ライフサイエンスコーパス: potency

1 viruses as candidates to enhance therapeutic potency.

2 F moiety confers highly desirable anti-HIV-1 potency.

3 f the scaffold 1 key to high transcriptional potency.

4 ol-20-one, and ganaxolone showed the highest potency.

5 e secondary binding and arrestin recruitment potency.

6 tion and many exhibit remarkable breadth and potency.

7 stitution confers a significant reduction in potency.

8 as synthesized and observed to maintain MC4R potency.

9 d polarity plays an important role in drugs' potency.

10 nce in the environment and strong estrogenic potency.

11 erts in vivo, shows high DREADD affinity and potency.

12 l, and butyl produced a stepwise decrease in potency.

13 s, such as RGS14, with comparable or greater potency.

14 wn to selectively target 12/15-LOX with high potency.

15 l ester moiety were essential for inhibitory potency.

16 uently leading to a low-nanomolar inhibitory potency.

17 and conducted SAR studies to optimize GPR120 potency.

18 in, the best having an 8-fold improvement in potency.

19 everal positions in the adenine core enhance potency.

20 that target ASICs with high specificity and potency.

21 micromolar antihuman cytomegalovirus (HCMV) potency.

22 ellular regions can affect their therapeutic potency.

23 get cell membrane increases fusion inhibitor potency.

24 d enables high drug loading for improved ADC potency.

25 (PF-543) with 2 orders of magnitude improved potency.

26 nhance uptake to hepatocytes and to increase potency.

27 relate with Dectin-1 agonism, antagonism, or potency.

28 BC cells-could increase TNBC cell metastatic potency.

29 ceptor subtypes without compromising agonist potency.

30 O), activate both channel types with similar potencies.

31 und to provide improvements in antimicrobial potency (200-fold) against vancomycin-resistant Enteroco

32 is of agelastatin derivatives with excellent potency (50-100 nM) as modulators for cancer invasion an

33 emonstrated that there existed variations in potency across different batches of the intermediates an

34 compound 1C8 as displaying strong anti-HIV-1 potency against a variety of clinical strains in vitro.

35 inhibitor, Acriflavine, and demonstrate its potency against brain cancer.

36 ernative lead candidate 4ab with a nanomolar potency against CDK2 and CDK9 and potent antiproliferati

37 s (BKIs) that have nearly identical in vitro potency against Cryptosporidium but display divergent PK

38 omolar concentrations and displays excellent potency against hepatitis B virus (HBV) and varicella-zo

39 type-specific immune responses with limited potency against heterologous viral strains and genotypes

40 ion with front-line antibiotics enhanced the potency against M. tuberculosis by more than 100-fold, t

41 one with improved in vitro and intracellular potency against Mycobacterium tuberculosis, including mu

42 Th17 clones and rhIL-26 lacked antimicrobial potency against P. acnes.

43 ynergistic effect and significantly enhanced potency against three esophageal adenocarcinoma cell lin

44 increases in fluorescence with rank order of potencies among GABAAR isoforms consistent with results

45 progenitors (ETPs) are endowed with diverse potencies and can give rise to myeloid and lymphoid line

46 series of VHL inhibitors with low nanomolar potencies and improved cellular permeability.

47 ZnO-NPs and ZnSO4, displayed different toxic potencies and resulted in different profiles of expressi

48 strate channel, albeit with vastly different potencies and with differential interactions with specif

49 nificantly increased MOR binding and agonist potency and a distinct binding mode compared with its an

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

51 Besides traditional in vitro parameters of potency and affinity, kinetic parameters kon, koff and r

52 SCs) sit atop the landscape of developmental potency and are characterized by their ability to genera

53 On the basis of potency and bioavailability, we selected a small molecul

54 These bNAbs display remarkable potency and breadth of coverage against cell-free virus;

55 products, and methods to better assess their potency and composition are needed for adequate studies

56 -mimetic compounds can help to improve their potency and coverage of diverse HIV-1 strains.

57 inding domain gating ring, enhancing kainate potency and diminishing the ensemble of desensitized sta

58 ntifies known cell subpopulations of varying potency and drug resistant cancer stem-cell phenotypes,

59 herefore sought an ultra-stable analog whose potency and duration of action on intravenous bolus inje

60 can have an impact on both their reinforcing potency and effectiveness, and suggest that such interac

61 In our hands, its potency and efficacy are comparable or superior to MRE26

62 holesterol-conjugated siRNAs increases their potency and efficacy in vitro, but when delivered system

63 novel targeting moiety for MM to improve the potency and efficacy of BTZ in MM cells and reduce the s

64 Induction period modulated potency and efficacy of response depending on cell line

65 Gi/o-proteins, while reducing or suppressing potency and efficacy toward beta-arrestin recruitment.

66 thienopyrimidinone SIRT2 inhibitor with good potency and excellent selectivity for SIRT2.

67 pe I p38alpha MAP kinase inhibitor with high potency and excellent selectivity in vitro and in vivo.

68 tion of the carboxylic acid, improving DGAT1 potency and gut permeability.

69 thesized novel amide derivatives that retain potency and have much improved solubility.

70 However, its relatively low neutralizing potency and high cost have limited its use to a restrict

71 ive aminomethyl linker that delivers similar potency and improved brain penetration relative to the a

72 nship (SAR) efforts aimed both at increasing potency and improving pharmacokinetic properties led to

73 Optimization of the series for potency and increased duration of action commensurate wi

74 ane-permeable compounds in terms of cellular potency and intracellular target engagement, compared wi

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

76 Indeed, Li et al. showed that the potency and magnitude of multiple HIV-1 broadly neutrali

77 e determined, allowing optimization of PDE1B potency and PDE selectivity.

78 We compared in vitro and in vivo the potency and protective efficacy of 5C4 and the murine pr

79 have been explored to improve antimicrobial potency and provide additional synergistic mechanisms of

80 We aimed to improve human nNOS potency and selectivity and reduce off-target binding by

81 compounds' basic scaffold could enhance the potency and selectivity for ALDH1A1 or ALDH2 and generat

82 lar strategies could be used to quantify the potency and selectivity of inhibitors of a variety of mi

83 insights into the structural determinants of potency and selectivity of these inhibitors.

84 lar contacts that explain the high levels of potency and selectivity we have measured.

85 ation of cancer cells and optimized hits for potency and selectivity, both in vitro and in cell cultu

86 known LRRK2 inhibitors rationalized compound potency and selectivity.

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

88 oncogenic Hippo pathway, and possessing the potency and stability necessary for consideration as a d

89 makes it a useful reagent for measuring both potency and stability.

90 lowing simultaneous monitoring of anti-tumor potency and systemic off-tumor toxicity, micromolar affi

91 ic and therapeutic applications due to their potency and their complementary neutralization patterns

92 D4mc should assist efforts to optimize their potency and utility.

93 icity of endogenous gene expression, and the potency and versatility of the system will enable high r

94 Td-246, which exhibits superior selectivity, potency, and antitumor activity.

95 portant determinant of antibody neutralizing potency, and defining the mechanisms of neutralization h

96 ty over host enzymes, improving antiparasite potency, and improving metabolic stability.

97 possesses notable biophysical properties and potency, and provide a platform for the cytosolic delive

98 stringent criteria for product homogeneity, potency, and quality control, and may exhibit a distinct

99 uding information regarding their structure, potency, and selectivity.

100 ding specificity, neutralization breadth and potency, and sequence/structural homology were observed

101 Significant improvements in delivery, potency, and stability have been achieved through modifi

102 y for the discovery and optimization of high-potency antibodies have greatly increased the chances fo

103 ation of the ATC series gave improvements in potency, aqueous solubility, and metabolic stability, wh

104 onucleotide drugs is that their delivery and potency are derived primarily from the chemical structur

105 y the lipophilicity of an anesthetic and its potency are generally proportional.

106 Decreases in cellular vs recombinant potency are often anticipated or explainable.

107 34 (RTICBM-74) had similar potencies as 2 in all in vitro assays but showed signifi

108 ands but displayed a range of efficacies and potencies as antiproliferative and ERalpha-downregulatin

109 001 also chelates copper, which enhanced its potency as a PTP1B inhibitor.

110 ore reliable results to evaluate antioxidant potency at high temperature.

111 ribbon and bead isomers typically have lower potency at nAChRs than the globular form.

112 in the same procedure, and find that cocaine potency at the DAT also tracks differences in perseverat

113 d alpha-GID[V13Y], had substantially reduced potency at the human alpha7 nAChR relative to alpha-GID,

114 idue previously shown to increase antagonist potency at the mMC4R.

115 okine reporter cell assays, we verified that potency at TLR7 correlates with IFN-alpha/beta productio

116 se-additive predictions of mixture mutagenic potency based on the concentrations and potencies of a s

117 were distinct differences in the effects and potencies between the different bisphenol chemicals.

118 lly, we identified differences in tau strain potency between AD-tau, CBD-tau, and PSP-tau in non-Tg m

119 xplanation for the differences in inhibitory potency between glucosyl and glucosaminyl derivatives an

120 -translational modifications to achieve high-potency binding.

121 ng are providing further improvements in MAb potency, breadth, and half-life.

122 s A1 and A2 were reported to possess similar potencies but different rates of cellular intoxication a

123 onstrate drastically improved antiretroviral potency but also are characterized by an expanded spectr

124 reflected not only by reductions of antibody potency but also by decreases in maximum neutralization

125 hat some antibodies exhibit not only reduced potency but also decreased maximum neutralization capaci

126 d heroin "immunoantagonism", reducing heroin potency by >15-fold.

127 d chemotherapeutics such as cisplatin by its potency, cellular mechanism, and selectivity for MMR-def

128 neric topical steroid from the corresponding potency class may reduce drug expenditures.

129 est topical steroid within the corresponding potency class were $944.8 million and $66.6 million, res

130 apest topical steroid from the corresponding potency class.

131 oclonal antibodies exhibit indistinguishable potency compared to bioprocessed IgG and protect against

132 hibitory activity and diminished antioxidant potency compared to non-sonicated samples.

133 Degraders of BRD9 exhibit markedly enhanced potency compared to parental ligands (10- to 100-fold).

134 ffinity, metabolic stability, and inhibitory potency compared with aptamers with single modifications

135 t of B-cell malignancies, which has improved potency compared with other ADCs.

136 pe I IFNs, albeit with 100-1000-fold reduced potency compared with rmIFNalpha1 and rmIFNbeta.

137 05 nMAb neutralized DENV3 with extraordinary potency (concentration to achieve half-maximal neutraliz

138 Allergenic potency correlated well among the three fractions tested

139 The improvements in potency directly correlated with target tubulin binding

140 -cytotoxic compounds with high antiparasitic potency, drug-likeness, structural diversity and scienti

141 y vehicles, and ultra-precise dosing of high potency drugs.

142 en solution structures, MAIT cell activation potencies (EC50 3-500 pM), and chemical stabilities are

143 f cardiac stomach preparations, with greater potency/efficacy than ArPPLN1b and with similar potency/

144 ency/efficacy than ArPPLN1b and with similar potency/efficacy to the SALMFamide neuropeptide S2.

145 Standardization for potency enhances safety and efficacy of immunotherapy by

146 ted using a dose-addition model that employs potency equivalency factors (PEFs) for targeted carcinog

147 a sensory nerve activation assay and in vivo potency established against capsaicin-induced cough in t

148 timate, and risk assessment by whole mixture potency evaluations has been suggested.

149 be an endpoint for developing whole mixture potency factors (MPFs) for airborne PAHs.

150 than predicted by established in vivo-based potency factors.

151 eveloped RgIA4, a peptide that exhibits high potency for both human and rodent alpha9alpha10 nAChRs,

152 as a cellular damage biomarker, with a clear potency for further developments for in vitro diagnosis

153 biologically active in rats, with an in vivo potency for glycemic control surpassing that of native G

154 substrate channel differentially altered the potency for individual URAT1 inhibitors.

155 vealed compounds with higher transcriptional potency for PPARgamma and identification of moieties of

156 t, with the potential to enhance ADC in vivo potency for producing more efficacious ADCs.

157 of heavy metal poisonings as well as having potency for reducing inflammation.

158 ined whilst there was marked loss of agonist potency for signalling via Gq/11 and G12/13 G proteins.

159 onselective pyridazinone hit to deliver high potency for the PCAF/GCN5 bromodomain, high solubility,

160 resulting in an 8-fold increase in oxacillin potency, for a MIC of 16 mug mL(-1).

161 ority of CTLA4 molecules showing the largest potency gains in primary in vitro and ex vivo human cell

162 o-neutralize tier-3 pseudoviruses with great potency (GMT > 600).

163 This proneural potency gradient correlated directly with ATH protein st

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

165 his compound series to improve otoprotective potency, improve pharmacokinetic properties and eliminat

166 these two scaffolds, resulting in nanomolar potencies in an ATP synthesis inhibition assay.

167 felone and sulindac sulfide exhibited higher potencies in human blood from females, and bioactive 5-L

168 affinities to BET proteins and low nanomolar potencies in inhibition of cell growth in acute leukemia

169 tected in the environment linked to relative potencies in pathway-based bioassays.

170 alpha/delta) inhibitor AZD8835 showed marked potency in ABC DLBCL models, whereas the protein kinase

171 Clinical candidate 6 shows good potency in an IDO-1 human whole blood assay and also sho

172 targeting CD19 have demonstrated remarkable potency in B cell malignancies.

173 ogical tools, we showed that although a high potency in beta-arrestin recruitment is required to full

174 75/mivebresib), which demonstrates excellent potency in biochemical and cellular assays, advantageous

175 inhibitors exhibiting single digit nanomolar potency in both biochemical and cell based assays.

176 maximal S1P1 receptor internalization a high potency in both G alphai signaling and beta-arrestin rec

177 ed to afford IRAK4 inhibitors with nanomolar potency in cellular assays.

178 red to fully internalize S1P1 receptors, the potency in inducing G alphai signaling determines the ra

179 es, which includes not only the neutralizing potency in key cell types but also the ability to protec

180 compound, D3-2, displayed a 180-fold higher potency in the beta-arrestin recruitment assay (EC50 0.9

181 reased selectivity profile while maintaining potency in the CD69 hWB assay.

182 19 allergenic extracts are standardized for potency in the United States.

183 g an imidazole moiety, exhibited the highest potency in this series with some selectivity for PAD2, a

184 However, existing platforms suffer from low potency, inability to generate long-term immune memory a

185 Compound potency is also taken into account when identifying the

186 The model highlights that their sweetness potency is comparable to known natural sweeteners.

187 Often compound potency is determined from assays using recombinantly ge

188 lthough the anilide moiety affords excellent potency, it simultaneously introduces a third hydrogen b

189 nd ADMET properties of 5, combined with high potency, led to a predicted low oral dose in humans.

190 during vaccine transport could cause vaccine potency loss that could go undetected.

191 1 thiopeptides have much lower beta-arrestin potency, making them novel agonists with altered signali

192 target engagement, compared with biochemical potency measurements alone.

193 xposed to PAH mixtures (p.o.), and mutagenic potency (MP) values were determined for five tissues.

194 ese analogues exhibited balanced profiles of potency (Mycobacterium bovis BCG, M tuberculosis H37Rv),

195 HDAC6 while maintaining nanomolar inhibitory potency: N-hydroxy-4-[(N(2-hydroxyethyl)-2-phenylacetami

196 Attesting to its potency, nearly half of the system's components are enga

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

198 Previously, we isolated a high-potency neutralizing antibody, 5C4, that specifically re

199 enic potency based on the concentrations and potencies of a small number of targeted PAHs results in

200 cells and a correlation existed between the potencies of these two activities.

201 electivity score of 0.006 and an outstanding potency of 1.0 nM.

202 Broad cellular antiproliferative potency of 24 is supported by demonstration of JAK-STAT

203 Verinurad specifically inhibits URAT1 with a potency of 25 nM.

204 mor and its associated stroma, and prove the potency of a novel combined approach suitable for immedi

205 , respectively, based on a difference in the potency of acetylcholine to activate them.

206 The risk increased with increasing potency of acid inhibition and decreased after medicatio

207 re found to be important determinants of the potency of activation and entry inhibition.

208 21CFR680.3(e) states that when measured, the potency of an allergenic extract is assessed according t

209 The trapping potency of anchors is dictated by association rates and

210 y, and significantly enhanced the inhibitory potency of ATRA on HCC cell growth, improving IC50 by ov

211 lls from reactive metabolites, increased the potency of curcumin and decreased the amount of curcumin

212 and molecular conformation in antioxidative potency of dihydrocaffeic acid (DHCA) and dihydroferulic

213 of Earth's biosphere; for understanding the potency of disease-causing microorganisms; and in biotec

214 otypes in EV-producing cells can enhance the potency of EVs for vascularization.

215 alanine at position 168 (D168A) reduced the potency of grazoprevir, its combination with R155K unexp

216 inhibition is at the base of the exceptional potency of herbicides and potentially a target for the d

217 RanBP9 significantly diminishes the anti-tau potency of Hsp90/Hsc70 inhibitors as well as Hsc70 varia

218 ardiac-lineage cells; and test the embryonic potency of iCPCs via injection into the cardiac crescent

219 362 is responsible for the generally greater potency of KCa activators on KCa3.1.

220 Overall, these results highlight the potency of localized TRM deposition as a means of pathog

221 continues, the effects of increased use and potency of marijuana on water and wastewater treatment p

222 vironmental changes from pFUS also increased potency of MSCs in situ to further enhance their efficac

223 We evaluated the prevalence, breadth, and potency of NAb responses in 98 CRF07_BC-infected individ

224 This study examines the potency of neoadjuvant TSL HT combination therapy in two

225 ecent studies have highlighted the increased potency of oxygen analogs of organophosphorus pesticides

226 We studied the antiviral potency of pegylated interferon-alpha (pegIFNalpha) agai

227 phenyl group to improve the selectivity and potency of PI3Kalpha.

228 al evaluation with respect to efficiency and potency of selected bioreceptors and biotransducers.

229 ng variation in target copy number, inherent potency of sgRNA guides, and expression level of Cas9 an

230 Prior efforts to improve the in vitro potency of site II-specific antibodies did not translate

231 corresponding residue in KCa2.3 reduces the potency of SKA-121 by 7-fold, suggesting that R362 is re

232 However, the potency of such antibodies is generally low.

233 hese findings demonstrate a greater in vitro potency of tedizolid than linezolid against NTM and sugg

234 mechanism, which enabled us to optimize the potency of the analogs.

235 ost on burying beetles, which rises with the potency of the antimicrobial defence.

236 Resynthesis confirmed the potency of the compound, which suppressed viral RNA synt

237 l and simple strategy to greatly enhance the potency of the existing peptide-based HIV fusion inhibit

238 rofiles is likely to enhance the breadth and potency of the humoral immune response against HCV.

239 esults further reveal that the difference in potency of the positive modulators in potentiating SK2 c

240 muli further enhances both the diversity and potency of the response.

241 elicit target mutation, particularly if the potency of the sgRNA is also low.

242 Thus, the potency of the T cell response to histoincompatible tiss

243 h the aim to improve nuclease resistance and potency of therapeutic siRNAs by introducing 4'-C-methox

244 ry, with the aim to estimate the antiradical potency of these molecules.

245 Such enhanced retention may increase the potency of this chemotherapy agent and allow for reduced

246 These results highlight the potency of this model and raise the question of how usef

247 Here we compare the potency of two previously described inhibitors of wild t

248 then created fusions of both stability- and potency-optimized CTLA4 moieties with human Fc variants

249 limited by technical challenges such as low potency or poor biophysical properties.

250 ial to provide an adjuvant effect on vaccine potency, or, conversely, it might establish a temporary

251 NA with (S)-GNA resulted in greater in vitro potencies over identical sequences containing (R)-GNA.

252 inity type I IFNs did not increase antiviral potency over wild-type type I IFNs.

253 e receptor presented on cells with a similar potency (pEC50 values between 9.53 and 9.78) and efficac

254 lineages immediately, whereas others retain potency, preserving self-renewing features established e

255 the model on another azole with a different potency: prochloraz.

256 ly, several inhibitors exhibited exceptional potency profiles with EC50 values </=5 nM against major

257 eta production with an ApoE4 > ApoE3 > ApoE2 potency rank order.

258 sic properties of TS1 TEM reduced their GVHD potency relative to TS1 TN Posttransplant, TS1 TEM proge

259 in prioritizing building blocks with better potency: selection by a medicinal chemist, manual modeli

260 new insights into how these networks control potency, self-renewal, differentiation, and aging of hig

261 on 4T1 and PC3-luc cells, respectively, with potencies similar to chemically conjugated counterparts,

262 n the 20031 patients not receiving a maximal-potency statin (HR, 0.85; 95% CI, 0.78-0.93; P = .88 for

263 Of 7533 patients (27.3%) receiving maximal-potency statins, evolocumab significantly reduced the pr

264 C termini with the GPCR increases signaling potency, suggesting an altered GPCR conformation as the

265 ed antinociceptive efficacies with increased potencies than U50,488, 1 and 2 in the writhing assay an

266 uce hallucinations with greater duration and potency than closely related compounds.

267 with orders of magnitude higher carcinogenic potency than predicted by established in vivo-based pote

268 a structural basis for grazoprevir's higher potency than simeprevir, an inhibitor to which the doubl

269 re, drove fission with substantially greater potency than smaller, structured proteins.

270 antibody appears to possess the breadth and potency that may be needed if it is to be used in the tr

271 Despite this high potency, the therapeutic potential of GeXIVA is limited,

272 queous solubility relative to their cellular potency to be compatible with the intravenous (iv) dosin

273 ch for relating drug-target interactions and potency to discrete motivational states during a single

274 antibodies (bnAbs) with maximum breadth and potency to ensure therapeutic efficacy.

275 ning the N-alkyl substituent of 4-MA reduces potency to inhibit transporters, eliminates substrate ac

276 e demonstrated that the transition from full potency to lineage priming is prevented by inhibition of

277 n airway epithelial cells coincided with its potency to resolve AAI supports a crucial role for trans

278 e to undergo such tautomerism, were equal in potency to the phenoxy analogues and demonstrated select

279 efficacy and safety of dupilumab with medium-potency topical corticosteroids versus placebo with topi

280 benzenesulfonamide (73) that exhibited high potency toward CDK2 (IC50 0.044 muM) but was approximate

281 econd-generation derivatives to improve drug potency towards inhibition of their molecular targets.

282 xamined Rosa species demonstrated inhibition potency towards production of some monitored eicosanoids

283 ecular engineering of insulin itself and its potency, towards a viable GRI.

284 s expected to pave the way for improving the potency, toxicity, and ADMET profile of this series of c

285 sts that MMLs have led to increased cannabis potency, unintentional childhood exposures, adult cannab

286 Potency was assessed by a fluorescence-based assay measu

287 PI3Kbeta/delta inhibitors in which PI3Kbeta potency was built in a PI3Kdelta-selective template.

288 Cellular potency was enhanced >600-fold in the tris-POM prodrug (

289 Potency was enhanced by methylation of the quinoline and

290 dependent and non-dependent animals, but its potency was higher in alcohol-dependent rats.

291 contribution of TCR clonotype to inhibitory potency was investigated by delineating the responsivene

292 nger hinge binder and would impart increased potency when substituted for benzodioxole in paroxetine

293 or pyrimidine showed improved solubility and potency, whereas more hydrophilic side chains reduced VL

294 pproach to providing high bone-antimicrobial potency while minimizing systemic exposure.

295 imide scaffold was optimized to subnanomolar potency while retaining good physical druglike propertie

296 and epithelial type with little tumorigenic potency, while SP cells are very similar to triple-negat

297 t reduction in glutamate and glycine agonist potency, whilst D731N was non-responsive.

298 s (LTDs) to achieve the required therapeutic potency with minimal toxicity.

299 t1/2 The combination of higher stability and potency with prolonged pharmacokinetics could be compati

300 eral blood T cells, but also enhances T-cell potency, with edited cells vastly outperforming conventi