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1 dy, thus underscoring its role as a vascular permeant.
2 ontaneously to MTA, which is stable and cell-permeant.
3 onium and N-methyl-D-glucamine are much less permeant.
4 Using LC-MS, we demonstrate that 6c is CNS-permeant.
5 tly determined by the size and charge of the permeant.
6 simply on the basis of size or charge of the permeants.
7 effective barriers for both liquid and vapor permeants.
10 by pre-exposure of the cone to the membrane-permeant acetoxymethyl ester of the Ca2+ chelator BAPTA.
11 ion of small molecules, translocation of the permeant across the biological membrane is traditionally
13 tivation of Gbetagamma using a specific cell-permeant activating peptide (myristoylated-SIRKALNILGYPD
14 ) up-regulated the current, whereas membrane-permeant activators of protein kinase A (PKA) were witho
15 We describe the synthesis and use of a cell-permeant active site-directed probe, which allows profil
16 with Cys and tested for reactivity with the permeant alkylating agent N-ethylmaleimide in right-side
18 s is significantly increased by the membrane-permeant allosteric agonist NPS R-568, which acts as a c
19 oxic to certain neuronal cells that carry Ca-permeant alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropi
20 rge movements were expressed by the non-Ca2+ permeant alpha1S(E1014K) variant, the alpha1C(E736K)/alp
21 family might control the protonated state of permeant ammonium to allow for its selective passage acr
24 ic-oxide donor, and 8-bromo-cGMP, a membrane-permeant analog of cGMP, mimic the effects of NECA on 5-
26 mami transduction is not known, but membrane-permeant analogs of cAMP antagonize electrophysiologic r
27 Ins(1,4,5)P(3)/AM (6-Ins(1,4,5)P(3)), a cell-permeant analogue of Ins(1,4,5)P(3), at 10 microm increa
30 ining a HaloTag in combination with membrane-permeant and -impermeant Halo dyes allows imaging of int
31 Ai and CAe) are distinguished using membrane-permeant and -impermeant pharmacological CA inhibitors,
32 tions Ba2+, Ca2+ and Zn2+ are not detectably permeant and block the gating pore at millimolar concent
33 engineered cysteines react with both channel-permeant and channel-impermeant probes occupy the outerm
34 screened for reactivity toward both channel-permeant and channel-impermeant thiol-directed reagents,
37 ntroduced cysteines was probed with membrane-permeant and membrane-impermeant sulfhydryl reagents und
39 selective binding and selective exclusion of permeant and nonpermeant cations, respectively, are impo
40 reversible binding and activation of a cell-permeant and nontoxic fluorogenic ligand (a so-called fl
41 cells is produced by the opening of a Na(+) permeant and yet largely TTX insensitive ion channel.
42 ic acid (small, hydrophilic, and ER membrane-permeant), and N-phenylmaleimide (small, hydrophobic, an
44 ic weak acid, its uncharged form is membrane-permeant, and its anion is consequently prone to distrib
45 rhodamine B (SRB), a fluorescent hydrophilic permeant, and of rhodamine B hexyl ester (RBHE), a fluor
46 istributed along the pore that interact with permeant anions and affect anion selectivity, as well as
49 insic property of the CLC-5 protein and that permeant anions, particularly Cl(-), modulate a voltage-
52 cells in the retina generate a gap junction-permeant apoptotic signal that mediates bystander killin
54 rossover between small-scale rattling of the permeant around its present position in the membrane and
55 yl]methanethiosulfonate (MTSES) molecule and permeant Au(CN)(2)(-) ions, were applied to either side
58 mined by whole cell labeling with a membrane-permeant biotin maleimide and a membrane-impermeant 2-((
59 cysteines, 8 were labeled with both membrane permeant (biotin maleimide (BM)) and impermeant (2-((5(6
61 ple kinetic model in which polyamines act as permeant blockers of Kir3.1/Kir3.4, but as relatively im
63 llent potency, is highly blood-brain barrier-permeant, but suffers from rapid first-pass metabolism.
64 not BPH FPs) can incorporate a more membrane-permeant BV analog, making smURFP fluorescence comparabl
67 tracellular CAs were inhibited by the poorly permeant CA blocker, benzolamide, or by inhibitory antib
68 lying 5% CO2 (Day 4), exposed oocytes to the permeant CA inhibitor ethoxzolamide (EZA), and measured
69 different pH and PCO2 with or without a cell-permeant CA inhibitor methazolamide (MTZ) or impermeant
70 s showed that endothelin-1, CPA and the cell-permeant Ca(2+) chelator BAPTA-AM activated the same 2.6
72 lls, we examined the effects of the membrane-permeant cADPR antagonist, 8-bromo-cADPR (8Br-cADPR), on
73 ratio of fluorescence signals from membrane permeant (calcein) and membrane impermeant (propidium io
74 (PKA) inhibitor, inhibits the ability of the permeant cAMP analog cpt-cAMP [8-(4-chlorophenylthio)-cA
76 ncluding PGE2, cholera toxin, and a membrane-permeant cAMP analog, protect normal and transformed int
77 n vitro or induction of capacitation by cell-permeant cAMP analogs decreased the depolarizing respons
79 8- fold in RAW cells treated with a membrane-permeant cAMP analogue (8-bromo-cyclic AMP; 8-Br-cAMP),
81 amitochondrial cAMP, but along with membrane-permeant cAMP analogues, failed to induce measureable ma
83 alysis using the ionotropic receptor channel-permeant cation agmatine indicated that ONH axon segment
87 een dipolar carbonyl ligands, water, and the permeant cation, which allow for selective flow of K+ ov
88 etation of signals from fluorescent membrane-permeant cations (usually termed "mitochondrial membrane
91 e indenes completely lacked, while the brain-permeant CB1R agonist HU-210 (1) exhibited strong CNS si
96 r Potential Melastatin 7 (TRPM7), a divalent-permeant channel-kinase of unknown function, is highly e
97 peptide of Alzheimer's disease forms calcium permeant channels in artificial membranes, we have propo
98 t receptor potential canonical (TRPC) Ca(2+)-permeant channels, especially TRPC3, are increasingly im
99 nt receptor potential (TRP) family of Ca(2+)-permeant channels, forms a signaling complex with TGF-al
102 ble in-pore environment, which would elevate permeant concentration within the pore and hence the flu
103 s, with no effect on basal secretion; a cell-permeant control peptide (Kal-C-helixKKED-Arg9) did not
107 phils, as disrupting the complex with a cell permeant CXCR2-specific peptide (containing the PDZ moti
108 nase-G system with nitroprusside or membrane-permeant cyclic GMP analogs mimicked the proexocytotic e
110 s relatively nontoxic prodrugs into membrane-permeant cytotoxic compounds with high bystander activit
111 ermal flux experiments, which showed greater permeant delivery both into and through the dual-frequen
112 When AtT-20 cells were treated with a cell-permeant derivative of the Kal-C-helix (Kal-C-helix-Arg9
113 rrelation (r(2) = 0.9993) when the following permeant descriptors were utilized: side-chain nonpolar
114 C5 channels responded to the addition of the permeant diacylglycerol (DAG) analogue, 1-oleoyl-2-acety
116 t and permeabilized glands, we used the cell-permeant, divalent cation chelator, tetrakis-(2-pyridylm
122 iabetic fatty rats by addition of a membrane permeant ester of a pyruvate cycling intermediate (dimet
123 he fluorescent metallosensor, calcein, and a permeant Fe2+ chelator to estimate labile cytoslic Fe2+,
124 en bonding and entropic factors arising from permeant flexibility substantially contribute to the ene
125 ng of the mTORC1 component RAPTOR and a cell permeant fluorescent analogue of di-leucine methyl ester
128 tance and are highly coupled via neurobiotin-permeant gap junctions, while midline cells are signific
130 rt the first total synthesis of the membrane permeant, hydrolytically stable, cADPR receptor agonist
131 that mitochondrial accumulation of membrane permeant, hydrophilic cations can be used to maximize lo
132 criterion for establishing that a blocker is permeant in a channel that has a complex permeation cycl
135 rasound treatments enabled delivery of large permeants, including microparticles, deep into colonic t
136 (269) was found to strongly bind the lactose permeant, indicating that proton transfer from water or
137 ll atomic ions (current) and fluorescent dye permeants, indicating that these permeants are distinctl
138 ing bristles with jasplakinolide, a membrane-permeant inhibitor of actin filament depolymerization, r
139 because of its ability to act as a membrane-permeant inhibitor of inositol 1,4,5-trisphosphate (IP3)
141 erichia coli beta-galactosidase and the cell-permeant inhibitor phenylethyl beta-D-thiogalactopyranos
144 n which occupation of either of two external permeant ion binding sites prevents Mg2+(o) entry into t
145 that differed in the locations and number of permeant ion bound; blocker dissociation occurs exclusiv
146 TRPM7 is a Ca(2)(+)-permeant and Mg(2)(+)-permeant ion channel in possession of its own kinase dom
147 (A) receptors (GABA(A)R), which are chloride-permeant ion channels, and GABA(B) receptors (GABA(B)R),
148 alinization was prevented by blocking proton-permeant ion channels, suggesting that distinct mechanis
150 e hyperpolarizing direction from high to low permeant ion concentrations consistent with charge scree
153 This regulation depends on the ability of a permeant ion to enter the selectivity filter (K(+) = Rb(
154 at the direction of the driving force on the permeant ion, as well as P(o), must be considered togeth
155 f C-type inactivation is a dependence on the permeant ion, but the mechanism by which permeant ions m
158 mode-shift of gating when having K(+) as the permeant ion; (ii) that Cs(+) or Rb(+), known to halt C-
159 unique in that its members display opposite permeant-ion charge selectivities despite sharing the sa
164 ted to gating and contains binding sites for permeant ions and pore-blocking molecules including quat
165 cking toxins show specific interactions with permeant ions and strong dependence on the ionic strengt
168 er a physiological electrochemical gradient, permeant ions are initially stabilized within the extrac
169 lter transport properties of hClC-4, varying permeant ions as well as mutating the "gating glutamate"
170 rturbed when positive charges occur near the permeant ions at a location that should counteract pore
171 at Ba(2+) and Na(+) compete effectively with permeant ions at a site near the boundary between the fi
173 ion channels have "charge rings" that focus permeant ions at the mouth of the pore and increase chan
175 riving force is coupled with the movement of permeant ions in the filter, maximizing the efficiency o
177 g and electrostatic repulsive forces between permeant ions is needed to achieve efficient conduction.
178 the permeant ion, but the mechanism by which permeant ions modulate C-type inactivation is not known.
179 hypothesis, we have examined the effects of permeant ions on gating of three Kv4 channels (Kv4.1, Kv
181 ecause Cd(2+) block is sensitive to voltage, permeant ions on the opposite side of the membrane (tran
182 reased internal K+ concentration as if these permeant ions prevented TBSb access to its site in the p
183 CLC channels are also known to couple to the permeant ions via their binding sites in the ion-permeat
184 ant Mg2+ influx only in the absence of other permeant ions, but not under physiological conditions.
185 rse a long (>70 A) pore, displacing multiple permeant ions, en route to a high affinity binding site
186 d to activation and is modulated by voltage, permeant ions, pore-blocking drugs, and membrane cholest
198 Here we examined the effects of external permeant (K+, Na+ and Li+) and non-permeant (NMG+) ions
199 rmeation mechanism, driven by a reduction in permeant [K(+)](o) following pore block (which would ret
201 ed nuclei were also loaded with the membrane-permeant low-affinity Ca(2+) probe fluo-5N AM which comp
202 ion; disruption of this complex using a cell-permeant LPA2-specific peptide reversed LPA2-mediated in
203 e were resolved and transport of hemichannel-permeant LY dye was visualized when the hemichannel was
204 ese channels are modulated by NO, a membrane-permeant messenger in various physiological and patholog
206 HCs were also less sensitive to block by the permeant MET channel blocker dihydrostreptomycin, whethe
207 we show that systemic injection of the brain-permeant mGlu2/3 receptor agonist (-)-2-oxa-4-aminobicyc
208 he basis of this model, we engineered a cell-permeant minipeptide to destabilize the fusion-constrain
209 sibility of cytoplasmic residues to membrane-permeant modifying reagents supports the idea that this
210 s framework for describing the motion of the permeant molecule on the pico- to nanosecond timescale.
211 ate (ITPP) is a recently identified membrane-permeant molecule that causes allosteric regulation of H
213 ty on ion concentration, competition between permeant molecules, anomalous mole-fraction effects, and
217 NAADP acetoxymethyl ester (NAADP-AM), a cell-permeant NAADP analog, increases cytosolic Ca(2+) concen
218 ported the potential of compound 37 as a BBB-permeant neuroprotective agent against H2O2-induced oxid
219 reover, 5b behaves as a water-soluble, brain-permeant neuroprotective agent against oxidative insults
220 derivative that has been described as a low-permeant neutral CB1 antagonist, though its pharmacology
223 in primary murine B cells reveal that Ca(2+)-permeant nonselective cation channels (NSCCs) operate in
224 al steps in the activation of novel (calcium-permeant) nonselective cation channels (NSCCs) and calci
227 s crossed, intracellular toxic IAPP membrane permeant oligomers (cylindrins) may form, compromising b
228 is potentially toxic, especially as membrane-permeant oligomers, which have been observed to accumula
232 icating that the increased tortuosity of the permeant path was effective on barrier properties of the
234 ing in regulating expression of the vascular permeant PDGF-B was confirmed in vitro using cell permea
235 urther demonstrate the efficacy of the brain-permeant PEGylated version of the anti-solTNF peptide, X
237 ably transduced with lenti-SUMO-1 and a cell-permeant peptide harboring SUMO-binding motif to interfe
238 pitating events that are sensitive to a cell-permeant peptide inhibitor of SRTF nuclear import (cSN50
240 minipumps containing either vehicle, a cell-permeant peptide that inhibits NAD(P)H oxidase (gp91ds-t
241 e tag can be reduced acutely with a membrane-permeant phosphine, labeled with ReAsH, monitored in the
243 g GABAergic postsynapses by using a membrane-permeant PI3P derivative, time-lapse confocal imaging, e
246 age apoptosis in vivo with a small, membrane-permeant probe, TcapQ(647) was synthesized comprising a
252 ine residues to modification by the membrane permeant reagent N-ethylmaleimide (NEM) and the membrane
253 30 unique cysteine residues to the membrane-permeant reagent N-ethylmaleimide and the membrane-imper
256 zed that methylene blue (MB), a mitochondria-permeant redox-active compound that can act as an altern
261 ctional IAPs by RNA interference or the cell-permeant Smac amino-terminal peptide blocked FGF-2-induc
262 bsorption and retention patterns of membrane-permeant small molecules in a cellular context could fac
263 not volume expansion by isoosmotic medium by permeant solutes (ethylene glycol, diethyl urea, or ammo
264 t the intracellular partitioning of membrane-permeant solutes manifests itself as a partial volume re
265 that intracellular partitioning of membrane-permeant solutes manifests itself as a partial volume re
266 ular environment, it is likely that membrane-permeant solutes may be excluded from a fraction of the
267 by treatment of Swiss 3T3 cells with the non-permeant solutes sucrose or sorbitol, rapidly and robust
269 following osmotic lysis of infected cells in permeant solutes, these experiments have been limited to
270 n to the selective binding of K(+) and other permeant species over Na(+), there is a selective exclus
271 ory transmission from that of a postsynaptic permeant species to a presynaptic regulatory element.
272 rmeability of hemichannels is regulated in a permeant-specific manner and underscores that hemichanne
273 The six esters render the probe membrane permeant, such that it can be loaded into intact living
280 hiP to be approximately 200-300 Da for small permeants that pass through by general diffusion while a
281 pH suggested that H(+) is not significantly permeant through OsHKT2;4 in most physiological ionic co
282 hylamine, ethylamine, and trimethylamine are permeant through the RyR but with reduced current amplit
286 vestigated delivery of fluorescently labeled permeants to colon tissues of Yorkshire pigs ex vivo and
287 Dye transfer studies using the gap junction permeant tracer Cascade Blue demonstrated a disruption t
288 the present study, we used the gap junction-permeant tracer Neurobiotin to compare the coupling patt
290 ng due to abnormal activation of the calcium permeant TRPC (Transient Receptor Potential Canonical) c
291 aused by depletion of the Ca(2+)- and Mg(2+)-permeant TRPM7 is suppressed by expression of a dominant
292 tive stimulus for acid taste is the membrane-permeant, uncharged acetic acid moiety (CH(3)COOH), not
293 exyl ester (RBHE), a fluorescent hydrophobic permeant, using dual-channel two-photon microscopy (TPM)
294 or R337X V2R by incubation with the membrane-permeant V2R antagonist, SR121463B, leads to a mature gl
296 , an extracellular concentration gradient of permeant weak acid readily induces pH(i) nonuniformity.
297 by superfusion of acetate (salt of membrane-permeant weak acid), evoked a [Ca(2+)]i rise, independen
298 leimide (small, hydrophobic, and ER membrane-permeant), were monitored by Western blot analysis.
299 ression analysis performed for the set of 14 permeants yielded the best correlation (r(2) = 0.9993) w
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