ライフサイエンスコーパス: selective inhibitor

1 ic dimethylation after PRMT5 inhibition by a selective inhibitor.

2 dentified a flavone compound, luteolin, as a selective inhibitor.

3 ther, posing a challenge for the design of a selective inhibitor.

4 17 selective inhibitor, but not by an ADAM10 selective inhibitor.

5 he flap pocket substituent led to one Plm IV selective inhibitor.

6 characterization, and development of potent, selective inhibitors.

7 COX-2 is also inhibited by COX-2-selective inhibitors.

8 on hABHD6 limits the discovery and design of selective inhibitors.

9 specific exosites also provides targets for selective inhibitors.

10 el readout of covalent activity for complex, selective inhibitors.

11 rol of dephosphorylation by conformationally selective inhibitors.

12 translate this knowledge into the design of selective inhibitors.

13 occupied, comprising a novel class of dimer selective inhibitors.

14 ha (HIF-1alpha) signaling was assessed using selective inhibitors.

15 he binding site of chroman-4-one-based SIRT2-selective inhibitors.

16 tion confirmed further by gene knockdown and selective inhibitors.

17 pment of rigorously characterized potent and selective inhibitors.

18 hobic pocket that was used to design isoform-selective inhibitors.

19 manner that is sensitive to certain Aurora-A-selective inhibitors.

20 over a new class of orally bioavailable BRD4-selective inhibitors.

21 how they can be leveraged for the design of selective inhibitors.

22 odomain (BD2) bias, to potent and highly BD2 selective inhibitors.

23 his knowledge can guide the design of fungal-selective inhibitors.

24 the basis for the development of potent and selective inhibitors.

25 nes that could not be observed for BD family selective inhibitors.

26 he host environment and to rationally design selective inhibitors.

27 way has been explored for the development of selective inhibitors.

28 truncating adenomatous polyposis coli (APC)-selective inhibitor 1 (TASIN-1), a small molecule that s

29 in, we describe the first highly potent PAD1-selective inhibitors (1 and 19).

30 uided molecular design to develop potent and selective inhibitors (10d and (S)-17b) of matrix metallo

31 without associated bleeding risks, the NOX1-selective inhibitor 2-acetylphenothiazine (2APT) and a s

32 0 inhibitors were not evident with our Grp94-selective inhibitor, 4-Br-BnIm.

33 Two potent BRD4 bromodomain 1 (BD1)-selective inhibitors 44 (ZL0513) and 45 (ZL0516) have be

34 e pharmacological effects of PDE4B and PDE4D selective inhibitors, A-33 and D159687, in mediating neu

35 hed, efforts were made to develop potent and selective inhibitors across the entire family.

36 aid in the design of a novel class of highly selective inhibitors acting against such specific target

37 tly reported that seviteronel, a CYP17 lyase-selective inhibitor, aedemonstrated a sustained reductio

38 The FabI isoform was inactivated by the FabI selective inhibitor AFN-1252, but the FabK isoform was n

39 The most active and selective inhibitors against isoforms implicated in glau

40 ogy designed to facilitate identification of selective inhibitors against RING type E3 ubiquitin liga

41 nsensitive, or rapidly evolve resistance, to selective inhibitors aimed at a single target.

42 The PI3Kalpha selective inhibitor alpelisib blocked PI3K/AKT activatio

43 ent antineoplastic effects for the PI3Kalpha selective inhibitor alpelisib in medulloblastoma.

44 Apoptosis-Inducing Ligand); is an extremely selective inhibitor, among kinases, of human RIPK1 enzym

45 Hdac3 deacetylase activity, we used an HDAC3 selective inhibitor and examined nascent transcription i

46 Here, we introduce subunit-selective inhibitors and dual-color fluorescent activity

47 fference between the responses of our highly selective inhibitors and published tool compounds sugges

48 Selective inhibitors and small interfering RNAs for NOX5

49 s and identified previously unrecognized SRM selective inhibitors and synergistic interactions betwee

50 ed, for other subtypes much less is known on selective inhibitors and the consequences of their inhib

51 Epacadostat, an IDO1 selective inhibitor, and pembrolizumab, a PD-1 inhibitor

52 ase (broad spectrum), PHD-selective, and FIH-selective inhibitors, and investigated their effects on

53 These RANKL-selective inhibitors are an excellent starting point for

54 PI3K isoform-selective inhibitors are in development for the treatmen

55 the clinic to treat leukemia, but tight and selective inhibitors are not available for Bcl-2 paralog

56 r efficacy and improve their safety profile, selective inhibitors are required.

57 hts the need for brain-penetrant IDH1 mutant-selective inhibitors as an alternative therapeutic optio

58 timal platform for the development of HDAC10-selective inhibitors, as exemplified with the Tubastatin

59 plex with a recently developed bioactive and selective inhibitor at 2.53 A resolution.

60 nhibitor ripretinib (DCC-2618) and the D816V-selective inhibitor avapritinib (BLU-285) are being furt

61 Treatment with the ATR-selective inhibitor AZ20 caused proliferation inhibition

62 key findings were confirmed with another ATR-selective inhibitor AZD6738.

63 In vivo inhibition of AURKB using the selective inhibitor Barasertib (AZD1152-HQPA) interfered

64 inhibitors, as well as a subseries of LOXL2-selective inhibitors, bearing an aminomethylenethiazole

65 oxidation and CO2 reduction are inhibited by selective inhibitor binding to the Mo(VI) horizontal lin

66 attributed the non-competitive character to selective inhibitor binding to the Neu5Ac site in a cyto

67 We hypothesized that the GLS1 selective inhibitor, bis-2-(5-phenylacetamido-1,3,4-thia

68 A disintegrin and metalloprotease) 10 and 17 selective inhibitor, but not by an ADAM10 selective inhi

69 We have synthesized a new GRK2 subfamily-selective inhibitor, CCG258747, which has nanomolar pote

70 argely blocked by TG4-155, TG6-10-1 or COX-2 selective inhibitor celecoxib, but not by GW627368X.

71 The CFTR-selective inhibitor, CFTRinh-172, modestly reduced MCCV-

72 The selective inhibitor CK-2018571 prevents strong binding t

73 kinetic properties, and have developed a new selective inhibitor, compound 27 (IPN60090), which is cu

74 TASIN (Truncated APC-Selective Inhibitors) compounds are selectively toxic to

75 Selective inhibitors could help unveil the mechanisms by

76 As, or PRKD1 activity was inhibited with the selective inhibitor CRT0066101.

77 ical inhibition of SUV39H1 using a novel and selective inhibitor decreased levels of H3K9me3 in the h

78 tion, unlike the pan BETi (+)-JQ1, these BD2-selective inhibitors demonstrated no rebound expression

79 s further suggest that the approach of using selective, inhibitor-dependent phosphoproteome analysis

80 ell conserved between family members, making selective inhibitor design challenging.

81 e with catalytic Lys, which can be tested in selective inhibitor design.

82 rious conformational states could accelerate selective inhibitor design.

83 deacetylase through small interfering RNA or selective inhibitor Ex527 greatly enhances MK-1775-induc

84 tease classes, making the development of the selective inhibitors exceedingly challenging.

85 R11935, a brain-penetrant and JNK2/3 isoform-selective inhibitor, exerted similar anorectic effects a

86 Here, a Grp94-selective inhibitor facilitated mutant myocilin degradat

87 examined in an initial study, an exquisitely selective inhibitor for a poorly characterized serine hy

88 ALDH1/2 isoenzymes, including compound 36, a selective inhibitor for ALDH2 (Ki = 2.4 muM), and compou

89 XDM-CBP is a highly potent and selective inhibitor for the bromodomains of CBP and p300

90 id progress in the development of potent and selective inhibitors for a wide range of DUBs and advanc

91 Selective inhibitors for each serine/threonine phosphata

92 the challenges in structure-based design of selective inhibitors for either enzyme.

93 The lack of potent and selective inhibitors for endocannabinoid transport has p

94 o assays were employed to develop potent and selective inhibitors for group VIA calcium-independent P

95 demonstrate an effective strategy to explore selective inhibitors for helicases, and 9 could be a pro

96 nt structural insight for the design of more selective inhibitors for hGLUTs and hGLUT1 in particular

97 is the absence of chemical tools designed as selective inhibitors for IKKalpha over IKKbeta.

98 may facilitate the rational design of PfPKG-selective inhibitors for improved management of malaria.

99 s a promising approach to develop potent and selective inhibitors for protein methyltransferases.

100 further developments toward more potent and selective inhibitors for the tumor-expressed CA IX.

101 ent cancer targets; however, very few highly selective inhibitors for these are available.

102 rovide useful insights to develop potent and selective inhibitors for undesired GUSs.

103 Several p110beta-selective inhibitors, for example, a molecule from the s

104 A highly potent, selective inhibitor, GNF362, ameliorated acute GVHD with

105 We found that the EZH2-selective inhibitor GSK126 induced lipid accumulation in

106 To date, no PAD2-selective inhibitor has been developed.

107 However, the design of selective inhibitors has been hampered because structura

108 iCP rather than the standard proteasome, and selective inhibitors have been developed to exploit this

109 tion has been hampered, partly because MIF-2-selective inhibitors have been elusive.

110 f mutant myocilin in vitro, to date no Grp94-selective inhibitors have been investigated in vivo.

111 While for HDACs 1-3 and 6 many potent selective inhibitors have been obtained, for other subty

112 hod were used to determine the effect of the selective inhibitor HFI-419 on insulin-regulated aminope

113 o determine the effect of the PI3K p110delta-selective inhibitor idelalisib on allergic responses.

114 ulting in regulatory approval of one isoform-selective inhibitor (idelalisib) for treatment of certai

115 etitive glutamate antagonists AP5 and GluN2B-selective inhibitor ifenprodil reduced NMDA-activated cu

116 Here we use PF-06840003 (IPD), a hIDO1-selective inhibitor in clinical trials, as a structural

117 olecule ligands and methodologies to produce selective inhibitors in a predictable fashion are in hig

118 potential of targeting the STAT/TET1 axis by selective inhibitors in AML treatment.

119 he efficacy and safety of fedratinib, a JAK2-selective inhibitor, in patients with ruxolitinib-resist

120 sect the contribution of HDAC isoforms using selective inhibitors, including the newly developed sele

121 mutations may derive benefit from p110alpha-selective inhibitors, including the recently FDA-approve

122 However, the recent finding that MDM2-selective inhibitors induce high levels of its homologue

123 er TBI, as post-TBI injection of a calpain-2 selective inhibitor inhibited c-Abl activation and tau o

124 le of the Rho GTPase proteins by injecting a selective inhibitor into the mPFC and found that activat

125 SZ, and preclinical efficacy of a p110delta-selective inhibitor is seen in rodent models of risk.

126 However, a CDK2-selective inhibitor is yet to be discovered.

127 now apparent that the targeting of RTKs with selective inhibitors is only transiently effective, as t

128 ent inhibitory activity of the first CYP26A1 selective inhibitors is reported.

129 Abemaciclib, a CDK4/6-selective inhibitor, is currently in phase III studies f

130 eferred, with 10 being the most potent SphK2-selective inhibitor (K(i) = 89 nM, 73-fold SphK2-selecti

131 Reversible, beta5i-selective inhibitors may be useful for treatment of dise

132 We attempt to provide an outlook on how CDK2-selective inhibitors may open new avenues for cancer the

133 re, we report that inhibiting NLRP3 with the selective inhibitor MCC950, blocked release of IL-1beta

134 tional regions, which allowed us to design a selective inhibitor, MPH-220.

135 The natural product colletoic acid (CA) is a selective inhibitor of 11beta-hydroxysteroid dehydrogena

136 The selective inhibitor of 2-AG biosynthesis O7460 abolished

137 study, we synthesized and evaluated a novel selective inhibitor of ABCB1 (TTT-28) with high efficacy

138 ed the safety and efficacy of selonsertib, a selective inhibitor of apoptosis signal-regulating kinas

139 by MAST3 kinase converts the protein into a selective inhibitor of B55alpha- and B56delta-containing

140 Venetoclax (ABT-199) is a small-molecule selective inhibitor of BCL2 currently in clinical trials

141 ontaining proteins shows that 31 is a highly selective inhibitor of BET proteins.

142 Dabrafenib is an oral selective inhibitor of BRAF kinase.

143 n of, to our knowledge, the first potent and selective inhibitor of CARM1 that exhibits anti-prolifer

144 highly potent (K(i) = 5 pM), reversible, and selective inhibitor of CD73.

145 in striatal medium spiny neurons, acts as a selective inhibitor of certain forms of the serine/threo

146 -induced toxicity was reduced/abolished by a selective inhibitor of CYP2E1 enzyme activity (diallyl e

147 Administration of EPZ5676, a highly selective inhibitor of DOT1L, attenuated renal fibrosis.

148 JNJ-42165279 is a selective inhibitor of fatty acid amide hydrolase (FAAH)

149 Sephin1 is reportedly a selective inhibitor of GADD34 (PPP1R15A), which is a str

150 The inhibitor FK506 and an isoform-selective inhibitor of GSK3alpha, BRD0705, also inhibite

151 Intraperitoneal injection of RGFP966 (a selective inhibitor of HDAC3) decreased infarct size and

152 Administration of PCI34051, a highly selective inhibitor of HDAC8, restored acetylation of co

153 ted the efficacy and safety of GSK2330672, a selective inhibitor of human ileal bile acid transporter

154 an 600 clinically approved drugs as a direct selective inhibitor of human MCU.

155 We investigated a novel selective inhibitor of IL-8 receptors, DF2726A, and show

156 have identified BMS-986126, a potent, highly selective inhibitor of IRAK4 kinase activity that demons

157 n monocytes treated with a highly potent and selective inhibitor of IRAK4, we show that IRAK4 kinase

158 Ruxolitinib, a selective inhibitor of Janus kinase 1 and Janus kinase 2

159 4 (GS-6615, eleclazine) a novel, potent, and selective inhibitor of late INa, is currently in clinica

160 Iadademstat is a novel, highly potent, and selective inhibitor of LSD1 (KDM1A), with preclinical in

161 ted the prophylactic effects of rapamycin, a selective inhibitor of mammalian target of rapamycin sig

162 elumetinib (AZD6244 or ARRY-142886), an oral selective inhibitor of MAPK kinase (MEK) 1 and 2, in chi

163 ine, suggesting that it may provide a highly selective inhibitor of MEK1/2 for use as a cancer therap

164 We identified that CL82198, a selective inhibitor of MMP13, decreased BACE1 protein le

165 CFI-402257 is a novel, selective inhibitor of Mps-1 with antineoplastic activit

166 Ivosidenib (AG-120) is a selective inhibitor of mutant IDH1 approved in the Unite

167 (AG-221/CC-90007) is a first-in-class, oral, selective inhibitor of mutant-IDH2 enzymes.

168 )benzyl)morpholine ((11)C-MeNER) is a highly selective inhibitor of noradrenaline transporters, and P

169 Selinexor is the first oral selective inhibitor of nuclear export compound tested fo

170 Selinexor, a selective inhibitor of nuclear export compound that bloc

171 Selinexor is a novel, first-in-class, selective inhibitor of nuclear export compound, which bl

172 response to single-agent selinexor, an oral selective inhibitor of nuclear export, in patients with

173 Lurbinectedin is a selective inhibitor of oncogenic transcription.

174 Mito-LND, a tumor-selective inhibitor of oxidative phosphorylation, inhibi

175 he identification of 52, a potent and highly selective inhibitor of PI3Kdelta that demonstrates effic

176 is work led to the discovery of 35, a highly selective inhibitor of PI3Kdelta which displays an excel

177 Idelalisib, a selective inhibitor of PI3Kdelta, is approved for the tr

178 CVM-05-002 is a potent and selective inhibitor of PI5P4Ks, and a 1.7 angstrom X-ray

179 Conversely, a selective inhibitor of PKC, calphostin C, blocks mbGR/PK

180 hway of cholesterol metabolism with MK886 (a selective inhibitor of PPARalpha) in RAW264.7 macrophage

181 This study reveals that the selective inhibitor of RNA polymerase I (Pol I) transcri

182 o the discovery of compound 14, a potent and selective inhibitor of RORgammat with good ADME properti

183 e approximately 400 nM) that is a potent and selective inhibitor of Rpn11 that blocks proliferation o

184 ate that ent-(+)-verticilide is a potent and selective inhibitor of RyR2-mediated diastolic Ca(2+) le

185 ght the discovery of IACS-13909 as a potent, selective inhibitor of SHP2 with drug-like properties, a

186 rm of the methylthioninium moiety, acts as a selective inhibitor of tau protein aggregation both in v

187 e discovery of ABBV-744, a highly potent and selective inhibitor of the BD2 domain of BET family prot

188 A selective inhibitor of the calcium-activated chloride ch

189 e profiling revealed 5-IT to be a potent and selective inhibitor of the dual-specificity tyrosine pho

190 GSK789, a potent, cell-permeable, and highly selective inhibitor of the first bromodomains of the BET

191 ucatinib is an investigational, oral, highly selective inhibitor of the HER2 tyrosine kinase.

192 Docking studies with GSK-J1, a selective inhibitor of the KDM6/KDM5 subfamilies, identi

193 sly, we reported the discovery of GNF6702, a selective inhibitor of the kinetoplastid proteasome, whi

194 ddC is a selective inhibitor of the mitochondrial DNA polymerase

195 B) approved in more than 40 y, and a species-selective inhibitor of the Mycobacterium tuberculosis (M

196 Furthermore, treatment with FK866, a selective inhibitor of the NAD(+) salvage pathway enzyme

197 s (CRIDs) such as MCC950/CRID3, a potent and selective inhibitor of the NLRP3 inflammasome pathway, f

198 ded phase 2 dose (RP2D) of oral selinexor, a selective inhibitor of the nuclear export protein XPO1.

199 We identified a selective inhibitor of the Plasmodium falciparum protein

200 of GSK046, also known as iBET-BD2, a highly selective inhibitor of the second bromodomains of the BE

201 r inhibits cyclooxygenases; R-ketorolac is a selective inhibitor of the small GTPases Ras-related C3

202 y, we used a pharmacologic approach (SM16, a selective inhibitor of the type 1 TGF-beta receptor acti

203 studies of GMII, we still lack a potent and selective inhibitor of this enzyme.

204 In this study, we have identified a selective inhibitor of TRESK, A2764.

205 ynthesized, and the synthesis of a potential selective inhibitor of tyrosyl DNA phosphodiesterase II

206 Selective inhibitors of ABHD12 would offer valuable phar

207 we report the identification of a series of selective inhibitors of apicomplexan KRSs.

208 ered Ceapins, a class of pyrazole amides, as selective inhibitors of ATF6alpha signaling that do not

209 Several potent and selective inhibitors of ATR have been reported showing s

210 onalized diterpenoids that act as potent and selective inhibitors of bacterial and mammalian fatty ac

211 enzimidazoles with terminal alkynyl linkers, selective inhibitors of bacterial topoisomerase I, have

212 lkysulfamide group(s) as highly specific and selective inhibitors of CAIX.

213 ing in human hepatocytes, there are no known selective inhibitors of CaMK1 kinases that can be used t

214 din-2-amine derivatives as highly potent and selective inhibitors of CDK4 and CDK6.

215 Selective inhibitors of CYP3A5 are, therefore, critical

216 In this study, we investigated how selective inhibitors of DGAT1 and DGAT2 affected lipid m

217 sis, and pave the way for the design of more selective inhibitors of each human CYP11B enzyme.

218 Using selective inhibitors of either PKG or cysteine proteases

219 substrate docking sites and act as function-selective inhibitors of ERK1/2 signaling.

220 , we discovered that UNC0638 and UNC0642-two selective inhibitors of euchromatic histone lysine N-met

221 afranal and its semisynthetic derivatives as selective inhibitors of five isoforms of human carbonic

222 llowing treatment of FLT3/ITD AML cells with selective inhibitors of FLT3.

223 ed a 1,2,3-triazole urea library to identify selective inhibitors of fluorophosphonate-binding serine

224 cuted a small-molecule screen and discovered selective inhibitors of FOXO-dependent glucose productio

225 analysis successfully identified potent and selective inhibitors of GATA4-NKX2-5 transcriptional syn

226 Selective inhibitors of gut bacterial beta-glucuronidase

227 progression and the potential use of highly selective inhibitors of HDAC11 in combating lung cancers

228 functions of JMJD6 and in the development of selective inhibitors of human 2OG oxygenases.

229 ntional and microscale parallel synthesis of selective inhibitors of human blood coagulation factor X

230 he first time a series of novel, potent, and selective inhibitors of IKKalpha.

231 Thus, potent, selective inhibitors of LDH represent an attractive ther

232 braries (PS-SCL), which was used to discover selective inhibitors of matriptase and hepsin.

233 rs a fruitful approach to the development of selective inhibitors of mosquito ACE enzymes as novel la

234 ies, a new chemical scaffold was designed as selective inhibitors of NLRP3 inflammasomes.

235 Over the years, a number of selective inhibitors of nuclear export have been develop

236 Veliparib and niraparib are selective inhibitors of PARP1 and PARP2; olaparib, rucap

237 pid dosing of human whole blood with isoform selective inhibitors of phosphatidylinositol 3-kinase do

238 insight into the activity of a collection of selective inhibitors of Plasmodium NMT and serve as a st

239 nyl benzo[d]isothiazol-3(2H)-ones as species-selective inhibitors of Plasmodium spp. 2-C-methyl-D-ery

240 ase 1 (Plk1), as suggested by the effects of selective inhibitors of Plk1.

241 fers the potential for development of highly selective inhibitors of PNMT.

242 Selective inhibitors of protein kinase CK2 with signific

243 ce of the CRAF-RBD, we identified potent and selective inhibitors of Ras in its active conformation t

244 dings provide a detailed characterization of selective inhibitors of rat brain DAGL and demonstrate t

245 vir, rupintrivir, and cobicistat as the most selective inhibitors of SARS-CoV-2-Nluc (EC(50) 0.77 to

246 ery of structures that are potent and highly selective inhibitors of SGLT2.

247 ut screening strategy to identify potent and selective inhibitors of SRM, quantitatively ranked the s

248 n human disease, the identification of novel selective inhibitors of TGFbeta superfamily receptors is

249 reports the development of highly potent and selective inhibitors of the beta5c catalytic activity of

250 Selective inhibitors of the CREB binding protein (CREBBP

251 Selective inhibitors of the GluN2B subunit of N-methyl-d

252 n similar to oligomycin A and apoptolidin A, selective inhibitors of the mammalian ATP synthase (comp

253 report the engineering of highly potent and selective inhibitors of the Nav1.7 channel based on tara

254 AIDs of the fenamate class are effective and selective inhibitors of the NLRP3 inflammasome via inhib

255 , has spurred considerable effort to develop selective inhibitors of this Na(+) ion channel target as

256 Here we report the development of selective inhibitors of three deltaPKC substrates (in vi

257 Potent and selective inhibitors of three recombinant human enzymes,

258 but its function there is unclear and potent selective inhibitors of TRAP are required to assess func

259 of a series of triazolopyridazines that are selective inhibitors of wild-type (WT) MET kinase and se

260 onitor by NMR the effect of conformationally selective inhibitors on kinase backbone dynamics.

261 reviously, we discovered two classes of GRK2-selective inhibitors, one stemming from GSK180736A, a Rh

262 tified a novel, state-dependent human Nav1.7 selective inhibitor (PF-05089771, IC50 = 11 nM) that int

263 a ligand series derived from the potent SK1-selective inhibitor, PF-543.

264 revented by pretreatment of GCs with the PKA-selective inhibitor PKA inhibitor (PKI), the MEK inhibit

265 b, an orally bioavailable clinical stage CDK-selective inhibitor, potently blocks CDK9, the transcrip

266 temic inhibition of this phosphatase using a selective inhibitor prevented cognitive decline, neuron

267 In contrast, IDH1 mutant-selective inhibitors provided considerable survival bene

268 ides and esters are cyclooxygenase-2 (COX-2)-selective inhibitors, providing a framework for the desi

269 dependent phospholipase A2gamma (iPLA2gamma)-selective inhibitor (R)-BEL suggested that iPLA2gamma is

270 Treatment with HDAC6-selective inhibitors recapitulates the HDAC6 loss-of-fun

271 king this interaction by RNA interference or selective inhibitors reduced SARS-CoV-2 entry and infect

272 Inhibition of IkappaKalpha/beta with a novel selective inhibitor reproduced the impaired monocyte phe

273 Biological evaluation of our isoform-selective inhibitors revealed a high degree of synergist

274 The HDAC3-selective inhibitor RGFP966 was used to examine its biol

275 find that the histone deacetylase 3 (HDAC3)-selective inhibitor, RGFP966, inhibits BACH2-mediated re

276 hylated (DM) CpGs, treatment with the ERK1/2-selective inhibitor SCH772984 showed less than 40 DM CpG

277 Upadacitinib, an oral Janus kinase (JAK)1-selective inhibitor, showed efficacy in combination with

278 retreatment of airway secretions with a KLK5-selective inhibitor significantly reduced the activation

279 or targeting this cysteine to identify FGFR4 selective inhibitor starting points are summarized which

280 structurally novel, brain penetrant, GluN2B-selective inhibitors suitable for evaluation in a clinic

281 nd 2 have resulted in development of paralog-selective inhibitors targeting these sites, but the rule

282 tion led to the identification of potent and selective inhibitors that demonstrated favorable pharmac

283 3 decades with an emphasis on the design of selective inhibitors that discriminate between the 11 hu

284 ly, HDAC6 is a target for the development of selective inhibitors that might be useful in new therape

285 chemistry design approaches to novel isoform-selective inhibitors through consideration of brief case

286 ach coupled with treatment using PDE isozyme-selective inhibitors to characterize the phosphoproteome

287 herapeutic interest in developing potent and selective inhibitors to control LMW-PTP activity.

288 The PDE10A selective inhibitor TP-10, and global PDE10A knock out m

289 PDE10A deficiency or inhibiting PDE10A with selective inhibitor TP-10, attenuated cardiac myocyte pa

290 itro testing for the discovery of potent and selective inhibitors using mixtures of membranelike subs

291 ubicin was conjugated to an immunoproteasome-selective inhibitor via light-cleavable linkers, yieldin

292 ted the effects of a phospholipase D1 (PLD1)-selective inhibitor (VU0155069) against sepsis and infla

293 e design of high-affinity and enzyme isoform-selective inhibitors, we applied an approach of augmenti

294 Using these selective inhibitors, we have clarified the specific rol

295 Selective inhibitors were used to disentangle the roles

296 ide-derived, potent, bioavailable and highly selective inhibitor, which is widely used for studies in

297 his work shows that Ponatinib and BRAF dimer selective inhibitors will be useful in treating BRAF-dep

298 ffold would allow access to a series of PAD2-selective inhibitors with enhanced cellular efficacy.

299 Both compounds are COX-2-selective inhibitors with IC(50) values of 0.76 and 0.17

300 epresent an opportunity for designing highly selective inhibitors with unexpected binding modes.