ライフサイエンスコーパス: high-potency

1 antibody against a broad range of H3N2 with high potency.

2 ctivated Galphai with high specificity and a high potency.

3 type II inhibitors are rare but usually have high potency.

4 tyl carbonate (2APT-D6) was selected for its high potency.

5 8L pentamer) neutralized HCMV infection with high potency.

6 njugates that can selectively engage AR with high potency.

7 BChE revealed the molecular basis for their high potency.

8 er confirmed the competitive interaction and high potency.

9 a pocket mimic that suggest sources of their high potency.

10 modify and irreversibly inactivate LSD1 with high potency.

11 ly activated alpha6beta2delta receptors with high potency.

12 oup is required at the 5-position to achieve high potency.

13 synthesis pathways, mechanism of action, and high potency.

14 bited beta-arrestin recruitment in CCR5 with high potency.

15 n shown to selectively target 12/15-LOX with high potency.

16 sping and achieved both high specificity and high potency.

17 secreted and integral membrane proteins with high potency.

18 ug due to its being long-acting and having a high potency against blood stage P. falciparum (Pf).

19 ed from films at lower temperature exhibited high potency against breast cancer cells.

20 Kalihinol B shows similarly high potency against chloroquine-resistant Plasmodium fa

21 of the newly synthesized compounds exhibited high potency against DNA-PK and potentiated the cytotoxi

22 c arenecarbonylcinnamoyl groups brings about high potency against drug efflux mediated by P-glycoprot

23 HSP targeted DOC conjugates exhibited high potency against DU145 cells with an IC(5)(0) of 2.4

24 otif in inhibitor 41H (GSK2236805) supported high potency against genotypes 1a and 1b as well as in g

25 The combination of high potency against HCMV deltaAla protease and high hum

26 The most active agent, 2j, showed high potency against human cancer cells with IC50s rangi

27 These compounds show modest to high potency against human umbilical vein endothelial ce

28 ber of these taxoids exhibited exceptionally high potency against multidrug-resistant cell lines, and

29 ability in rats, dogs, and monkeys while the high potency against PDE5 and desirable selectivity vers

30 ides the basis for developing novel PIs with high potency against PI-resistant HIV-1 variants with a

31 llins, transition state analogs that exhibit high potency against PNP in the malaria parasite Plasmod

32 tives, known as Hoechst nuclear stains, with high potency against poxvirus infection.

33 le addition to the antiviral inhibitors with high potency against resistant strains of HIV.

34 Compound 40 exhibits high potency against several BRAF(V600E)-dependent cell

35 proved metabolic stability while maintaining high potency against TbrPDEB1 and T. brucei.

36 These antibodies exhibited high potency against the 2009 virus in vitro, and one ex

37 Until recently, despite achieving high potency against the enzyme, these efforts have been

38 protein 5A (NS5A), such as daclatasvir, have high potency against the hepatitis C virus (HCV).

39 yl)dibe nzothiophen-1-yl]acetamide) combined high potency against the target enzyme (DNA-PK IC = 8 nM

40 FTY720 phosphate (FTY720P) is a high potency agonist for all the endothelial differentia

41 igh affinity" binding per se, but requires a high-potency agonistic interaction for its induction.

42 Lack of high potency agonists has restricted analysis of the G p

43 related compounds lodoxamide and bufrolin as high potency agonists of human GPR35.

44 Most derivatives proved to be high potency agonists of TRPA1, with a potency higher th

45 Unlike previously identified high potency agonists that are highly selective for huma

46 residue in the o3/TM7 region for gallamine's high potency, although 419Asn can substitute for 423Thr

47 tely specific to their in vivo targets, with high potencies and relatively few off-target side effect

48 These ligands with their high potencies and strong positive functional cooperativ

49 L-AP4 exhibited high potency and a pharmacological profile consistent wi

50 Despite these peptides high potency and ability to evade acquired bacterial dru

51 these mutant-complementing thyromimics show high potency and activity with a strong preference for t

52 -adenosyl position of NAADP while preserving high potency and agonist efficacy and an NAADP derivativ

53 egimens in sub-Saharan Africa because of its high potency and barrier to resistance, good tolerabilit

54 oach to target TfR1-tropic arenaviruses with high potency and breadth.

55 teristics of bicyclic peptides, coupled with high potency and chemical versatility, thus offer high-c

56 mouse skin shows that these analogs maintain high potency and efficacy for phase 2 enzyme induction a

57 ombinant human mGlu2/3 subtypes, a number of high potency and efficacy mGlu2 receptor agonists exhibi

58 Most interesting was the high potency and efficacy of this compound in blocking p

59 in several nude mouse xenograft models, with high potency and efficacy, when dosed either orally or i

60 ancer of ligand-induced MOR endocytosis with high potency and efficacy.

61 ies of JAK1-selective kinase inhibitors with high potency and excellent JAK family subtype selectivit

62 a type I p38alpha MAP kinase inhibitor with high potency and excellent selectivity in vitro and in v

63 a soluble catalytic subunit of V-ATPase with high potency and exquisite proteomic selectivity as reve

64 oach offers a variety of potential benefits (high potency and extended duration of action), concerns

65 of importance for design of inhibitors with high potency and favorable resistance profiles.

66 (CQ) and other 4-aminoquinolines have shown high potency and good bioavailability.

67 agents such as entecavir and tenofovir with high potency and high genetic barrier to resistance are

68 ssay showed that neither compound showed the high potency and kappa opioid receptor selectivity of JD

69 self from known RIP1 inhibitors in combining high potency and kinase selectivity with good pharmacoki

70 most serious threat to humans because of its high potency and long duration of action.

71 ssess high ligand efficiency: compounds with high potency and low molecular weight.

72 compound was chosen because of its combined high potency and low selectivity index.

73 nificant danger to opioid users due to their high potency and rapid acting depression of respiration.

74 ent of long-acting protein therapeutics with high potency and safety.

75 bis-aryl ureas as Limk inhibitors to obtain high potency and selectivity and appropriate pharmacokin

76 .59 nM, selectivity versus MAO-A>6000-fold), high potency and selectivity are optimally combined with

77 the first bile acid derivative endowed with high potency and selectivity at the FXR receptor, 3alpha

78 ompounds exhibited low cellular toxicity and high potency and selectivity for ADAM17.

79 mpaign produced several compounds possessing high potency and selectivity for GRK2 over other GRK sub

80 Twenty of the 22 new analogues had high potency and selectivity for PDE10A: 18a-j, 19d-j, 2

81 cell extracts, and living cells demonstrated high potency and selectivity for POP over FAPalpha and D

82 in vitro binding potency measured; four had high potency and selectivity for S1P1 (S1P1 IC50 < 10 nM

83 escribed a series of antagonists that showed high potency and selectivity for the NK(1) receptor.

84 dentify suitable lipophilic compounds having high potency and selectivity for vesicular acetylcholine

85 so-transdiene (MTD) and lobelane, which have high potency and selectivity for VMAT2.

86 We rationalize the high potency and selectivity of the oxazoles by molecula

87 he legendary magic bullet, i.e., a drug with high potency and selectivity toward a specific biologica

88 imidine -2,4-dione (43, UBP304) demonstrated high potency and selectivity toward native GLU(K5)-conta

89 Novel pyrazolopyrimidines displaying high potency and selectivity toward SRC family kinases h

90 New compounds with high potency and selectivity were identified.

91 aneously inhibit FAAH, Cox-1, and Cox-2 with high potency and selectivity.

92 er controlled-deactivation cannabinoids with high potency and short duration of action, we report the

93 In vivo pigmentation study shows high potency and short duration.

94 Key to these potential applications is their high potency and species specificity that enables a sing

95 ion directly to living yeast cultures caused high potency and specific stimulation of Hmg2p degradati

96 Peptide drugs offer the benefits of high potency and specificity but pose a significant deli

97 The lead compound, MB05032, exhibited high potency and specificity for human FBPase.

98 to induce matriptase activation, suggesting high potency and specificity of the induction.

99 High potency and specificity towards a subset of human b

100 tor tropomyosin-related kinase B (TrkB) with high potency and specificity, promoting neuronal surviva

101 eting the molecular target of rapamycin with high potency and specificity, the immunosuppressant and

102 entification of novel GSK3beta inhibitors of high potency and specificity.

103 ne proteins" (CLAMP), can yield ligands with high potency and specificity.

104 ine amines are unique CXCR4 antagonists with high potency and specificity.

105 escribed class of AC inhibitors that display high potency and systemic activity in mice.

106 d not be differentiated from 1b due to their high potency and the limit of our HTRF assay conditions.

107 n provides a bipartite inhibitor having very high potency and very low susceptibility to target-based

108 bitor (SCIN) protein exhibits a particularly high potency and was previously shown to block complemen

109 Pharmacological assessment revealed high potency and wash resistance (an index of membrane a

110 rhythms are maintained during treatment with high-potency and mid-potency CS in healthy skin.

111 BHPI's novel mode of action, high potency, and effectiveness in therapy-resistant tum

112 bodies having diverse epitope specificities, high potency, and wide breadth.

113 nology for the discovery and optimization of high-potency antibodies have greatly increased the chanc

114 odel, most of the RR/SS diastereomers showed high potency as dopamine reuptake inhibitors.

115 or obtaining potent CB receptor ligands with high potency at either CB(1) or CB(2) and a broad spectr

116 Compound 20 also displayed high potency at GSK-3beta.

117 compound 7 (ABT-239) elevated the series to high potency at H3R.

118 ne (Cpg); ZZZ = Phe, d-Phe; d-Nal(2')], show high potency at melanocortin receptors.

119 tial agonist at PPARalpha in addition to the high potency at PPARdelta.

120 post-translational modifications to achieve high-potency binding.

121 and [(3)H]norepinephrine (IC(50)=26 nM) with high potency but has weak effects on uptake of [(3)H]ser

122 ss-genotype-reactive antibody AR3A has shown high potency, but the ability of the virus to rapidly es

123 mACs are inhibited with high potency by 2 '(3')-O-(N-methylanthraniloyl) (MANT)-

124 tantly, these T(reg) cells can be induced to high potency by simply vaccinating against irrelevant Ag

125 e nicotine analogue epibatidine achieves its high potency by taking advantage of both the cation-pi i

126 The ready availability of high potency cannabis in south London might have resulte

127 bly because of the high prevalence of use of high-potency cannabis (218 [53%] of 410 patients) in our

128 ce in controls across the 11 sites of use of high-potency cannabis (r = 0.7; p=0.0286) and daily use

129 requency of daily cannabis use and in use of high-potency cannabis contributed to the striking variat

130 The use of high-potency cannabis is associated with cannabis use di

131 erlie neuropsychiatric risks associated with high-potency cannabis use.

132 The PAFs calculated indicated that if high-potency cannabis were no longer available, 12.2% (9

133 Given the increasing availability of high-potency cannabis, this has important implications f

134 investigate how frequent use of skunk-like (high-potency) cannabis in south London affected the asso

135 We also demonstrate that exosomes from high-potency cardiosphere-derived cells exhibit enhanced

136 cause a severe allergic reaction, suggesting high potency comparable with other tree nuts and peanuts

137 ith DCs for several hours after encountering high-potency complexes of peptide and major histocompati

138 mic properties of BACE1 inhibitor AZ-4217, a high potency compound (IC50 160 pM in human SH-SY5Y cell

139 tors of IDO exist, there remains a dearth of high-potency compounds offering in vivo efficacy and cli

140 nzyme binding site and a rationale for their high potency despite their small molecular size.

141 panel, Synergy Quad plate agar dilution, and high-potency disk diffusion screening methods for the de

142 livery vehicles, and ultra-precise dosing of high potency drugs.

143 o amine oxidases and low toxicity as well as high potency (EC50 = 1.4 muM) in inhibiting the uptake o

144 A lead compound 11a was identified as having high potency (EC50 = 4 nM) and 2.3-fold induction of the

145 S represents the first identified relatively high potency endogenous AHR ligand that plays a key role

146 ioavailability (approximately 100%) in rats, high potency (ET(A) IC(50) = 0.08 nM), and optimal ET(A)

147 Annonacinone showed high potency ex vivo on thromboelastography and was able

148 vity near that of wild-type alpha-RgIA, with high potency for alpha9alpha10 and low potency for alpha

149 While all tested chemotherapeutics revealed high potency for apoptosis induction in neuroblastoma ce

150 veral 5-substituted NAADP derivatives showed high potency for binding and full agonist activity for C

151 we developed RgIA4, a peptide that exhibits high potency for both human and rodent alpha9alpha10 nAC

152 The resulting compounds retain high potency for FKBP51 and excellent selectivity over t

153 It is concluded that, although high potency for inhibiting FDP synthase is favored when

154 The high potency for inhibition of cathepsin K coupled with

155 ther characterized conantokins, con-Br has a high potency for NMDA receptors with NR2D subunits.

156 in the C1b domain of PKCdelta abolished its high potency for phorbol 12,13-dibutyrate in vitro, with

157 idues from PKCdelta C1b (deltaC1b) conferred high potency for phorbol ester binding.

158 Despite high potency for purified Cry48Aa1/Cry49Aa1 proteins (LC

159 nt, nonselective pyridazinone hit to deliver high potency for the PCAF/GCN5 bromodomain, high solubil

160 Thus, gallamine and W84 derive high potency from the same receptor domains (epitopes in

161 o propionic acid 29 (BG9928), which retained high potency (hA1, Ki=7 nM) and selectivity for the aden

162 nts that inhibit system xc (-) activity with high potency have long been sought, but have remained el

163 These novel ROCK inhibitors possess high potency, high selectivity, and appropriate pharmaco

164 se inhibitors with some analogues exhibiting high potency (IC(50) < 2 nM) against CpIMPDH, excellent

165 High potency (IC50 = 16 nM) and FBPase specificity were

166 The high potency (IC50 of 31 nM [MMP-10] and 5 nM [MMP-13])

167 pment strategy is to identify molecules with high potency in animal models.

168 ding hexamers and nonomers with an extremely high potency in apoptosis induction.

169 macological tools, we showed that although a high potency in beta-arrestin recruitment is required to

170 BIR2 and BIR3 domains and achieve extremely high potency in binding and functional assays.

171 and maximal S1P1 receptor internalization a high potency in both G alphai signaling and beta-arresti

172 nactive troglitazone derivative, STG28, with high potency in cyclin D1 ablation.

173 rom this series, several compounds exhibited high potency in distinct functional assays in addition t

174 All analogues showed high potency in HL-60 cell differentiation and vitamin D

175 with acetylene groups at C-8a show extremely high potency in in vitro and in vivo bioassays for anti-

176 logically because the related compound 4 has high potency in inflammation models in vitro and in vivo

177 mode of 15a with c-KIT and may elucidate its high potency in inhibiting c-KIT kinase activity.

178 retain the structural features important for high potency in sulforaphane analogs: the sulfoxide or k

179 ost promising compounds in this report, with high potency in the cellular assay and a good overall pr

180 ty (Ki = 0.27 and 0.34 nM, respectively) and high potency in the GTPgammaS assay (EC 50 = 1.6 and 4.1

181 common to deserving candidate antimalarials (high potency in vitro against pan-sensitive and multi-dr

182 ellent pharmacokinetic profile and exhibited high potency in vitro and in vivo effecting c-Myc downre

183 ation mediated by EAPC2, but not EPAC1, with high potency in vitro.

184 It also exhibits high potency in vivo.

185 ving controller medications after the use of high-potency inhaled corticosteroids became common.

186 istidine converted rP2X2 from low potency to high potency inhibition.

187 al analysis revealed that the basis for this high potency is a unique sulfur-aromatic interaction net

188 onist, the molecular basis for its extremely high potency is not clear.

189 aminomethyl-5-chlorobenz ylamide (19b), with high potency (K(i) = 0.40 nM, 2x APTT = 0.18 microM), ex

190 Tipranavir inhibits wild-type protease with high potency (K(i) = 19 pM) and demonstrates durable eff

191 cleotides inhibited VC1:IIC2 with moderately high potency (Ki values in the 100 nM range).

192 ed this concept, favoring the development of high-potency kinase inhibitors.

193 ical and ADMET properties of 3 combined with high potency led to a predicted low oral dose in humans.

194 cal and ADMET properties of 5, combined with high potency, led to a predicted low oral dose in humans

195 We have characterized three high potency ligands that can be used to explore the phy

196 We observed that the most selective, high potency ligands were achieved through N(6)-adamanty

197 led that the purine 6-amino is essential for high potency, likely because of strong hydrogen bonding

198 We identified the first high-potency linear U-II analogues.

199 or =60 years old demonstrated efficacy of a high-potency live-attenuated Oka/Merck varicella-zoster

200 ferences in cardiotoxicity caused by low and high-potency local anesthetics.

201 amenable to long-acting therapy owing to its high potency, low in vivo systemic clearance and slow re

202 les decorated with the cognate receptor of a high potency, low solubility drug (Rapa) efficiently imp

203 The high potency, low toxicity, facile chemical synthesis, a

204 ts that display sub-maximal efficacy (~50%), high potency (<500 nM) and high selectivity for thrombin

205 A high-potency monovalent oral type 1 poliovirus vaccine (

206 of diarrhoea and other infections, a dose of high-potency mOPV1 is almost three times more effective

207 we present a series of novel, short-acting, high-potency MOR agonist/DOR antagonist ligands with ant

208 nt agricultural crop for the production of a high-potency natural sweetener, sensitive to low tempera

209 era from naturally infected subjects contain high-potency neutralizing activities specific for this c

210 We isolated a pre-F protein-specific, high-potency neutralizing antibody (5C4) that recognizes

211 Previously, we isolated a high-potency neutralizing antibody, 5C4, that specifical

212 Despite their high potency, NS5A inhibitors were slow to inhibit viral

213 Neural stem cells (NSCs) possess high potencies of self-renewal and neuronal differentiat

214 The high potency of 1-py correlates with its ability to incr

215 oraxella catarrhalis were minimal due to the high potency of ceftaroline.

216 or interactions and explain the unexpectedly high potency of certain inhibitors such as 3-(3H-imidazo

217 presence of Pro10 was found to be key to the high potency of conRl-B for NR2B, whereas the epsilon-am

218 igand binding pocket and likely underlie the high potency of Diprovocim.

219 Moreover, the high potency of E6 allowed us to administer this peptide

220 It is expected that the high potency of FA-displaying exosome in cytosolic siRNA

221 , we found that mFPR1 is responsible for the high potency of fMIVIL and fMIFL.

222 Therefore, our results indicate that the high potency of GA in cell culture and in vivo can be ac

223 The high potency of inhibition, coupled with high specificit

224 igen presentation by sDCs contributes to the high potency of lentivector-mediated genetic immunizatio

225 nuclear export inhibitors (NEI) maintain the high potency of LMB, are up to 16-fold better tolerated

226 The high potency of MalH-lectin conjugates results from "anc

227 n by the two antibodies and explain the very high potency of one of the antibodies.

228 te reductase (DHFR) inhibitors combining the high potency of piritrexim (PTX) with the high antiparas

229 combine the high selectivity of TMP with the high potency of PTX and TMX.

230 Together, these results help to explain the high potency of RDV against RNA viruses in cell-based as

231 The high potency of selenocystamine in Gbetagamma inhibition

232 O-binding landscape together with relatively high potency of such interactions translates into a cons

233 d 1 to platinate DNA, this suggests that the high potency of such photoactive platinum complexes is r

234 oward the natural hormone contrasts with the high potency of synthetic Gce agonists of disparate chem

235 D-Phe/D-Nal(2') residues, which explains the high potency of the corresponding peptides.

236 Our results demonstrate the high potency of the IBPR compounds in reducing tumorigen

237 the alternative pathway, which explains the high potency of the inhibitor.

238 The high potency of the target compounds together with the o

239 nd HCV cell culture models demonstrates very high potency of the top-scoring shRNAs.

240 n and the inhibitor provide insight into the high potency of this class of macrocylic compounds and m

241 The high potency of tipranavir results from a very large fav

242 In addition, the high potency of Toc-HDO results in a reduction of liver

243 The high potency of TP analogues in inducing the phase 2 res

244 Altogether, our results demonstrate the high potency of Ucns for improving dystrophic muscle str

245 ielding metabolically stable inhibitors with high potency on enzymatic, NanoBRET, and whole blood ass

246 , ideal targets for solid tumor targeting by high-potency oncology compounds.

247 Following stimulation with a high potency peptide and exogenous IL-4, CD4-dependent s

248 rase sites, other novel quinolones that have high potency, peptide deformylase inhibitors, and new li

249 However, only high-potency pMHC complexes expressed by DCs induced cal

250 f Ole e 1 exposure in Evora was explained by high-potency pollen originating from the south of Spain.

251 d IE63 expression in cadaver ganglia using a high-potency rabbit anti-IE63 antibody and corresponding

252 Focal cryotherapy shows very high potency rates and warrants further investigation.

253 onally constrained alpha-RgIA analogues with high potency, receptor selectivity, and enhanced human s

254 High-potency RSPOs may be of value for regenerative medi

255 ceptor binding assays, and we engineer novel high-potency RSPOs.

256 A systematically optimized high potency RXR agonist revealed activity in vivo and a

257 o elucidate the molecular mechanisms used by high-potency SCFADs, chromatin immunoprecipitation (ChIP

258 Budesonide is a high-potency, second-generation corticosteroid designed

259 s can be used to deliver PTP inhibitors with high potency, selectivity, and cellular efficacy.

260 One compound, 20, displayed high potency, selectivity, and good human nNOS inhibitio

261 desirable pharmacological benefits including high potency, selectivity, and prolonged target inhibiti

262 this series based on its overall profile of high potency, selectivity, low brain penetration, lack o

263 The high potency, significant gene induction, excellent PK p

264 cy users (ie, daily use in all 24 months) of high-potency (skunk-like) cannabis had the worst outcome

265 P-ATP III LDL-C goal of <70 mg/dl, even with high-potency statin therapy.

266 ulation; however, given their low-potency, a high-potency statin, such as atorvastatin, may be necess

267 When generic high-potency statins are available, noninvasive cardiac

268 High-potency steroids have been shown to cause growth re

269 ease in cannabis use and the availability of high-potency strains.

270 ribed for all other evaluated drugs, and its high potency suggests that mAbs like J199 offer an econo

271 ) antibody NC6.8 Fab fragment complexed with high-potency sweetener compound SC45647 and nontasting h

272 ity of 2 sugars (glucose and fructose) and 2 high-potency sweeteners (neohesperidin dihydrochalcone a

273 is likely a discriminator for super- versus high-potency sweeteners, which can be exploited in the d

274 o two categories: low potency (THC <10%) and high potency (THC >=10%).

275 Despite this high potency, the therapeutic potential of GeXIVA is lim

276 taining deimmunized HN3-T20 immunotoxins are high-potency therapeutics ready to be evaluated in clini

277 Thus, while a high potency therapy usually is less effective when give

278 specific competitive antagonist with equally high potencies to mouse, rat, dog, and human GIP recepto

279 fold of imatinib but which bind with equally high potency to c-Src and Abl.

280 ata show that T(reg) cells can be induced to high potency to non-disease-inducing Ags using a bacteri

281 can prioritize small molecules that present high potency to reverse expression of signature genes fo

282 approach, we predict four compounds showing high potency to reverse gene expression in liver cancer

283 ers that achieve the required combination of high potency to tumors and low hepatotoxicity to provide

284 icosteroid treatment received rituximab with high-potency topical corticosteroids as first-line treat

285 For disease limited to the nails, high-potency topical corticosteroids with or without cal

286 , we found ARM-Ps to exhibit extraordinarily high potencies toward PSMA, compared to previously repor

287 mino) benzenesulfonamide (73) that exhibited high potency toward CDK2 (IC50 0.044 muM) but was approx

288 to be good mimics of AMPs in terms of their high potency toward microbes and low hemolytic activitie

289 ting DDS works exactly as designed and shows high potency toward specific cancer cell lines, thereby

290 y five-times increased odds for daily use of high-potency types of cannabis (4.8, 2.5-6.3).

291 tion of neutralization potency revealed that high potency was a predictor of survival.

292 Also exhibiting a relatively high potency was thiol-conjugate M13, with IC(50) values

293 While the N-propyl group was crucial for high potency, we hypothesized that the terminal methyl m

294 Although several compounds showed high potency when assayed against Plasmodium falciparum

295 onfiguration but retaining coplanarity has a high potency, whereas the N-trifluoromethanesulfonylimin

296 ibodies show minimal affinity maturation and high potency, which is promising for vaccine design.

297 cleotides inhibited telomerase activity with high potency, which was not observed with Scramble or Mi

298 However, the high potency with nNOS as well as high selectivity of nN

299 CoV-2 in vitro, nine of which exhibited very high potency, with 50% virus-inhibitory concentrations o

300 used to study miRNA function and can achieve high potency, with low cytotoxicity.