ライフサイエンスコーパス: high-potency

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

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

3 modify and irreversibly inactivate LSD1 with high potency.

4 ly activated alpha6beta2delta receptors with high potency.

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

6 sping and achieved both high specificity and high potency.

7 One population was blocked with high potency.

8 genes in transfected MCF-7 cells, also with high potency.

9 system as a desirable structural feature for high potency.

10 ythrine nor angoline inhibited activity with high potency.

11 secreted and integral membrane proteins with high potency.

12 ctivated Galphai with high specificity and a high potency.

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

14 8L pentamer) neutralized HCMV infection with high potency.

15 njugates that can selectively engage AR with high potency.

16 er confirmed the competitive interaction and high potency.

17 gainst the tumor cells, but some of them had high potencies against the L1210 cells and were more pot

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 All inhibitors showed very high potency against HIV PR in vitro, and their Ki value

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

62 hannels expressed in oocytes with relatively high potency and high selectivity.

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

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

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

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

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

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

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

70 .59 nM, selectivity versus MAO-A>6000-fold), high potency and selectivity are optimally combined with

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

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

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

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

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

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

77 The compound 4b similarly exhibited high potency and selectivity for the DAT.

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

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

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

81 The high potency and selectivity of L-054, 522 for sst2 will

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

83 g the cloned human transporters demonstrated high potency and selectivity of these compounds for the

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

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

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

87 New compounds with high potency and selectivity were identified.

88 position of the indolin-2-one (16) exhibited high potency and selectivity when tested against the PDG

89 d to the NMDA receptor ion-channel site with high potency and selectivity.

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

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

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

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

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

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

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

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

98 High potency and specificity towards a subset of human b

99 PKI-amide, a peptide that inhibits PKA with high potency and specificity, led to a reversible inhibi

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

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

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

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

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

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

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

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

110 These high-potency antagonists are >1000 times more potent at

111 ptors expressed in Xenopus oocytes show that high-potency antagonists at the NR1A/2B subtype are obta

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

113 lism (odds ratio 24.1 [3.3-172.7]) than were high potency antipsychotic drugs such as haloperidol (3.

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

115 -d]pyrimidine (14) which combined relatively high potency at 10(-7)-10(-8) M along with selectivity r

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

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

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

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

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

121 ected compounds indicated that despite their high potency at the DAT, these compounds stimulated loco

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

137 7 nM), and was activated by dY-bombesin with high potency (EC(50) = 1.8 +/- 0.5 nM).

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

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

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

141 did activate this receptor with efficacy and high potency equal to that of 9-cis-retinoic acid (9-c-R

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

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

144 cture may in part account for the relatively high potency exhibited by this inhibitor.

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

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

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

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

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

150 The high potency for inhibition of cathepsin K coupled with

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

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

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

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

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

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

157 ces flanking the RGS4 box were essential for high potency GAP activity.

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

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

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

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

162 ana-1,9(11)-dien-28-oate (29) have extremely high potency (IC(50) = 0.1 nM level).

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

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

165 , cyclo[Asp(4)-Dpr(10)]GnRH antagonists with high potencies in vitro and in vivo had been identified.

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

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

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

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

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

171 stability in vitro (T1/2(HLM) >120 min) and high potency in both RPA (pA2 = 8.9) and human bladder s

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

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

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

175 s a novel histone deacetylase inhibitor with high potency in inducing differentiation of cultured mur

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

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

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

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

180 Two analogues (1a,b) had extremely high potency in the mouse tetrad tests.

181 at the features contributing to the observed high potency in this series are the orientation of the 3

182 irality at the propanol 2-position is key to high potency in this series.

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

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

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

186 14 (K(i) = 0.15 nM) correlates well with its high potency in vivo (full inhibition of ovulation at 25

187 It also exhibits high potency in vivo.

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

189 New high-potency inhaled steroid preparations are clearly ef

190 e each required for receptor selectivity and high potency inhibition of receptor-coupled Gq signaling

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

192 ST is exceptionally sensitive to each of the high-potency inhibitors mentioned above.

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

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

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

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

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

198 study demonstrates that administration of a high-potency ligand that selectively desensitizes kainat

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

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

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

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

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

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

205 The compound with the best combination of high potency, low toxicity, and favorable bioavailabilty

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

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

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

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

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

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

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

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

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

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

216 The high potency of 67Ga, together with its low nonspecific

217 is study was to test the hypothesis that the high potency of adenosine and adenosine analogues to cau

218 of coronary conductance can explain both the high potency of adenosine to cause coronary vasodilation

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

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

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

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

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

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

225 The high potency of inhibition, coupled with high specificit

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

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

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

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

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

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

232 The high potency of selenocystamine in Gbetagamma inhibition

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

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

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 this peptide is likely to arise from the

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

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

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

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

246 g with [(3)H](-)-nicotine) while maintaining high potency on both insect nAChRs (Drosophila and Myzus

247 It also had high potency on in vitro inhibition of sst5 mediated int

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

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

250 ization of PAR2 receptors indicated that the high potency phase was mediated by PAR2.

251 The high-potency phenolic antagonist 21 and its low-potency

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

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

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

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

256 ecular modeling were used to rationalize the high potency resulting from incorporation of this struct

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

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

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

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

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

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

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

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

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

266 roxyl group of the propanol was required for high potency, since acylation or alkylation reduced acti

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

268 Marked LDL reduction (<100 mg/dL) with a high-potency statin provides superior efficacy for ather

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

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

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

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

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

274 rine IgG2b(lambda) antibody (NC10.14) with a high potency sweet tasting hap- ten, N-(p-cyanophenyl)-N

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

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

277 t extensive conformational analysis of three high-potency sweeteners: neotame, superaspartame, and SC

278 clotrimazole (CLT) blocks directly and with high potency the Ca2+-activated K+ channels of human ery

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

280 The ADF inhibits tubule secretion with high potency: the EC(50) is around 10 fM.

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

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

283 domain 7 of gpH2R (Ala-271 in hH2R) confers high potency to guanidines.

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

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

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

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

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

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

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

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

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

293 The high potency was also retained in analogue 2c.

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

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

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

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

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

299 didate molecules were predicted to bind with high potency (with R isomer binding stronger than S), bu

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