ライフサイエンスコーパス: non-competitive

1 echanism of PTX blockade from competitive to non-competitive.

2 ermine the contribution of uncompetitive vs. non-competitive actions, respectively.

3 To address this limitation, we present a non-competitive active transport strategy to overcome in

4 he imprinting factors for these compounds in non-competitive adsorption experiments were 3.2, 1.5, 1.

5 inted nanocomposites, binary competitive and non-competitive adsorption experiments were performed wi

6 poly(lactide-co-glycolide) (PLGA) have shown non-competitive affinity to TfR evaluated in cell/cell-f

7 increase) following chronic blockade with a non-competitive AMPA receptor antagonist, GYKI 52466 (1-

8 osyl-l-methionine (AdoMet), displayed AdoMet non-competitive and DNA competitive behavior.

9 he endofacial inhibitor, cytochalasin B, was non-competitive and inhibition by the exofacial inhibito

10 nAChR-mediated currents in a dose-dependent, non-competitive and use-independent manner.

11 el blocking drug memantine was evaluated for non-competitive and/or uncompetitive components of antag

12 te antagonists but not by the AMPA-selective non-competitive antagonist 1-(4-aminophenyl)-4-methyl-7,

13 Ketamine is a non-competitive antagonist at the N-methyl-d-aspartate r

14 Decanoic acid acts as a non-competitive antagonist at therapeutically relevant c

15 MDA subtype of glutamate receptors using the non-competitive antagonist dizocilpine maleate (MK801) a

16 tive agonists and changes the potency of the non-competitive antagonist mecamylamine.

17 GYKI 52466, a selective non-competitive antagonist of AMPA receptors, did not af

18 The potency of Zn2+ as a non-competitive antagonist of GABA-activated responses o

19 ng an intraperitoneal injection of MK-801, a non-competitive antagonist of N-methyl-d-aspartate (NMDA

20 The main action of phencyclidine is as a non-competitive antagonist of the NMDA class of glutamat

21 Phencyclidine (PCP), a non-competitive antagonist of the NMDA subtype of glutam

22 The effect of MK-801, a non-competitive antagonist of the NMDA subtype of glutam

23 t from that for GABA, and that CTZ acts as a non-competitive antagonist on the GABA(C) receptor.

24 The non-competitive antagonist picrotoxin blocked nearly 50%

25 petitive antagonist 3-APMPA, but not for the non-competitive antagonist picrotoxin.

26 We used the NMDA receptor non-competitive antagonist, [3H]MK-801, as a ligand for

27 n inducible receptor expression system and a non-competitive antagonist, in conjunction with the tran

28 ctivation, desensitization and inhibition by non-competitive antagonists and pore blockers.

29 vity in the striatum, and 2) competitive and non-competitive antagonists of the NMDA receptor differe

30 Another current animal model utilizes non-competitive antagonists of the NMDA/glutamate recept

31 AMPA receptor potentiators and non-competitive antagonists represent potential targets

32 ng but inhibitable by subsequent exposure to non-competitive antagonists.

33 and relatively resistant to displacement by non-competitive antagonists.

34 5 and confers sensitivity to displacement by non-competitive antagonists.

35 50295 potentiator binding to displacement by non-competitive antagonists.

36 e-set behavior in individual samples using a non-competitive approach that is fundamentally distinct

37 versatile platform to design competitive and non-competitive AR modulators with potential therapeutic

38 nity, whereas binding of ligands known to be non-competitive are not affected.

39 t of subcutaneous infusion of candesartan, a non-competitive AT(1) receptor antagonist, 0.5 mg/kg/day

40 es arylsulfonamides and benzodiazepines, but non-competitive binding between the transition state ana

41 tudy of their inhibitory kinetics revealed a non-competitive binding mode, with an IC50 value against

42 dem Affinity Reagents (MegaSTAR) to identify non-competitive binding pairs of recombinant affinity re

43 damage in the immature hippocampus but that non-competitive blockade of the NMDA receptor may be a d

44 Intermolecular non-competitive deuterium isotope effects of 3.1-3.8 wer

45 nd was sensitive to competitive (S58035) and non-competitive (DuP 128) ACAT inhibitors.

46 achieve a mechanistic understanding of these non-competitive effects, we used a combination of dicati

47 Attenuation of the high (D)k in the non-competitive experiments implies that C-H bond breaki

48 DEN was approximately 3 and not expressed in non-competitive experiments.

49 ly expressed in a variety of competitive and non-competitive experiments.

50 on-response curves were depressed in a mixed/non-competitive fashion.

51 te competitive fitness is similar to that of non-competitive fitness.

52 Trifluoperazine inhibition is non-competitive for NADH, whereas the inhibition kinetic

53 h as drugs, metabolites and pollutants, with non-competitive formats, bringing advantages previously

54 ion of ZBP-89 as well as its competitive and non-competitive functional interactions with other regul

55 Treatment with ketamine, a non-competitive glutamate N-methyl-d-aspartic acid (NMDA

56 reviously observed for either competitive or non-competitive glutamate NMDA antagonists.

57 The non-competitive, glutamatergic NMDAR (N-methyl-d-asparta

58 glutamate-release inhibitor Riluzole or the non-competitive GRM1 antagonist BAY 36-7620 we were able

59 Non-competitive import studies demonstrated that prSSU a

60 bition by tannic acid was found to be purely non-competitive in the dry state.

61 locked and pristine sites at depth exhibited non-competitive inhibition (decreased V max), whilst unc

62 ition state analogs inhibit their targets by non-competitive inhibition are discussed.

63 mechanism of action involves competitive and non-competitive inhibition as well as generation of unst

64 The non-competitive inhibition mode of CS was determined by

65 Because of the non-competitive inhibition observed, docking of Trp-Val

66 Thus, non-competitive inhibition of ATP hydrolysis, combined w

67 urin both in vitro and in vivo, leading to a non-competitive inhibition of calcineurin activity.

68 mall molecule inhibitors, which also display non-competitive inhibition of gamma-secretase, inhibit t

69 f aspartyl proteases, also displayed potent, non-competitive inhibition of gamma-secretase.

70 er and L685458 unexpectedly displayed linear non-competitive inhibition of gamma-secretase.

71 CDI is caused instead by non-competitive inhibition of NMDA receptors.

72 This non-competitive inhibition of the ATPase by ADP is consi

73 some proliferator, WY 14,643 exhibits a pure non-competitive inhibition pattern in the aldehyde reduc

74 Such irreversibility may explain the non-competitive inhibition pattern with respect to ATP s

75 dolichol toward the substrate UDP-GlcNAc and non-competitive inhibition toward dolichol phosphate.

76 e anions in the absence of inhibitor exhibit non-competitive inhibition with respect to FPP.

77 mathematical solutions to uncompetitive and non-competitive inhibition, and demonstrate that in most

78 meters in the presence of UVM-7-SH suggested non-competitive inhibition, which indicated that the mat

79 s suggest that Val-Glu-Leu-Tyr-Pro acts as a non-competitive inhibitor against ACE.

80 inhibitor of caspase-3 activity, becoming a non-competitive inhibitor at higher concentrations.

81 Quercetin was a reversible and non-competitive inhibitor of ascorbate transport; K(i) 1

82 TP], suggesting that GaTx1 may function as a non-competitive inhibitor of ATP-dependent channel gatin

83 Cycloheximide is a non-competitive inhibitor of both eEF3 and ATP.

84 YP2C9, CYP2D6, CYP2E1 and CYP3A4, but also a non-competitive inhibitor of CYP1A2, with Ki values no m

85 racterization showed that this compound is a non-competitive inhibitor of cytochrome c When tested in

86 Quercetin was a potent non-competitive inhibitor of GLUT2 expressed in Xenopus

87 microM, indicating that betaxolol acts as a non-competitive inhibitor of glutamate response in retin

88 hat tamoxifen is a low micromolar, partially non-competitive inhibitor of hCE1.

89 ess and autophagy impairments induced by the non-competitive inhibitor of sarco/ER Ca(2+)-ATPase, tha

90 Lithium acts as both an uncompetitive and non-competitive inhibitor of several lithium- sensitive

91 4-aminobenzohydrazide was determined to be a non-competitive inhibitor of TBR-POD and Turnip-POD.

92 te for hCE1, and instead acts as a partially non-competitive inhibitor of the enzyme.

93 evealed that BMS-791325 is a time-dependent, non-competitive inhibitor of the polymerase.

94 Tetrabenazine (TBZ) is a non-competitive inhibitor of VMAT2 that is used in the t

95 aver and Burk analysis showed that Trp was a non-competitive inhibitor of XO and a competitive inhibi

96 We show that IP6 is a non-competitive inhibitor that acts by blocking the stim

97 petitive inhibitor versus IkappaBalpha and a non-competitive inhibitor versus ATP for both kinases.

98 was a competitive inhibitor versus ATP and a non-competitive inhibitor versus IkappaBalpha.

99 At elevated concentrations, UTP is a non-competitive inhibitor with respect to ATP in the for

100 g, 3-ethoxy-5,6-dibromosalicylaldehyde, is a non-competitive inhibitor with respect to the XBP-1 RNA

101 s that interact with ClpA N-domains and is a non-competitive inhibitor with substrates that depend on

102 bstrate analog, and G418 (Geneticin), a weak non-competitive inhibitor, was determined to 2.5-A resol

103 tate, inward-open state, and competitive and non-competitive inhibitor-bound states, have revealed a

104 Kinetic assays revealed that BV is a non-competitive inhibitor.

105 ibitors against ACE, whereas PSSNK acts as a non-competitive inhibitor.

106 This cavity binds numerous non-competitive inhibitors and is a target for selective

107 ysis, reveals that bile salts act as partial non-competitive inhibitors of ATX, thereby attenuating L

108 e extracellular vestibule of LeuT and act as non-competitive inhibitors of transport.

109 Hence, in addition to channel blocking, non-competitive interactions with heteromeric neuronal n

110 The non-competitive intramolecular deuterium isotope effect,

111 -O(2) complex (29 s(-1)), (iv) the lack of a non-competitive kinetic deuterium isotope effect, (v) th

112 High intermolecular non-competitive kinetic deuterium isotope effects on bot

113 nhibits the enzymatic function of LOXL2 in a non-competitive manner thereby allowing inhibition of LO

114 d have found that the inhibition occurs in a non-competitive manner with respect to both spermine and

115 ulations revealed that pRB binds to PP1 in a non-competitive manner.

116 h K(i) approximately 10 muM in an apparently non-competitive manner.

117 Each compound functions by a unique, non-competitive mechanism and synergizes with competitiv

118 inhibited glycation of ovalbumin by a mixed non-competitive mechanism in both dry and in solution co

119 e EC50 or the Hill coefficient, indicating a non-competitive mechanism of action.

120 voltage dependence, and was due mainly to a non-competitive mechanism that reduced the maximum respo

121 inhibited cyclase activity through a mixed, non-competitive mechanism that was only observable under

122 ibits the kinetoplastid proteasome through a non-competitive mechanism, does not inhibit the mammalia

123 m, whereas verapamil inhibits transport by a non-competitive mechanism, thus suggesting the possibili

124 achieved via a competitive, uncompetitive or non-competitive mechanism.

125 , but inhibited ciprofloxacin transport by a non-competitive mechanism.

126 that absolute activity levels, or some other non-competitive mechanisms, determine the degree of reco

127 We saw no evidence of non-competitive mechanisms.

128 ack inhibition (allosteric, competitive, and non-competitive) mechanisms, the channeling of metabolic

129 hibited reversibly by 1 mM (R,S)-MCPG or the non-competitive mGluR1 antagonist CPCCOEt (20 microM), i

130 ous work has shown that blockade of NMDAR by non-competitive (MK-801) and competitive (AP5) antagonis

131 ith either competitive (AP7, 3-10 microg) or non-competitive (MK-801, 3-10 microg) NMDA antagonists,

132 and for binding to AR in vitro, suggesting a non-competitive mode of action.

133 tested whether a single dose of ketamine, a non-competitive N-methyl-D-aspartate (NMDA) glutamate re

134 after intraperitoneal injection of MK-801, a non-competitive N-methyl-D-aspartate (NMDA) receptor ant

135 p.) were analysed to determine whether other non-competitive N-methyl-D-aspartate (NMDA) receptor ant

136 The non-competitive N-methyl-d-aspartate (NMDA) receptor ant

137 Local infusion of the non-competitive N-methyl-D-aspartate (NMDA) receptor ant

138 ent with systemic MK-801 (0.25 mg/kg, ip), a non-competitive N-methyl-d-aspartate (NMDA) receptor ant

139 fashion by intrathecal administration of the non-competitive N-methyl-D-aspartate (NMDA) receptor cha

140 ute treatment with subanesthetic ketamine, a non-competitive N-methyl-D-aspartic acid (NMDA) receptor

141 his release was sensitive to blockade by the non-competitive nAChR antagonist, mecamylamine (Mec).

142 Non-competitive nicotinic ligands bind AChBP with high a

143 Antiserum to dynorphin A((1-17)) or the non-competitive NMDA antagonist MK-801 increased the ant

144 e antagonists, intrastriatal infusion of the non-competitive NMDA antagonist MK-801 partially decreas

145 For comparison we also evaluated a non-competitive NMDA antagonist, (5R,10S)-(+)-5-methyl-1

146 Ketamine (100 microM), a non-competitive NMDA antagonist, and L-689,560 (20 micro

147 Dizocilpine (MK-801), a non-competitive NMDA antagonist, at 1-45 microM abolishe

148 ment with dizocilpine (MK-801; 10 microM), a non-competitive NMDA antagonist, was started before NMDA

149 phoinositide hydrolysis, it also serves as a non-competitive NMDA antagonist; in contrast, other resu

150 used spinal cord slices with competitive and non-competitive NMDA antagonists in the presence and abs

151 y, the effects of subanesthetic doses of the non-competitive NMDA antagonists ketamine and MK-801 wer

152 The potent neuroprotective, non-competitive NMDA receptor antagonist dizocilpine (MK

153 This study investigated whether memantine, a non-competitive NMDA receptor antagonist is neuroprotect

154 tionship was true in the cat, using the same non-competitive NMDA receptor antagonist MK-801, and a t

155 MK-801, a non-competitive NMDA receptor antagonist that indirectly

156 MK-801, a non-competitive NMDA receptor antagonist that is known t

157 The non-competitive NMDA receptor antagonist, dizocilpine (0

158 aring its metabolic profile with that of the non-competitive NMDA receptor antagonist, dizocilpine (M

159 In the presence of MK-801, a non-competitive NMDA receptor antagonist, microinjection

160 We investigated whether the non-competitive NMDA receptor antagonist, MK-801, could

161 receptors by intra-CA3 infusion of MK-801, a non-competitive NMDA receptor antagonist, reversed behav

162 Recent studies indicate that competitive and non-competitive NMDA receptor antagonists can be readily

163 y a role in the aetiology of depression with non-competitive NMDA receptor antagonists such as amanta

164 Non-competitive NMDA receptor antagonists, such as phenc

165 ned whether ketamine, a clinically available non-competitive NMDA receptor channel blocker, could blo

166 The efficacy of ketamine (KET), a non-competitive NMDA receptor-channel blocker, was asses

167 utamate (CPP, competitive NMDA; dizocilpine, non-competitive NMDA; NBQX, AMPA) and GABA (bicuculline,

168 Local infusion of the non-competitive non-selective nAChR antagonist mecamylam

169 We tested the ability of the non-competitive, NR2B-selective NMDA antagonist eliprodi

170 ull agonist to an antagonist (competitive or non-competitive) of the same receptor type may form a hy

171 that the dominant mechanism of antagonism is non-competitive, originating from conformational arrest

172 The non-competitive pattern of inhibition was not present in

173 isotope effects on k(cat) and k(cat)/K(m) in non-competitive reactions were only 2-3.

174 pectedly, inhibition by peptide aldehydes is non-competitive, revealing that in the Michaelis complex

175 Mechanistically, non-competitive, reversible binding of the inhibitor to

176 d set of potential interactions in a largely non-competitive setting.

177 nvergence zone, methyl sulphides served as a non-competitive substrate supporting methane generation

178 The reaction kinetic fit with a non-competitive substrate-inhibition equation.

179 ms the apparent mechanism of antagonism from non-competitive to competitive.

180 med the transfection results and suggested a non-competitive type of inhibition with a K(i) in the lo

181 inhibitors exhibited a mixed competitive and non-competitive type of inhibition.

182 Ketamine, a non-competitive, voltage-dependent N-Methyl-D-aspartate

183 nhibition of halpha4beta2-nAChR function was non-competitive, voltage-independent, and use-independen

184 various concentrations of agonist for "pure' non-competitive vs. uncompetitive inhibition was compute

185 X by aprotinin (Ki 0.89 +/- 0.52 microM) was non-competitive, whereas inhibition by active site-inhib

186 R3 mutant (K650E) in a fashion that appeared non-competitive with ATP.

187 44muM, respectively, they are reversible and non-competitive with nucleotides.

188 ATPase activity for the mutant proteins were non-competitive with respect to ATP (altering catalytic

189 ible, uncompetitive with respect to ATP, and non-competitive with respect to bicarbonate, acetyl-CoA,

190 Catechol estrogen inhibition is non-competitive with respect to the substrate ATP, and w

191 re both found to be competitive with ATP and non-competitive with S1, indicating binding of ATP and S

192 is competitive with autocamtide-2 substrate, non-competitive with syntide-2 substrate, and uncompetit

193 Inhibition appears mostly non-competitive with the substrate ATP, indicating that