ライフサイエンスコーパス: competitive inhibitor

1 A non-hydrolyzable ATP analog was a competitive inhibitor.

2 BoNT protein as a landscape for assembling a competitive inhibitor.

3 ors against ACE, whereas PSSNK acts as a non-competitive inhibitor.

4 , given its status as a TBK1 substrate, as a competitive inhibitor.

5 Galactose was found to be the competitive inhibitor.

6 k incorporation and rather behaved as a dNTP-competitive inhibitor.

7 CHK1 selective adenosine triphosphate (ATP) competitive inhibitor.

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

9 nd Tideglusib) that bind GSK3beta as non-ATP-competitive inhibitors.

10 ATP and therefore leads to resistance to ATP competitive inhibitors.

11 hes biochemical potency and synergy with ATP-competitive inhibitors.

12 ifically target TdT and behave as nucleotide-competitive inhibitors.

13 lone or in combination with conventional ATP-competitive inhibitors.

14 y slowly and cannot be disrupted by strictly competitive inhibitors.

15 nct from that observed for kinase domain ATP-competitive inhibitors.

16 the ATP binding pocket by either ATP or ATP-competitive inhibitors.

17 We identified two classes of ATP-competitive inhibitors.

18 2 or Escherichia coli IDI-1 but instead were competitive inhibitors.

19 D-glucopyranoside and reduced sensitivity to competitive inhibitors.

20 AKAP79 also protects PKC from certain ATP-competitive inhibitors.

21 nges in protein expression compared with ATP-competitive inhibitors.

22 r and that 1-thia-Trp and 1-oxa-Trp serve as competitive inhibitors.

23 d screening strategy for Ras interfacial and competitive inhibitors.

24 efficiency, and increased resistance to SDH competitive inhibitors.

25 ructure-based design of dual JCV and BKV ATP-competitive inhibitors.

26 ower concentrations in comparison to the ATP-competitive inhibitors.

27 Hcy), D-Cys, thiosulfate, and azide bound as competitive inhibitors.

28 bition of CRK9(AS) in these cells by the ATP-competitive inhibitor 1-NM-PP1 reproduced the splicing d

29 2N variant in the presence of pyruvate and a competitive inhibitor (2R,3R)-2,3,4-trihydroxy-N,N-dipro

30 An inhibitor screen identified the competitive inhibitor 3-pyridine carboxaldehyde with a K

31 f DHBPS from Vibrio cholerae (vDHBPS) with a competitive inhibitor 4-phospho-d-erythronohydroxamic ac

32 ading to the development of a very promising competitive inhibitor (8r, IC50 = 200 nM, K(i) = 82 nM).

33 cal" Akt hyperphosphorylation induced by ATP-competitive inhibitor, A-443654.

34 ggest that Val-Glu-Leu-Tyr-Pro acts as a non-competitive inhibitor against ACE.

35 ies revealed that this compound behaves as a competitive inhibitor against the peptide substrate and

36 etics and docking studies suggested they are competitive inhibitors against a dimethylated H3K4 subst

37 plots suggested that AHEPVK and RIGLF act as competitive inhibitors against ACE, whereas PSSNK acts a

38 tructural basis for the design of nucleotide-competitive inhibitors against clinically relevant APH e

39 osine-containing tetrapeptides functioned as competitive inhibitors against mushroom tyrosinase by us

40 n exploited in the development of reversible competitive inhibitors against SK from Mycobacterium tub

41 ATP-competitive inhibitors against this complex have been re

42 estigated two IL-1 receptor antagonists, the competitive inhibitor anakinra (Kineret) and a potent no

43 ase-3 the resulting DEVD-T peptide acts as a competitive inhibitor and entraps the active site of cas

44 irst structure of CDK1 bound to a potent ATP-competitive inhibitor and identify aspects of CDK1 struc

45 ts indicates that octyl protocatechuate is a competitive inhibitor and the inhibition constant (Ki) w

46 ase progression in patients treated with ATP-competitive inhibitors and are therefore highly clinical

47 insight into the activation of B-Raf by ATP-competitive inhibitors and can aid in the design of more

48 The development of efficient competitive inhibitors and chaperones to treat diseases

49 Here, we go beyond competitive inhibitors and classic amphetamines and intr

50 late G protein-coupled receptor signaling as competitive inhibitors and protein adaptors.

51 We identified four promising PC1/3 competitive inhibitors and three PC2 inhibitors that exh

52 ne-derived antagonists, the newly identified competitive inhibitors are uncharged at physiological pH

53 r crosslink promotes activity and how select competitive inhibitors bind.

54 nal and computational studies to demonstrate competitive inhibitor binding poses and provide evidence

55 Finally, the substrate-competitive inhibitor bisindolylmaleimide I displaces lo

56 euT, in substrate-bound outward-occluded and competitive inhibitor-bound outward-facing states have a

57 , inward-open state, and competitive and non-competitive inhibitor-bound states, have revealed a mech

58 alytic activity in vitro, unlike typical ATP-competitive inhibitors, but acted in a mechanistically d

59 inhibitor PKC 20-28, but not the activation-competitive inhibitor calphostin C.

60 g site and that combining allosteric and ATP-competitive inhibitors can overcome resistance to either

61 ide derived from beta-neurexin is a powerful competitive inhibitor capable of efficiently blocking su

62 Arl8b and can be blocked by the Rab7 GTPase competitive inhibitor CID1067700.

63 2,6-Dibromophenol is the strongest competitive inhibitor, consistent with PcpA's substrate

64 Inhibition of POX activity by a competitive inhibitor "dehydroproline" decreased ROS lev

65 oscillations are blocked by coinjection of a competitive inhibitor, derived from the WWI domain-bindi

66 activity using small interfering RNA or the competitive inhibitor difluoromethylornithine restored i

67 molecule allosteric inhibitors, but not ATP-competitive inhibitors, disrupts this interaction.

68 Unlike TOP2A poisons, ATP-competitive inhibitors do not damage DNA, potentially li

69 ling was inhibited by the small molecule ATP competitive inhibitors dorsomorphin and LDN-193189.

70 TopoIIalpha N-terminal ATP-competitive inhibitors, exemplified by the marine alkalo

71 ffinity for arginine, and arginine acts as a competitive inhibitor for glutamine transport.

72 Flouride is a competitive inhibitor for lpLSD but an apparent activato

73 ) 11-13 in Notch1, and therefore serves as a competitive inhibitor for Notch ligands to decrease expr

74 ydrolysis of small model substrates, it is a competitive inhibitor for physiologically relevant longe

75 aled that derivative 17b is a mixed-type and competitive inhibitor for TGK and TAO, respectively.

76 ibe an approach to accelerate the search for competitive inhibitors for carbohydrate-recognition doma

77 ies demonstrate that both TCAs and SSRIs are competitive inhibitors for eukaryotic BATs and bind to t

78 provide an alternative to rapidly search for competitive inhibitors for lectins.

79 food protein hydrolysates, are selective and competitive inhibitors for the C-domain with a selectivi

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

82 and pharmacological inhibition by the lipid-competitive inhibitor GW4869.

83 Recently, the targeting of ERK with ATP-competitive inhibitors has emerged as a potential clinic

84 t classes of adenosine 5'-triphosphate (ATP)-competitive inhibitors have been described for CK2alpha,

85 finity (Kd approximately 12-30 nM) selective competitive inhibitors (IC50 approximately 20-150 nM) fo

86 interleukin (IL)-1beta has co-evolved with a competitive inhibitor, IL-1 receptor antagonist (IL-1Ra)

87 ted form of cardiolipin could not serve as a competitive inhibitor in vitro.

88 a in favor of abundant and highly potent ATP-competitive inhibitors in screening libraries.

89 h the kinetic data, the affinity of peptidic competitive inhibitors is diminished at acidic pH.

90 Binding studies disclosed that the competitive inhibitor isoeugenol is predominantly in its

91 itionally, the dissociation constant for the competitive inhibitor isopropyl beta-d-1-thiogalactopyra

92 dates allowed us to disclose the most potent competitive inhibitor known to date (10, K(i) = 4 muM),

93 ystal structure of NDM-1 bound to the potent competitive inhibitor l-captopril, which reveals a uniqu

94 s by feeding leaves with the PEP carboxylase competitive inhibitors malate and diethyl oxalacetate (D

95 1/2, complete inhibition of ERK1/2 using ATP-competitive inhibitors may lead to unwanted off-target e

96 Development of competitive inhibitor molecules such as miRNA sponges ha

97 n be antagonized by ectopically expressing a competitive inhibitor mutant form of HdrR that lacks its

98 genetic action of CLO with that of the DNMT1 competitive inhibitor N-phthalyl-l-tryptophan (RG108).

99 strate binding domain, we identified a novel competitive inhibitor, N-(3,5-dimethylphenyl)-2-[[5-(4-e

100 ibition of ferrochelatase using the specific competitive inhibitor, N-methylprotoporphyrin, produced

101 vitro in the presence and absence of a known competitive inhibitor (NaClO4).

102 Simvastatin (SMV) is a specific competitive inhibitor of 3-hydroxy-2-methyl-glutaryl coe

103 Atorvastatin (ATV) is a specific competitive inhibitor of 3-hydroxy-2-methyl-glutaryl coe

104 GTP binding and the first demonstration of a competitive inhibitor of a receptor guanylyl cyclase.

105 ions in the heart, attributed to its being a competitive inhibitor of ACE, leading to decreased AngII

106 intracellular conversion to CMP-3F-NeuAc, a competitive inhibitor of all sialyltransferases.

107 from 'Oncometabolite 2-hydroxyglutarate is a competitive inhibitor of alpha-ketoglutarate-dependent d

108 Unlike known inhibitors, JIB-04 is not a competitive inhibitor of alpha-ketoglutarate.

109 ing the intracellular levels of succinate (a competitive inhibitor of alphaKG-dependent dioxygenases)

110 Titration of aspartate, a competitive inhibitor of Ans, revealed an increase in N(

111 migration through sequestration of Arpin, a competitive inhibitor of Arp2/3 complex.

112 ogen peroxide and AMP-PNP, an ATP analog and competitive inhibitor of ATPases.

113 Compound 17k is a potent and selective ATP-competitive inhibitor of Aurora B and C with K(i)* value

114 ent, selective and cell active acetyl-lysine competitive inhibitor of BAZ2A and BAZ2B bromodomains as

115 Dasatinib is a novel, potent, ATP-competitive inhibitor of Bcr-Abl, cKIT, and Src family k

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

117 In contrast, compound 3 was a competitive inhibitor of both FS-3 and the phosphodieste

118 AMD3100, a competitive inhibitor of C-X-C motif chemokine receptor-

119 substrate demonstrated that alpha-PanAm is a competitive inhibitor of Cab1.

120 factor ATF4 and that this complex acted as a competitive inhibitor of cAMP response element-binding (

121 pound was shown to be a highly specific, ATP-competitive inhibitor of CDK9/CycT1 with antiviral activ

122 alidated using AZD7762, a small-molecule ATP-competitive inhibitor of CHK1 activation.

123 We present evidence that MDMX is a potent competitive inhibitor of CK1alpha kinase activity (K(i)

124 s a potent and selective DAT inhibitor and a competitive inhibitor of cocaine binding to the DAT.

125 adenosine diphosphate ribose (8Br-cADPr), a competitive inhibitor of cyclic ADP-ribose (cADPr) signa

126 9, CYP2D6, CYP2E1 and CYP3A4, but also a non-competitive inhibitor of CYP1A2, with Ki values no more

127 y, the effects of tetrahydrouridine (THU), a competitive inhibitor of cytidine deaminase, on the phar

128 erization showed that this compound is a non-competitive inhibitor of cytochrome c When tested in cel

129 ocholesterol is a bioactive sterol, a potent competitive inhibitor of cytochrome P450 7A1, and toxic

130 on, we demonstrated that Phe-Ade is a strong competitive inhibitor of CYTOKININ OXIDASE/DEHYDROGENASE

131 A known competitive inhibitor of DES, C(8)-cyclopropenylceramide

132 was a non-competitive inhibitor of XO and a competitive inhibitor of DPP-IV.

133 rious cellular stresses converts eIF2 into a competitive inhibitor of eIF2B, which triggers the integ

134 have previously reported a low nanomolar ATP-competitive inhibitor of EphB4 discovered in silico by f

135 sed if synthetic STR5 could serve as a novel competitive inhibitor of ERalpha and AR signaling by dis

136 m, where extracellular Na(+) should act as a competitive inhibitor of extracellular K(+) binding, whi

137 ite of IXa within Xase, acted as a classical competitive inhibitor of factor X activation.

138 4 pockets, respectively, proved to be potent competitive inhibitor of factor Xa (fXa, Ki = 0.090 nM)

139 a secreted form, sFlt1, that functions as a competitive inhibitor of Flt1.

140 he resulting generation of UMP, a potent and competitive inhibitor of GnT-IX.

141 Hypoxanthine was a competitive inhibitor of guanine rescue, consistent with

142 % from d-lyxonolactone, is a potent specific competitive inhibitor of gut disaccharidases [K(i) 0.081

143 demonstrate that one of these fragments is a competitive inhibitor of HIV-1 RT with respect to deoxyr

144 s and in planta application of lovastatin, a competitive inhibitor of HMG1, we show that defects in H

145 in the presence or absence of simvastatin, a competitive inhibitor of HMGCR.

146 nd characterized from Escherichia coli, is a competitive inhibitor of human ADAM9 catalytic/disintegr

147 ane protein (Omp) 19 from Brucella spp. is a competitive inhibitor of human cathepsin L.

148 This molecule is a competitive inhibitor of K. pneumoniae OHCU decarboxylas

149 concept, we applied this approach to an ATP-competitive inhibitor of kinesin-5, a widely conserved m

150 rmine inhibition constants (K(i)) for a weak competitive inhibitor of Klenow fragment and two strong

151 aracterized the binding site of phosphate, a competitive inhibitor of LMW-PTPs, on MptpA and elucidat

152 ition to Hsp90 modulation, gedunin acts as a competitive inhibitor of LPS, blocking the formation of

153 AZD8055 is an ATP-competitive inhibitor of mammalian target of rapamycin (

154 dly reduced in the presence of gentamicin, a competitive inhibitor of megalin-dependent endocytosis.

155 se of these properties, Ago1x can serve as a competitive inhibitor of miRNA pathway.

156 The compound behaves as a selective and competitive inhibitor of mouse and human MAGL, which pot

157 s and was markedly inhibited by dicumarol, a competitive inhibitor of naphthoquinone oxidoreductases.

158 he thyroid (distinguished using ClO(4)(-), a competitive inhibitor of NIS), indicating that KCNQ1-KCN

159 The competitive inhibitor of NQO1 dicoumarol synergized with

160 ract the ISR at its very core by acting as a competitive inhibitor of p-eIF2-eIF2B interaction.

161 We also designed a competitive inhibitor of PD-L1 palmitoylation that decre

162 GSK2656157 is an ATP-competitive inhibitor of PERK enzyme activity with an IC

163 aminobenzamidine (pAB), acted as a classical competitive inhibitor of PF-3688 cleavage by Xase.

164 showed that HG-829 is not a Pgp substrate or competitive inhibitor of Pgp-mediated drug efflux but ra

165 hat itself bears a Zalpha domain, a putative competitive inhibitor of PKZ.

166 ed 2-aminoacetophenone as a pathway-inherent competitive inhibitor of PqsBC, whose fluorescence prope

167 The most promising competitive inhibitor of PvSUB1 (compound 2) was equally

168 We found triacsin C to be a competitive inhibitor of RPE65 (IC50 = 500 nm).

169 P) substrate, whereas a second compound is a competitive inhibitor of RT polymerase activity with res

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

171 iated IC(5)(0) values produced by glycine, a competitive inhibitor of serine racemase (SR).

172 report the discovery of the first substrate-competitive inhibitor of SETD8, UNC0379 (1).

173 otent, selective, and cell-active, substrate-competitive inhibitor of SMYD2, which is the first repor

174 but denaturation converted BSA into a strong competitive inhibitor of such proteolysis.

175 f 3MG uptake with Ki(app) = 0.3 mum but is a competitive inhibitor of sugar exit indicating that WZB1

176 ggest that the C terminus of SPI-1 acts as a competitive inhibitor of target proteases as it remains

177 nation, we found that chenodeoxycholate is a competitive inhibitor of taurocholate-mediated germinati

178 inobenzohydrazide was determined to be a non-competitive inhibitor of TBR-POD and Turnip-POD.

179 tion showed that it was a moderately potent, competitive inhibitor of the ABCB1-mediated transport of

180 -a thienopyrimidine-was a moderately potent, competitive inhibitor of the ABCC1-mediated transport of

181 o the BH4 domain of Bcl-2 and functions as a competitive inhibitor of the Bcl-2-IP(3)R interaction.

182 at beta-aminoproprionitrile, an irreversible competitive inhibitor of the enzymatic activity of all l

183 One of these molecules acts as a competitive inhibitor of the enzyme and cures mice of th

184 4-Methyltryptophan is a competitive inhibitor of the enzyme that has been used i

185 ehyde and yield tagatose 1,6-bisphosphate, a competitive inhibitor of the enzyme.

186 as enhanced in cells treated with lactose, a competitive inhibitor of the galectin lattice, suggestin

187 e and following treatment with brodalumab, a competitive inhibitor of the IL-17 Receptor A subunit.

188 ommodating pyridine-2,6-dicarboxylic acid, a competitive inhibitor of the native enzyme, suggesting t

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

190 Atovaquone, a 2-hydroxynaphthoquinone, is a competitive inhibitor of the quinol oxidation (Q(o)) sit

191 Methenyl-dH(4)MPT is shown to be a competitive inhibitor of the reduction of methenyl-H(4)F

192 that UDP-(5F)-GlcNAc acts as a slow-binding, competitive inhibitor of the retaining glycosyltransfera

193 e kinetic studies showed that Crescent was a competitive inhibitor of Tolloid activity, which bound t

194 Notably, ibogaine is a non-competitive inhibitor of transport but displays competit

195 We found that 2-phosphoglycolate is a competitive inhibitor of triose phosphate isomerase, an

196 calculated, caftaric acid was shown to be a competitive inhibitor of tyrosinase, more potent than th

197 AKB-9778 is a small-molecule competitive inhibitor of vascular endothelial-protein ty

198 Sunitinib is an orally available, ATP-competitive inhibitor of VEGF and PDGF receptors used cl

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

200 Adamantyl Gb(3) is an amphipathic competitive inhibitor of VT1/VT2 Gb(3) binding.

201 more tightly, suggesting that Nan KLF1 is a competitive inhibitor of wild-type KLF1.

202 nalog Ubc5BC85S-ubiquitin oxyester acts as a competitive inhibitor of wild-type Ubc5B approximately (

203 and Burk analysis showed that Trp was a non-competitive inhibitor of XO and a competitive inhibitor

204 inetic analysis revealed that flavonoids are competitive inhibitors of ACE.

205 administration of "classical" antiandrogens, competitive inhibitors of androgen receptor (AR) ligands

206 on and may guide the rational drug design of competitive inhibitors of Arno enzymatic activity.

207 Competitive inhibitors of ATP binding to Hsp90 prevent c

208 aging chemotherapy is through the use of ATP-competitive inhibitors of ATR or Chk1.

209 , reveals that bile salts act as partial non-competitive inhibitors of ATX, thereby attenuating LPA r

210 Compounds 1 and 2 were competitive inhibitors of ATX-mediated hydrolysis of the

211 OPP, 4-SPP/SPP, and 5-SPP/SPP were excellent competitive inhibitors of avian farnesyl diphosphate syn

212 The final compounds behave as selective competitive inhibitors of beta-glucosidase and are promi

213 e discovered, as well as the first substrate-competitive inhibitors of c-Src with activity in both bi

214 trast, a subset of steroid hormones acted as competitive inhibitors of C. difficile spore germination

215 GNF-2 (1) and GNF-5 (2) as selective non-ATP competitive inhibitors of cellular Bcr-Abl kinase activi

216 l molecules and identified 13 small molecule competitive inhibitors of ctRAGE interaction with DIAPH1

217 -1-carbonyl)cyclohexyl)-3-(p-tolyl)urea) are competitive inhibitors of ERAP1 aminopeptidase activity.

218 etic compounds (CD4mc) bind gp120 and act as competitive inhibitors of gp120-CD4 engagement.

219 based hydroxamic acids to serve as selective competitive inhibitors of histone deacetylase-6 (HDAC6).

220 Competitive inhibitors of IDO are currently being tested

221 Fortunately, non-ATP-competitive inhibitors of MK2 have been already discover

222 We suggest that dimers might be competitive inhibitors of monomer binding to iterons and

223 de phosphonates (ANPs) have been shown to be competitive inhibitors of MtHGPRT with Ki values as low

224 dy was to investigate adenosine triphosphate-competitive inhibitors of mTOR kinase previously unrepor

225 ngs should allow for the rationale design of competitive inhibitors of mycolactone binding to N-WASP,

226 e more potent than any previously documented competitive inhibitors of NQO2 and represent the first m

227 ion in a program to identify pan-isoform ATP-competitive inhibitors of PDHK.

228 Competitive inhibitors of PLB reduced the ability of spe

229 onic acid (6a), were recognized as nanomolar competitive inhibitors of PNP isolated from cell lines w

230 H3 K27M and EZHIP are competitive inhibitors of Polycomb Repressive Complex 2

231 phenylboronic acid (PBA) function as potent competitive inhibitors of PtNHase.

232 Nalpha-bis(carboxymethyl)-L-lysine (BCML) as competitive inhibitors of quinine-activated T2R4 with an

233 jugated linear and cyclic oligophosphates as competitive inhibitors of RNase A.

234 cluding benzoquinone and phenylquinone, were competitive inhibitors of sepiapterin reduction but nonc

235 amidine-based sphingosine analogues that are competitive inhibitors of sphingosine kinases exhibiting

236 We have developed ATP competitive inhibitors of TgCDPK1 that block invasion of

237 be broadly grouped into four categories: (1) competitive inhibitors of the accessory gene regulator (

238 contains the ATPase active site, but are not competitive inhibitors of the ATPase reaction.

239 ATP competitive inhibitors of the BRAF(V600E) oncogene parad

240 with TdT, explaining why these compounds are competitive inhibitors of the deoxynucleotide triphospha

241 phenols to generate potent and selective ATP-competitive inhibitors of the DNA damage response signal

242 hly selective non-metal chelating, substrate-competitive inhibitors of the JmjC KDMs.

243 hat combine the activities of allosteric and competitive inhibitors of the type-I insulin-like growth

244 n and therefore have the potential to act as competitive inhibitors of this interaction.

245 starting point for a new class of substrate-competitive inhibitors of TNKS with potential for suppre

246 Interestingly, non-ATP-competitive inhibitors of TopoIIalpha, etoposide and mer

247 tracellular vestibule of LeuT and act as non-competitive inhibitors of transport.

248 eretin and (2S)-naringenin were validated as competitive inhibitors of UGM against NADPH with Ki valu

249 the functional domain of BAI1 was used as a competitive inhibitor or BAI1 expression was inhibited b

250 ATP-competitive inhibitors OSI-027 and OXA-01 targeted both

251 and mTORC1 were completely inhibited by ATP competitive inhibitors PI103 and BEZ235 and partially in

252 mpetitive inhibitor Go6976 and the substrate-competitive inhibitor PKC 20-28, but not the activation-

253 We show that the ATP-competitive inhibitor PP242, but not rapamycin, signific

254 We found that 2 structurally distinct competitive inhibitors (PP242 and AZD8055), both of whic

255 These competitive inhibitors presumably act as KpnI binding si

256 Glutathione-competitive inhibitors produced dose-dependent thermal s

257 VMAT transport is inhibited by the competitive inhibitor reserpine, a second-line agent to

258 A competitive inhibitor rich in arginine residues reduced

259 ol-open model could identify a pseudopeptide competitive inhibitor showing >100-fold higher affinity

260 While many dications act as purely competitive inhibitors, some fail to displace protein ef

261 .7 cell lines expressing an inducible miR-29 competitive inhibitor (sponge construct), miR-29 knockdo

262 n together, our data lead us to suggest that competitive inhibitors stabilize hSERT in a state that i

263 depends on autophosphorylation, and that ATP-competitive inhibitors staurosporin and sunitinib, which

264 brief overview of results obtained with ATP-competitive inhibitors such as palbociclib and dinacicli

265 f various psychoactive substances, including competitive inhibitors, such as tricyclic antidepressant

266 f LpxA inhibition; compound 1 is a substrate-competitive inhibitor targeting apo LpxA, and compound 2

267 thiadiazolidinone drug, TDZD-8, is a non-ATP-competitive inhibitor targeting GSK3beta with demonstrat

268 We show that IP6 is a non-competitive inhibitor that acts by blocking the stimulat

269 CB-5083 functions as a competitive inhibitor that binds selectively to the ATP-

270 Lysine is a competitive inhibitor that binds to the active site of T

271 We demonstrate activin A functions as a competitive inhibitor that blocks the ligand binding epi

272 erization of Torin2, a second-generation ATP-competitive inhibitor that is potent and selective for m

273 ent quenching can be realized by designing a competitive inhibitor that is structurally very similar

274 distal carboxy tail that resembles an enzyme competitive inhibitor that retunes channel affinity for

275 11s is an ATP-competitive inhibitor that showed remarkable selectivity

276 h N(G)-nitro-L-arginine, a slowly reversible competitive inhibitor that stabilizes nNOS, decreases bo

277 e drug discovery has been the finding of ATP-competitive inhibitors that behave as agonists, rather t

278 n vivo pharmacokinetic analysis of TOP2A ATP-competitive inhibitors that prevent TCF-transcription an

279 inally, we describe the first antibody-based competitive inhibitors that target both the zymogen and

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

283 ory concentration of 0.89 +/- 0.10 muM) is a competitive inhibitor to the peptide substrate and nonco

284 Binding of a competitive inhibitor to the transporter leads to reduct

285 We apply these tools as competitive inhibitors to dissect the polyubiquitin-link

286 eactions, where inactivated proteases become competitive inhibitors to remaining, active proteases, o

287 rted CpIMPDH inhibitors, these compounds are competitive inhibitors versus NAD(+).

288 showing that d-2-HGA, but not l-2-HGA, is a competitive inhibitor vs 4PE and a noncompetitive inhibi

289 the receptors TLR2, TLR4, RAGE, and P2Y1 as competitive inhibitors, we demonstrate that polyP amplif

290 similarity of these inhibitors to known ATP-competitive inhibitors, we have investigated them furthe

291 Interestingly, ATP-/substrate-competitive inhibitors were found to be highly selective

292 rent K(i) values of a small set of LRRK2 ATP-competitive inhibitors were within 5-fold between Mg(2+)

293 lucosidic ellagitannin roburin D (RobD) is a competitive inhibitor, whereas alpha-pentagalloylglucose

294 avathrin." Avathrin is a fast, tight binding competitive inhibitor with an affinity of 545 pM for thr

295 mGluR1 and mGluR2, combining the same mGluR1 competitive inhibitor with an mGluR1 or mGluR2 NAM yield

296 We identified (-)-fenchone as a competitive inhibitor with different potencies at the tw

297 s been conducted showing that triclosan is a competitive inhibitor with respect to NADH and an uncomp

298 NADP(+) is a competitive inhibitor with respect to NADPH, demonstrati

299 -ethoxy-5,6-dibromosalicylaldehyde, is a non-competitive inhibitor with respect to the XBP-1 RNA subs

300 TP binding pocket making it sensitive to ATP-competitive inhibitors with bulky substituents that comp