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1 ors against ACE, whereas PSSNK acts as a non-competitive inhibitor.
2 , given its status as a TBK1 substrate, as a competitive inhibitor.
3 Galactose was found to be the competitive inhibitor.
4 P binding pocket of the kinase and is an ATP competitive inhibitor.
5 CHK1 selective adenosine triphosphate (ATP) competitive inhibitor.
6 Kinetic assays revealed that BV is a non-competitive inhibitor.
7 A non-hydrolyzable ATP analog was a competitive inhibitor.
8 BoNT protein as a landscape for assembling a competitive inhibitor.
9 ATP and therefore leads to resistance to ATP competitive inhibitors.
10 hes biochemical potency and synergy with ATP-competitive inhibitors.
11 ifically target TdT and behave as nucleotide-competitive inhibitors.
12 lone or in combination with conventional ATP-competitive inhibitors.
13 y slowly and cannot be disrupted by strictly competitive inhibitors.
14 nct from that observed for kinase domain ATP-competitive inhibitors.
15 the ATP binding pocket by either ATP or ATP-competitive inhibitors.
16 r and that 1-thia-Trp and 1-oxa-Trp serve as competitive inhibitors.
17 We identified two classes of ATP-competitive inhibitors.
18 d screening strategy for Ras interfacial and competitive inhibitors.
19 efficiency, and increased resistance to SDH competitive inhibitors.
20 2 or Escherichia coli IDI-1 but instead were competitive inhibitors.
21 D-glucopyranoside and reduced sensitivity to competitive inhibitors.
22 AKAP79 also protects PKC from certain ATP-competitive inhibitors.
23 for Chagas disease, looking for reversible, competitive inhibitors.
24 t may not be apparent using conventional ATP-competitive inhibitors.
25 g site that has been effectively targeted by competitive inhibitors.
26 ructure-based design of dual JCV and BKV ATP-competitive inhibitors.
27 r the determination of costructures with ATP competitive inhibitors.
28 ower concentrations in comparison to the ATP-competitive inhibitors.
29 Hcy), D-Cys, thiosulfate, and azide bound as competitive inhibitors.
30 2N variant in the presence of pyruvate and a competitive inhibitor (2R,3R)-2,3,4-trihydroxy-N,N-dipro
31 es of ternary complexes of WT HMGCL with the competitive inhibitor 3-hydroxyglutaryl-CoA and of the c
33 f DHBPS from Vibrio cholerae (vDHBPS) with a competitive inhibitor 4-phospho-d-erythronohydroxamic ac
34 ading to the development of a very promising competitive inhibitor (8r, IC50 = 200 nM, K(i) = 82 nM).
38 ies revealed that this compound behaves as a competitive inhibitor against the peptide substrate and
39 etics and docking studies suggested they are competitive inhibitors against a dimethylated H3K4 subst
40 plots suggested that AHEPVK and RIGLF act as competitive inhibitors against ACE, whereas PSSNK acts a
41 tructural basis for the design of nucleotide-competitive inhibitors against clinically relevant APH e
42 osine-containing tetrapeptides functioned as competitive inhibitors against mushroom tyrosinase by us
43 n exploited in the development of reversible competitive inhibitors against SK from Mycobacterium tub
45 estigated two IL-1 receptor antagonists, the competitive inhibitor anakinra (Kineret) and a potent no
46 ase-3 the resulting DEVD-T peptide acts as a competitive inhibitor and entraps the active site of cas
47 irst structure of CDK1 bound to a potent ATP-competitive inhibitor and identify aspects of CDK1 struc
48 ts indicates that octyl protocatechuate is a competitive inhibitor and the inhibition constant (Ki) w
49 insight into the activation of B-Raf by ATP-competitive inhibitors and can aid in the design of more
53 ne-derived antagonists, the newly identified competitive inhibitors are uncharged at physiological pH
54 EK1, a nucleotide, and an allosteric non-ATP competitive inhibitor: ATP-gammaS with compound 1 and AD
58 euT, in substrate-bound outward-occluded and competitive inhibitor-bound outward-facing states have a
59 , inward-open state, and competitive and non-competitive inhibitor-bound states, have revealed a mech
60 alytic activity in vitro, unlike typical ATP-competitive inhibitors, but acted in a mechanistically d
61 nti-apoptotic BCL-2 members that function as competitive inhibitors by binding to the hydrophobic cle
63 g site and that combining allosteric and ATP-competitive inhibitors can overcome resistance to either
64 ide derived from beta-neurexin is a powerful competitive inhibitor capable of efficiently blocking su
67 oscillations are blocked by coinjection of a competitive inhibitor, derived from the WWI domain-bindi
68 activity using small interfering RNA or the competitive inhibitor difluoromethylornithine restored i
73 ) 11-13 in Notch1, and therefore serves as a competitive inhibitor for Notch ligands to decrease expr
74 ibe an approach to accelerate the search for competitive inhibitors for carbohydrate-recognition doma
75 ies demonstrate that both TCAs and SSRIs are competitive inhibitors for eukaryotic BATs and bind to t
77 food protein hydrolysates, are selective and competitive inhibitors for the C-domain with a selectivi
79 o determine accurate inhibitor constants for competitive inhibitors from measurements at a single inh
80 g pure proteins, treatment of cells with the competitive inhibitors Go 6983 or bisindolylmaleimide I,
81 less susceptible to inhibition from the ATP-competitive inhibitor Go6976 and the substrate-competiti
83 finity (Kd approximately 12-30 nM) selective competitive inhibitors (IC50 approximately 20-150 nM) fo
84 interleukin (IL)-1beta has co-evolved with a competitive inhibitor, IL-1 receptor antagonist (IL-1Ra)
85 rties, when used in combination with the ATP-competitive inhibitors imatinib or nilotinib, suppressed
90 itionally, the dissociation constant for the competitive inhibitor isopropyl beta-d-1-thiogalactopyra
91 ystal structure of NDM-1 bound to the potent competitive inhibitor l-captopril, which reveals a uniqu
92 s by feeding leaves with the PEP carboxylase competitive inhibitors malate and diethyl oxalacetate (D
96 strate binding domain, we identified a novel competitive inhibitor, N-(3,5-dimethylphenyl)-2-[[5-(4-e
97 ibition of ferrochelatase using the specific competitive inhibitor, N-methylprotoporphyrin, produced
99 As a test, we examined the effects of three competitive inhibitors (nimesulide, flurbiprofen, and di
103 GTP binding and the first demonstration of a competitive inhibitor of a receptor guanylyl cyclase.
104 ions in the heart, attributed to its being a competitive inhibitor of ACE, leading to decreased AngII
106 from 'Oncometabolite 2-hydroxyglutarate is a competitive inhibitor of alpha-ketoglutarate-dependent d
111 Compound 17k is a potent and selective ATP-competitive inhibitor of Aurora B and C with K(i)* value
112 ent, selective and cell active acetyl-lysine competitive inhibitor of BAZ2A and BAZ2B bromodomains as
117 factor ATF4 and that this complex acted as a competitive inhibitor of cAMP response element-binding (
118 sphonate derivative of l-lysine was a potent competitive inhibitor of Cc2672 with a K(i) value of 120
119 pound was shown to be a highly specific, ATP-competitive inhibitor of CDK9/CycT1 with antiviral activ
120 ro kinetic studies revealed that FTY720 is a competitive inhibitor of ceramide synthase 2 toward dihy
122 s a potent and selective DAT inhibitor and a competitive inhibitor of cocaine binding to the DAT.
123 adenosine diphosphate ribose (8Br-cADPr), a competitive inhibitor of cyclic ADP-ribose (cADPr) signa
124 9, CYP2D6, CYP2E1 and CYP3A4, but also a non-competitive inhibitor of CYP1A2, with Ki values no more
125 y, the effects of tetrahydrouridine (THU), a competitive inhibitor of cytidine deaminase, on the phar
126 erization showed that this compound is a non-competitive inhibitor of cytochrome c When tested in cel
127 ocholesterol is a bioactive sterol, a potent competitive inhibitor of cytochrome P450 7A1, and toxic
128 on, we demonstrated that Phe-Ade is a strong competitive inhibitor of CYTOKININ OXIDASE/DEHYDROGENASE
131 rious cellular stresses converts eIF2 into a competitive inhibitor of eIF2B, which triggers the integ
132 have previously reported a low nanomolar ATP-competitive inhibitor of EphB4 discovered in silico by f
133 sed if synthetic STR5 could serve as a novel competitive inhibitor of ERalpha and AR signaling by dis
134 m, where extracellular Na(+) should act as a competitive inhibitor of extracellular K(+) binding, whi
135 4 pockets, respectively, proved to be potent competitive inhibitor of factor Xa (fXa, Ki = 0.090 nM)
136 Finally, we demonstrate using Zn2+, a potent competitive inhibitor of Fe2+ binding and oxidation, tha
140 % from d-lyxonolactone, is a potent specific competitive inhibitor of gut disaccharidases [K(i) 0.081
141 demonstrate that one of these fragments is a competitive inhibitor of HIV-1 RT with respect to deoxyr
142 s and in planta application of lovastatin, a competitive inhibitor of HMG1, we show that defects in H
143 nd characterized from Escherichia coli, is a competitive inhibitor of human ADAM9 catalytic/disintegr
147 concept, we applied this approach to an ATP-competitive inhibitor of kinesin-5, a widely conserved m
148 rmine inhibition constants (K(i)) for a weak competitive inhibitor of Klenow fragment and two strong
150 aracterized the binding site of phosphate, a competitive inhibitor of LMW-PTPs, on MptpA and elucidat
151 ition to Hsp90 modulation, gedunin acts as a competitive inhibitor of LPS, blocking the formation of
154 dly reduced in the presence of gentamicin, a competitive inhibitor of megalin-dependent endocytosis.
155 The compound behaves as a selective and competitive inhibitor of mouse and human MAGL, which pot
156 s and was markedly inhibited by dicumarol, a competitive inhibitor of naphthoquinone oxidoreductases.
157 he thyroid (distinguished using ClO(4)(-), a competitive inhibitor of NIS), indicating that KCNQ1-KCN
160 showed that HG-829 is not a Pgp substrate or competitive inhibitor of Pgp-mediated drug efflux but ra
162 ntified a potent, selective, reversible, ATP-competitive inhibitor of Plk1, GSK461364A, capable of in
164 ed 2-aminoacetophenone as a pathway-inherent competitive inhibitor of PqsBC, whose fluorescence prope
166 l 2-methyl-2-hydroxypropyl-CoM (M-HPC) was a competitive inhibitor of R-HPCDH-catalyzed R-HPC oxidati
168 P) substrate, whereas a second compound is a competitive inhibitor of RT polymerase activity with res
169 and autophagy impairments induced by the non-competitive inhibitor of sarco/ER Ca(2+)-ATPase, thapsig
172 otent, selective, and cell-active, substrate-competitive inhibitor of SMYD2, which is the first repor
174 f 3MG uptake with Ki(app) = 0.3 mum but is a competitive inhibitor of sugar exit indicating that WZB1
175 ggest that the C terminus of SPI-1 acts as a competitive inhibitor of target proteases as it remains
176 nation, we found that chenodeoxycholate is a competitive inhibitor of taurocholate-mediated germinati
180 f double-stranded DNA and a highly effective competitive inhibitor of the bacterial type I restrictio
181 o the BH4 domain of Bcl-2 and functions as a competitive inhibitor of the Bcl-2-IP(3)R interaction.
182 erwent apoptosis after treatment with an ATP-competitive inhibitor of the BCR-associated spleen tyros
183 Our study revealed that this compound is a competitive inhibitor of the binding of ATP and inhibits
185 at beta-aminoproprionitrile, an irreversible competitive inhibitor of the enzymatic activity of all l
189 as enhanced in cells treated with lactose, a competitive inhibitor of the galectin lattice, suggestin
190 e and following treatment with brodalumab, a competitive inhibitor of the IL-17 Receptor A subunit.
191 ommodating pyridine-2,6-dicarboxylic acid, a competitive inhibitor of the native enzyme, suggesting t
193 Atovaquone, a 2-hydroxynaphthoquinone, is a competitive inhibitor of the quinol oxidation (Q(o)) sit
196 that UDP-(5F)-GlcNAc acts as a slow-binding, competitive inhibitor of the retaining glycosyltransfera
197 e kinetic studies showed that Crescent was a competitive inhibitor of Tolloid activity, which bound t
204 nalog Ubc5BC85S-ubiquitin oxyester acts as a competitive inhibitor of wild-type Ubc5B approximately (
205 and Burk analysis showed that Trp was a non-competitive inhibitor of XO and a competitive inhibitor
207 administration of "classical" antiandrogens, competitive inhibitors of androgen receptor (AR) ligands
211 , reveals that bile salts act as partial non-competitive inhibitors of ATX, thereby attenuating LPA r
213 OPP, 4-SPP/SPP, and 5-SPP/SPP were excellent competitive inhibitors of avian farnesyl diphosphate syn
214 The final compounds behave as selective competitive inhibitors of beta-glucosidase and are promi
215 e discovered, as well as the first substrate-competitive inhibitors of c-Src with activity in both bi
216 trast, a subset of steroid hormones acted as competitive inhibitors of C. difficile spore germination
217 GNF-2 (1) and GNF-5 (2) as selective non-ATP competitive inhibitors of cellular Bcr-Abl kinase activi
218 l molecules and identified 13 small molecule competitive inhibitors of ctRAGE interaction with DIAPH1
221 lly identified miRNA targets may actually be competitive inhibitors of miRNA function, preventing miR
224 de phosphonates (ANPs) have been shown to be competitive inhibitors of MtHGPRT with Ki values as low
225 dy was to investigate adenosine triphosphate-competitive inhibitors of mTOR kinase previously unrepor
227 ngs should allow for the rationale design of competitive inhibitors of mycolactone binding to N-WASP,
228 e more potent than any previously documented competitive inhibitors of NQO2 and represent the first m
231 onic acid (6a), were recognized as nanomolar competitive inhibitors of PNP isolated from cell lines w
233 Nalpha-bis(carboxymethyl)-L-lysine (BCML) as competitive inhibitors of quinine-activated T2R4 with an
234 cked signaling activity while functioning as competitive inhibitors of RIG-I binding and IFN-beta exp
235 difications that convert activator RNAs into competitive inhibitors of RIG-I signaling may be useful
236 cluding benzoquinone and phenylquinone, were competitive inhibitors of sepiapterin reduction but nonc
237 amidine-based sphingosine analogues that are competitive inhibitors of sphingosine kinases exhibiting
239 be broadly grouped into four categories: (1) competitive inhibitors of the accessory gene regulator (
242 with TdT, explaining why these compounds are competitive inhibitors of the deoxynucleotide triphospha
243 phenols to generate potent and selective ATP-competitive inhibitors of the DNA damage response signal
246 hat combine the activities of allosteric and competitive inhibitors of the type-I insulin-like growth
247 Is), gefitinib and erlotinib, are reversible competitive inhibitors of the tyrosine kinase domain of
249 starting point for a new class of substrate-competitive inhibitors of TNKS with potential for suppre
252 eretin and (2S)-naringenin were validated as competitive inhibitors of UGM against NADPH with Ki valu
254 the functional domain of BAI1 was used as a competitive inhibitor or BAI1 expression was inhibited b
256 and mTORC1 were completely inhibited by ATP competitive inhibitors PI103 and BEZ235 and partially in
257 mpetitive inhibitor Go6976 and the substrate-competitive inhibitor PKC 20-28, but not the activation-
263 binary complexes with ADP and K252a, an ATP-competitive inhibitor (see Table 1), at 1.9 and 2.7 A re
264 ol-open model could identify a pseudopeptide competitive inhibitor showing >100-fold higher affinity
266 .7 cell lines expressing an inducible miR-29 competitive inhibitor (sponge construct), miR-29 knockdo
267 n together, our data lead us to suggest that competitive inhibitors stabilize hSERT in a state that i
268 depends on autophosphorylation, and that ATP-competitive inhibitors staurosporin and sunitinib, which
269 brief overview of results obtained with ATP-competitive inhibitors such as palbociclib and dinacicli
271 f various psychoactive substances, including competitive inhibitors, such as tricyclic antidepressant
274 We demonstrate activin A functions as a competitive inhibitor that blocks the ligand binding epi
275 erization of Torin2, a second-generation ATP-competitive inhibitor that is potent and selective for m
276 distal carboxy tail that resembles an enzyme competitive inhibitor that retunes channel affinity for
277 h N(G)-nitro-L-arginine, a slowly reversible competitive inhibitor that stabilizes nNOS, decreases bo
278 e drug discovery has been the finding of ATP-competitive inhibitors that behave as agonists, rather t
280 Ire1alpha as a target for development of ATP-competitive inhibitors that will modulate the UPR in hum
281 single agents, but when combined with an ATP-competitive inhibitor, they completely suppress the acti
282 that interacts with the ITK SH3 domain as a competitive inhibitor to disrupt the association between
286 showing that d-2-HGA, but not l-2-HGA, is a competitive inhibitor vs 4PE and a noncompetitive inhibi
287 the receptors TLR2, TLR4, RAGE, and P2Y1 as competitive inhibitors, we demonstrate that polyP amplif
288 irus-expressed short hairpin RNA (shRNA) and competitive inhibitors, we show that Ad-induced IL-1beta
290 rent K(i) values of a small set of LRRK2 ATP-competitive inhibitors were within 5-fold between Mg(2+)
291 studies, we propose that these compounds are competitive inhibitors, which mimics the oligonucleotide
292 avathrin." Avathrin is a fast, tight binding competitive inhibitor with an affinity of 545 pM for thr
293 mGluR1 and mGluR2, combining the same mGluR1 competitive inhibitor with an mGluR1 or mGluR2 NAM yield
296 s been conducted showing that triclosan is a competitive inhibitor with respect to NADH and an uncomp
298 -ethoxy-5,6-dibromosalicylaldehyde, is a non-competitive inhibitor with respect to the XBP-1 RNA subs
299 at interact with ClpA N-domains and is a non-competitive inhibitor with substrates that depend on int
300 TP binding pocket making it sensitive to ATP-competitive inhibitors with bulky substituents that comp
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