ライフサイエンスコーパス: selective inhibition

1 possibility of monitoring its modulation and selective inhibition.

2 alytic domain held little promise to achieve selective inhibition.

3 in flexibility appears to be responsible for selective inhibition.

4 dynamic signal profiles that are amenable to selective inhibition.

5 t the proteolytic sites directly but fail in selective inhibition.

6 oop pockets may be responsible for its HDAC6-selective inhibition.

7 karyotic cells, while also being amenable to selective inhibition.

8 s shown to be expressed by NK cells, and its selective inhibition abrogated CD16 and CD62L shedding,

9 This chemotype exhibits highly selective inhibition against ALDH1A1 over ALDH3A1, ALDH1

10 rvation that could enable therapeutic mTORC2-selective inhibition as a therapeutic strategy.

11 activity may be druggable and support HDAC3-selective inhibition as an attractive therapy in some tr

12 benzyl)-ATP as a phosphate donor and for its selective inhibition by 1NA-PP1 and 2MB-PP1.

13 The selective inhibition by alkaloids from the class produce

14 Here we report beta5i-selective inhibition by asparagine-ethylenediamine (AsnE

15 SOAT1-selective inhibition by BeauIII was reproduced in intact

16 important mechanistic component of substrate-selective inhibition by flufenamic acid, mefenamic acid,

17 d the extent to which they could prepare for selective inhibition by providing or withholding informa

18 n AlkB, which reveal it as being amenable to selective inhibition by small molecules.

19 Strategies to achieve selective inhibition continue to be intensively pursued,

20 d structural analysis showed that potent and selective inhibition could be achieved by just two subst

21 Combined knockdown of FIH and PHD-selective inhibition did not further increase pericellul

22 nance imaging data show that preparation for selective inhibition engages the inferior frontal gyrus,

23 e examine the behavioral and neural basis of selective inhibition focusing on the role of preparation

24 these inhibitors and the molecular basis of selective inhibition for PRMT1.

25 derlying mechanism responsible for substrate-selective inhibition has remained elusive.

26 or pan-group I, pan-group II, or PAK isoform selective inhibition has yet to be demonstrated.

27 onal ligand tethering (BOLT) and demonstrate selective inhibition (iBOLT) of protein function.

28 eveloped derivatives demonstrated potent and selective inhibitions (IC(50): 5.4-12 nM) compared to la

29 human homologs to suggest the possibility of selective inhibition if the MtTrxR-Trx interaction site

30 critical for resorptive function, and their selective inhibition in mature osteoclasts retards patho

31 ursued as attractive therapeutic targets for selective inhibition in patients with cancer.

32 As predicted, both lines demonstrated a selective inhibition in spontaneous release, suggesting

33 to decipher the driving forces that lead to selective inhibition in such cases.

34 iated platelet activation is attributed to a selective inhibition in VWF/GPIb-IX-induced phosphorylat

35 Our results suggest proactive selective inhibition is implemented within frontostriata

36 However, whether direction-selective inhibition is indispensable for direction sele

37 ctive drug targets to treat malaria as their selective inhibition leads to an arrest of the parasite'

38 dium, and raise the possibility that isoform-selective inhibition may allow inotropic responses witho

39 gnificantly to DMD arrhythmogenesis and that selective inhibition may provide substantial benefit.

40 ecular dynamics simulations to elucidate the selective inhibition mechanism of NQ inhibitors of ThyX

41 Our study suggests that selective inhibition of a distinct Hsp90 family member h

42 Our results demonstrate the selective inhibition of a highly conserved metabolic enz

43 lass of compounds that protect cells through selective inhibition of a lipid kinase, PIP4Kgamma.

44 We further show that selective inhibition of A(3)R-mediated signaling reduced

45 t MMV675968 inhibits A. baumannii growth via selective inhibition of AbDHFR and is therefore a promis

46 Selective inhibition of aberrant Cdk5 activity via genet

47 In myasthenic rats, selective inhibition of AChE is more effective in rescui

48 nt inhibition of NF-kappaBp65 activation and selective inhibition of activation of IFN regulatory fac

49 In summary, selective inhibition of activin A with a monoclonal anti

50 We aimed at determining whether selective inhibition of activin A would provide a regene

51 This event results in a selective inhibition of activity-dependent bulk endocyto

52 Selective inhibition of ADAM17 prevented the shedding of

53 The selective inhibition of ADAMTSs provides the possibility

54 nhances mammary tumor metastasis, results in selective inhibition of Akt3 expression and phosphorylat

55 Consequently, selective inhibition of ALDH3A1 could increase chemosens

56 Selective inhibition of alpha-helix-mediated protein-pro

57 phagia exhibited by BDNF mutant mice because selective inhibition of alpha2delta-1 by gabapentin infu

58 following suprathreshold neuronal activity, selective inhibition of alpha3 almost completely abolish

59 Under basal conditions, selective inhibition of alpha3 using a low concentration

60 ion of cyclin-dependent kinase 12 (CDK12) or selective inhibition of an analog-sensitive CDK12 reduce

61 Selective inhibition of APC might therefore be effective

62 We propose that selective inhibition of astrocytic GABA synthesis or rel

63 Our findings suggest selective inhibition of AT1 receptors within the nephron

64 f Huntington's disease (HD), suggesting that selective inhibition of ATM could provide a novel clinic

65 In addition, selective inhibition of AURKA suppressed cuSCC cell prol

66 Selective inhibition of BCAT1 activity results in decrea

67 Data presented herein demonstrate that selective inhibition of BD1 domains is sufficient to dri

68 we report a novel pharmacologic approach for selective inhibition of beta-catenin via targeting a cry

69 of the steviamine analogues showed good and selective inhibition of beta-mannosidase (Helix pomatia)

70 Importantly, selective inhibition of BIRC3 reversed therapeutic resis

71 uced neurodegeneration and demonstrates that selective inhibition of c-Abl may be neuroprotective.

72 We demonstrate that selective inhibition of calpain 1 activation improves wo

73 Selective inhibition of cancer cells remains a challenge

74 The selective inhibition of cancer-associated human carbonic

75 tivation of caspase-3 and conversely whether selective inhibition of caspase-3 would abate calpain ac

76 Selective inhibition of CaV1.3 over other LTCC isoforms,

77 KACh either in Cav1.3(-/-) mice or following selective inhibition of Cav1.3-mediated L-type Ca(2+) (I

78 CK increased cholesterol absorption, whereas selective inhibition of CCK1R and CCK2R with antagonists

79 ype and mutated p53, leading subsequently to selective inhibition of CDK2 and cyclin A expression and

80 By selective inhibition of CDK4/CDK6 with PD 0332991, which

81 Here we show selective inhibition of Cdk5/p25 -hyperactivation by TFP

82 To account for the selective inhibition of Cdk5/p25 activity, we propose th

83 Here we show that TFP5/TP5 selective inhibition of Cdk5/p25 hyperactivation in vivo

84 /cyclin T or CDK2/cyclin A, we conclude that selective inhibition of CDK9/cyclin T by members of the

85 Selective inhibition of cell adhesion, wound healing, an

86 THL treatment of M. tuberculosis resulted in selective inhibition of Chp2 over PapA3, confirming Chp2

87 uation of these inhibitors demonstrates that selective inhibition of CK1delta at sufficient central e

88 Selective inhibition of class IIa HDACs did not prevent

89 Selective inhibition of class IIa histone deacetylases a

90 In contrast, selective inhibition of class III PI3Ks does not activat

91 in coresident fibroblasts and was blocked by selective inhibition of CN or PKC alpha/epsilon or elimi

92 In this study, we show that selective inhibition of Cnk1 blocks growth and Raf/Mek/E

93 oma growth and invasiveness and suggest that selective inhibition of collagen prolyl 4-hydroxylase is

94 Furthermore, selective inhibition of corresponding circuit elements i

95 It is not known whether selective inhibition of COX-2 makes asthmatic responses

96 Behaviorally, substrate-selective inhibition of COX-2 reduced anxiety-like behav

97 pharmacological strategy involving substrate-selective inhibition of COX-2 to augment eCB signaling w

98 Only myofiber-selective inhibition of CTGF protected delta-sarcoglycan

99 While selective inhibition of CysLT(1)R has been used for trea

100 Selective inhibition of cytoplasmic Nsp1 or inactivation

101 educed excessive alcohol consumption, as did selective inhibition of D1-MSNs or excitation of D2-MSNs

102 ited distal cholesterol biosynthesis through selective inhibition of Delta(24)-dehydrocholesterol red

103 made to bring new chemical entities for the selective inhibition of DUBs based on these tools are al

104 et al. (2017) induce stem cell quiescence by selective inhibition of EGF/MAPK signaling and define cu

105 duces DNA damage repair gene expression, but selective inhibition of endogenous CDK12 is difficult.

106 astasis by inhibiting tumor angiogenesis via selective inhibition of endothelial cell proliferation.

107 knowledge for the first time, indicate that selective inhibition of EP2/EP4: (i) decreases growth an

108 Selective inhibition of EphB4 using a functional blockin

109 d kinase 1/2 (ERK1/2) in both cell lines and selective inhibition of ERK1/2 similarly decreases the b

110 Selective inhibition of exocytosis in SOD1G93A astrocyte

111 nyl fluoride analogs that exhibit potent and selective inhibition of FAAH.

112 gulants, which attenuate fibrin formation by selective inhibition of factor Xa or thrombin, has renew

113 Selective inhibition of FKBP51 has emerged as possible n

114 Selective inhibition of FtsZ polymerization without impa

115 Therefore, selective inhibition of GLS has gained substantial inter

116 ed increase in [Ca](i) levels was reduced by selective inhibition of GluA2-lacking AMPARs.

117 Selective inhibition of GOT1 with (aminooxy)acetic acid

118 Selective inhibition of GSK3beta is sufficient to mainta

119 These results suggest that selective inhibition of HDAC3 could be useful in treatme

120 Selective inhibition of HDAC3/6, but not specific HDAC1,

121 Selective inhibition of HDAC6 does not show cytotoxic ef

122 In particular, the selective inhibition of HDAC6 has been reported to decre

123 understanding of factors contributing to the selective inhibition of HDAC6, particularly regarding in

124 Indeed, selective inhibition of hepatic aPKC by adenoviral-media

125 old Kinase Suppressor of Ras 2 (KSR2) causes selective inhibition of hepatic GH signaling in neonatal

126 ffinity binding, the most effective, isoform-selective inhibition of HIF-2 in cells, and trigger the

127 ral input from the cranial dura, and found a selective inhibition of high-threshold but not wide-dyna

128 action may partly account for fremanezumab's selective inhibition of high-threshold, as a result of a

129 Selective inhibition of histone deacetylase 6 (HDAC6) is

130 Selective inhibition of hLDH5 using small molecules hold

131 Pharmacological selective inhibition of hOAT has been shown to be a pote

132 Previous studies reported potent and allele-selective inhibition of human huntingtin expression by s

133 P34.5beta protein level is attributed to its selective inhibition of ICP34.5 splicing, which results

134 h therapeutic potential for the targeted and selective inhibition of IgE-mediated allergic responses,

135 ed lumen patency via adaptive remodeling and selective inhibition of IH without affecting endothelium

136 These data support the use of selective inhibition of IL-23 to treat psoriatic arthrit

137 oth compounds bind to GP130 and demonstrated selective inhibition of IL-6 induced STAT3 phosphorylati

138 Both global IL-6 blockade and selective inhibition of IL-6 trans-signaling results in

139 Moreover, selective inhibition of inappropriately dispersed GAPDH

140 Furthermore, selective inhibition of individual GSK3 isozymes yields

141 Selective inhibition of individual ligands revealed that

142 cystine knot protein that shows exquisitely selective inhibition of insect V-ATPases.

143 To determine the effects of selective inhibition of intrarenal dopamine production,

144 be unique among IPKs, could be exploited for selective inhibition of IPK1 in future studies that inve

145 uences of cytokine/chemokine responses after selective inhibition of IRAK-1/4 or TAK1 in response to

146 This study was undertaken to investigate how selective inhibition of JAK with tofacitinib (CP-690,550

147 teraction, with ARS-1620, which demonstrates selective inhibition of K-RAS(G12C) mutant tumor models

148 nt interaction, ARS-1620, which demonstrates selective inhibition of K-RAS(G12C) mutant tumor models

149 Selective inhibition of KDAC isoforms while maintaining

150 nases and provides an opportunity for highly selective inhibition of kinase activity through a non-AT

151 ubstrates more potently leading to substrate selective inhibition of kinase activity.

152 Selective inhibition of LC-NE neurons during stress prev

153 ied two 2'-C-methyladenosine analogs showing selective inhibition of LRV1.

154 otentiates neutrophilic inflammation through selective inhibition of LTA4H aminopeptidase activity.

155 ncreased PGP, neutrophilic inflammation, and selective inhibition of LTA4H aminopeptidase, which ordi

156 Here, we shed light on how selective inhibition of MAO-A and MAO-B can be achieved

157 ted optogenetics to test the hypothesis that selective inhibition of mGlu(2) or mGlu(3) potentiates P

158 understanding the biological implications of selective inhibition of mGlu2 in the CNS.

159 Selective inhibition of microRNAs (miRNAs) offers a new

160 The selective inhibition of mitochondrial Ca(2+) uptake demo

161 etyl-p-benzoquinoneimine (NAPQI), caused the selective inhibition of mitochondrial complex II activit

162 These changes reflect selective inhibition of mitochondrial protein synthesis

163 Nonspecific inhibition of collagenases or selective inhibition of MMP-9 decreased pathological vas

164 n of a repressive form of Sp8 results in the selective inhibition of motor neuron generation and the

165 Later on, at 400 ms, a selective inhibition of motor resonance was found for ac

166 Selective inhibition of mPGES-1 might be a promising ste

167 of mTORC1 can be achieved in vivo, and that selective inhibition of mTORC1 significantly reduces the

168 Notably, selective inhibition of mTORC2 triggered proteasome-medi

169 a divalent cation binding residue can enable selective inhibition of mutant IDH1 and suggest that dif

170 However, selective inhibition of mutant IDH1 enzyme function coul

171 The compounds exhibit potent and selective inhibition of Mycobacterium tuberculosis, the

172 tes both in vitro and in vivo, and show that selective inhibition of N-myristoylation leads to catast

173 Selective inhibition of Na(V)1.6, while sparing Na(V)1.1

174 genetic inactivation procedure, which allows selective inhibition of neuronal ensembles identified by

175 Selective inhibition of neuronal nitric oxide synthase (

176 Pharmacological selective inhibition of neuronal NOS (nNOS) has the pote

177 These findings suggest that selective inhibition of NF-kappaB activation that result

178 In addition, selective inhibition of nitric oxide synthase 1 restores

179 kbones, play critical roles in their subunit-selective inhibition of NMDAR ion channels, a finding th

180 involved in diverse physiological functions, selective inhibition of nNOS over other isoforms is esse

181 Therefore, developing small molecules for selective inhibition of nNOS over related isoforms (eNOS

182 Selective inhibition of NOD1 and NOD2 signaling could be

183 stimulation of insulin secretion through the selective inhibition of Nogo-A could be a novel therapeu

184 Selective inhibition of oncogenic targets and associated

185 Conversely, selective inhibition of OSM by neutralizing antibody and

186 Such a rate regulation allows selective inhibition of osteosarcoma cells over hepatocy

187 se model in which p68 depletion results in a selective inhibition of p21 induction in several tissues

188 Here we show that the selective inhibition of p25/Cdk5 hyperactivation in vivo

189 Knockdown of pyrin and selective inhibition of p38 MAPK greatly attenuated casp

190 eatment for human cancer cachexia due to its selective inhibition of p38beta MAPK.

191 phthoflavone-like flavone derivatives showed selective inhibition of P450 1A1.

192 Selective inhibition of P450 enzymes is the key to block

193 Finally, we demonstrate selective inhibition of PABA biosynthesis in M. tubercul

194 se phenotypes are similar to those caused by selective inhibition of Pbp2x by methicillin that preven

195 function of the PD-1/PD-L1 axis, and suggest selective inhibition of PD-L1 on donor T cells as a pote

196 Here, we show that PAN-selective inhibition of PDE4, but not inhibition of PDE3

197 Antiplatelet therapy or selective inhibition of PDGFB might reduce biliary fibro

198 activated by designer drugs), we found that selective inhibition of Pdyn-expressing neurons in the r

199 he general mode of macrolide action involves selective inhibition of peptide bond formation between s

200 e-activity relationship study of AsnEDAs for selective inhibition of Pf20S over human proteasomes.

201 Nevertheless, our results indicate that selective inhibition of PfHsp70-x function using small m

202 Here, we show that selective inhibition of PFKFB3 activity by the small mol

203 Importantly, selective inhibition of PFKFB3 expression and activity u

204 Selective inhibition of PGF2alphaEA versus prostaglandin

205 uctokinase-1; and by marked G6P elevation by selective inhibition of phosphofructokinase-1; but not b

206 ctivation in EBV+ B cell lymphomas, and that selective inhibition of PI3Kdelta by either siRNA, or a

207 Selective inhibition of PI3Kgamma and PI3Kdelta (using P

208 elta deficiency prolongs graft survival, but selective inhibition of PI3Kgamma or PI3Kdelta reveals a

209 Selective inhibition of PKA activity in AgRP neurons par

210 Thus, potent and selective inhibition of PKCtheta is expected to block au

211 ies of docked alkaloids correlate with their selective inhibition of PLA2 activity.

212 e mycoplasma from the tumor cell cultures or selective inhibition of PNPHyor by a PNP inhibitor resto

213 Selective inhibition of polarized endothelial cell migra

214 Selective inhibition of PRDX6 blocks Galphai depalmitoyl

215 3-d in a panel of cancer cell lines showed a selective inhibition of proliferation of a subset of AML

216 mpounds synthesized by this method exhibited selective inhibition of proliferation of MCF-7 breast ca

217 We previously demonstrated that selective inhibition of protein kinase Ctheta (PKCtheta)

218 Also dissimilar to ToxB, selective inhibition of Rac does not inhibit MEK1/2/ERK1

219 In a manner similar to ToxB, selective inhibition of Rac induces CGN apoptosis associ

220 In contrast, selective inhibition of Rac induces CGN apoptosis by rep

221 to attenuate neuronal cell death induced by selective inhibition of Rac with NSC23766 but not apopto

222 Selective inhibition of Rac1 in just the proximal or dis

223 tion of estrogen receptor-alpha (ERalpha) or selective inhibition of RANKL in hematopoietic vs. mesen

224 and ALK that conferred dramatic responses to selective inhibition of RET (selpercatinib) and crizotin

225 Selective inhibition of RGS proteins increases G-protein

226 Selective inhibition of Rho GTPases (particularly Rac1)

227 ase-binding loop alone is sufficient for the selective inhibition of serine proteases or whether othe

228 ell proliferation, nahuoic acid A (1) showed selective inhibition of SETD8 in U2OS osteosarcoma cells

229 Selective inhibition of SGLT2 over SGLT1 is critical for

230 imization in our continued effort to explore selective inhibition of SIRT2 as a potential therapy for

231 Furthermore, selective inhibition of SMAD3 or CCT6A efficiently suppr

232 their potential therapeutic application for selective inhibition of smooth muscle cell proliferation

233 Hence, the selective inhibition of specific integrins is of great m

234 Selective inhibition of specific isoforms of the CDKs is

235 Selective inhibition of spinal 5-hydroxytryptamine-2 rec

236 he immunodominance hierarchy in part through selective inhibition of subdominant CD8(+) T cell prolif

237 Selective inhibition of T-channels and global deletion o

238 However, selective inhibition of TBK1 precludes phosphorylation o

239 Altered membrane events induced selective inhibition of TCR-induced phosphorylation of r

240 Selective inhibition of TGFbr2/ALK5 signaling in microgl

241 ed substructural features that influence the selective inhibition of the activation by p38alpha of th

242 ved aberrant Tau, but it remained unknown if selective inhibition of the activity of this Hsp70 isofo

243 chia coli by the T7 phage leads to rapid and selective inhibition of the bacterial RNA polymerase (RN

244 d strong interactions with DCs, resulting in selective inhibition of the binding of T(naive) cells to

245 tension with reduced side effects due to its selective inhibition of the C-domain.

246 major therapeutic challenge is the need for selective inhibition of the canonical pathway without im

247 Selective inhibition of the cytoplasmic class IIb HDAC6

248 Selective inhibition of the EP4 PGE(2) receptor by the s

249 More importantly, selective inhibition of the extracellular Hsp90alpha-Del

250 sed-loop optogenetic approach, we found that selective inhibition of the IL immediately after unreinf

251 The selective inhibition of the lipid signaling enzyme PI3Kg

252 The selective inhibition of the MAO-A and MAO-B isoforms was

253 rmal cells with suppressed tumorigenicity by selective inhibition of the MAPK/ERK/MYC signaling casca

254 rescue with mitochondria-targeted Ago2, and selective inhibition of the microRNA machinery in the cy

255 ed transcriptional coactivator BRD4 leads to selective inhibition of the MYC oncogene in multiple mye

256 ubtypes of malignant glioma are sensitive to selective inhibition of the NAD(+) salvage pathway enzym

257 Selective inhibition of the NKA alpha2 isoform by low do

258 These findings suggest that selective inhibition of the PI3K catalytic subunit p110d

259 Importantly, selective inhibition of the protein kinases Akt or mTOR

260 Ion parking depends upon the selective inhibition of the reaction of a selected charg

261 In addition, selective inhibition of the ROS generator NADPH oxidase

262 Selective inhibition of the slowly inactivating or late

263 Here, we report that selective inhibition of the subset of VMN neurons that e

264 In addition, selective inhibition of the TGFbetaRI/RII receptors was

265 Selective inhibition of the transporter protein sodium-g

266 ng, we implemented a novel strategy aimed at selective inhibition of the TrkB-activated signaling pat

267 step manner, and modeling indicated that the selective inhibition of the two P450 17A1 steps by the d

268 al connectivity between these two areas, and selective inhibition of these projections mimicked the b

269 Selective inhibition of these protein-protein interactio

270 l of megakaryopoiesis and reveal the lineage-selective inhibition of this axis as a likely mechanisti

271 ) influx is necessary for LTD induction, and selective inhibition of this distal dendritic Ca(2)(+) i

272 minant negative Hsc70 that resembles isoform selective inhibition of this important chaperone, we fou

273 nvestigated potential therapeutic effects of selective inhibition of this pathway in mice with establ

274 Selective inhibition of this Treg cell wave completely a

275 icidal and herbicidal activities through the selective inhibition of threonyl-tRNA synthetase (ThrRS)

276 also provide insights for IFN-gamma-mediated selective inhibition of TLR4-induced transcription.

277 Selective inhibition of TNF receptor (TNFR) 1 signaling

278 We here show the therapeutic potential of selective inhibition of TNFR1 and activation of TNFR2 by

279 Selective inhibition of translation of mRNAs harboring l

280 us to suggest a mechanism of action for the selective inhibition of TRPV5 and lay the groundwork for

281 interferon-gamma (IFNgamma), suggesting that selective inhibition of TYK2 kinase activity might be su

282 These effects were not mimicked by selective inhibition of VEGFR2 despite equivalent vascul

283 Here, we report that the selective inhibition of VLA-4 expression on B cells impe

284 ssive symptoms in humans and, because of its selective inhibition of VMAT-2, it preferentially deplet

285 ribe a novel role for IFN in the direct, and selective, inhibition of Cxcr2 chemokine ligands, which

286 ipomoeassin F results in a substantial, yet selective, inhibition of protein translocation in vitro

287 om in vitro and in vivo models confirmed its selective inhibition on the NLRP3 inflammasome and its b

288 ntrosomes, mitotic spindles and midbody, and selective inhibition or silencing of TBK1 triggers defec

289 Their selective inhibition over off-target CAs is expected to

290 veral of these exhibited a highly potent and selective inhibition profile against CA IX.

291 s highly expressed in tumor tissues, and its selective inhibition provides a potential target for the

292 different abasic duplexes achieve potent and selective inhibition, providing a broad platform for sub

293 is critical for osteoclast function, and its selective inhibition retards physiological bone loss.

294 s narrowly tuned and receives prominent odor-selective inhibition through both direct and indirect pa

295 ty profile of a ligand from ca. 100-fold SK1-selective inhibition, through equipotent SK1/SK2 inhibit

296 essing interneurons (FS-PARV), which provide selective inhibition to CCort pyramidal neurons.

297 ate that these interneurons convey direction-selective inhibition to wide-field neurons with opposite

298 studies provide a structural basis for Grp94-selective inhibition using site 3.

299 Substrate-selective inhibition was attenuated by the addition of t

300 This allosteric site allows for selective inhibition with respect to the homologous huma