ライフサイエンスコーパス: constitutive activity

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

2 a strikingly high, physiologically relevant, constitutive activity.

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

4 the cell from plasma membrane expression of constitutive activity.

5 DAR signaling in AD without disrupting their constitutive activity.

6 molecular mechanisms of GPCR activation and constitutive activity.

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

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

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

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

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

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

13 n in Mec1, conserved in ATR, that results in constitutive activity.

14 -type receptor, properties characteristic of constitutive activity.

15 chimera were also observed, consistent with constitutive activity.

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

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

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

19 ng that multimerization is essential for the constitutive activity.

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

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

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

23 y desensitized, which partially masked their constitutive activity.

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

25 TRPM5 does not display constitutive activity.

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

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

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

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

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

31 iptional start site, involving repression of constitutive activity.

32 341D/T491E/S494D (DDED), in C-Raf results in constitutive activity.

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

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

35 on model incorporating negative feedback and constitutive activity.

36 ownstream pathways (biased agonism), and (d) constitutive activity.

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

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

39 and that disease-associated mutations cause constitutive activity.

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

41 ntrol of receptor functional selectivity and constitutive activity.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

58 GHSR has high constitutive activity and may act independently of ghrel

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

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

61 , is expressed in glioblastoma and possesses constitutive activity and oncomodulatory properties.

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

63 human chemokine receptors, but some display constitutive activity and promiscuous G protein coupling

64 2 or FFA3 agonist binding pocket to regulate constitutive activity and SCFA potency.

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

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

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

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

69 examined to better understand the origin of constitutive activity and the potential for retinal dege

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

71 ticles had greatly enhanced levels of basal (constitutive) activity and displayed increased sensitivi

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

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

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

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

76 ctively targeting GHSR and reducing its high constitutive activity appears to be a good candidate for

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

78 ugh the ERK cascade and mutations leading to constitutive activity are key drivers of human tumors, a

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 proteins that could not bind SAURs exhibited constitutive activity, as they were immune to SAUR inhib

83 2 altered GHSR1a signaling by inhibiting its constitutive activity, as well as by enhancing its G pro

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

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

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

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

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

89 Constitutive activity because of deletion of this region

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

91 CAMKK2 relevance is highlighted by its constitutive activity being implicated in several human

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

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

94 rmation has been hypothesized to result from constitutive activity, but how the receptor could escape

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

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

97 CAR inactivates its constitutive activity by phosphorylation at threonine 38

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

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

100 This constitutive activity can desensitize rod photoreceptor

101 le species can potentially contribute to the constitutive activity causing night blindness.

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

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

104 T205M(5.54) displayed high constitutive activity, enhanced dopamine potency, and en

105 Receptor activation Efficacy (epsilon), and constitutive activity (epsilon(R0)).

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

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

108 ck-Hall operational model, we quantified the constitutive activity for both pathways and conclude tha

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

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

111 o specific values, e.g., epsilon(R0) = 0: no constitutive activity, gamma = 1: no amplification (E(ma

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

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

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

115 The promoter of SfHsp70D showed the high constitutive activity in cell line and embryos, while th

116 LCgamma(2) variants typically do not exhibit constitutive activity in cell-free systems, leading to t

117 contrast between the low levels of beta(2)AR constitutive activity in cells and the high constitutive

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

140 This constitutive activity is independent of the intracellula

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

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

143 Constitutive activity is strongly reduced by silencing e

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

145 Importantly, because apo-opsin has weak constitutive activity, it triggers transduction to produ

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

147 The constitutive activity leads to basal phosphorylation of

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

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

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

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

152 constitutive activity in cells and the high constitutive activity observed in an isolated phospholip

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

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

155 7.49) also seem to be necessary for the high constitutive activities of D556(6.44)H and D556(6.44)Q a

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

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

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

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

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

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

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

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

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

165 Constitutive activity of Bcr-abl fusion protein kinase c

166 ulate agonist potency, maximal efficacy, and constitutive activity of beta-arrestin2 recruitment.

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

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

169 Although a mutation that regulates constitutive activity of CXCR4 also results in monomeriz

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

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

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

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

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

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

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

177 411S loss-of-function mutations abrogate the constitutive activity of gain-of-function Ste5 alleles,

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

179 Traditionally, constitutive activity of GPCRs has been described in ter

180 erved upon G-protein activation; however, no constitutive activity of GPR158 could be detected throug

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

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

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

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

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

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

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

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

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

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

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

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

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

194 3-associated phenotypes, indicating that the constitutive activity of MPK3 can bypass SA and ethylene

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

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

197 We now examined the possibility that constitutive activity of neuronal RXR and/or RAR alters

198 e B-cell lymphoma (PMBL) cells depend on the constitutive activity of NF-kappaB and STAT transcriptio

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

200 The constitutive activity of oncogenic STAT3C was reported t

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

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

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

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

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

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

207 Constitutive activity of STAT5 or protection from apopto

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

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

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

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

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

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

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

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

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

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

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

219 5-HT2cR decreased in parallel with increased constitutive activity of the isoforms.

220 Constitutive activity of the isolated Smad-binding regio

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

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

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

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

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

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

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

228 Constitutive activity of the putative HAS2-AS1 promoter

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

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

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

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

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

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

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

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

237 Constitutive activity of the serine/threonine kinase Akt

238 Constitutive activity of the serotonin receptors 5-HT2B/

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

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

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

242 This constitutive activity of the truncated BAI1 mutant also

243 Constitutive activity of these alleles was dependent on

244 s in the ENaC M2 helix may contribute to the constitutive activity of these channels at a resting pH.

245 The constitutive activity of these mutants is not dependent

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

247 Constitutive activity of this cyclase contributes to bas

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

249 Constitutive activity of TLR4 in the intestinal epitheli

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

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

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

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

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

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

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

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

258 ns and highly selective to Ca(2+) ; it shows constitutive activity regulated negatively by Ca(2+) and

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

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

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

262 This constitutive activity results from an unconventional res

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

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

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

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

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

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

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

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

271 Although the H443P mutant shows constitutive activity, the mechanism involved in hyperac

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

292 Mutating Ser162 to Alanine produces constitutive activity, whereas the phosphomimetic Ser162

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

294 that result in KIT receptor tyrosine kinase constitutive activity, which drives proliferation.

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