ライフサイエンスコーパス: constitutive activity

1 a strikingly high, physiologically relevant, constitutive activity.

2 to identify the domain on Nox4 that confers constitutive activity.

3 the cell from plasma membrane expression of constitutive activity.

4 molecular mechanisms of GPCR activation and constitutive activity.

5 ariants of Staphylococcus aureus AgrC-I with constitutive activity.

6 This phenomenon is referred to as basal or constitutive activity.

7 type, while Nox2-based chimeras never gained constitutive activity.

8 eptor and may be mistaken for high levels of constitutive activity.

9 resistance of the hFSHR to mutation-induced constitutive activity.

10 Adr1 mutant that by itself confers only weak constitutive activity.

11 -type receptor, properties characteristic of constitutive activity.

12 chimera were also observed, consistent with constitutive activity.

13 utant CB(1) receptor T210I, with established constitutive activity.

14 ation generally leads to loss of function or constitutive activity.

15 s that GluR1Lc channels exhibit little or no constitutive activity.

16 ng that multimerization is essential for the constitutive activity.

17 e previously proposed "hallmark criteria" of constitutive activity.

18 ght be one of the mechanisms underlying GPCR constitutive activity.

19 ting this cysteine-containing motif leads to constitutive activity.

20 acidic amino acid, aspartic acid, stimulates constitutive activity.

21 y desensitized, which partially masked their constitutive activity.

22 aused by the high level of 5-HT(2A) receptor constitutive activity.

23 TRPM5 does not display constitutive activity.

24 hagocytic NADPH oxidases have very low-level constitutive activity.

25 active, edited forms show lesser degrees of constitutive activity.

26 were found: moderate, high, and "locked-on" constitutive activity.

27 y active, whereas B2R exhibits little if any constitutive activity.

28 o acid substitutions at Leu-394 also display constitutive activity.

29 iptional start site, involving repression of constitutive activity.

30 341D/T491E/S494D (DDED), in C-Raf results in constitutive activity.

31 e counterparts, exhibited ligand-independent constitutive activity.

32 exhibits a high level of ligand-independent, constitutive activity.

33 loop sites in B-Raf are sufficient to confer constitutive activity.

34 element is the most critical element for the constitutive activity.

35 receptor activity in intact cells, revealing constitutive activity.

36 ptor escapes the Hsp90 pathway, resulting in constitutive activity.

37 e R domain to the C terminus did not prevent constitutive activity.

38 pioids, but rather to its ligand-independent constitutive activity.

39 on model incorporating negative feedback and constitutive activity.

40 but also occur in their absence, leading to constitutive activity.

41 ing properties, which are linked to its high constitutive activity.

42 and that disease-associated mutations cause constitutive activity.

43 ted by substance P, but it lacks any sign of constitutive activity.

44 ntrol of receptor functional selectivity and constitutive activity.

45 effects at the MOR, suggesting enhanced MOR constitutive activity.

46 the 6.34D or 6.34K mutants display enhanced constitutive activities.

47 nd that Smo, by virtue of what appears to be constitutive activity, activates all members of the G(i)

48 y held view, CK2 can exist in a state of low constitutive activity allowing for its regulation by ino

49 e of phenotypes, including hypersensitivity, constitutive activity, altered ligand binding, and loss

50 a ligand-activated transcription factor with constitutive activities and those induced by xenobiotic

51 re, the R156 receptor variant showed greater constitutive activity and a higher affinity for ligand.

52 monstrated that these mutants confer ERalpha constitutive activity and antiestrogen resistance and su

53 Asn and p.Asp538Gly) were shown to result in constitutive activity and continued responsiveness to an

54 L6.30(275)E/T6.34(279)D mutants displayed no constitutive activity and could not be activated by the

55 FR yields evidence for a unique mechanism of constitutive activity and dual kinase domain activation.

56 gain of function characterized by increased constitutive activity and elevated channel activation by

57 ast, lack of Cdk phosphorylation resulted in constitutive activity and elevated crossover-associated

58 the CB1 cannabinoid receptor is crucial for constitutive activity and G-protein sequestration.

59 resulted in the induction (or repression) of constitutive activity and in most cases also yielded cor

60 hibitor binding and four variants conferring constitutive activity and inhibitor resistance, illumina

61 A G90D point mutation in rhodopsin causes constitutive activity and leads to congenital stationary

62 ctive conformation of MEK1, resulting in its constitutive activity and making it more prone to Raf-me

63 The CDK9 promoter possesses high constitutive activity and may therefore have utility in

64 The highest level of constitutive activity and nearly complete loss of epider

65 maintain mechanosensitivity but have greater constitutive activity and no change in unitary conductan

66 inking core in between where mutations cause constitutive activity and other defects.

67 2 or FFA3 agonist binding pocket to regulate constitutive activity and SCFA potency.

68 mbrane by either of two different means, has constitutive activity and shows modified ligand specific

69 ENaCs exhibit constitutive activity and strict Na(+) selectivity.

70 the CB1 receptor (CB1-417) enhanced both the constitutive activity and the ability of the receptor to

71 s the two SD mutant sites resulted in strong constitutive activity and the complete lack of Ca(2+)-Ca

72 dited and encodes receptors with the highest constitutive activity and the highest agonist affinity a

73 is or a consequence of preventing endogenous constitutive activity and/or internalization.

74 localized in the endoplasmic reticulum, has constitutive activity, and generates hydrogen peroxide (

75 physiological occurrence and function of MOR constitutive activity, and have important implications f

76 nism, allosteric modulation, signaling bias, constitutive activity, and inverse agonism.

77 Homology (PH) domain also inhibits receptor constitutive activity, and PH domain expression rescues

78 es are basally inactive; previous reports of constitutive activity are artifacts of in vitro manipula

79 onist-dependent mutant, we further establish constitutive activity as a requirement for vGPCR sarcoma

80 emonstrate that certain hallmark features of constitutive activity as originally established with cla

81 ric P2Y(12) mutant exhibited a high level of constitutive activity, as evidenced by decreased cAMP le

82 (1) receptors displayed a ligand-independent constitutive activity, assessed through inositol phospha

83 bstitutions displayed gain-of-function (GOF) constitutive activities at both the plasma membrane (PM)

84 vates a sustained alkaline mode leading to a constitutive activity at resting pH.

85 The possibility that constitutive activity at the CB(1) receptor is required

86 These data suggest that constitutive activity at the CB(1) receptor maintains th

87 Constitutive activity because of deletion of this region

88 ion of hyperalgesia by MORs was due to their constitutive activity because of the following: (1) CFA-

89 provide evidence that the differences in Lck constitutive activity between CD8(+) TCM and TEM are due

90 alpha-GFP fusion proteins were found to have constitutive activity both in vivo and in vitro.

91 ue properties of human CAR, such as its high constitutive activity, both direct (ligand-binding domai

92 Several of these mutations result in MEK1 constitutive activity, but how they affect MEK1 regulati

93 or 3, from LH receptors showed decreases in constitutive activity, but ligand treatment stimulated c

94 The L6.30(275)E/T6.34(279)K mutant had some constitutive activity, but much less than the T6.34(279)

95 CAR inactivates its constitutive activity by phosphorylation at threonine 38

96 Insights into the molecular basis of CAR constitutive activity can be exploited in the design of

97 rse agonist lead, was used to show that SF-1 constitutive activity can be pharmacologically modulated

98 at confer decreased sensitivity to agonists, constitutive activity, decreased activation kinetics, or

99 We tested whether inhibiting D5R constitutive activity depresses burst firing and allevia

100 ERbeta1 and ERbeta2delta3 displayed constitutive activity (ERbeta1 more than ERbeta2delta3).

101 he intracellular module together suffice for constitutive activity even at low densities, the intrace

102 This hypothesis predicts constitutive activity for CCTalpha[Delta257-309]; howeve

103 that enables inter-domain communication and constitutive activity from the N-terminal coactivator-bi

104 stems, but in the P2Y receptors, to date, no constitutive activity has been reported.

105 and an unphosphorylated R domain may prevent constitutive activity, i.e. opening with ATP alone.

106 he MKK7-JNK fusion proteins, which exhibited constitutive activity in 293T cells, were stably express

107 Strikingly, the IFN-gamma promoter exhibited constitutive activity in both Th1 and Th2 subsets, in co

108 ctivity in classical receptors also mediated constitutive activity in CAR.

109 Bruton's tyrosine kinase (BTK) shows constitutive activity in CLL and is the target of irreve

110 cancer (NSCLC) cell lines exhibited elevated constitutive activity in CREB, in its immediate upstream

111 ter and functions as a positive regulator of constitutive activity in fibroblasts.

112 struct, termed fully activated (FA) Rsk, had constitutive activity in G(2) phase, with a specific act

113 has been proposed that mutations that induce constitutive activity in G-protein-coupled receptors (GP

114 We found that the Il-33 promoter exhibits constitutive activity in mouse lymphoid organs, epitheli

115 h the 5-HT6 receptor fail to rescue receptor constitutive activity in neurofibromin-depleted cells.

116 n inhibit several AR splice variants showing constitutive activity in PCa cells.

117 oter lacks a TATA element and possesses high constitutive activity in plasmid transfection assays.

118 , three of which (Hck, Src, and Fyn) exhibit constitutive activity in self-renewing ES cells.

119 RKs, ERK7 has been shown to have significant constitutive activity in serum-starved cells, which is n

120 tion of both TM2 and TM7 but does not induce constitutive activity in suppressing the C296A mutant ef

121 cellular receptors in that it maintains high constitutive activity in the absence of agonist.

122 The K281P receptors displayed constitutive activity in the absence of glycine, and unl

123 increased rates of nucleotide exchange, and constitutive activity in the absence of receptor activat

124 Drosophila mutant allele (F550I) that causes constitutive activity in the canonical TRP channel, resu

125 The physiological role of this constitutive activity in the control of energy balance a

126 ted protein kinase (MAPK) pathway as well as constitutive activity in the phosphoinositide 3-kinase (

127 s, human FFA2 and mouse FFA3, displayed high constitutive activity in this assay, whereas the ortholo

128 e serine converted to glutamic acid displays constitutive activity in vivo; expression of an estrogen

129 onstitutively active receptor suppressed the constitutive activity; in contrast, the N205K/Y266D/P258

130 inding sites, most ProD2 mutations decreased constitutive activity (increased DeltaG0).

131 In the absence of constitutive activity, inverse agonists behave as simple

132 nalysis of additional mutations suggest that constitutive activity is caused by allosteric oligomeriz

133 current study, we present evidence that MOR constitutive activity is highly relevant in the mouse VT

134 This constitutive activity is independent of the intracellula

135 rently constitutive transactivator, and this constitutive activity is inhibited by androstanes acting

136 bl, which is a protein tyrosine kinase whose constitutive activity is responsible for chronic myeloge

137 The measured constitutive activity is similar in its extent to that o

138 Constitutive activity is strongly reduced by silencing e

139 teristics of the H3R, namely, its structure, constitutive activity, isoforms, signal transduction pat

140 okine receptor 1 (CCR1) exhibits significant constitutive activity leading to a variety of cellular r

141 The constitutive activity leads to basal phosphorylation of

142 ith betaarrestin2, which correlated with the constitutive activity level of each isoform.

143 D5 receptors (D5Rs), characterized by a high constitutive activity, may contribute to the emergence o

144 ly to block alpha-MSH binding and blocks the constitutive activity mediated by the ligand-mimetic ami

145 sue injury produced mu-opioid receptor (MOR) constitutive activity (MOR(CA)) that repressed spinal no

146 d pocket-filling mutations did not alter the constitutive activity observed.

147 This activity was 2-fold higher than the constitutive activity obtained with the Simian Virus 40

148 A dramatic loss of constitutive activity occurred when the fourth intracell

149 7.49) also seem to be necessary for the high constitutive activities of D556(6.44)H and D556(6.44)Q a

150 ed outward receptor currents by reducing the constitutive activities of odorant receptors, inhibiting

151 nd was not the result of the reversal of the constitutive activities of the mutant receptors.

152 Furthermore, this abrogated constitutive activity of 5-HT2B/C receptors and abolishe

153 e further suggests a molecular basis for the constitutive activity of 6.40 substitutions and the stro

154 ucidated the effects of ABA plus knockout or constitutive activity of 79 nodes on both the outcome of

155 ons that disrupt some of these fingers cause constitutive activity of a bifunctional Gal4 DNA-binding

156 in magnitude and direction depending on the constitutive activity of a receptor.

157 en-dependent AR transcriptional activity and constitutive activity of a splice variant-like AR.

158 lytic site of calpain reduce the increase in constitutive activity of AKT1 and survival of trastuzuma

159 The ligand-independent, constitutive activity of B1R therefore depends on epitop

160 ative resting membrane potential through the constitutive activity of background K+ channels.

161 Constitutive activity of Bcr-abl fusion protein kinase c

162 their CD95 apoptosis sensitivity, depend on constitutive activity of CD95, stimulated by cancer-prod

163 Yet given the constitutive activity of CK1 alpha, it remained unclear

164 r macrophages, we observed a requirement for constitutive activity of ERK MAPK and the PI3K downstrea

165 This inverse agonist inhibits the constitutive activity of ERRalpha in both biochemical an

166 ptor alpha (ERalpha)) is responsible for the constitutive activity of ERRalpha-1.

167 Recent studies have implicated the constitutive activity of estrogen receptor (ER) beta as

168 of mutant, but not wild-type, MEK1 leads to constitutive activity of extracellular signal-regulated

169 Surprisingly, however, we find that the constitutive activity of Fab-7 is generated by combining

170 Instead, constitutive activity of FGFR maintains a basal level of

171 Such constitutive activity of G90D rhodopsin in vivo would de

172 411S loss-of-function mutations abrogate the constitutive activity of gain-of-function Ste5 alleles,

173 he development of metabolic systems; (b) the constitutive activity of GHSR; and (c) gender difference

174 The high apparent constitutive activity of GPR40-Galpha(q) was also revers

175 d transfection assays, PK11195 inhibited the constitutive activity of hCAR more than 80% at the conce

176 We found that constitutive activity of Hif-1alpha resulted in diminish

177 ion of F508-CFTR are partially suppressed by constitutive activity of Hsc70 and Hsp90 chaperone/co-ch

178 y of the malignant cells and is sustained by constitutive activity of IkappaB kinase (IKK) in the cyt

179 on factor, a phenomenon often resulting from constitutive activity of IkappaB kinase beta (IKKbeta).

180 tribute to the augmented phosphorylation and constitutive activity of its substrate bcr/abl and provi

181 approach to eliminate arrestin unmasked the constitutive activity of K296E and caused photoreceptor

182 We also provide evidence that constitutive activity of kappaORs governs the prolonged

183 red intramolecular ligand that maintains the constitutive activity of MC4R and may provide novel aven

184 hat the tonic satiety signal provided by the constitutive activity of MC4R may be required for mainta

185 thers suggest that endogenous opioids and/or constitutive activity of MORs participate in maintaining

186 Progesterone and testosterone repress the constitutive activity of mouse CAR (mCAR) in cell-mediat

187 3-associated phenotypes, indicating that the constitutive activity of MPK3 can bypass SA and ethylene

188 d exposure to morphine would produce greater constitutive activity of mu-opioid receptors than exposu

189 va are severalfold more potent in inhibiting constitutive activity of mutant EGFR isoforms compared w

190 Significantly, the constitutive activity of NF-kappaB has been implicated a

191 The constitutive activity of oncogenic STAT3C was reported t

192 Under isotonic conditions, there was constitutive activity of p38 MAP kinase that was selecti

193 ty of CD103(+) DCs, such DC subset contained constitutive activity of p38alpha and abundant expressio

194 These in situ studies identify constitutive activity of PP1 and the counteracting activ

195 IL-10 activation of STAT1 was suppressed by constitutive activity of protein kinase C and Src homolo

196 LMP-1 represses the constitutive activity of Qp reporter constructs.

197 To determine the role of the constitutive activity of RelA in tumorigenesis, we gener

198 Here we show that scrambling is a constitutive activity of rhodopsin, distinct from its li

199 Given that hypoxia-induced constitutive activity of some mammalian TRPs leads to ne

200 Constitutive activity of STAT5 or protection from apopto

201 re, these AR variant proteins maintained the constitutive activity of the AR transcriptional program

202 In the pathophysiology of CML, the constitutive activity of the Bcr-Abl tyrosine kinase (TK

203 The constitutive activity of the Bcr-Abl tyrosine kinase pla

204 colorectal cancers, and its loss results in constitutive activity of the beta-catenin-Tcf4 transcrip

205 his position, in particular, could result in constitutive activity of the channel.

206 ysplasias, probably because of the increased constitutive activity of the channel.

207 that is highly correlated with the extent of constitutive activity of the different mutants.

208 that may harbor PTCH1 mutations, leading to constitutive activity of the embryonic Hedgehog (Hh) sig

209 eta receptor tyrosine kinase by blocking the constitutive activity of the G-protein coupled receptor.

210 is is the first direct evidence for the high constitutive activity of the ghrelin receptor being an i

211 It is concluded that the high constitutive activity of the ghrelin receptor is depende

212 nist, in a direct relationship with the high constitutive activity of the ghrelin receptor.

213 5-HT2cR decreased in parallel with increased constitutive activity of the isoforms.

214 Constitutive activity of the isolated Smad-binding regio

215 r suggest that the structural trigger of the constitutive activity of the L457R mutant may also be re

216 ity of MC4R PVN neurons is controlled by the constitutive activity of the MC4R and that expression of

217 These observations confirm constitutive activity of the mda-7 promoter in HO-1 cell

218 iption factors, raising the possibility that constitutive activity of the NF-kappaB pathway may contr

219 AEG-1 knockdown also attenuated the constitutive activity of the nuclear factor kappaB (NF-k

220 for GTPases in PAK1 activation, whereas the constitutive activity of the PAK1 mutant (PAK1(H83,86L))

221 R2) to the NINAE(pp100) mutant opsin and the constitutive activity of the phototransduction cascade.

222 The high constitutive activity of the pleckstrin homology (PH) do

223 Constitutive activity of the putative HAS2-AS1 promoter

224 erexpressed systems, nor does it explain the constitutive activity of the R92Q mutant associated with

225 PI3K via LY294002 or p85alpha knockdown, or constitutive activity of the Rab5 pathway, enhanced the

226 Keratinocytes exhibit high constitutive activity of the Ras-ERK signaling cascade e

227 GPCR phosphorylation cannot be explained by constitutive activity of the receptor or membrane associ

228 Moreover, the constitutive activity of the receptor was inhibited by Z

229 tion in vitro revealed that it leads to high constitutive activity of the receptor, compatible with s

230 rminal mutations that selectively impair the constitutive activity of the receptor.

231 level of GTP-bound RhoA, suggesting that the constitutive activity of the Rho-Rho kinase pathway may

232 Constitutive activity of the serine/threonine kinase Akt

233 Constitutive activity of the serotonin receptors 5-HT2B/

234 Activating mutations in Smo that lead to constitutive activity of the Shh pathway have been ident

235 nce of AD in females could be due to greater constitutive activity of the synaptic Zn transporter ZnT

236 uppressed the retinal degeneration caused by constitutive activity of the TRP channel.

237 This constitutive activity of the truncated BAI1 mutant also

238 e (R*) state although there is no detectable constitutive activity of the WT receptor in the absence

239 Constitutive activity of these alleles was dependent on

240 The constitutive activity of these mutants is not dependent

241 le is known about the molecular basis of the constitutive activity of these receptors.

242 Constitutive activity of this cyclase contributes to bas

243 mutations of NF-kappaB regulators that cause constitutive activity of this oncogenic pathway have bee

244 Constitutive activity of TLR4 in the intestinal epitheli

245 recent studies have suggested that low-level constitutive activity of TRPV3 induces EGFR-dependent si

246 This gating mechanism, which defines the constitutive activity of TRPV6, is, to our knowledge, un

247 strated that the human MC4R has an intrinsic constitutive activity on which AGRP also acts as an inve

248 an be changed either by mutation to increase constitutive activity or by the addition of a second ago

249 ce has been reported, suggesting either weak constitutive activity or nonconventional THPO-dependent

250 ssion of mutated PIEZO2 cDNAs does not cause constitutive activity or toxicity to cells, indicating t

251 s cause receptor mislocalization, diminished/constitutive activity, or faulty protein-protein interac

252 e on transfection, whereas maximal levels of constitutive activity ranging from 30 to 45% were observ

253 also show that ligand-mediated repression of constitutive activity reflects both a displacement of co

254 underlying G protein-coupled receptor (GPCR) constitutive activity remain largely to be explored.

255 r mechanisms by which these mutations confer constitutive activity remain unresolved.

256 In contrast, prevention of constitutive activity required a short specific sequence

257 Many G protein-coupled receptors show constitutive activity, resulting in the production of a

258 This constitutive activity results from an unconventional res

259 structure of a NTSR1 variant that has little constitutive activity reveals uncoupling of the ligand-b

260 echanism and is directly correlated with the constitutive activity status of the RNA edited receptor

261 The ghrelin receptor displays a high constitutive activity suggested to be involved in the re

262 e specific sets of PKMs in each neuron whose constitutive activities sustain long-term synaptic plast

263 d SH2 domain (R47G mutation) displays higher constitutive activity than wild-type SHIP2.

264 vity in the absence of Ca(2+)/CaM, cMLCK has constitutive activity that is stimulated by Ca(2+)/CaM.

265 In inside-out patches with relatively high constitutive activity the G-protein activator GTPgammaS

266 ctions as a canonical GPCR, albeit with high constitutive activity, the CCR1.beta-arrestin-2 complex

267 ic domain of ADAM10 negatively regulates its constitutive activity through an ER retention motif but

268 calmodulin and the subsequent maintenance of constitutive activity through autophosphorylation at thr

269 , but show differential sensitivity of their constitutive activity to be inhibited by the inhibitor i

270 at positions 419 and 425 confer a degree of constitutive activity to the Gpa2p alpha-subunit.

271 , suggesting that the N841I mutation confers constitutive activity to the receptor.

272 d RAF mutations found in human cancer confer constitutive activity to these signaling molecules there

273 Consistent with its constitutive activity, Tyr134Phe CREB strongly promoted

274 l activity of KirNB remained intact with its constitutive activity unaltered.

275 cating that the photoreceptor reverses their constitutive activity upon light exposure, initiating ph

276 hosphorylation sites is sufficient to confer constitutive activity upon lin-45 Raf and induce multi-v

277 The level of constitutive activity was 4-5 times greater at the DOP t

278 Constitutive activity was identified by the increase in

279 ions, marked variation in ligand-independent constitutive activity was identified using a [(35)S]GTPg

280 arrestin recruitment was eliminated, whereas constitutive activity was observed in Galphai-mediated s

281 This constitutive activity was resistant to inhibition by cyc

282 ceptor subtype (B2R), which exhibits minimal constitutive activity, was substituted in either B1R or

283 ne the molecular contacts that underlie this constitutive activity, we created a three-dimensional mo

284 lecular mechanisms responsible for this high constitutive activity, we have reconstituted a purified

285 To gain insight into mechanistic aspects of constitutive activity, we report here the 3.3 A crystal

286 table in the PM, the GOF mutations with high constitutive activities were not restricted to LEL compa

287 Two additional MAC1 mutations exhibiting constitutive activity were in-frame deletions encompassi

288 , therefore, that the mutations resulting in constitutive activity were not involved in the UreR.urea

289 Also, the L226C mutation in TMD5 caused constitutive activity when combined with either the M250

290 old more sensitive to serotonin and produced constitutive activity when combined with the 5-HT3B subu

291 terestingly, a V223C mutation in TMD5 caused constitutive activity when combined with the L247C, L248

292 omain of R2 is sufficient to confer moderate constitutive activity when this subunit is expressed alo

293 een found to exhibit significantly increased constitutive activity when truncated to mimic GAIN domai

294 ns on Snf1/Snf4 kinase function demonstrated constitutive activity, which could foster glycogen accum

295 Ralpha) produces receptors having a range of constitutive activity, which suggests that this residue

296 activity of SoxR from enterics - inhibiting constitutive activity while allowing sensitivity to drug

297 The Zp CRE motif was necessary for this constitutive activity, while the ZIA and ZIB MEF2D motif

298 Specifically, suppression of MOR constitutive activity with the inverse agonist KC-2-009

299 hat application of flupenthixol inhibits D5R constitutive activity within the STN.

300 Type IV (NodD1 D284N) shows moderate constitutive activity yet can still be induced by luteol