ライフサイエンスコーパス: SAR

1 SAR analysis of the new series of azetidinones enabled t

2 SAR analysis of the resulting analogs suggests that for

3 SAR analysis revealed the size of the aliphatic chains a

4 SAR analysis showed that the amine-binding region serves

5 SAR analysis, using cell culture assays, led to the disc

6 SAR identified a spirocyclic analogue 19 that inhibited

7 SAR investigation of fragment 1, aided by X-ray structur

8 SAR investigations around the screening hits provided a

9 SAR revealed tolerance for 4-Cl isosteres with 4-F (8),

10 SAR studies of 3-substituted indazoles yielded analog 7

11 SAR study indicated that the allyl group could be replac

12 SAR-related proteins THIOREDOXIN h3, ACYL-COENZYME A-BIN

13 nasal spray (MFNS; 200 mug daily, n = 2140) SAR or PAR trials.

14 ose a more restricted upper limit for HOU-3 (SAR approximately 3).

15 A SAR case was defined as the association between an oral

16 Rational design and a SAR study of this class of compounds led to a new series

17 These differences define a SAR of Tg for SPCA1a distinct from that of SERCA1a, indi

18 To close this gap, a SAR study was carried out to search for pHLIP variants w

19 ittle transmission occurring in its absence (SAR, 0.8% [95% CI, 0%-2.3%]).

20 ective of the present study is to develop an SAR (Structure-Activity Relationship) model that can be

21 Here, we report an SAR exploration of a series of biphenyl-N-[4-[4-(2,3-sub

22 series of fragment modifications revealed an SAR and, after several expansions, potent lead compounds

23 4.1), CRC (1.8 +/- 0.9; range, 0.4-6.6), and SAR (1.7 +/- 1.1; range, 0.3-3.9).

24 or further griseusin mechanism-of-action and SAR studies.

25 -independent component of SAR activation and SAR gene expression is revealed.

26 This article will detail the discovery and SAR of a potent and selective series of isoxazole based

27 ral pool syntheses, in vitro evaluation, and SAR studies of a series of d- and l-proline- as well as

28 ted molecular pattern-triggered immunity and SAR, which is targeted by multiple bacterial effectors.

29 Comparing mock- and SAR-induced phloem exudate proteomes, 16 proteins were e

30 Herein, we report the pharmacology and SAR studies both in vitro and in vivo of mitragynine pse

31 ays an important role in defense priming and SAR In addition, we show that Pst inhibits proteasome ac

32 ve oxygen species, and expression of SA- and SAR-related genes, including the SAR regulatory AZELAIC

33 The synthesis and SAR of a series of 4,5,6,7-tetrahydro-imidazo[4,5-c]pyri

34 in report the enantioselective synthesis and SAR of sterically constricted benzofurans at RXR.

35 Here, we report a shortened synthesis and SAR profiling of 4, enabling the design of analogues tha

36 ent work, we describe design, synthesis, and SAR study of a new series of compounds (1-16) obtained b

37 ompound preparation, biological testing, and SAR interpretation, robust and flexible synthetic routes

38 interferometry (InSAR) and multiple-aperture SAR interferometry (MAI) techniques were integrated to r

39 The Arabidopsis SAR phloem proteome is a valuable resource for understan

40 In beta-arrestin assays, SARs were different, indicating biased agonism.

41 AR-signal-producing mutant plants associated SAR with monoterpene emissions.

42 By developing cell-based SAR and using chemical proteomics, we identified pirin a

43 t vs proficient MMR had significantly better SAR (adjusted hazard ratio [AHR], 0.70; 95% CI, 0.52-0.9

44 MMR was significantly associated with better SAR, and this benefit was limited to primary tumors of t

45 biological and pharmacological activities by SAR studies.

46 experimental rate coefficients to calculate SAR factors for reduced organic nitrogen compounds.

47 sk factor was the provision of nursing care (SAR, 47.9% [95% CI, 23.3%-72.6%]).

48 Through careful SAR, the successful replacement of a polar pyrazole grou

49 s, in combination with the observed chemical SAR, suggest that Mitragyna alkaloids adopt a binding po

50 mplex and frequent complication of childhood SAR, with five distinct endotypes marked by peculiar pro

51 Classical SAR based cellular optimization provided us with a PORCN

52 Both results revealed cohesive SARs, demonstrating that the methylenedioxy functional g

53 optimize the CV profile, and these combined SARs led to the discovery of BMS-890068 (29).

54 We present comprehensive SAR of this inhibitor class as well as demonstration of

55 acid series of GPR120 agonists and conducted SAR studies to optimize GPR120 potency.

56 ack displacements produced with conventional SAR interferometry (InSAR) and multiple-aperture SAR int

57 nists, 18a and 25a, which further delineates SAR associated with allosterism at D3R and provides lead

58 The derived SAR along with free energy calculations and a consensus

59 Well-developed SAR models exist for beta-hematin inhibition, parasite a

60 s syringae pv tomato generates long-distance SAR signals that travel from locally infected to distant

61 This cell-based driven SAR produced compounds with strong single agent in vivo

62 During SAR, Pip orchestrates SA-dependent and SA-independent pr

63 role for these proteins in the phloem during SAR To identify novel components of SAR, transfer DNA mu

64 o understand the molecular regulation during SAR induction, we examined mRNA levels, microRNA (miRNA)

65 uced SA synthesis in systemic tissues during SAR.

66 Knowledge from empirical SAR investigations was combined with an understanding of

67 energetics, and mutagenesis studies enables SAR exploration to map GPCR-ligand binding hot spots.

68 stant leaves through the phloem to establish SAR In this study, a proteomics approach was used to ide

69 The established SAR, using whole cell functional assays, lead to the ful

70 SAR factors are an improvement over existing SAR models because they predict the experimental rate co

71 pproach gives new dimensions to the existing SAR and opens a new opportunity for the lead optimizatio

72 d structurally manipulate, exhibit exquisite SARs, are nontoxic, and elicit improved and qualitativel

73 Herein, we developed an extended SAR study using sumanirole (1) as the primary pharmacoph

74 We extended SAR by chemically manipulating the oxidation states of t

75 In this paper we describe an extension SAR study of pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimi

76 Herein, we report an extensive SAR study of this chemical series and identify the key p

77 For SAR that could not be rationalized through the cocrystal

78 ly abundant phloem proteins were assayed for SAR competence.

79 than with montelukast and desloratadine for SAR.

80 mplex molecules, highly diverse elements for SAR campaigns, integral components of peptidomimetic dru

81 ystemic Pip elevations are indispensable for SAR and necessary for virtually the whole transcriptiona

82 ng proteins (PDLP) 1 and 5 were required for SAR even though PD permeability in pdlp1 and 5 mutants w

83 was 5.4%, 8.5%, and 22.2%, respectively, for SAR trials, and 3.7%, 4.8%, and 11.2%, respectively, for

84 and KRAS (P = .02) by primary tumor site for SAR.

85 disparity provided the perfect templates for SAR investigation.

86 e enriched in phloem exudates collected from SAR-induced plants, while 46 proteins were suppressed.

87 parallel with SA The volatile emissions from SAR signal-emitting plants induced defense in neighborin

88 increase over 1-hour imaging time with high SAR can reach 2.5 degrees C.

89 Finally, a high-SAR regimen maximized the radiofrequency energy depositi

90 increase (0.31 degrees C +/- 0.21), and high-SAR regimens resulted in the highest increase (0.56 degr

91 Longer imaging time, especially with high-SAR regimens, can lead to an increase of 2.5 degrees C.

92 Achieving higher SAR is desirable for improved zeolite (hydro)thermal sta

93 d with the small set of available historical SAR data, they highlight both localized rates of high su

94 There was evidence of a decline in household SAR for direct contact between 1976 and 2014 (P = .018).

95 The estimated overall household SAR is 12.5% (95% confidence interval [CI], 8.6%-16.3%).

96 stress "druglikeness", and rapidly identify SAR trends.

97 y reduced PD permeability, yet also impaired SAR.

98 Improved SAR was observed for patients with deficient MMR tumors

99 ient cell, suggesting regulatory function in SAR.

100 PR-10 in salicylic acid pathway involved in SAR were significantly regulated.

101 regulatory role of PD-localizing proteins in SAR.

102 f novel spiropiperidine templates for use in SAR studies of beta-secretase (BACE) inhibitors and also

103 NA and miRNA regulation enhances AHO-induced SAR.

104 ke protein required for AzA- and G3P-induced SAR) and contributed to its intracellular partitioning.

105 ng an RNA-dependent ATPase assay and initial SAR study identified two different Brr2 inhibitors, 3 an

106 Building on the known SAR of this compound series, we now describe a number of

107 eumonia and influenza cases in the Hong Kong SAR, People's Republic of China, from 2004 to 2010.

108 nts NPR1 turnover under non-inducing and LAR/SAR-inducing conditions, but how cellular NPR1 homeostas

109 The second regimen consisted of five low-SAR sequences, for which three gradient-echo sequences w

110 Results Low-SAR regimens resulted in the lowest temperature increase

111 The main SAR trends identified within the series were substantiat

112 f SAR-related emissions of wild-type and non-SAR-signal-producing mutant plants associated SAR with m

113 agnets for diagnostic MR imaging with normal SAR regimens does not lead to temperature increases abov

114 Numerous SAR studies have revealed that the Arg(7) residue is ess

115 further details accounting for the observed SAR for this series.

116 mpounds in detail and explained the observed SAR, i.e. the strong dependence of the potency on a basi

117 Docking studies supported the observed SAR.

118 hE permitted rationalization of the observed SAR.

119 n indispensable switch for the activation of SAR and associated defense priming events and that SA am

120 phy coupled to mass spectrometry analyses of SAR-related emissions of wild-type and non-SAR-signal-pr

121 ble to rationalize a Free-Wilson analysis of SAR data from a fragment-based drug design project.

122 ostic tool and enables graphical analysis of SAR redundancy and project progression.

123 , which is consistent with the large body of SAR data that we have obtained.

124 but significant SA-independent component of SAR activation and SAR gene expression is revealed.

125 m during SAR To identify novel components of SAR, transfer DNA mutants of differentially abundant phl

126 RELATED1 were enriched in phloem exudates of SAR-induced plants, demonstrating the strength of this a

127 mmation, supporting the idea of an impact of SAR on cognitive functions.

128 oem exudates in response to the induction of SAR To accomplish this, phloem exudates collected from m

129 In this study, the influence of SAR on memory and multitasking performance, as two poten

130 ch should be considered in the management of SAR symptoms.

131 these results reveal the transport routes of SAR chemical signals and highlight the regulatory role o

132 oteins form complexes and act at the site of SAR establishment.

133 to different degrees in the distal tissue of SAR-activated plants.

134 substituents, scaffold hopping, transfer of SAR, conformation analysis, and molecular overlays.

135 The approach is based on the use of SAR matrix data structures as a diagnostic tool and enab

136 We primarily focus on SAR data for the different families of compounds and the

137 m exudates collected from mock-inoculated or SAR-induced leaves of wild-type Columbia-0 plants were s

138 Our SAR campaign also yielded RI(dl)-2 (hereafter termed 9h)

139 Our SAR results have also revealed that further modification

140 Here, we report our SAR studies that focus on modifications to various regio

141 the opioid receptor crystal structures, our SAR analysis of the common chemotype of AT-076 suggests

142 consistent between independent, overlapping SAR tracks covering a region 100 km in extent.

143 the cocrystal complex, we sought to predict SAR through a QSAR model developed in house.

144 Preliminary SAR correlations suggested that the nature of chains on

145 The present SAR of those CXCL12-oligopeptide grafts reveals the key

146 The principal SAR insight was that the hydantoin core of 1 is required

147 ation while maintaining the overall profile, SAR was developed at the C2' position for a series of cl

148 monoterpenes, particularly pinenes, promote SAR, acting through ROS and AZI1, and likely function as

149 These proposed SAR factors are an improvement over existing SAR models

150 cLogD values and the discovery of subtle PXR SAR that was not lipophilicity dependent.

151 itative) structure-activity relationship ((Q)SAR) analysis to show that the descriptors governing the

152 ive feature in the synthetic aperture radar (SAR) imagery of the sea surface.

153 , including normal specific absorption rate (SAR).

154 is of Ebola household secondary attack rate (SAR), disaggregating by type of exposure (direct contact

155 kers with patient survival after recurrence (SAR) of cancer is poorly understood but may guide manage

156 Structure-activity relationship (SAR) analysis led to the discovery of several more activ

157 Qualitative structure-activity relationship (SAR) analysis revealed that the presence of a methoxy gr

158 ry program, structure-activity relationship (SAR) analysis, as well as a detailed pharmacological pro

159 Through structure-activity relationship (SAR) analysis, we obtained an optimized lead compound (3

160 hesized for structure-activity relationship (SAR) analysis.

161 focused on structure-activity relationship (SAR) and structure-affinity relationship (SAfiR) studies

162 Structure-activity relationship (SAR) concerning primarily the length and flexibility of

163 as based on structure-activity relationship (SAR) data generated in vitro.

164 ET-specific structure-activity relationship (SAR) effort, and specific binding assessment using a LC-

165 Additional structure-activity relationship (SAR) efforts aimed both at increasing potency and improv

166 we describe structure-activity relationship (SAR) efforts that resulted in the optimization of novel

167 to further structure-activity relationship (SAR) for identifying RNase H inhibitors with antiviral a

168 ineated the structure-activity relationship (SAR) for these different targets and correlated them to

169 ounded upon structure activity relationship (SAR) fundamentals.

170 R), and its structure-activity relationship (SAR) has been extensively studied at the KOR to develop

171 volution of structure-activity relationship (SAR) information over a time course.

172 ll describe structure-activity relationship (SAR) leading to the discovery of 4 that is vastly improv

173 ion of this structure-activity relationship (SAR) led to the identification of (1S,2R,3S,4S,5R,6R)-2-

174 nsidered in structure-activity relationship (SAR) models.

175 nthesis and structure-activity relationship (SAR) of a novel series of 2,4,5-trisubstituted-7H-pyrrol

176 ssessed the structure-activity relationship (SAR) of Tg for SPCA1a by in silico modeling, site-direct

177 escribe the structure-activity relationship (SAR) of the antimalarial ozonide artefenomel (OZ439).

178 mation, the structure-activity relationship (SAR) of the quinolinol-5-sulfonamide scaffold was explor

179 o probe the structure-activity relationship (SAR) of the scaffold 1, we synthesized 14 analogs of com

180 xplored the structure-activity relationship (SAR) of this compound series to improve otoprotective po

181 tion of the structure-activity relationship (SAR) resulted in the identification of potent dual TAK1

182 e conducted structure-activity relationship (SAR) studies and explored three regions of this scaffold

183 n performed structure-activity relationship (SAR) studies by synthesizing a series of analogs of XIE1

184 Further structure-activity relationship (SAR) studies identified numerous analogues inhibiting TD

185 Further structure-activity relationship (SAR) studies led to 8, which had desirable potency (IC50

186 Structure-activity relationship (SAR) studies of 6 demonstrate that the absence of the th

187 the lack of structure-activity relationship (SAR) studies of these compounds.

188 neffective, structure-activity relationship (SAR) studies on cinnamic hydroxamic acid and benzo[b]thi

189 Further structure-activity relationship (SAR) studies on the recently identified pyrido[1,2-a]ben

190 subsequent structure-activity relationship (SAR) studies provided insights into conserved structural

191 Structure-activity relationship (SAR) studies resulted in a series of compounds with impr

192 Structure-activity relationship (SAR) studies were therefore completed here with 23 penta

193 systematic structure-activity relationship (SAR) study involving the bis-guanidinium toxin saxitoxin

194 A structure-activity relationship (SAR) study showed that, in the absence of the 3-OH group

195 performed a structure-activity relationship (SAR) study to investigate the effect of lipid chain leng

196 systematic structure-activity relationship (SAR) study to investigate the selectivity between EZH2 a

197 conducted a structure-activity relationship (SAR) study to probe ligand recognition features importan

198 uantitative structure-activity relationship (SAR) study, 25 disulfide bond-containing analogues were

199 From this structure-activity relationship (SAR) study, novel irreversible inhibitors were identifie

200 tigation of structure-activity relationship (SAR) utilizing biochemical and transformed Ba/F3 cellula

201 lot in vivo structure-activity relationship (SAR) was explored, evaluating the efficacy of its analog

202 pled with a structure-activity relationship (SAR) were investigated.

203 synthesis, structure-activity relationship (SAR), and evolution of a novel series of oxadiazole-cont

204 hemistry or structure-activity relationship (SAR), or appear to be of particular interest to the medi

205 mprehensive structure-activity relationship (SAR).

206 a revealed structure-activity relationships (SAR) and identification of potent new monobactam antibio

207 etails the structure-activity relationships (SAR) leading to a novel series of highly potent and sele

208 report the structure-activity relationships (SAR) of a previously reported small molecule ATX inhibit

209 ion of the structure-activity relationships (SAR) of the 4-, 6-, and 8-substituents of the quinoline

210 cidate the structure-activity relationships (SAR) of the resulting PSMA inhibitors.

211 ed through structure-activity relationships (SAR) studies.

212 xplore the structure-activity relationships (SAR) through the design, synthesis, and biological evalu

213 pronounced structure-activity relationships (SAR) with respect to inhibition of TAFIa.

214 unexplored structure-activity relationships (SAR) within the Mitragyna scaffold.

215 oration of structure activity relationships (SAR), the generation of oxidized metabolites, the blocki

216 to uncover structure-activity relationships (SARs) and guide drug design via microisolation-structura

217 lores both structure-activity relationships (SARs) and the biology of PBDs, and the strategies for th

218 Structure-activity relationships (SARs) at each of the structural subsites in 2 were explo

219 a study of structure-activity relationships (SARs) disclosed properties with respect to ring size, su

220 prehensive structure-activity relationships (SARs) for NNMT inhibitors.

221 delineate structure-activity relationships (SARs) for PPARdelta-selective targeting and structural m

222 Yet, no structure-activity relationships (SARs) have been identified to predict lipid self-assembl

223 expand the structure-activity relationships (SARs) in this family.

224 extensive structure-activity relationships (SARs) investigations were carried out on both its aromat

225 detail the structure-activity relationships (SARs) leading to a novel second generation series of pot

226 o generate structure-activity relationships (SARs) of INSL5 and use it to develop a potent and simple

227 ion of the structure-activity relationships (SARs) of this new class of small-molecule mouse Toll-lik

228 h-pointing structure-activity relationships (SARs) that provide guidance for further improvements in

229 Structure-activity relationships (SARs) were steep.

230 ion of the structure-activity-relationships (SARs) of the phenylthiazoles revealed two important stru

231 ance (LAR) and systemic acquired resistance (SAR) in adjacent and systemic tissues, respectively, and

232 (AHO) induces systemic acquired resistance (SAR) in Nicotiana.

233 Systemic acquired resistance (SAR) in plants is mediated by the signaling molecules az

234 Systemic acquired resistance (SAR) is a plant defense response that provides long-last

235 tablishment of systemic acquired resistance (SAR) is impaired in proteasome mutants, suggesting that

236 c compounds in systemic acquired resistance (SAR), a salicylic acid (SA)-associated, broad-spectrum i

237 hment of plant systemic acquired resistance (SAR), SAR-associated defense priming, and basal immunity

238 rmacotherapy for seasonal allergic rhinitis (SAR) and perennial allergic rhinitis (PAR).

239 Seasonal allergic rhinitis (SAR) caused by intermittent exposure to seasonal pollen

240 h, patients with seasonal allergic rhinitis (SAR) showed poorer school and work performance during pe

241 eated seasonal allergic rhinoconjunctivitis (SAR) on the basis of anti-allergic medication prescripti

242 with seasonal allergic rhinoconjunctivitis (SAR).

243 ecule glucokinase activators led to a robust SAR in agreement with structural data that also helped t

244 of plant systemic acquired resistance (SAR), SAR-associated defense priming, and basal immunity.

245 ximately 10% of CF recovery while sarcosine (SAR) showed insignificant effects.

246 , including design, validation, and selected SAR around the novel iminothiadiazinane dioxide core as

247 Sequential SAR studies led to the identification of highly potent a

248 analogs were examined to develop a stronger SAR profile.

249 inhibitor 27b, including details surrounding SAR, in vitro/in vivo pharmacology, and pharmacokinetics

250 t paper, we described the design, synthesis, SAR, and biological profile of a novel spirocyclic sulfo

251 Here, we present a systematic SAR investigation of the benzoxazolone carboxamides, a r

252 In contrast, our systematic SAR studies on [des-Arg(7)]Dyn A analogues found that Ar

253 On the basis of the systematic SAR study of U-II, we created 33 further short and linea

254 Transcriptome analyses reveal that SAR establishment in Arabidopsis is characterized by a s

255 Our findings suggest that SAR has a differentiated and complex impact on cognitive

256 The SAR data formed the basis for a three-dimensional pharma

257 The SAR study also identified a key residue (K(A15)) in the

258 ted compounds exhibited cytotoxicity and the SAR analysis showed that the intact D ring was indispens

259 ion, augmented by crystal structures and the SAR from the cyanopyridones, enabled us to drive the pot

260 Apart from the SAR exploration around the initial hits, the optimizatio

261 groups (P < .001) compared with those in the SAR group.

262 of SA- and SAR-related genes, including the SAR regulatory AZELAIC ACID INDUCED1 (AZI1) gene and thr

263 ibacter ubique and most other members of the SAR 11 clade of the Alphaproteobacteria, can evade filtr

264 tensive spatial and temporal coverage of the SAR dataset, present an unprecedented opportunity to ima

265 Further studies on the SAR of compound 2e may result in good anticancer activit

266 we examined the effect of cationicity on the SAR of these analogues.

267 resent work, we now further elaborate on the SAR of these compounds, which has led in turn to the ide

268 drug discovery campaign involves probing the SAR around one or more fragment hits.

269 TANCE8 photoreceptor) that contribute to the SAR response.

270 notherapy groups (P < .05) compared with the SAR group.

271 putational modelling was used to explain the SARs of certain key compounds and set the stage for the

272 These SARs may help predict the formation and survival of prot

273 Molecules stemming from this SAR exercise were theorized to be protease inhibitors.

274 natural products, including contributions to SAR development, mode of action studies, and eventually

275 dence for the mechanisms involved in tobacco SAR, which are likely to be present in other plants.

276 sary for virtually the whole transcriptional SAR response, a moderate but significant SA-independent

277 The prevalence of treated SAR cases rose by about 55% in 10 years.

278 and 2012, the total yearly number of treated SAR cases rose from 7265 to 11 315.

279 ome is a valuable resource for understanding SAR long-distance signaling and the dynamic nature of th

280 putational modeling, revealed the unexpected SAR of these carbasugar SGLT2 inhibitors, and enabled th

281 ense signaling and that SA accumulation upon SAR activation leads to the downregulation of photosynth

282 August 2014 M6.0 South Napa earthquake using SAR data from the Italian Space Agency's COSMO-SkyMed an

283 Interestingly, we find that in vivo SARs differ from those collected in vitro, and most impo

284 ained by the 2-W per kilogram of body weight SAR limitations) by using five single-shot turbo spin-ec

285 s with reduced monoterpene biosynthesis were SAR-defective but mounted normal local resistance and me

286 Associations of biomarkers with SAR were analyzed using Cox proportional hazards models

287 tumor on the association of biomarkers with SAR.

288 odynamically feasible to synthesize FAU with SAR=2-7, though kinetic factors seemingly impose a more

289 Non-medicated patients with SAR (n = 41) and healthy non-allergic controls (n = 42)

290 ushings were collected from 29 patients with SAR and 31 control subjects during and after the pollen

291 l barrier function, were DA in patients with SAR and control subjects, irrespective of season.

292 fferentially regulated between patients with SAR and control subjects, with inverse abundance dynamic

293 Moreover, when compared with patients with SAR, healthy subjects exhibit an antagonistic proteomic

294 ated proteins as biomarkers in patients with SAR, potentially playing an important role in its pathog

295 nctioning, was investigated in patients with SAR.

296 to-oncogene (KRAS) in the primary tumor with SAR in patients with stage III colon carcinomas treated

297 icantly associated with worse SAR, and worse SAR for BRAFV600E or KRAS mutant tumors was more strongl

298 .57; 95% CI, 0.40-0.83; P = .003), and worse SAR was observed for tumors of the distal colon with mut

299 1.21; 95% CI, 1.00-1.47; P = .052) had worse SAR compared with those whose tumors had wild-type copie

300 00E were significantly associated with worse SAR, and worse SAR for BRAFV600E or KRAS mutant tumors w