ライフサイエンスコーパス: ligand binding

1 and "closed", which could potentially affect ligand binding.

2 eptide.MHC-binding site, remarkably affected ligand binding.

3 rk and salt bridges involving side chains on ligand binding.

4 and alpha7-helix, required for high-affinity ligand binding.

5 egrin cytoplasmic tails and through integrin-ligand binding.

6 erent techniques to characterize the protein-ligand binding.

7 that are modulated by external stimuli like ligand binding.

8 lization assay based on antibody blockade of ligand binding.

9 ath Receptor 5 TM-dimers open in response to ligand binding.

10 o stabilization of assemblies, catalysis and ligand binding.

11 ng about apoE unfolding and its changes upon ligand binding.

12 le probes for local structure, dynamics, and ligand binding.

13 quitinated and degraded by proteasomes after ligand binding.

14 ional changes in the receptor occurring upon ligand binding.

15 op structure-activity relationships of beta2 ligand binding.

16 erved extracellular cysteine rich domain for ligand binding.

17 ulfate binding site of A27, likely affecting ligand binding.

18 ibit the transport cycle, and affect in part ligand binding.

19 rgy conformation, which might be involved in ligand binding.

20 e alphaIIbbeta3 clustering in the absence of ligand binding.

21 the octasaccharide complex is necessary for ligand binding.

22 s and (B) to the lack of a helical kink upon ligand binding.

23 is mirrored by increased TSPO expression or ligand binding.

24 he efficacy of orbital overlap and therefore ligand binding.

25 visualized by microscopy and probed by radio-ligand binding.

26 nges in EGFR kinase domain polarization upon ligand binding.

27 ow increased stability (less unfolding) upon ligand binding.

28 and that overexpression of La enhances RIG-I-ligand binding.

29 ons represents the most important factor for ligand binding.

30 ability of simvastatin to target CR3 in its ligand binding-activated conformation is a novel mechani

31 then discuss GPCR dynamics in the context of ligand binding, activation, allosteric modulation, and b

32 -CFC homologs have distinct, highly specific ligand binding activities.

33 AD strains had increased ClfB ligand binding activity compared to normal nasal carriag

34 Our data show that LFA-1 has a low ligand-binding activity in resting human NK cells, but i

35 (TopologyNet) for the predictions of protein-ligand binding affinities and protein stability changes

36 Whereas protein-ligand binding affinities have long-established prominen

37 Here, we present crystal structures and ligand binding affinities of periplasmic binding protein

38 latest methods in the prediction of protein-ligand binding affinities, mutation induced globular pro

39 hod provides chemical information to protein/ligand binding affinity measurements.

40 e plasmon resonance showed a NOTA-conjugated ligand binding affinity of 1 nM.

41 trapped high-energy state displayed improved ligand binding affinity, compared with the wild-type enz

42 glutaminase kinetic activity and allosteric ligand binding affinity.

43 Here, recent measurements of the intrinsic ligand-binding affinity and free energy of each integrin

44 dy reveals that IFNAR1 flexibility modulates ligand-binding affinity, which, in turn, regulates biolo

45 hypoglycosylation and reduced extracellular ligand-binding affinity.

46 96 from GII.17.2015 into GII.17.1978 ablated ligand binding and altered antigenicity, defining an imp

47 ng serial pandemics as the virus evolves new ligand binding and antigenicity features.

48 Furthermore, we evaluated their impact on ligand binding and antiproliferative activity against PD

49 ation of integrins is generally required for ligand binding and cellular signalling.

50 from bacteria, riboswitches couple specific ligand binding and changes in RNA structure to mRNA expr

51 lerance than wild type, while also retaining ligand binding and immunogenic properties indistinguisha

52 Ligand binding and integrin clustering subsequently stim

53 modulate quaternary architecture, as well as ligand binding and kinetic parameters involved with RFK

54 op have critical roles in modulating peptide ligand binding and receptor activation.

55 clearly defining the role of this domain in ligand binding and receptor activation.

56 We used ligand binding and second-messenger assays to show that

57 tudies revealed the crucial interactions for ligand binding and selectivity.

58 Most of these monobodies competed with pY ligand binding and showed strong selectivity for either

59 The analysis of the combined process of ligand binding and structure formation even for small RN

60 mplitudes allow calculation of the degree of ligand binding and the concentration of unbound ligand,

61 e distal side-chain dynamics is modulated on ligand binding and the origin has been attributed to ent

62 criptional regulators, but the dependence of ligand binding and the subsequent allosteric conformatio

63 Olaratumab blocks ligand binding and thereby inhibits activation of PDGFRA

64 Mutants of key residues involved in ligand binding and/or proposed to be involved in domain

65 e alterations, as mutations lead to impaired ligand binding and/or signaling capacity.

66 vities and provides a route to custom design ligand-binding and catalytic sites.

67 emerged as a powerful tool to study folding, ligand binding, and motor enzymes.

68 ropose for the first time an electrochemical ligand-binding approach for antipsychotic drug screening

69 of structures and rates involved in protein ligand binding are essential for drug design.

70 ith an engineered sequence is used to detect ligand binding as blocking events during DNA unzipping,

71 a novel workflow is presented by hybridizing ligand binding assay (LBA) with liquid chromatography-hi

72 In solid phase ELISA-based ligand binding assays, purified pentameric H2O2-treated

73 ules, which meet the requirements for use in ligand-binding assays and absorption, distribution, meta

74 Ligand-binding assays are the linchpin of drug discovery

75 In vitro ligand-binding assays suggest that CTDP-32476 is a poten

76 Allosteric effect implies ligand binding at one site leading to structural and/or

77 Ligand binding at the extracellular domain of RAGE initi

78 lization of the nucleotide-binding domain by ligand binding; (b) a temperature-induced increase in in

79 The ligand-binding betaI and alphaI domains of integrin are

80 of S. pyogenes show a dichotomous switch in ligand binding between human tissue and blood environmen

81 A panel of ligand-binding blocking and non-blocking anti-EGFR antib

82 sp-168 is important in anchoring Arg-155 for ligand binding but is not critical for Lys-155 because o

83 raphically resolved the masking of unlabeled ligand binding by the increase of radioligand free fract

84 gradient and chemotaxes, stochastic receptor-ligand binding can be a fundamental limit to the cell's

85 ter cytokine priming, Siglec-8 mAb or glycan ligand binding causes eosinophil apoptosis associated wi

86 Active sites and ligand-binding cavities in native proteins are often for

87 -occluded intermediate state, with a defined ligand binding cavity.

88 polymorphism and POL5551's effects on CXCR4 ligand binding, cell viability, and migration.

89 a significant impact on the topology of the ligand binding cleft and thus ligand specificity.

90 f the CD300lf ectodomain reveals a potential ligand-binding cleft composed of residues that are criti

91 In all conjugates, the ligand binding competence toward alphaVbeta3 (using both

92 nformational species present under different ligand-binding conditions throughout the allosteric cycl

93 tal ion-dependent adhesion site of the open, ligand-binding conformation of the CR3 I domain by direc

94 We report the direct measurement of ligand-binding constants of organolithium complexes usin

95 The results suggest a model in which VAP-ligand binding couples proteostasis and lipid homeostasi

96 emporal synchronization of RNA synthesis and ligand binding-dependent conformational refolding.

97 ur data suggest E172ECL2 is a key allosteric ligand-binding determinant, whereas hydrogen-bonding net

98 tified on AR, both located in its C-terminal ligand binding domain (LBD).

99 activated fusion protein, which contains the ligand binding domain from a target NHR (human thyroid r

100 ructure was obtained of 1b when bound in the ligand binding domain of GluK1.

101 depended on the source of the extracellular ligand binding domain of the subunit.

102 w approaches that use genotyping of the AHR1 ligand binding domain to screen for DLC sensitivity amon

103 ciable pre-complex, enabling its neighboring ligand binding domain to tightly clamp the two polypepti

104 fied, full-length LRH-1, as well as isolated ligand binding domain, bound to PGC1alpha with higher af

105 l transactivation domain, and the C-terminal ligand binding domain, but not the DNA-binding domain of

106 tor (MR) on Ser-843, a residue placed on the ligand binding domain, lowers affinity for agonists, pro

107 nel and kinetics of glycine binding with its ligand binding domain.

108 nd UT-155) also binding the carboxy-terminal ligand binding domain.

109 ring (SAXS) experiments using isolated GluA2 ligand-binding domain (GluA2-LBD) are consistent with bi

110 The RARbeta ligand-binding domain (LBD) and DNA-binding domain (DBD)

111 of the GluA2 AMPA subtype glutamate receptor ligand-binding domain (LBD) dimers to characterize a nat

112 The presence of intact ligand-binding domain (LBD) ensures the strict androgen-

113 mined the crystal structure of the PPARgamma ligand-binding domain (LBD) in complex with VSP-51, whic

114 tallography reveals that SJB7 resides in the ligand-binding domain (LBD) of hPXR, interacting with th

115 nnects the DNA-binding domain (DBD) with the ligand-binding domain (LBD) via a mix of positively char

116 Agonists bind to the ligand-binding domain (LBD) which is arranged as a dimer

117 amolecular interaction between CAR's DBD and ligand-binding domain (LBD), enabling the homodimer-hete

118 h subtype-specific residues in the PPARdelta ligand-binding domain (LBD).

119 ulated ectodomain cleavage that releases the ligand-binding domain (sTie2) into the circulation.

120 on of diverse AR variant species lacking the ligand-binding domain and possessing ligand-independent

121 nzalutamide-resistant prostate cancers where ligand-binding domain antagonists are ineffective.

122 ents in the AMPAR extracellular domain, with ligand-binding domain dimers losing their local 2-fold r

123 stitutive activity reveals uncoupling of the ligand-binding domain from conserved connector residues,

124 We show how TARPs sculpt the ligand-binding domain gating ring, enhancing kainate pot

125 Structures of a soluble ligand-binding domain have provided atomic-scale insight

126 stablishment of a ring-like structure in the ligand-binding domain layer of the receptor.

127 lecule positive allosteric modulators of the ligand-binding domain of (S)-2-amino-3-(3-hydroxy-5-meth

128 te the potential of Nanobodies to target the ligand-binding domain of EphA4.

129 ded mostly by the three-layer, alpha-helical ligand-binding domain of nuclear receptors.

130 We found that AA binds to and stabilizes the ligand-binding domain of peroxisome proliferator-activat

131 hown that heme decreases the affinity of the ligand-binding domain of Rev-erb NRs for NCoR1 peptides.

132 re, we report the crystal structures for the ligand-binding domain of RORgammat in both apo and ligan

133 resent the crystal structure of the isolated ligand-binding domain of the GluN1-GluN2A NMDA receptor

134 % sequence similarity with the extracellular ligand-binding domain of the human alpha7 nAChR, to inve

135 potent and selective Nanobodies against the ligand-binding domain of the human EphA4 receptor.

136 of non-steroidal ligands able to bind to the ligand-binding domain of the MR and recruit different co

137 ng products lacking the entire extracellular ligand-binding domain of the receptor while retaining th

138 isoform of ERbeta (mERbeta2) with a modified ligand-binding domain sequence.

139 ZNF764 physically interacted with GR at ligand-binding domain through its KRAB domain, and both

140 uctures of the three modulators in the GluK1 ligand-binding domain were determined, locating two modu

141 n fluorescent protein (GFP) insertion into a ligand-binding domain, generating the requisite alloster

142 C-terminal angiopoietin domains to the Tie2 ligand-binding domain, the mechanisms for Tie2 activatio

143 its high constitutive activity, both direct (ligand-binding domain-dependent) and indirect activation

144 lar dynamics simulations of GluN1 and GluN2B ligand binding domains (LBDs) of NMDARs to investigate t

145 bimagrumab binds to both ActRIIA and ActRIIB ligand binding domains in a competitive manner at the cr

146 Crystal structures of the ligand binding domains of most of the phylogenetically w

147 ated that many bacterial chemoreceptors have ligand-binding domains (LBD) of the dCACHE family, a str

148 However, steroid receptor ligand-binding domains (LBDs) are inherently unstable, a

149 those produced by NMDAR mutants in which the ligand-binding domains (LBDs) are locked in the closed c

150 reaches the recessed binding pocket in iGluR ligand-binding domains (LBDs).

151 -GluN2A dimer interface of the extracellular ligand-binding domains (LBDs).

152 sion system was used to express SdrF and its ligand-binding domains.

153 combined matching of transcription rates and ligand binding enables transcription intermediates to un

154 Because protein-ligand binding energy is in the THz range, especially, m

155 For many biological processes such as ligand binding, enzymatic catalysis, or protein folding,

156 vered key residues for structural stability, ligand binding, enzyme activity, and protein interaction

157 s as a competitive inhibitor that blocks the ligand binding epitope on type II receptors.

158 energetic contribution of the solvent during ligand binding evaluated.

159 methods used for the calculation of protein-ligand binding free energies, the challenges associated

160 We insert GFP into the rigid, ligand-binding head of the integrin, model with Rosetta

161 leg domains in each subunit that connect the ligand-binding head to the membrane repel or crowd one a

162 studies enables SAR exploration to map GPCR-ligand binding hot spots.

163 The PET images matched ligand binding in post-mortem tissue, and histological m

164 sothermal titration calorimetry to show that ligand binding in rhodopsin is enthalpy driven with -22

165 Ligand binding in target cells promotes activation of Vg

166 ptor antagonists by identifying a cavity for ligand binding in which variations exist between GluN2A

167 unbound, sensing riboswitch refolds into the ligand binding-induced output state.

168 ics during turnover are dominated by protein-ligand binding interactions.

169 otifs playing important roles in transducing ligand binding into distinct signaling responses, we com

170 nding site is not preformed in solution, and ligand binding is fundamental for the binding site forma

171 us detection of changed states (for example, ligand binding) is difficult unless signal is strong.

172 To decipher the mechanisms of cooperative ligand binding it is necessary to define at a microscopi

173 yrosine kinase (TK) that-once activated upon ligand binding-leads to receptor dimerization, recruitme

174 performed with these GPCR mutants, including ligand binding, ligand-induced receptor internalization,

175 and functional assays, we posit that dynamic ligand binding may be the mechanism underlying protean a

176 method, which combines direct ESI-MS protein-ligand binding measurements and competitive protein bind

177 Site-directed mutagenesis, ligand-binding measurements, steady-state kinetics, and

178 nes the highly collaborative and promiscuous ligand binding mechanism.

179 erLOGSY titration experiments give access to ligand binding modes even in the case of weak binders as

180 Two ligand binding modes have been identified as the lowest

181 New insights into kinase-ligand binding modes were obtained.

182 and efficiently distinguish between possible ligand binding modes.

183 ural and energetic terms, we calculated 1100 ligand-binding molecular dynamics trajectories and teste

184 in a significant fraction of the population, ligand binding occurs over a time scale that is approxim

185 ly, electrophysiological studies showed that ligand binding of 11-cis-retinal in dark-adapted Rho was

186 Ligand binding of GII.17 cluster IIIb VLP was blocked on

187 lar recognition of DCL- and AG-PEGylation on ligand binding on PSMA active site.

188 lass of biomolecules that can exhibit either ligand binding or enzymatic activity.

189 gand uptake by CTLA-4, which is sensitive to ligand-binding or -trafficking mutations, that would oth

190 etic constants of two representative protein-ligand binding pairs (streptavidin/biotin; IgG/anti-IgG)

191 lve this discrepancy and to characterize the ligand-binding path in structural and energetic terms, w

192 following structural changes that occur upon ligand binding, pH change, and membrane binding.

193 , that the changes in flexibility induced by ligand binding play an important role and that supercoil

194 a wild type neuronal nAChR ECD and the full ligand binding pocket conferred by two adjacent alpha su

195 cluding a 53% reduction in the volume of the ligand-binding pocket and an increase in the surface are

196 his conformation, wherein W72 flips into the ligand-binding pocket and renders the protein incapable

197 is strictly dependent on an intact receptor ligand-binding pocket and that FES binds to ERalpha with

198 g-term storage and relies on the hydrophobic ligand-binding pocket of AHR, with identical structural

199 ), a natural ligand binding to the classical ligand-binding pocket of RXRalpha.

200 ophobic residues on TM3 and TM7 form a broad ligand-binding pocket that can accommodate the diverse s

201 s other than those in the headpiece near the ligand-binding pocket, and the alpha- and beta-subunits

202 gand and a conserved aromatic residue in the ligand-binding pocket.

203 rounding amino acid residues in the receptor ligand-binding pocket.

204 The ligand binding pockets are allosterically tuned by monop

205 A comparative analysis of ligand binding pockets in chemokine receptors is present

206 cocrystallized with Brd4 for determining the ligand binding pose and rationalizing subsequent structu

207 site residues in each case, and the probable ligand binding pose.

208 To better understand the dynamics of the ligand binding process, pulsed electron-electron double

209 to the heme and phenylalanine cluster in the ligand binding process.

210 -energy surface (FES) describing the protein-ligand binding process.

211 We report the catalytic properties, ligand-binding profiles, and inhibition of enzymatic act

212 to characterize the structure, dynamics, and ligand binding properties of avian SC, avian SC domain v

213 ng-site definition as a central principle of ligand-binding protein design.

214 em among the most significantly reengineered ligand-binding proteins to date.

215 action between the alphaMI domain, the major ligand-binding region of Mac-1, and PTN.

216 studies have shown how Angs bind to the Tie2 ligand-binding region, but do not explain Tie2 activatio

217 Here we identify alternate ligand binding regions using nematode iPGM to select and

218 ceptors display near-identical extracellular ligand-binding regions but have intracellular sequences

219 ption of hydrogen bonds between Q177 and the ligand-binding residue R65.

220 Our recent analysis revealed that ligand binding residues had a significantly higher mutat

221 g site flexibility, we also explored whether ligand-binding resulted in common dynamical changes in A

222 ple interactions, ligands stabilize both the ligand binding site and the local secondary structure.

223 ls common structural rearrangements near the ligand binding site induced by the bound (S)-enantiomers

224 The planar ligand binding site, observed in a parallel orientation

225 as MRS2500 blocks signaling by occupying the ligand binding site.

226 Moreover, we identified a ligand-binding site in the dimer interface, suggesting t

227 subunits to complementary components of the ligand-binding site is nonequivalent.

228 The two most common are binding to the ligand-binding site of the receptor and, conversely, bin

229 et-blocking antibody which binds outside the ligand-binding site, and determined the crystal structur

230 rgo a conformational change that exposes its ligand-binding site, but it is poised to rapidly assembl

231 CD and a conserved, membrane-distal putative ligand-binding site.

232 al PASTA domain that has the properties of a ligand-binding site.

233 targeting PAR1 with an orthosteric-tethered ligand binding-site antagonist results in bleeding, poss

234 Mutations at the ligand binding sites (LBSs) can influence protein struct

235 heories for the predictions of metal ion and ligand binding sites and metal ion-dependent RNA stabili

236 ntial allosteric paths between catalytic and ligand binding sites of hPDI.

237 natural carrier protein possessing multiple ligand binding sites with a plasma half-life ~19days, fa

238 These studies identify three separable ligand binding sites within GPR84 and suggest that if me

239 on of individual orthosteric contacts in the ligand binding sites, allowing us to rank the energetic

240 the effects of SNVs on enzyme active sites, ligand binding sites, and various types of post translat

241 neered form of sTie2, which presents dimeric ligand binding sites, inhibits Angpt1 signalling at seve

242 cluding gene ontology, enzyme commission and ligand-binding sites from various analogous and homologo

243 Allosteric communication between two ligand-binding sites in a protein is a central aspect of

244 Structural studies of the beta1AR define ligand-binding sites in the transmembrane helices and ef

245 , and co-existent, exo- and endofacial GLUT1 ligand-binding sites.

246 protein domain that can accommodate multiple ligand-binding sites.

247 g two benchmark databases and two particular ligand-binding sites.

248 moothened, a GPCR that contains two distinct ligand-binding sites: one in its TMD and one in the CRD.

249 ppear ready to discriminate other enzyme and ligand binding states.

250 ynamics and equilibrium and pre-steady-state ligand-binding studies.

251 Upon ligand binding, the Notch intracellular domain (NOTCH IC

252 h as the the isomerization of receptors upon ligand binding, the sequential binding of receptors to m

253 tivation mechanism where, upon extracellular ligand binding, this intramolecular agonist isomerizes a

254 Upon ligand binding, TLRs and IL-1Rs recruit adaptor proteins

255 d and an expression platform that transduces ligand binding to a gene expression output.

256 scence anisotropy (FA) DNA-based assays, the ligand binding to a given receptor is typically signalle

257 is study examined the effects of ketamine on ligand binding to a metabotropic glutamatergic receptor

258 ing of fast time scale motions observed upon ligand binding to adenylate kinase is dominated by enzym

259 Taken together, our results show that ligand binding to BTN3A1 induces a conformational change

260 Ligand binding to certain classes of G protein coupled r

261 op, which critically contributes to coupling ligand binding to channel opening in human alpha7 nAChR.

262 However, the molecular pharmacology of ligand binding to CXCR3 alternative splice variants and

263 Our study indicates a marked reduction of ligand binding to D1 and D2 and 5-HT2A receptors as well

264 erate plant sensors for fentanyl by coupling ligand binding to design stability.

265 Computational studies on ligand binding to GPCRs have revealed transient, low-aff

266 BACKGROUND & AIMS: Ligand binding to inhibitory receptors on immune cells,

267 Motivated by the desire to screen for ligand binding to intact protein complexes we report the

268 Ligand binding to membrane proteins may be significantly

269 GPR39 for synthetic ligands and knowledge of ligand binding to other receptors with similar binding p

270 between segments S2 and S3 probably couples ligand binding to pore opening.

271 ecedented means for the FA monitoring of the ligand binding to short DNA molecules, allowing the elab

272 ry" M1 macrophages, specific (68)Ga-DOTATATE ligand binding to SST2 receptors occurred in CD68-positi

273 Through studies with ligand binding to the acetylcholine binding protein (ACh

274 During regulation of gene expression, ligand binding to the aptamer domain of a riboswitch tri

275 Ligand binding to the aptamer domain of the riboswitch i

276 th 9-cis-retinoic acid (9-cis-RA), a natural ligand binding to the classical ligand-binding pocket of

277 Structural comparison reveals that ligand binding to the heme a3 iron in the SFX structure

278 ion on the conformational changes induced by ligand binding to the hTS active site.

279 -selectin suggest a two-state model in which ligand binding to the lectin domain closes loop 83-89 ar

280 Canonical Hh signaling is mediated by Hh ligand binding to the receptor Patched (Ptch), which in

281 Ligand binding to the TCR causes a conformational change

282 membrane that dimerize on the membrane after ligand binding to their extracellular domain, the TLR4-T

283 ong need for suitable tracers to interrogate ligand binding to this receptor.

284 uman fetal retinal pigment epithelium cells, ligand binding to TLR2 induced robust expression of proi

285 Ligand binding to Toll-like receptors (TLRs) results in

286 e used three complementary assays to compare ligand binding to WT selectins and to E88D selectins tha

287 d as important probes sensing the effects of ligand-binding to the catalytic site of the H-cluster.

288 ary approaches enabled the identification of ligands binding to different subpockets of the latent Fa

289 ug design not only deals with the search for ligands binding to interesting and promising validated t

290 s extensively used to obtain epitope maps of ligands binding to protein receptors, thereby revealing

291 Ligands binding to the N-terminal domain abolish the spo

292 ted relative binding free energies for three ligands binding to the progesterone receptor are in very

293 Few opioid ligands binding to the three classic opioid receptor sub

294 g the structural and energetic requisites of ligand binding toward its molecular target is of paramou

295 phA2 "canonical" signaling involves ephrin-A ligand binding, tyrosine autophosphorylation, and kinase

296 hierarchical mechano-regulation of receptor-ligand binding.Von Willebrand factor (VWF) is a blood pr

297 en used to investigate general properties of ligand binding: we observe both a direct stabilizing eff

298 osterically couples and synchronizes initial ligand binding with channel opening.

299 exible binding region that is predisposed to ligand binding with the desired geometry.

300 overall structure, and stability, as well as ligand binding, without the need for purification.