog, adenylyl 1,1,5,5-tetrafluoropentane-
23 substrate-free enzyme and the complex with a bisubstrate analog, coenzyme A-S-acetyltryptamine, demon
24 ak inhibition of the coupled reaction by the bisubstrate analog, N-(phosphonacetyl)-L-aspartate (PALA
25 ugs to generate a tight, noncovalently bound bisubstrate analog.
26 tween the active C trimer and the holoenzyme:bisubstrate-analog complex call into question the view t
27 in the T state enzyme than in the holoenzyme:bisubstrate-analog complex, which has been considered as
28 Unlike the C trimer in either the T state or bisubstrate-analog-bound holoenzyme, the isolated C trim
29 transferase, we demonstrate that a series of bisubstrate analogs are only micromolar inhibitors.
30         1.35 A TAT cocrystal structures with bisubstrate analogs constrain TAT action to the microtub
31                                              Bisubstrate analogs for the aminoglycoside N-acetyltrans
32 evious studies of the interaction of similar bisubstrate analogs with other aminoglycoside N-acetyltr
33  the bisubstrate analogues indicate that the bisubstrate analogue approach can produce more potent in
34                                            A bisubstrate analogue approach offers the potential for d
35  herein is the synthesis and evaluation of a bisubstrate analogue designed to inhibit estrogen sulfot
36 in PCAF(Wloop), binding of the high-affinity bisubstrate analogue H3-CoA-20 led to a 2-fold fluoresce
37  ammonium hydrochloride (AAI), to generate a bisubstrate analogue inhibitor of PRMT1.
38 sinefungin suggest that potent and selective bisubstrate analogue inhibitor(s) for PRMT1 can be devel
39 PPK and the minimum length of the link for a bisubstrate analogue is approximately 7 A.
40 e of wild-type AOTCase in a complex with the bisubstrate analogue N(delta)-(phosphonoacetyl)-N(alpha)
41                           The binding of the bisubstrate analogue N-(phosphonoacetyl)-l-aspartate (PA
42                     The concentration of the bisubstrate analogue N-phosphonacetyl-L-aspartate (PALA)
43  ATCase substrate carbamoyl phosphate or the bisubstrate analogue N-phosphonacetyl-L-aspartate unexpe
44                                            A bisubstrate analogue of the riboflavin synthase-catalyze
45                                          The bisubstrate analogue strategy is a promising approach to
46 -C to 4-C atom linker enables its respective bisubstrate analogue to occupy both substrate- and cofac
47 and cofactor-binding sites of NTMT1, but the bisubstrate analogue with a 5-C atom linker only interac
48 ture of MshC in complex with a tight binding bisubstrate analogue, 5'-O-[N-(L-cysteinyl)sulfamonyl]ad
49                                     A stable bisubstrate analogue, 5'-O-[N-(l-cysteinyl)sulfamonyl]ad
50                                          The bisubstrate analogue, N1-spermine-acetyl-coenzyme A, exh
51                 As further test, the PALA, a bisubstrate analogue, was displaced by citrate and phosp
52 unication, it should be possible to generate bisubstrate analogue-based inhibitors of PRMT isozymes t
53 tal and multiscale simulation approach using bisubstrate analogues (BAs), conjugates of a SAM-like mo
54         The key features of the synthesis of bisubstrate analogues 3-OPP and 4-OPP are a regioselecti
55 OPP, and 5-OPP/OPP and bis-thiolodiphosphate bisubstrate analogues 3-SPP/SPP, 4-SPP/SPP, and 5-SPP/SP
56                                    All three bisubstrate analogues consist of a pterin, an adenosine
57                                              Bisubstrate analogues containing the allylic and homoall
58                                        Three bisubstrate analogues have been synthesized for HPPK and
59 he biochemical and structural studies of the bisubstrate analogues indicate that the bisubstrate anal
60                                          The bisubstrate analogues were substrates for FPP synthase,
61      Herein, the interactions of a series of bisubstrate analogues with protein N-terminal methyltran
62                                         Four bisubstrate analogues, compounds 1-4, were designed and
63                             Here we designed bisubstrate analogues-based inhibitors, by mimicking eac
64 ntity of the aminoglycoside component of the bisubstrate and the number of carbon atoms that are used
65       Small molecules, and peptides that are bisubstrate, and/or PRMT transition state mimic inhibito
66 ibitors by being non-sulfhydryl and by being bisubstrate based rather than peptide or FPP derived inh
67 vity relationships of these inhibitors and a bisubstrate-based mechanism of action.
68     The high inhibition potency and apparent bisubstrate behavior of 3-phenyl-1,5-bisthioglutarimide
69 ted mutagenesis studies were consistent with bisubstrate binding.
70 k are consistent with the observed ping-pong bisubstrate--biproduct reaction kinetics.
71  large subunit methyltransferase in a pseudo-bisubstrate complex with S-adenosylhomocysteine and a HE
72 tants are not constrained covalently as in a bisubstrate complex, so it is possible to measure how pr
73 he three-dimensional structure of the enzyme-bisubstrate complex.
74 ctures of yeast Esa1 (yEsa1/KAT5) bound to a bisubstrate H4K16CoA inhibitor and human MOF (hMOF/KAT8/
75  we describe the discovery of a potent NTMT1 bisubstrate inhibitor 4 (IC(50) = 35 +/- 2 nM) that exhi
76                                         This bisubstrate inhibitor approach has resulted in one of th
77                                          The bisubstrate inhibitor binds with its phosphate and phosp
78                     Structural analysis of a bisubstrate inhibitor bound to the enzyme suggests that
79                              The most potent bisubstrate inhibitor displayed an apparent K(i) value o
80  the structure-activity relationships of the bisubstrate inhibitor glycosyl domain resulting in the i
81 Herein, we report the first cell-potent NNMT bisubstrate inhibitor II399, demonstrating a K(i) of 5.9
82 ure of the MYST domain bound to an H3K14-CoA bisubstrate inhibitor is consistent with a model in whic
83                                              Bisubstrate inhibitor kinetics is a powerful diagnostic
84 y to design and synthesize the tight-binding bisubstrate inhibitor LL320 through a novel propargyl li
85  bound trifluoromethylketal, shikimate-based bisubstrate inhibitor of 5-enolpyruvylshikimate-3-phosph
86 '-O-[N-(Salicyl)sulfamoyl]adenosine (1) is a bisubstrate inhibitor of MbtA and exhibits exceptionally
87            We previously demonstrated that a bisubstrate inhibitor of the adenylation enzyme MbtA, wh
88 protein in complex with the adenylate kinase bisubstrate inhibitor P(1),P(5)-di(adenosine-5') pentaph
89  decreased by 12.1 A upon the binding of the bisubstrate inhibitor P1, P5-bis(5'-adenosyl) pentaphosp
90 EP) and ribose 5-phosphate (R5P), and with a bisubstrate inhibitor that mimics the postulated linear
91                   We fluorescently labeled a bisubstrate inhibitor to generate a fluorescent probe/tr
92  thymidine kinase (TmTK) in complex with the bisubstrate inhibitor TP4A.
93 nsional crystal structure of SSAT with bound bisubstrate inhibitor was determined at 2.3 A resolution
94 mechanisms and provide two examples in which bisubstrate inhibitors allow the kinetic mechanism to be
95            Structures of rationally designed bisubstrate inhibitors are also presented.
96           Biochemical studies indicated that bisubstrate inhibitors are competitive to the peptide su
97  and prepared a series of highly potent NatD bisubstrate inhibitors by covalently linking coenzyme A
98 lines general guidance on the development of bisubstrate inhibitors for any methyltransferases.
99  of 5-phenyl-2-thiooxazolidone were apparent bisubstrate inhibitors for DbetaM with respect to tyrami
100                                          The bisubstrate inhibitors have extended interactions with T
101 dict the binding affinities of aryl acid-AMP bisubstrate inhibitors of MbtA.
102  development of potent and selective alkynyl bisubstrate inhibitors of NNMT.
103 ely 150 nM, making them the most cell-potent bisubstrate inhibitors reported to date.
104                                              Bisubstrate inhibitors represent a potentially powerful
105        We here report the development of new bisubstrate inhibitors that include electron-deficient a
106  PBMCs suggest that these compounds could be bisubstrate inhibitors that occupy both the phosphate an
107 nds from this class are predicted to bind as bisubstrate inhibitors through interactions with the AcC
108                            Conversion of KAT bisubstrate inhibitors to clickable photoaffinity probes
109 ives may have utility as chemical probes and bisubstrate inhibitors to reveal valuable mechanistic an
110  suggest the intriguing possibility that the bisubstrate inhibitors utilize a transporter for entry a
111 e site were studied using a series of chiral bisubstrate inhibitors.
112 edict the existence of a noncovalently bound bisubstrate intermediate, not previously anticipated, wh
113                                              Bisubstrate kinetic analysis indicates that Sir2 enzymes
114 monstrated by using it to conduct a complete bisubstrate kinetic analysis of rat heart SKase.
115 e synthase as explored by the combination of bisubstrate kinetic analysis, product inhibition studies
116     In this study, we used NMR spectroscopy, bisubstrate kinetic assays, and product inhibition exper
117        Using steady-state, pre-steady-state, bisubstrate kinetic studies, and high-resolution electro
118                                 Steady-state bisubstrate kinetics, inhibition kinetics, isotope parti
119 ct of steric and heteroatom substitutions on bisubstrate ligand binding and to predict second generat
120 ons, significantly increases the activity of bisubstrate-like NNMT inhibitors (half-maximal inhibitor
121 and farnesyl subunits is suggestive of their bisubstrate nature.
122           Here, we report the first covalent bisubstrate PK inhibitor whose electrophilic warhead rea
123 SA) and 4,7-dioxosebacic acid (4,7-DOSA) are bisubstrate reaction intermediate analogs for PBGS.
124                                          The bisubstrate reaction that it catalyzes between retinol a
125  The latter type is well represented by some bisubstrate reactions, where they have been defined as "
126 c reaction with kinetics that approximates a bisubstrate-substituted enzyme mechanism in which millim
127 orientation of the two substrates within the bisubstrate system could be used to maximize enzyme inhi
128                      Both monosubstrates and bisubstrates systems together with TLC and HPLC techniqu
129  C9 position of the aTC D-ring, we generated bisubstrate TDase inhibitors.
130 bamoyl phosphate, and in the presence of the bisubstrate/transition state analog N-phosphonacetyl-L-a
131 sted that these derivatives behave as pseudo bisubstrates with respect to ascorbic acid and the amine

 
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