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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 ch that no ion possessing a methyl group was permeant.
5 tly determined by the size and charge of the permeant.
6 Using LC-MS, we demonstrate that 6c is CNS-permeant.
7 effective barriers for both liquid and vapor permeants.
8 simply on the basis of size or charge of the permeants.
11 by pre-exposure of the cone to the membrane-permeant acetoxymethyl ester of the Ca2+ chelator BAPTA.
12 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 uctural determinants that make pentamidine a permeant although most other diamidine drugs are exclude
22 family might control the protonated state of permeant ammonium to allow for its selective passage acr
23 ic-oxide donor, and 8-bromo-cGMP, a membrane-permeant analog of cGMP, mimic the effects of NECA on 5-
25 mami transduction is not known, but membrane-permeant analogs of cAMP antagonize electrophysiologic r
26 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
29 ining a HaloTag in combination with membrane-permeant and -impermeant Halo dyes allows imaging of int
30 Ai and CAe) are distinguished using membrane-permeant and -impermeant pharmacological CA inhibitors,
31 tions Ba2+, Ca2+ and Zn2+ are not detectably permeant and block the gating pore at millimolar concent
32 engineered cysteines react with both channel-permeant and channel-impermeant probes occupy the outerm
33 screened for reactivity toward both channel-permeant and channel-impermeant thiol-directed reagents,
35 ntroduced cysteines was probed with membrane-permeant and membrane-impermeant sulfhydryl reagents und
37 selective binding and selective exclusion of permeant and nonpermeant cations, respectively, are impo
38 reversible binding and activation of a cell-permeant and nontoxic fluorogenic ligand (a so-called fl
39 esent the synthesis of two enantiomeric cell-permeant and photocaged (PP)(2)-InsP(4) derivatives and
40 cells is produced by the opening of a Na(+) permeant and yet largely TTX insensitive ion channel.
41 ic acid (small, hydrophilic, and ER membrane-permeant), and N-phenylmaleimide (small, hydrophobic, an
43 rhodamine B (SRB), a fluorescent hydrophilic permeant, and of rhodamine B hexyl ester (RBHE), a fluor
44 istributed along the pore that interact with permeant anions and affect anion selectivity, as well as
47 insic property of the CLC-5 protein and that permeant anions, particularly Cl(-), modulate a voltage-
50 rated with liposomes containing the non-cell-permeant antibiotic gentamicin and a fluorescent marker.
52 rossover between small-scale rattling of the permeant around its present position in the membrane and
53 yl]methanethiosulfonate (MTSES) molecule and permeant Au(CN)(2)(-) ions, were applied to either side
56 mined by whole cell labeling with a membrane-permeant biotin maleimide and a membrane-impermeant 2-((
57 cysteines, 8 were labeled with both membrane permeant (biotin maleimide (BM)) and impermeant (2-((5(6
60 ple kinetic model in which polyamines act as permeant blockers of Kir3.1/Kir3.4, but as relatively im
62 llent potency, is highly blood-brain barrier-permeant, but suffers from rapid first-pass metabolism.
63 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 ratio of fluorescence signals from membrane permeant (calcein) and membrane impermeant (propidium io
73 (PKA) inhibitor, inhibits the ability of the permeant cAMP analog cpt-cAMP [8-(4-chlorophenylthio)-cA
75 n vitro or induction of capacitation by cell-permeant cAMP analogs decreased the depolarizing respons
77 8- fold in RAW cells treated with a membrane-permeant cAMP analogue (8-bromo-cyclic AMP; 8-Br-cAMP),
79 amitochondrial cAMP, but along with membrane-permeant cAMP analogues, failed to induce measureable ma
81 alysis using the ionotropic receptor channel-permeant cation agmatine indicated that ONH axon segment
86 een dipolar carbonyl ligands, water, and the permeant cation, which allow for selective flow of K+ ov
87 etation of signals from fluorescent membrane-permeant cations (usually termed "mitochondrial membrane
88 , we identified a diverse group of minimally permeant cations for wildtype NaChBac, ranging in sizes
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
114 t and permeabilized glands, we used the cell-permeant, divalent cation chelator, tetrakis-(2-pyridylm
120 owever, it is unknown whether such ionizable permeants dynamically neutralize at the membrane surface
121 iabetic fatty rats by addition of a membrane permeant ester of a pyruvate cycling intermediate (dimet
122 en bonding and entropic factors arising from permeant flexibility substantially contribute to the ene
123 ng of the mTORC1 component RAPTOR and a cell permeant fluorescent analogue of di-leucine methyl ester
126 tance and are highly coupled via neurobiotin-permeant gap junctions, while midline cells are signific
128 rt the first total synthesis of the membrane permeant, hydrolytically stable, cADPR receptor agonist
129 that mitochondrial accumulation of membrane permeant, hydrophilic cations can be used to maximize lo
130 nts on the physicochemical properties of the permeants imposed by these channels must be better under
131 criterion for establishing that a blocker is permeant in a channel that has a complex permeation cycl
132 trast, changes in selectivity made gluconate permeant in L46P EAAT2, and nonstationary noise analysis
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 because of its ability to act as a membrane-permeant inhibitor of inositol 1,4,5-trisphosphate (IP3)
140 erichia coli beta-galactosidase and the cell-permeant inhibitor phenylethyl beta-D-thiogalactopyranos
145 n which occupation of either of two external permeant ion binding sites prevents Mg2+(o) entry into t
146 that differed in the locations and number of permeant ion bound; blocker dissociation occurs exclusiv
147 TRPM7 is a Ca(2)(+)-permeant and Mg(2)(+)-permeant ion channel in possession of its own kinase dom
148 (A) receptors (GABA(A)R), which are chloride-permeant ion channels, and GABA(B) receptors (GABA(B)R),
149 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
155 This regulation depends on the ability of a permeant ion to enter the selectivity filter (K(+) = Rb(
156 at the direction of the driving force on the permeant ion, as well as P(o), must be considered togeth
157 f C-type inactivation is a dependence on the permeant ion, but the mechanism by which permeant ions m
159 mode-shift of gating when having K(+) as the permeant ion; (ii) that Cs(+) or Rb(+), known to halt C-
160 unique in that its members display opposite permeant-ion charge selectivities despite sharing the sa
165 ted to gating and contains binding sites for permeant ions and pore-blocking molecules including quat
166 cking toxins show specific interactions with permeant ions and strong dependence on the ionic strengt
169 er a physiological electrochemical gradient, permeant ions are initially stabilized within the extrac
170 lter transport properties of hClC-4, varying permeant ions as well as mutating the "gating glutamate"
171 rturbed when positive charges occur near the permeant ions at a location that should counteract pore
173 ion channels have "charge rings" that focus permeant ions at the mouth of the pore and increase chan
174 with a tight binding, we show that external permeant ions enhance CTX-dissociation, implying a path
175 ly-Tyr-Gly signature filter sequence and the permeant ions generate four equidistant K(+) binding sit
177 riving force is coupled with the movement of permeant ions in the filter, maximizing the efficiency o
179 g and electrostatic repulsive forces between permeant ions is needed to achieve efficient conduction.
180 the permeant ion, but the mechanism by which permeant ions modulate C-type inactivation is not known.
182 CLC channels are also known to couple to the permeant ions via their binding sites in the ion-permeat
183 rse a long (>70 A) pore, displacing multiple permeant ions, en route to a high affinity binding site
184 d to activation and is modulated by voltage, permeant ions, pore-blocking drugs, and membrane cholest
197 rmeation mechanism, driven by a reduction in permeant [K(+)](o) following pore block (which would ret
200 ed nuclei were also loaded with the membrane-permeant low-affinity Ca(2+) probe fluo-5N AM which comp
201 ion; disruption of this complex using a cell-permeant LPA2-specific peptide reversed LPA2-mediated in
202 e were resolved and transport of hemichannel-permeant LY dye was visualized when the hemichannel was
203 ese channels are modulated by NO, a membrane-permeant messenger in various physiological and patholog
205 HCs were also less sensitive to block by the permeant MET channel blocker dihydrostreptomycin, whethe
206 we show that systemic injection of the brain-permeant mGlu2/3 receptor agonist (-)-2-oxa-4-aminobicyc
207 Recently, we discovered a class of cell-permeant miniature proteins (CPMPs) containing a precise
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
217 NAADP acetoxymethyl ester (NAADP-AM), a cell-permeant NAADP analog, increases cytosolic Ca(2+) concen
219 ported the potential of compound 37 as a BBB-permeant neuroprotective agent against H2O2-induced oxid
220 reover, 5b behaves as a water-soluble, brain-permeant neuroprotective agent against oxidative insults
221 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
230 nce, translocation, and exit of these simple permeants (one hydrophilic and one hydrophobic) can be s
233 icating that the increased tortuosity of the permeant path was effective on barrier properties of the
235 ing in regulating expression of the vascular permeant PDGF-B was confirmed in vitro using cell permea
236 urther demonstrate the efficacy of the brain-permeant PEGylated version of the anti-solTNF peptide, X
238 ably transduced with lenti-SUMO-1 and a cell-permeant peptide harboring SUMO-binding motif to interfe
239 pitating events that are sensitive to a cell-permeant peptide inhibitor of SRTF nuclear import (cSN50
242 e tag can be reduced acutely with a membrane-permeant phosphine, labeled with ReAsH, monitored in the
245 g GABAergic postsynapses by using a membrane-permeant PI3P derivative, time-lapse confocal imaging, e
248 age apoptosis in vivo with a small, membrane-permeant probe, TcapQ(647) was synthesized comprising a
254 ine residues to modification by the membrane permeant reagent N-ethylmaleimide (NEM) and the membrane
255 30 unique cysteine residues to the membrane-permeant reagent N-ethylmaleimide and the membrane-imper
257 zed that methylene blue (MB), a mitochondria-permeant redox-active compound that can act as an altern
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
279 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 eneration, human IAPP (hIAPP) forms membrane permeant toxic oligomers implicated in misfolded protein
288 the present study, we used the gap junction-permeant tracer Neurobiotin to compare the coupling patt
290 (PC2 or TRPP1, formerly TRPP2) is a calcium-permeant Transient Receptor Potential (TRP) cation chann
291 ng due to abnormal activation of the calcium permeant TRPC (Transient Receptor Potential Canonical) c
292 aused by depletion of the Ca(2+)- and Mg(2+)-permeant TRPM7 is suppressed by expression of a dominant
293 tive stimulus for acid taste is the membrane-permeant, uncharged acetic acid moiety (CH(3)COOH), not
294 y more strongly than did their more membrane-permeant unconjugated counterparts, suggesting that bile
295 exyl ester (RBHE), a fluorescent hydrophobic permeant, using dual-channel two-photon microscopy (TPM)
297 , an extracellular concentration gradient of permeant weak acid readily induces pH(i) nonuniformity.
298 by superfusion of acetate (salt of membrane-permeant weak acid), evoked a [Ca(2+)]i rise, independen
299 leimide (small, hydrophobic, and ER membrane-permeant), were monitored by Western blot analysis.