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1 ical binding sites, their binding to SecY is noncompetitive.
2 ner, whereas the interaction of VU0360172 is noncompetitive.
4 A kinetic model for transport describing the noncompetitive action of ibogaine and the competitive ac
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
26 rmacologically targeting the linkers through noncompetitive and subunit-specific modes of action.
27 antagonists are classified as competitive or noncompetitive and surmountable or insurmountable based
28 t QNZ46 inhibits NMDA receptor function in a noncompetitive and voltage-independent manner by an unco
29 ced by these quinazolin-4-one derivatives is noncompetitive and voltage-independent, suggesting that
30 and efficient identification of competitive, noncompetitive, and covalent inhibitors of MIF in a mann
31 various inhibition mechanisms (competitive, noncompetitive, and mixed), with sub- and low micromolar
32 the substituted quinoline HG-829 as a novel, noncompetitive, and potent P-glycoprotein inhibitor that
33 and 5d were identified as extremely potent, noncompetitive, and reversible FAAH inhibitors endowed w
34 h reduced desensitization (type II PAMs), 4) noncompetitive antagonism (NAMs), and 5) compounds that
35 ted neuroactive steroids, those that exhibit noncompetitive antagonism of GABA(A) receptors, altered
37 xinin, TETS has been proposed to bind to the noncompetitive antagonist (NCA) site in the pore of the
41 responses were relatively insensitive to the noncompetitive antagonist mecamylamine compared with GAT
43 yl)-vinyl]-6-fluoro- 3H-quinazolin-4-one), a noncompetitive antagonist of AMPA-selective glutamate re
47 ent nicotinic acetylcholine receptor (nAChR) noncompetitive antagonist, binds with higher affinity in
52 centrations, it inhibited the binding of the noncompetitive antagonists [(3)H]tetracaine and [(3)H]ph
53 sition 6, respectively, were the most potent noncompetitive antagonists at the NMDA receptor with IC5
57 offer an alternative strategy that combines noncompetitive antibodies to achieve robust degradation
62 for the first time, a new strategy using the noncompetitive assay format via a biomimetic material, n
64 reptavidin and used them to setup phage-free noncompetitive assays for the herbicide clomazone (MW 24
67 We have used this approach to confirm the noncompetitive binding of alitame and cyclamate to the r
68 ory targeted nonagonist binding sites (i.e., noncompetitive binding sites, negative allosteric bindin
70 played a concentration-dependent, reversible noncompetitive blockade of AP-sensitive tonic current in
75 evaluate the role of MyD88 in T cells under noncompetitive conditions, bone marrow chimeras were gen
77 sulted in the identification of two bivalent noncompetitive D3R-selective antagonists, 18a and 25a, w
79 ; (-)-2-amino-5-phosphonopentanoic acid] and noncompetitive (dizocilpine, or MK-801 [(5S,10R)-(+)-5-m
82 cyl-CoA-to-CoA ratio), whereby CoA acts as a noncompetitive feedback inhibitor through interaction wi
84 the detection of these small molecules in a noncompetitive format (PHAIA) with increased sensitivity
90 facilitate the development of sandwich-type noncompetitive immunoassays for the detection of small a
91 ensitivity and direct proportional signal of noncompetitive immunoassays to develop a new Phage Anti-
94 m), whereas a Ubc5BC85A product analog shows noncompetitive inhibition (Ki = 2.2 +/- 0.5 mum), consis
97 proteins by differentiating competitive and noncompetitive inhibition demonstrates its ability as a
98 hibition in regard to external [K(+)] versus noncompetitive inhibition in respect to external [Cl(-)]
100 , the hydroxamic acid, SC81956, demonstrated noncompetitive inhibition kinetics with a Ki of 23 nM.
101 time-dependent inhibitors of PC2, exhibiting noncompetitive inhibition kinetics; the most potent inhi
102 ibited hTP in the submicromolar range with a noncompetitive inhibition mode with both thymidine and i
103 tly inhibit monocyte recruitment through the noncompetitive inhibition of CCL2-induced ERK1/2 activat
107 tory compound, termed JF5, also demonstrated noncompetitive inhibition of the alpha(2A)-adrenergic re
108 resulting in binding to activated fVIII and noncompetitive inhibition of the intrinsic fXase complex
109 d that copper (I) and (II) cations displayed noncompetitive inhibition of the LC (Ki approximately 1
111 l molecule analinopyrimidine, exhibited pure noncompetitive inhibition versus ATF2 and competitive in
112 such compound, ALS 1-0635, indicated linear, noncompetitive inhibition, and Dixon plot analysis from
113 Consistent with the observed time-dependent noncompetitive inhibition, the cocrystal X-ray structure
116 ve inhibitor anakinra (Kineret) and a potent noncompetitive inhibitor 101.10, for efficacy in blockin
119 titive inhibitor against R-3-OHC14-ACP and a noncompetitive inhibitor against UDP-3-O-(R-3-OHC14)-Glc
123 cate that phenamacril is a species-specific, noncompetitive inhibitor of class I myosin in susceptibl
125 e substrate, we demonstrate that E acts as a noncompetitive inhibitor of detergent-solubilized MraY,
127 f migrating neurons with Dynasore, a soluble noncompetitive inhibitor of Dynamin, rapidly arrests the
128 s substrates demonstrated that I3C acts as a noncompetitive inhibitor of elastase activity with an in
129 ells and characterized as a slow, tight, and noncompetitive inhibitor of factor (F) XIa by a mechanis
133 rons of NAD(+) with FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosylt
134 transport substrate clotrimazole, which is a noncompetitive inhibitor of Pdr5 ATPase activity, has a
135 containing residues 1-14 of GRK2 served as a noncompetitive inhibitor of receptor phosphorylation by
136 coralloides synthesizes corallopyronin A, a noncompetitive inhibitor of RNA polymerase ineffective a
138 ysis characterized NSC48300 as a reversible, noncompetitive inhibitor of Taspase1 (K(i) = 4.22 mumol/
139 ABCB1-mediated transport of calcein AM, and noncompetitive inhibitor of the ABCG2-mediated pheophorb
141 idinyl)-2,4-dichlorobenzamide 5 (BPDBA) is a noncompetitive inhibitor of the betaine/GABA transporter
142 We have previously shown that TriCHQ is a noncompetitive inhibitor of the thiol-disulfide exchange
144 cated in the channel pore and equates with a noncompetitive inhibitor site found in many pLGICs.
145 line agent to treat hypertension, and by the noncompetitive inhibitor tetrabenazine, presently in use
147 sults show that the aptamer we isolated is a noncompetitive inhibitor that selectively inhibits the o
148 tion of the inhibitor revealed that it was a noncompetitive inhibitor that showed a time-dependent on
152 gh the screen was further characterized as a noncompetitive inhibitor with both ATP and PLK-peptide a
153 o the isoprenylated cysteine substrate and a noncompetitive inhibitor with respect to AdoMet, the met
154 ive with respect to pyrophosphate (PP(i)), a noncompetitive inhibitor with respect to ATP, but at >10
155 in part by the cellular concentrations of a noncompetitive inhibitor, nicotinamide, that reacts with
156 Complete inhibition of aromatase with ATD, a noncompetitive inhibitor, significantly and similarly re
157 K-3 inhibitor, CHIR99021 (CHIR), and the ATP noncompetitive inhibitor, Tideglusib (TG), can equally e
161 oped herein allowed identifying new original noncompetitive inhibitors against cN-II that act in a sy
162 rs from compound library screens because ATP-noncompetitive inhibitors are often weaker and commonly
163 inase 4 (CDK4) and the identification of ATP-noncompetitive inhibitors by high-throughput screening a
166 enation of arachidonic acid (AA) but potent, noncompetitive inhibitors of 2-arachidonoylglycerol (2-A
168 thyl thiohistidines of marine origin, act as noncompetitive inhibitors of GGT, with an apparent K(i)
169 inhibitor of Klenow fragment and two strong noncompetitive inhibitors of HIV-1 reverse transcriptase
170 ternate amino acids act as rapid equilibrium noncompetitive inhibitors of MtIPMS failing to display b
173 cid esters have recently been reported to be noncompetitive inhibitors of the N-acylethanolamine acid
174 analysis indicates that these compounds are noncompetitive inhibitors of the p-hydroxyphenylpyruvate
176 n growing interest in the development of ATP-noncompetitive inhibitors to overcome these problems.
177 studies that analogues of this chemotype are noncompetitive inhibitors, and by using a crystal struct
188 and cell migration that is consistent with a noncompetitive inhibitory mechanism of Met signal transd
189 ablished second generation GSM, E2012, but a noncompetitive interaction between AZ GSMs and the first
193 exhibited time-dependent FAAH inhibition and noncompetitive irreversible inactivation of the enzyme,
194 PDE4-specific activator displays reversible, noncompetitive kinetics of activation (increased V (max)
196 reported that treatment with combinations of noncompetitive mAbs can induce receptor clustering, lead
197 highly potent combinations consisting of two noncompetitive mAbs that target EGFR domain 3 reduce sur
198 Ch competitor dihydro-beta-erythroidine in a noncompetitive manner and that morantel still potentiate
199 s, FliW allosterically antagonizes CsrA in a noncompetitive manner by excluding the 5'UTR from the Cs
201 R and inhibits IR kinase activity in a mixed noncompetitive manner to ATP, through which piceatannol
203 s the FeS cluster scaffold protein IscU in a noncompetitive manner, generating a complex that contain
204 IIalpha ATPase activity in a dose-dependent noncompetitive manner, this was secondary to salicylate-
215 We conclude that FliW inhibits CsrA by a noncompetitive mechanism that differs dramatically from
217 mpounds that inhibited UT-A selectively by a noncompetitive mechanism with IC50 down to approximately
218 tolerated AMPA receptor inhibitors act via a noncompetitive mechanism, but many of them produce adver
223 mpetitive PI3K inhibitor ZSTK474 and the ATP-noncompetitive MEK inhibitor PD0325901 is described.
224 e beta-arrestin-dependent pathway, whereas a noncompetitive mGlu1 receptor antagonist blocked both pa
226 ch provides a compelling explanation for the noncompetitive mode of binding of this novel class of in
227 nding at the targeted interface supports the noncompetitive mode of inhibition determined by kinetic
228 ic characterization of coumestans revealed a noncompetitive mode of inhibition with respect to nucleo
229 er inhibition was not observed, indicating a noncompetitive mode of viral resistance to the drug.
231 te that HG-829 is a potent, long-acting, and noncompetitive modulator of P-glycoprotein export functi
232 gp-mediated drug efflux but rather acts as a noncompetitive modulator of P-glycoprotein transport fun
237 Mechanistic characterization revealed a noncompetitive nature of these inhibitors with binding c
238 r the competitive NMDA antagonist AP5 or the noncompetitive NMDA antagonist MK-801 does not selective
239 LTD, but not LTP, was also observed when the noncompetitive NMDA channel blocker MK-801 was added to
240 f methadone (dextromethadone; REL-1017) is a noncompetitive NMDA receptor antagonist with an apparent
241 Two experiments examined the effect of the noncompetitive NMDA receptor antagonist, dizocilpine mal
245 hem have interfering effects (competitive or noncompetitive) on a specific protein-receptor binding r
248 t mechanisms of inhibition (ATP-competitive, noncompetitive, or uncompetitive) in PoA compared to IoC
249 the inhibitor binds to an exosite, displays noncompetitive partial inhibition, and is synergistic wi
250 pect to the first substrate, pyruvate, and a noncompetitive partial inhibitor with respect to ASA, an
252 king studies support that 2 binds to the ATP-noncompetitive pocket of glycogen synthesis kinase-3beta
253 a unique single-disulfide conopeptide with a noncompetitive, potentially allosteric inhibitory mechan
255 isual cortex is the outcome of two distinct, noncompetitive processes, a loss of deprived-eye respons
257 strate the feasibility of the development of noncompetitive proteasome inhibitors as additives and/or
258 Herein, we describe the optimization of noncompetitive proteasome inhibitors to yield derivative
261 and long-term engraftment in competitive and noncompetitive repopulation assays (<1.5% chimerism of V
262 ) (IC50 = 669 pM), acting as competitive and noncompetitive reversible inhibitors, respectively.
263 an existing competitive assay to a versatile noncompetitive sandwich-type format using immunocomplex
266 nal validation, we identified BHPI, a potent noncompetitive small molecule ERalpha biomodulator that
271 P, but this activity is inhibited by ATP via noncompetitive substrate inhibition and by GTP via mixed
273 These compounds represent a new class of noncompetitive subunit-selective NMDA receptor antagonis
274 e converted the mechanism of inhibition from noncompetitive to competitive, such that the antagonist
276 itive inhibitor to the peptide substrate and noncompetitive to the cofactor S-adenosylmethionine.
281 for direct detection of small compounds in a noncompetitive two-site immunoassay format that performs
282 y two antibodies impeding their detection by noncompetitive two-site immunoassays, which are superior
283 ng the Streptomyces enzymes are of the mixed noncompetitive type, suggesting that (p)ppGpp binds to a
284 -nanomolar inhibitors of Mtb's Lpd that were noncompetitive versus NADH, NAD(+), and lipoamide and >1
286 hibition by NADP is competitive vs NADPH and noncompetitive vs alpha-AASA and L-glutamate, suggesting
287 ncompetitive vs saccharopine, L-glutamate is noncompetitive vs both NADP and saccharopine, while L-AA
290 both NADP and saccharopine, while L-AASA is noncompetitive vs saccharopine and uncompetitive vs NADP
291 oxidation, NADPH is competitive vs NADP and noncompetitive vs saccharopine, L-glutamate is noncompet
293 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