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1 e ABL001 (asciminib), a potent and selective allosteric ABL1 inhibitor that is undergoing clinical de
4 our study provides a compelling and unifying allosteric activation mechanism in STKR1 kinases that re
6 s Asp residue in nSMase2 disrupts catalysis, allosteric activation, stimulation by phosphatidylserine
15 en the possibility that direct activation by allosteric agonism, rather than allosteric modulation, c
16 ere conducted using PAMs that also exhibited allosteric agonist activity, leaving open the possibilit
17 actions between the transmitter GABA and the allosteric agonists propofol, pentobarbital, or alfaxalo
18 ite, (ii) G-protein interactions at distinct allosteric and cognate sites on the GPCR, and (iii) asym
21 es, however, indicate multiple, interacting (allosteric), and co-existent, exo- and endofacial GLUT1
22 e, using a silent allosteric modulator as an allosteric antagonist, that BMS-986187 and BMS-986122 bi
24 information has precluded elucidation of the allosteric basis for the decreased DNA affinity in RcnR'
25 mutation is sufficient to change the global allosteric behavior of the dimer even when one subunit w
28 tudy provides first insights into a proposed allosteric binding pocket in BGT1, which accommodates th
30 osteric site in BGT1 that corresponds to the allosteric binding pocket revealed by the hSERT crystal
31 nt-based screening approach, we uncovered an allosteric binding site located near the beta8-beta9 loo
34 expands our understanding of the topology of allosteric binding sites in AChBP and, by extrapolation,
36 le binding sites may provide a new source of allosteric binding sites that could be exploited in the
41 n with computational modeling, identified an allosteric BTB-1-binding site near loop5, where it block
43 harmonic generation observations and reveal allosteric changes in the G receptor binding and F-activ
44 o hIRE1alpha LD's MHC-like groove and induce allosteric changes that lead to its oligomerization.
45 netics, which we faithfully reproduced by an allosteric channel gating scheme where the channel is ab
49 t Arabidopsis thaliana mutants for the three allosteric committed enzymes in the biosynthetic network
51 ulation approaches, the structure reveals an allosteric communication pathway that connects the dista
52 m (Dd) is proposed to be a key residue in an allosteric communication pathway that mediates actin-nuc
53 s not conform to the commonly held view that allosteric communication pathways generally originate at
54 hism towards inactivation through long-range allosteric communication within the structural ensemble
61 the C-terminal pilin domain exerts negative allosteric control over binding of the N-terminal lectin
63 nto cooperative aggregation, intermolecular (allosteric) cooperativity, intramolecular (chelate) coop
65 chemical shift changes provides evidence of allosteric coupling between the direct binding site and
66 ticular, we identify a prominent role in the allosteric coupling for the Na(+)-coordinating residue D
68 designed to disrupt millisecond motions and allosteric coupling to identify regions that are critica
70 l ensemble is populated at each point of the allosteric cycle and how ligands control these populatio
71 ent ligand-binding conditions throughout the allosteric cycle of the Escherichia coli Hsp70 DnaK by t
74 egulatory beta1-subunit, sensitizing AMPK to allosteric drugs, and activates signaling pathways that
78 ry near the M4 helix and exerts a long-range allosteric effect on the pore across domain-interfaces.
83 s been achieve using light, applied voltage, allosteric effects, chemical reagents, pH, and mechanica
88 ity are impacted by a collection of opposing allosteric features that inhibit or promote photoconvers
95 al electronic influence combined with a weak allosteric hydrogen-bonding interaction that significant
97 sites, isoform G-domain differences must be allosteric in origin, due to remote isoform-specific res
99 ant for the utilization of amino sugars, and allosteric inhibition of Adk activity by HPr-P, but not
100 -nanosecond motions impact zinc (Zn)-induced allosteric inhibition of DNA binding by the Zn efflux re
101 discovery efforts have focused primarily on allosteric inhibition of hFPPS and the discovery of non-
104 tal structure of LmFBPase complexed with its allosteric inhibitor AMP shows an inactive form of the t
106 port the identification of a highly specific allosteric inhibitor of Akt through a FRET-based high-th
109 a-IL-PFC treatment with apamin (KCa2 channel allosteric inhibitor) significantly enhanced extinction
110 The Si site offers a novel target site for allosteric inhibitors and a molecular explanation for th
111 adouts for the binding of the BPTES class of allosteric inhibitors as well as for inorganic phosphate
112 s were solved of the monomeric protease with allosteric inhibitors bound to the dimer interface site.
114 ctural constraints also explain one-third of allosteric inhibitors, a finding rationalized by crystal
115 f three structurally distinct NS5B palm site allosteric inhibitors, the high-throughput screening hit
118 rase (IN) binding to the viral RNA genome by allosteric integrase inhibitors (ALLINIs) or through mut
119 residue dependencies in the construction of allosteric interaction networks and signaling pathways.
122 l to directly quantify the thermodynamics of allosteric interactions, but usually falls short of enab
123 targets for many diseases, fully mapping an allosteric landscape of a molecular chaperone like DnaK
125 ics can be harnessed by nature to evolve new allosteric ligand specificities in a compact molecular s
126 ese sites are less well-conserved, therefore allosteric ligands have greater selectivity on the speci
128 ted the allosteric modulatory effects of two allosteric ligands, SRI-20041 and SRI-30827 on cocaine b
129 M macrocyclic peptide complex illuminated an allosteric, locked-open inhibition mechanism placing the
136 ne residues reveal a previously unidentified allosteric mechanism in which the binding affinity of LA
137 her investigated and found to display an ago-allosteric mechanism of action and increased stability i
139 Here, we find evidence of a PAM-induced allosteric mechanism revealed by microsecond molecular d
142 ng leads to rapid signal transduction via an allosteric mechanism, where global protein conformationa
146 mportant role for its bulky sidechain in the allosteric mechanism; we show that the energetic strengt
147 r TPR domains may be similarly influenced by allosteric mechanisms as a general feature of protein-pr
149 kinetics and elucidates the orthosteric and allosteric mechanisms regulating its channel gating.
150 iles that inhibit enzymes by active site and allosteric mechanisms, as well as disrupt protein-protei
153 ing of the orthosteric ligands, implying its allosteric mode of action at the Y4R and evidence for a
154 TGF-beta1 stimulation was ameliorated by the allosteric modifier of Sirt1 deacetylase, SRT3025, in as
155 es a highly sensitive yardstick to probe the allosteric modulation in contrast to the traditionally u
156 in gating and represents a hub for powerful allosteric modulation of AMPA receptor function that can
158 lecules act on synaptic transmission via the allosteric modulation of ligand-gated chloride channels,
161 provide insights into how substrate-coupled allosteric modulation of structure and dynamics facilita
162 f 9-aminoacridine compounds that demonstrate allosteric modulation of the alpha1A- and alpha1B-adrene
164 o identify level and type (positive/negative allosteric modulation or full antagonism) of mGluR5 modu
167 ctivation by allosteric agonism, rather than allosteric modulation, could be responsible for the adve
168 and stereochemistry can affect the degree of allosteric modulation, indicating an unforeseen selectiv
171 ore, treatment with orally bioavailable PAK4 allosteric modulator (KPT-9274) significantly impacted M
173 M1 receptor by a subtype-selective positive allosteric modulator (PAM) contributes to the gastrointe
174 f-administration, suggesting that a positive allosteric modulator (PAM) of alpha7 receptors, JNJ-3939
180 uggested a competitive mechanism between the allosteric modulator and the dibenzodiazepinone derivati
181 oreover, we provide evidence, using a silent allosteric modulator as an allosteric antagonist, that B
183 ects of cannabinoids by acting as a negative allosteric modulator of alpha7 nicotinic receptors (alph
186 dopamine receptors, was actually a negative allosteric modulator of D2- and D3-receptor dimers, thus
187 formulation of allopregnanolone, a positive allosteric modulator of gamma-aminobutyric acid (GABAA)
191 s regulators then co-binding with a positive allosteric modulator would greatly enhance their functio
196 utic utility of mGluR5 negative and positive allosteric modulators (an mGluR5 NAM and PAM) for TSC, u
200 Using novel mGlu receptor subtype-selective allosteric modulators along with knockout mice we now re
203 of quinoline-3-carbohydrazide derivatives as allosteric modulators of GSK-3beta are presented here.
209 entify further specific agonists or positive allosteric modulators of RXFP1, affirming the low drugga
210 Whereas numerous small-molecule positive allosteric modulators of the ligand-binding domain of (S
212 traditionally been pursued to target GPCRs, allosteric modulators provide several mechanistic advant
213 study may enable the design of new positive allosteric modulators selective for KARs, which will be
215 nesis studies indicate that agonist positive allosteric modulators target the same general region, bu
217 reveal a common binding pocket for negative allosteric modulators, present in both GLP-1R and GCGR a
218 uantify the potentiating effects of positive allosteric modulators, which can be used to quantify in
221 te that tyrosine 470 and 88 are critical for allosteric modulatory effects of SRI-compounds on the in
225 f alternative conformations (microstates) in allosteric molecules complicates interpretation of both
226 n binding experiments in the presence of the allosteric MR modulators W84 (8) or LY2119620 (9) (Schil
228 d attenuated the inhibitory potential of the allosteric myosin inhibitor pentabromopseudilin (PBP).
230 odel system, we sought to dissect a putative allosteric network linking a cryptic site at the dimeriz
231 nt-flow betweenness scores, we identified an allosteric network of residue-residue contacts between t
232 tly demonstrated that Src kinase features an allosteric network that couples substrate-binding sites.
233 lusion is accelerated when Na(+) binds to an allosteric, nonspecific site, leading to a 2-fold increa
234 tron microscopy revealed that substrates and allosteric nucleotides shift the equilibrium between act
236 esidue interactions that represent potential allosteric paths between catalytic and ligand binding si
238 tations pointed to an unexpected, long-range allosteric pathway towards the active site of the protei
242 Herein we report the identification of a new allosteric pocket on Ube2T through a fragment screening
244 elucidate the molecular mechanism of complex allosteric processes in large biomolecular systems.
246 d that the pilin domain is essential for the allosteric propagation within the lectin domain that wou
247 h opposite cooperative effects had different allosteric properties depending on the arrangement of th
249 We found that functional sites involved in allosteric regulation of Hsp70 may be characterized by s
250 to the chaperone activity is an ATP-induced allosteric regulation of polypeptide substrate binding a
251 s of topo II, and reveals a new mode for the allosteric regulation of topo II through modulation of A
254 catalytic mechanism, substrate specificity, allosteric regulation, and inhibition by a class of smal
255 tory mechanisms, including redox modulation, allosteric regulation, and protein oligomerization, that
260 referred physiological negative and positive allosteric regulators, adenosine 5'-monophosphate (AMP)
262 ional changes associated with the binding of allosteric regulatory proteins, and show that the greate
263 that the cis interaction with P2Y2R provides allosteric resistance to the membrane-normal motion asso
264 ribed herein streamlines design of synthetic allosteric riboswitches and small molecule-nucleic acid
270 majority of regulatory residues involved in allosteric signaling, suggesting that these sites could
271 structures revealed 3 binds to an unexpected allosteric site between the C-terminal and the N-termina
272 ng mode involving residues within TM10 in an allosteric site in BGT1 that corresponds to the alloster
274 thway connecting the active site to the main allosteric site that remains in the substrate-bound form
276 rtant insights into the structural bases for allosteric site-to-active site communication and for bet
278 rovides new insights into the mechanisms and allosteric sites [alpha(-)-interface containing] by whic
280 straightforward approach to identify hidden allosteric sites is demonstrated in protein tyrosine pho
281 were more significantly enriched at protein allosteric sites than tolerated mutations, suggesting a
282 t propofol is not binding at the ATP site or allosteric sites that modulate microtubule-activated ATP
284 -receptor dimers, thus identifying the first allosteric small molecule acting on these important ther
286 linker-docking site is available in only one allosteric state, that with high affinity for substrate.
287 -M306D mutation to uncouple the sTF-mediated allosteric stimulation of FVIIa provided a final complex
288 ure to translocate to nucleus, underlying an allosteric structural pathway for mediating ligand-induc
289 teristics may be necessary for regulation of allosteric structural transitions and could distinguish
294 Thus, these mutants represent a minimalistic allosteric system of FimH, useful for further mechanisti
295 ectral changes indicative of binding to both allosteric thumb sites I and II of NS5BDelta21 and induc
296 ys loop acts as a key control element in the allosteric transduction pathway for potentiating betaEST
297 e PDZ domain (PDZ2S) have indicated that the allosteric transition occurs on multiple timescales.
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