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1 ner, whereas the interaction of VU0360172 is noncompetitive.
3 A kinetic model for transport describing the noncompetitive action of ibogaine and the competitive ac
5 vely, and are uncompetitive against NADH and noncompetitive against alpha-Kg and lysine, respectively
6 novel allosteric Syk inhibitor, X1, that is noncompetitive against ATP (K(i) 4 +/- 1 muM) and substr
7 e novo design of a potent and selective C5aR noncompetitive allosteric inhibitor, DF2593A, guided by
12 two compounds (23 and 26) is consistent with noncompetitive allosteric modulation of dopamine signali
15 e prevented by treatment with the prototypic noncompetitive alpha-amino-3-hydroxy-5-methyl-4-isoxazol
18 here, for the first time, the discovery of a noncompetitive AMPA receptor antagonist that is dependen
20 s indicate, however, that this inhibition is noncompetitive and caused by the interaction of clotrima
21 the inhibition kinetics are mixed, with both noncompetitive and competitive components, and fluoresce
22 ing this technique, we developed methods for noncompetitive and competitive immunoassays, using thyro
23 nzotriazolyl species makes the leaving group noncompetitive and generates the nucleofuge that has bee
24 nanoparticles is the basis of the developed noncompetitive and homogeneous method for the estimation
27 rmacologically targeting the linkers through noncompetitive and subunit-specific modes of action.
28 antagonists are classified as competitive or noncompetitive and surmountable or insurmountable based
29 t QNZ46 inhibits NMDA receptor function in a noncompetitive and voltage-independent manner by an unco
30 ced by these quinazolin-4-one derivatives is noncompetitive and voltage-independent, suggesting that
31 and efficient identification of competitive, noncompetitive, and covalent inhibitors of MIF in a mann
32 various inhibition mechanisms (competitive, noncompetitive, and mixed), with sub- and low micromolar
33 the substituted quinoline HG-829 as a novel, noncompetitive, and potent P-glycoprotein inhibitor that
34 and 5d were identified as extremely potent, noncompetitive, and reversible FAAH inhibitors endowed w
35 h reduced desensitization (type II PAMs), 4) noncompetitive antagonism (NAMs), and 5) compounds that
36 ted neuroactive steroids, those that exhibit noncompetitive antagonism of GABA(A) receptors, altered
38 s (IC50 = 600 microM) and the binding of the noncompetitive antagonist [3H]tetracaine to nAChR-rich m
43 yl)-vinyl]-6-fluoro- 3H-quinazolin-4-one), a noncompetitive antagonist of AMPA-selective glutamate re
48 this pattern of fluorescence change, but the noncompetitive antagonist picrotoxin failed to elicit op
49 ent nicotinic acetylcholine receptor (nAChR) noncompetitive antagonist, binds with higher affinity in
55 centrations, it inhibited the binding of the noncompetitive antagonists [(3)H]tetracaine and [(3)H]ph
56 sition 6, respectively, were the most potent noncompetitive antagonists at the NMDA receptor with IC5
62 offer an alternative strategy that combines noncompetitive antibodies to achieve robust degradation
67 for the first time, a new strategy using the noncompetitive assay format via a biomimetic material, n
69 reptavidin and used them to setup phage-free noncompetitive assays for the herbicide clomazone (MW 24
72 We have used this approach to confirm the noncompetitive binding of alitame and cyclamate to the r
73 ory targeted nonagonist binding sites (i.e., noncompetitive binding sites, negative allosteric bindin
75 played a concentration-dependent, reversible noncompetitive blockade of AP-sensitive tonic current in
80 evaluate the role of MyD88 in T cells under noncompetitive conditions, bone marrow chimeras were gen
82 sulted in the identification of two bivalent noncompetitive D3R-selective antagonists, 18a and 25a, w
84 ; (-)-2-amino-5-phosphonopentanoic acid] and noncompetitive (dizocilpine, or MK-801 [(5S,10R)-(+)-5-m
85 e baseline assessment, 12.6% reported other (noncompetitive) employment activity, and 72.9% reported
87 cyl-CoA-to-CoA ratio), whereby CoA acts as a noncompetitive feedback inhibitor through interaction wi
89 the detection of these small molecules in a noncompetitive format (PHAIA) with increased sensitivity
95 facilitate the development of sandwich-type noncompetitive immunoassays for the detection of small a
96 ensitivity and direct proportional signal of noncompetitive immunoassays to develop a new Phage Anti-
99 m), whereas a Ubc5BC85A product analog shows noncompetitive inhibition (Ki = 2.2 +/- 0.5 mum), consis
103 proteins by differentiating competitive and noncompetitive inhibition demonstrates its ability as a
104 hibition in regard to external [K(+)] versus noncompetitive inhibition in respect to external [Cl(-)]
106 , the hydroxamic acid, SC81956, demonstrated noncompetitive inhibition kinetics with a Ki of 23 nM.
107 time-dependent inhibitors of PC2, exhibiting noncompetitive inhibition kinetics; the most potent inhi
108 Our results represent a molecular view into noncompetitive inhibition of a sodium-coupled transporte
111 tory compound, termed JF5, also demonstrated noncompetitive inhibition of the alpha(2A)-adrenergic re
112 resulting in binding to activated fVIII and noncompetitive inhibition of the intrinsic fXase complex
113 d that copper (I) and (II) cations displayed noncompetitive inhibition of the LC (Ki approximately 1
115 l molecule analinopyrimidine, exhibited pure noncompetitive inhibition versus ATF2 and competitive in
116 hibits competitive inhibition versus ATP and noncompetitive inhibition versus cysteine, with an inhib
117 such compound, ALS 1-0635, indicated linear, noncompetitive inhibition, and Dixon plot analysis from
118 Consistent with the observed time-dependent noncompetitive inhibition, the cocrystal X-ray structure
120 ve inhibitor anakinra (Kineret) and a potent noncompetitive inhibitor 101.10, for efficacy in blockin
124 titive inhibitor against R-3-OHC14-ACP and a noncompetitive inhibitor against UDP-3-O-(R-3-OHC14)-Glc
129 e substrate, we demonstrate that E acts as a noncompetitive inhibitor of detergent-solubilized MraY,
131 f migrating neurons with Dynasore, a soluble noncompetitive inhibitor of Dynamin, rapidly arrests the
132 s substrates demonstrated that I3C acts as a noncompetitive inhibitor of elastase activity with an in
133 ells and characterized as a slow, tight, and noncompetitive inhibitor of factor (F) XIa by a mechanis
134 nt form of vitamin E present in humans, is a noncompetitive inhibitor of glutathione S-transferase pi
137 rons of NAD(+) with FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosylt
138 transport substrate clotrimazole, which is a noncompetitive inhibitor of Pdr5 ATPase activity, has a
139 containing residues 1-14 of GRK2 served as a noncompetitive inhibitor of receptor phosphorylation by
140 coralloides synthesizes corallopyronin A, a noncompetitive inhibitor of RNA polymerase ineffective a
142 ysis characterized NSC48300 as a reversible, noncompetitive inhibitor of Taspase1 (K(i) = 4.22 mumol/
144 idinyl)-2,4-dichlorobenzamide 5 (BPDBA) is a noncompetitive inhibitor of the betaine/GABA transporter
145 We have previously shown that TriCHQ is a noncompetitive inhibitor of the thiol-disulfide exchange
147 cated in the channel pore and equates with a noncompetitive inhibitor site found in many pLGICs.
148 line agent to treat hypertension, and by the noncompetitive inhibitor tetrabenazine, presently in use
150 sults show that the aptamer we isolated is a noncompetitive inhibitor that selectively inhibits the o
151 tion of the inhibitor revealed that it was a noncompetitive inhibitor that showed a time-dependent on
155 gh the screen was further characterized as a noncompetitive inhibitor with both ATP and PLK-peptide a
156 o the isoprenylated cysteine substrate and a noncompetitive inhibitor with respect to AdoMet, the met
157 ive with respect to pyrophosphate (PP(i)), a noncompetitive inhibitor with respect to ATP, but at >10
158 in part by the cellular concentrations of a noncompetitive inhibitor, nicotinamide, that reacts with
159 Complete inhibition of aromatase with ATD, a noncompetitive inhibitor, significantly and similarly re
164 oped herein allowed identifying new original noncompetitive inhibitors against cN-II that act in a sy
165 rs from compound library screens because ATP-noncompetitive inhibitors are often weaker and commonly
166 inase 4 (CDK4) and the identification of ATP-noncompetitive inhibitors by high-throughput screening a
168 designing conformation-specific, more potent noncompetitive inhibitors for the GluR2 AMPA receptor.
170 enation of arachidonic acid (AA) but potent, noncompetitive inhibitors of 2-arachidonoylglycerol (2-A
171 PAR1-wt exodomain and P4 and P3 mutants were noncompetitive inhibitors of alpha-thrombin hydrolyzing
174 inhibitor of Klenow fragment and two strong noncompetitive inhibitors of HIV-1 reverse transcriptase
175 ternate amino acids act as rapid equilibrium noncompetitive inhibitors of MtIPMS failing to display b
178 ucleotide exchange on beta-tubulin, and were noncompetitive inhibitors of the binding of radiolabeled
179 cid esters have recently been reported to be noncompetitive inhibitors of the N-acylethanolamine acid
180 analysis indicates that these compounds are noncompetitive inhibitors of the p-hydroxyphenylpyruvate
182 n growing interest in the development of ATP-noncompetitive inhibitors to overcome these problems.
183 studies that analogues of this chemotype are noncompetitive inhibitors, and by using a crystal struct
193 and cell migration that is consistent with a noncompetitive inhibitory mechanism of Met signal transd
194 ablished second generation GSM, E2012, but a noncompetitive interaction between AZ GSMs and the first
198 exhibited time-dependent FAAH inhibition and noncompetitive irreversible inactivation of the enzyme,
201 reported that treatment with combinations of noncompetitive mAbs can induce receptor clustering, lead
202 highly potent combinations consisting of two noncompetitive mAbs that target EGFR domain 3 reduce sur
203 Ch competitor dihydro-beta-erythroidine in a noncompetitive manner and that morantel still potentiate
204 s, FliW allosterically antagonizes CsrA in a noncompetitive manner by excluding the 5'UTR from the Cs
206 R and inhibits IR kinase activity in a mixed noncompetitive manner to ATP, through which piceatannol
208 s the FeS cluster scaffold protein IscU in a noncompetitive manner, generating a complex that contain
209 IIalpha ATPase activity in a dose-dependent noncompetitive manner, this was secondary to salicylate-
222 We conclude that FliW inhibits CsrA by a noncompetitive mechanism that differs dramatically from
224 mpounds that inhibited UT-A selectively by a noncompetitive mechanism with IC50 down to approximately
225 tolerated AMPA receptor inhibitors act via a noncompetitive mechanism, but many of them produce adver
230 mpetitive PI3K inhibitor ZSTK474 and the ATP-noncompetitive MEK inhibitor PD0325901 is described.
231 e beta-arrestin-dependent pathway, whereas a noncompetitive mGlu1 receptor antagonist blocked both pa
233 nding at the targeted interface supports the noncompetitive mode of inhibition determined by kinetic
234 ic characterization of coumestans revealed a noncompetitive mode of inhibition with respect to nucleo
235 er inhibition was not observed, indicating a noncompetitive mode of viral resistance to the drug.
237 te that HG-829 is a potent, long-acting, and noncompetitive modulator of P-glycoprotein export functi
238 gp-mediated drug efflux but rather acts as a noncompetitive modulator of P-glycoprotein transport fun
243 Mechanistic characterization revealed a noncompetitive nature of these inhibitors with binding c
244 r the competitive NMDA antagonist AP5 or the noncompetitive NMDA antagonist MK-801 does not selective
245 LTD, but not LTP, was also observed when the noncompetitive NMDA channel blocker MK-801 was added to
247 Two experiments examined the effect of the noncompetitive NMDA receptor antagonist, dizocilpine mal
251 hem have interfering effects (competitive or noncompetitive) on a specific protein-receptor binding r
254 t mechanisms of inhibition (ATP-competitive, noncompetitive, or uncompetitive) in PoA compared to IoC
255 the inhibitor binds to an exosite, displays noncompetitive partial inhibition, and is synergistic wi
256 pect to the first substrate, pyruvate, and a noncompetitive partial inhibitor with respect to ASA, an
258 king studies support that 2 binds to the ATP-noncompetitive pocket of glycogen synthesis kinase-3beta
260 isual cortex is the outcome of two distinct, noncompetitive processes, a loss of deprived-eye respons
262 strate the feasibility of the development of noncompetitive proteasome inhibitors as additives and/or
263 Herein, we describe the optimization of noncompetitive proteasome inhibitors to yield derivative
265 and long-term engraftment in competitive and noncompetitive repopulation assays (<1.5% chimerism of V
266 ) (IC50 = 669 pM), acting as competitive and noncompetitive reversible inhibitors, respectively.
267 an existing competitive assay to a versatile noncompetitive sandwich-type format using immunocomplex
270 nal validation, we identified BHPI, a potent noncompetitive small molecule ERalpha biomodulator that
274 P, but this activity is inhibited by ATP via noncompetitive substrate inhibition and by GTP via mixed
276 These compounds represent a new class of noncompetitive subunit-selective NMDA receptor antagonis
277 e converted the mechanism of inhibition from noncompetitive to competitive, such that the antagonist
283 for direct detection of small compounds in a noncompetitive two-site immunoassay format that performs
284 y two antibodies impeding their detection by noncompetitive two-site immunoassays, which are superior
285 ng the Streptomyces enzymes are of the mixed noncompetitive type, suggesting that (p)ppGpp binds to a
286 -nanomolar inhibitors of Mtb's Lpd that were noncompetitive versus NADH, NAD(+), and lipoamide and >1
288 hibition by NADP is competitive vs NADPH and noncompetitive vs alpha-AASA and L-glutamate, suggesting
289 ncompetitive vs saccharopine, L-glutamate is noncompetitive vs both NADP and saccharopine, while L-AA
292 both NADP and saccharopine, while L-AASA is noncompetitive vs saccharopine and uncompetitive vs NADP
293 oxidation, NADPH is competitive vs NADP and noncompetitive vs saccharopine, L-glutamate is noncompet
295 upies a novel allosteric binding site and is noncompetitive with both the peptide substrate and cofac
297 not bind to the catalytic zinc ion, they are noncompetitive with respect to substrate binding, and th
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