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 ng effect, being this classified as mixed or non-competitive.

3 nd after the addition of the competitive and non-competitive AChR blockers d-tubocurarine and alpha-b

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

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

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

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

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

9 PTPsigma and antagonizes PTPsigma via unique non-competitive, allosteric binding.

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

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

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

13 Targeting AKR1B1 with its non-competitive and reversible inhibitor epalrestat dela

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

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

16 ar, ascorbic acid inhibited HPA activity via non-competitive antagonism from two allosteric sites, by

17 CKD significantly inhibits CaSR activity via non-competitive antagonism.

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

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

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

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

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

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

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

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

26 he memory deficit caused by phencyclidine (a non-competitive antagonist of NMDAR), and prevented the

27 Broflanilide acts as a non-competitive antagonist of the gamma-aminobutyric aci

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

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

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

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

32 The non-competitive antagonist picrotoxin blocked nearly 50%

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

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

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

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

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

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

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

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

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

42 5 and confers sensitivity to displacement by non-competitive antagonists.

43 50295 potentiator binding to displacement by non-competitive antagonists.

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

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

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

47 Finally, we identify a novel non-competitive ASCT2 inhibitor, through virtual screeni

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

49 Moreover, the non-competitive BDNF/TrkB inhibitor ANA-12 reduced E2-in

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

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

52 Our previous simulations of non-competitive binding of the coreNLS, in which it nati

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

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

55 ulate the blood system after competitive and non-competitive BM transplantation.

56 and molecular docking studies attributed the non-competitive character to selective inhibitor binding

57 ld be associated with either a single image (non-competitive condition) or two competing images, and

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

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

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

61 lts suggest that P. falciparum has adopted a non-competitive evolutionary strategy of resource exploi

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

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

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

65 tions, but, on larger spatiotemporal scales, non-competitive factors may have driven biogeographic pa

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

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

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

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

70 This finding allows a general non-competitive, function-independent, quantitative, iso

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

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

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

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

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

76 ates the potential of anti-IC antibodies and non-competitive immunoassays for the analysis of small m

77 Non-competitive import studies demonstrated that prSSU a

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

79 We introduce an uncertain non-competitive incentive scheme along with the certain

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

81 These TMD mimetics exhibited non-competitive inhibition and occupy both the exosite a

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

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

84 tified proximal allosteric sites and utilize non-competitive inhibition mechanisms.

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

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

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

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

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

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

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

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

93 We find that it exhibits non-competitive inhibition of serotonin uptake and imped

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

95 ently of double-stranded DNA, resulting in a non-competitive inhibition of the second messenger cycli

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

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

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

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

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

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

102 mation and providing a mechanistic basis for non-competitive inhibition.

103 a mixed-type (combination of competitive and non-competitive) inhibition mechanism, FBG reduced the V

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

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

106 A non-competitive inhibitor may produce a more favorable t

107 a-(4-fluorophenyl)tropane(2) (beta-CFT), the non-competitive inhibitor MRS7292(3) and Zn(2)(+) (ref.

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

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

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

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

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

113 etermined in complex with UCPH-101, apotent, non-competitive inhibitor of EAAT1.

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

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

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

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

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

119 4-aminobenzohydrazide was determined to be a non-competitive inhibitor of TBR-POD and Turnip-POD.

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

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

122 Notably, ibogaine is a non-competitive inhibitor of transport but displays comp

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

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

125 tion of CXCL8 receptor by the small-molecule non-competitive inhibitor repertaxin attenuated the prog

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

127 VMAT2 complexed with tetrabenazine (TBZ), a non-competitive inhibitor used in the treatment of Hunti

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

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

130 ibition kinetics study indicated that 6 is a non-competitive inhibitor while 30 inhibits tyrosinase c

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

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

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

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

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

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

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

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

139 However, allosteric modulation of ASCT2 via non-competitive inhibitors is unknown.

140 nists (angiotensin receptor blockers) act as non-competitive inhibitors of all these nanobody-peptide

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

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

143 Non-competitive inhibitors targeting these pockets may b

144 han substrate or Na(+) binding, confirming a non-competitive inhibitory mechanism, but only partially

145 dase (IC(50) = 1.53 ug/mL), acting through a non-competitive inhibitory mechanism.

146 ase (IC(50) = 1.53 mug/mL), acting through a non-competitive inhibitory mechanism.

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

148 The non-competitive intramolecular deuterium isotope effect,

149 571 mg/mL, respectively, whereas BT was pure non-competitive, K(i) = 0.36 mg/mL.

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

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

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

153 tylneuraminic acid 1 (Neu5Ac) transport in a non-competitive manner with IC(50) ~ 2.5 muM, a value 40

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

155 d SSIIIa starch polymerization activity in a non-competitive manner.

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

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

158 s recognition of ssrA-tagged substrates by a non-competitive mechanism and also slows subsequent unfo

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

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

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

162 metabolite, D-imidazole lactate, exhibits a non-competitive mechanism of urease inhibition along wit

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

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

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

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

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

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

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

170 ldose reductase (K(i) = 127.5 ug/mL) through non-competitive mechanisms.

171 We saw no evidence of non-competitive mechanisms.

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

173 educing sediments through the utilization of non-competitive methylated compounds; however, the occur

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

175 2, which is orally bioavailable, potent, ATP non-competitive, microtubule-dependent, and highly selec

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

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

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

179 to the identification of several drug-like, non-competitive modulators of some of these enzymes - in

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

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

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

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

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

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

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

187 e antidepressant-like effects of ketamine, a non-competitive N-methyl-D-aspartate receptor antagonist

188 Sub-anaesthetic doses of ketamine, a non-competitive N-methyl-D-aspartate receptor antagonist

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

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

191 Non-competitive nicotinic ligands bind AChBP with high a

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

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

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

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

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

197 ) showed enhanced locomotory response to the non-competitive NMDA antagonist, MK-801, which was poten

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

214 Non-competitive NMDA receptor antagonists, such as phenc

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

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

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

218 o ethylene with >=99% selectivity under both non-competitive (no ethylene co-feed) and competitive (e

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

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

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

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

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

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

225 avenging could be an important factor in the non-competitive relationship of resource exploitation be

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

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

228 tive incentive scheme along with the certain non-competitive scheme and the (uncertain) competitive s

229 the prevalence) of cheating relative to both non-competitive schemes, with the effect of competition

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

231 f pro-inflammatory cytokines by binding to a non-competitive STING surface site that is distinct from

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

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

234 red how people behaved under competitive and non-competitive tasks that were associated with differen

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

236 This results in competitive or non-competitive transport inhibition.

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

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

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

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

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

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

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

244 44muM, respectively, they are reversible and non-competitive with nucleotides.

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

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

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

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

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

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

251 OT inhibition of glucose uptake was partial non-competitive, with an inhibitor constant (K(i) ) = 0.