ライフサイエンスコーパス: druggable

1 y inactivated in cancers and is not directly druggable.

2 ng mapping, suggesting that MtMetX is highly druggable.

3 also have associated proteins, which may be druggable.

4 hibition requires that the target protein be druggable.

5 ith germline P/LP variants have at least one druggable alteration, while more than half of them are f

6 PML nuclear bodies are druggable and could be harnessed in other conditions.

7 this so-called switch I/II pocket is indeed druggable and provide the scientific community with a ch

8 he results suggest expansion activity may be druggable and support HDAC3-selective inhibition as an a

9 Many of them are not druggable and therefore it is necessary to identify targ

10 perceptions of what targets are considered "druggable" and provide support for drug design in beyond

11 ult of UppS inhibition, validating UppS as a druggable antibacterial target.

12 rate that FtsH1 is a novel and, importantly, druggable antimalarial target.

13 rus-host interactome identified 110 putative druggable antiviral targets and prioritized several exis

14 factors with the end goal of discovering new druggable antiviral targets.

15 Furthermore, a druggable AP-1 inhibitory small molecule suppresses skin

16 Identification of novel, non-classical and druggable AR-target genes may provide new approaches to

17 ative 5-HTP immediate release (IR) is poorly druggable, as rapid absorption causes rapid onset of adv

18 therapeutic targets that are considered non-druggable because they do not have binding sites for sma

19 pproaches are required to reveal potentially druggable binding sites.

20 ed drug design consists in the prediction of druggable binding sites.

21 that conditions are now met to consider PDs druggable biologicals.

22 cate the presence of several new potentially druggable BTK states.

23 These targets are conventionally druggable, but reaching additional hot spots enables imp

24 and identify an anti-tumour target rendered druggable by cereblon modulation.

25 triggered by low [TF]wall, thrombosis may be druggable by contact pathway inhibition, although thromb

26 nities to modulate intracellular targets not druggable by conventional small molecules.

27 ryptic binding sites, which can be rendered "druggable" by small molecule ligands.

28 ding mode and allows the identification of a druggable cadherin interface, thus paving the way to a f

29 reens and a small-molecule screen focused on druggable cancer targets.

30 yltransferase gene 5 (PRMT5) as an effective druggable candidate whose inhibition creates synergistic

31 is dispensable for murine viability and has druggable catalytic activity.

32 Furthermore, relatives within druggable CATH functional families occupy central positi

33 milies that are currently enriched in drugs (druggable CATH functional families) and we use the netwo

34 Analysis of selected druggable CATH functional families, enriched in drug tar

35 d (ProCare) was calibrated on a large set of druggable cavities and applied to the comparison of frag

36 l (3D) structure, to identify and prioritize druggable cavities at and nearby PPIs of pharmacological

37 ied to the entire Protein Data Bank, 164 514 druggable cavities were identified and classified in fou

38 gence of a novel pocket that appears to have druggable characteristics.

39 e conducted an RNAi-based screen to identify druggable chromatin regulator-based targets in leukemias

40 ibe knockoff, a generalizable method for the druggable control of membrane protein stability.

41 e a simple approach to distinguish them from druggable cryptic pockets.

42 dently regulate Tau and Abeta and identify a druggable CYP46A1-CE-Tau axis in AD.

43 Hence, we sought to discover a druggable downstream transcriptional target of LIN9.

44 Druggable driver oncogenes, identified by molecular anal

45 udies indicate that KDM5C is a conserved and druggable effector molecule across a number of NDDs for

46 he KRAS oncoprotein is, as yet, not directly druggable, efforts to target KRAS mutant cancers focus o

47 y are essential in breast cancer cell lines, druggable, enriched in stem-like breast cancer cells, an

48 ral progeny and thus provides an attractive, druggable enzymatic target.

49 irmed our previous finding that CYP27A1 is a druggable enzyme and found additional drugs as well as t

50 The human kinome, a major druggable enzyme class has been exploited to treat a wid

51 noma and are under regulation of potentially druggable enzymes.

52 that not all oncogenic driver proteins are "druggable" enzymes or receptors with activities that can

53 rian degeneration in mice; the discovery of 'druggable' enzymes, including SARM1 and MYCBP2 (also kno

54 evelopment and highlights the involvement of druggable epigenetic factors in cancer.

55 extraterminal (BET) protein activation is a druggable epigenetic mechanism of disease pathogenesis i

56 excised tissue, thus suggesting a promising druggable etiology.

57 and progression, suggesting that apelin is a druggable factor in glioblastoma.

58 our Drosophila RMS-related model to isolate druggable FC-specific fusogenic elements underlying RMS,

59 n interplay is thus critical to define novel druggable fungal targets and to exploit novel immune-bas

60 Novel druggable fusion events have been recognized in genitour

61 The total number of druggable gene claims has also increased by 30%.

62 nbiased discovery of potentially driving and druggable gene fusions in primary tumors.

63 These ADHD-associated druggable genes and pathways were also examined in co-mo

64 siRNA)-based screening of approximately 4800 druggable genes in 3-dimensional CSLC cultures in compar

65 We identify 123 Bonferroni-significant druggable genes outside the MHC, and 128 FDR-significant

66 previously performed a screen of potentially druggable genes that led to the identification of 60 mod

67 ant association with ADHD and contained nine druggable genes, five of which encode established drug t

68 percent of advanced HCC harbored potentially druggable genetic alterations, and MET amplification was

69 t network analysis reveals several potential druggable genetic interactions by targeting tumor vulner

70 r of several members of the Illuminating the Druggable Genome (IDG) list of understudied dark kinases

71 The Illuminating the Druggable Genome (IDG) program was initiated in 2014, ha

72 wn ADHD drugs and present the exploration of druggable genome associated with ADHD, which may offer i

73 ionship network now defines a data-supported druggable genome encompassing 7% of human proteins.

74 ensive and user friendly tool for mining the druggable genome for precision medicine hypothesis gener

75 nclude, we present a framework to assess the druggable genome in a disorder, exemplified by ADHD.

76 Here, we explored the druggable genome in ADHD by utilising GWA studies on ADH

77 f small-molecule inhibitors, 33 genes of the druggable genome increased progranulin levels in mouse p

78 s on cardiac clinical testing panels and the druggable genome reveals striking patterns of cellular s

79 Substituting genome wide (or druggable genome wide) association studies for preclinic

80 points to GRM1/mGlu(1) as a gene within the "druggable genome" that could be targeted for the treatme

81 The 'druggable genome' encompasses several protein families,

82 Considering that GPCRs comprise much of the druggable genome, these data suggest alternative strateg

83 In the examined druggable genome, three loci on chromosomes 1, 4 and 12

84 ein structures are particularly suitable for druggable genome-wide predictions of DPIs.

85 ruitment to mitochondria and screened both a druggable genome-wide siRNA library and a small neuroact

86 ruggable targets, dramatically expanding the druggable genome.

87 of side effects as well as expansion of the druggable genome.

88 To date, only about 17% of druggable GPCRs have had their structures characterized

89 esentation are limited, we aimed to identify druggable HLA-I pathway targets.

90 enome-wide screening in the search for novel druggable host targets for adjunctive TB therapies.

91 Our structures reveal cryptic druggable hot spots in the shallow inhibitor binding sit

92 Among these, we identify 66 druggable human proteins or host factors targeted by 69

93 oSite increases the size of the potentially "druggable" human proteome from ~40% to ~78% of disease-a

94 an increase in the size of the potentially 'druggable' human proteome.

95 epresses Vegfa messenger RNA translation, is druggable in a selective manner.

96 TFFs are not readily "druggable" in a direct pharmacologic manner and thus hav

97 ated PPIs, uncovering a trove of potentially druggable interactions.

98 omes was proposed as a therapeutic strategy, druggable interactors for rescue of ATP7B mutants remain

99 r idea was to improve the selectivity toward druggable isoforms through the introduction of additiona

100 Together, our data reveal a druggable K2P site that stabilizes the C-type gate 'leak

101 Potentially druggable kinase fusions involving ALK, ROS, RET, NTRK a

102 ize a robust signaling network consisting of druggable kinase pathways.

103 and organoids and show that it depends on a druggable lipid-peroxidase pathway that protects against

104 p53 DNA-binding domain phosphorylation as a druggable mechanism that balances tumorigenesis and agin

105 Here, we systematically investigated druggable mechanisms of CAR T-cell cytotoxicity using >5

106 cells, with the specific goal of identifying druggable metabolic susceptibilities from a series of pa

107 ve (normal) hosts and identifies potentially druggable microbial factors, such as pyruvate dehydrogen

108 Our study advances this approach for mining druggable modifiers of disease-associated proteins, whil

109 he identification of previously undiscovered druggable molecular pathways.

110 inus of PrP(C) as a new and potentially more druggable molecular target for treating Alzheimer's dise

111 rtance of T(reg) cells, there is a dearth of druggable molecular targets capable of increasing their

112 AC) offers an optimal model for discovering "druggable" molecular pathways that participate in inflam

113 n data to pinpoint regulated subnetworks and druggable molecules.

114 we find that a consensus topology of highly druggable motifs consists of a negative feedback loop wi

115 ), and SMAD4 (11.3%), as well as potentially druggable mutations (e.g., HER2/ERBB2).

116 ents with non-small-cell lung cancer without druggable mutations and in patients with triple-negative

117 Given the paucity of druggable mutations in high-risk neuroblastoma (NB), we

118 for the lack of progress are the absence of druggable mutations in the majority of liver cancers and

119 predicted over 800 promising candidates for druggable mutations, raising new possibilities for desig

120 ndings of previously missed, but potentially druggable, mutations in the EGFR, MET and KIT oncogenes.

121 ETD8, the H4(K20me1) methyltransferase, as a druggable NB target.

122 domain predictive algorithm for identifying druggable neighborhoods based on network parameters.

123 To discover druggable neuroprotective compounds for dopamine neurons

124 cell lymph node egress, we conclude that the druggable Notch signaling pathway licenses the Th2 respo

125 We identified multiple potentially druggable, novel and known kinase fusions in diseases be

126 suggest that inhibition of Nrf2 or discrete druggable Nrf2 target genes such as IGF1R could be an ef

127 domain has been described as among the least druggable of that target class.

128 ocal amplifications, many of which contained druggable oncogenes (ERBB2, MET, FGFR1, CDK6, PIK3R3 and

129 fraction of tumors with aberrant activity of druggable oncoproteins despite a lack of mutations, and

130 Altogether, our findings uncover a druggable pathway as a potential therapeutic target for

131 B cell self-tolerance and thus represents a druggable pathway to treat antibody-mediated autoimmunit

132 To identify druggable pathways, we generated a medaka (Oryzias latip

133 tory disease and report the discovery of new druggable pathways.

134 subgroups, including relationships to known druggable pathways.

135 ol over tumour-initiating stem cells via the druggable PGE(2)-Ptger4-Yap signalling axis.

136 y of mutant oncogenic K-Ras, are devoid of a druggable pocket and lack an accessible cysteine for the

137 This druggable pocket provides potentially complementary oppo

138 CCR2-RA-[R] binds in a novel, highly druggable pocket that is the most intracellular alloster

139 on with the AR AF-1 are within a potentially druggable pocket, implicating Bag-1L as a potential ther

140 mplex was screened for the presence of small druggable pockets formed from contributions from both pr

141 -p53 in the presence of DNA is revealed, and druggable pockets of p53 are identified via solvent mapp

142 Because many proteins appear to lack druggable pockets, understanding and accurately identify

143 nd processive UTP incorporation, and predict druggable pockets.

144 kinase inhibition represents a potentially "druggable" point of intervention.

145 roperty space, suggesting that even the most druggable PPI cavities are unlikely to be addressed with

146 out to investigate whether Galphai-GIV is a druggable PPI.

147 Targeting this druggable process could extend the lifespan of current f

148 ) and we use the network properties of these druggable protein families to analyse their association

149 as largely been focused on a small number of druggable protein families.

150 ibitor-bound kinases and, potentially, other druggable protein targets.

151 on of PPI cavities with pockets deduced from druggable protein-ligand complexes shows almost no overl

152 ic hotspot for DMF action that constitutes a druggable protein-protein interface crucial for initiati

153 identified for >700 cysteines found in both druggable proteins and proteins deficient in chemical pr

154 cascade is incompletely understood and novel druggable proteins in the pathway are in high demand.

155 cause of this problem, we sought to identify druggable proteins on the HCL surface that were dependen

156 Protein kinases are a large family of druggable proteins that are genomically and proteomicall

157 Here, we use chemical proteomics to map druggable proteins that are selectively expressed in KEA

158 echanisms, as well as the discovery of novel druggable proteins within the ubiquitin pathway.

159 To identify potentially druggable proximate mechanisms, we performed a chemical

160 ts and opens new perspectives and identifies druggable receptors from characterization of the ligand

161 reveal conformational switching in KSR as a druggable regulator of oncogenic Ras, and further sugges

162 tors (GPCRs) in brown adipocytes to identify druggable regulators of BAT.

163 on sites and Cxcl9l and Cxcr3.2 as potential druggable regulators of bone homeostasis and osteoporosi

164 oma formation, revealing new and potentially druggable schwannoma vulnerabilities with future therape

165 Resistance mapping revealed a druggable site formed by the G protein fusion loops that

166 er, the novel allosteric pocket was proved a druggable site, offering an excellent perspective to dev

167 ed in flavivirus MTase that can be used as a druggable site.

168 cket, which therefore represents a potential druggable site.

169 ery of a pocket with features found on known druggable sites and covalent modification of a bystander

170 to quantify changes in the accessibility of druggable sites due to conformational changes induced by

171 r the identification and characterization of druggable sites in drug targets.

172 ings may assist in the identification of new druggable sites in hMGL.

173 utp53(R175H) complex, and found one critical druggable small molecule binding site in the DNAJA1 glyc

174 We have screened over a million druggable small molecules in silico and selected putativ

175 entity, which accounts for nearly the entire druggable space of GPCRs.

176 les of the zincates and the informers toward druggable-space coverage.

177 erotrimer assembly provides insight into the druggable structure of PP2A, guiding future phosphatase

178 Each trajectory exhibits unique druggable susceptibilities, thus updating the paradigm o

179 entify the fatty acid synthesis pathway as a druggable susceptibility for differentiated melanocytic

180 he growth of KRAS-mutant cells, suggesting a druggable synthetic lethal interaction between KRAS and

181 ts support the idea of VcPilQ as a potential druggable target and provide insight into the channel th

182 is work establishes the Galphai-GIV PPI as a druggable target and sets the conceptual and technical f

183 Collectively, our data suggest that FTO is a druggable target and that targeting FTO by small-molecul

184 enzymes allows this axis to emerge as a new druggable target and unfolds its promising therapeutic p

185 cates that extracellular PPIA is a promising druggable target for ALS and support further studies to

186 es cerevisiae genome instability genes, is a druggable target for an inhibitor-based approach to kill

187 lopodia formation, is expected to be a novel druggable target for angiogenesis during poststroke prog

188 ng SWI/SNF-BET cooperation and uncover a new druggable target for AR-positive prostate cancers, inclu

189 eam mediator of PERK-driven metastasis and a druggable target for breast cancer therapy.

190 D2 production and could serve as a potential druggable target for inhibiting tumor initiation and met

191 pendent mechanism and suggest C/EBPbeta as a druggable target for managing fibrosis.

192 st that Anopheles VKR could be a potentially druggable target for novel vector control strategies.

193 ppression of OMA1, providing a new potential druggable target for PD.

194 is information introduces IL6 as a potential druggable target for prevention and treatment of K-ras-m

195 tential utility of the endosomal system as a druggable target for signaling.

196 l interrogation spotlights IAV HA as a major druggable target for small-molecule inhibition.

197 Recently CDK9 has emerged as a druggable target for the development of cancer therapeut

198 e results demonstrate that M1 is a promising druggable target for the discovery of a completely new l

199 we show that this system presents as a novel druggable target for the treatment of Alzheimer's diseas

200 ously validated T. brucei NMT as a promising druggable target for the treatment of HAT in both stages

201 They also point to ErbB4/EGFR as a novel, druggable target for therapeutic intervention, especiall

202 21 as a PDAC oncogene, providing a potential druggable target for this intractable disease.

203 y in solid tumors and a generally applicable druggable target for tumor radiosensitization.

204 data suggest that PHB1 may serve as a novel, druggable target in CRAF-mediated vemurafenib resistance

205 lin-sensitive tissues and postulate sEH as a druggable target in metabolic diseases.

206 Our data suggest MARCKS as a druggable target in pulmonary fibrosis and also provide

207 d the ability to interrogate every potential druggable target in the same experiment.

208 myristoyltransferase (NMT), an essential and druggable target in Trypanosoma cruzi, the causative age

209 strated here has the potential to expand the druggable target range of small-molecule therapeutics.

210 ity and identifies the STAT3/Sin3A axis as a druggable target to antagonize STAT3-addicted tumors.

211 ndocannabinoid signaling can be an appealing druggable target to dampen neuronal activity if pre-exis

212 ator of T cell dysfunction and an attractive druggable target to improve immune therapy responses.

213 ch signaling, implicating AIBP as a possible druggable target to modulate angiogenesis under patholog

214 orts the idea that MutLgamma may be a useful druggable target to reduce somatic expansion in those di

215 ked gene was PPIA, encoding cyclophilin A, a druggable target using cyclosporine.

216 , these results suggest that PIP4Kgamma is a druggable target whose inhibition enhances productive au

217 Thus, the PH domain of Cnk1 is a druggable target whose inhibition selectively blocks mut

218 While it has long been clear the mPTP is a druggable target, current agents are limited by off-targ

219 em, the RAS has not been explored fully as a druggable target.

220 suggest Bcl-xL as a potential biomarker and druggable target.

221 roader acceptance of RNA as a small molecule druggable target.

222 ehavioral syllables represent a new class of druggable target.

223 the reduction site of cytochrome b is also a druggable target.

224 mechanoreceptor, representing a potentially druggable target.

225 anti-tumor immunosuppression and a potential druggable target.

226 esent the first evidence that gankyrin is a "druggable" target with small molecules.

227 Loss-of-function screens of druggable targetome against cancer stem-like cells.

228 drug pressure, suggesting that profiling for druggable targets (i.e. mutations) alone may be insuffic

229 well as serving as a discovery platform for druggable targets across multiple pathways that promote

230 To identify signaling networks and potential druggable targets across tumor microenvironments (TMEs),

231 lso used extensively to identify potentially druggable targets and facilitate discovery and developme

232 ow that 14-3-3 adaptor protein complexes are druggable targets and identify a new class of small mole

233 Most druggable targets are membrane components, including mem

234 foundation toward identifying and predicting druggable targets based on their network topology.

235 nhibit cancer-associated genes including non-druggable targets facilitates personalized medicine appr

236 ments novel disease mechanisms and validates druggable targets for diabetic retinopathy.

237 nome and identify novel regulatory nodes and druggable targets for individualized EBV and cancer-spec

238 d ECM metalloproteinases may be particularly druggable targets for intervention.

239 o identify both small molecule compounds and druggable targets for MBNL1 upregulation.

240 nto carcinogenesis and discerned potentially druggable targets for metastatic colorectal cancer.

241 these findings highlight the JAKs as novel, druggable targets for mitigating the cytokine-driven hyp

242 HGAP1 axes have the potential to uncover new druggable targets for the treatment of drug resistant me

243 genes in fate decisions may offer potential druggable targets for the treatment of fractures, non-un

244 ia and anemia of chronic diseases and reveal druggable targets for therapeutic interventions.

245 impair recovery after trauma and may provide druggable targets for treating victims of acute nervous

246 hanisms in a pervasive disease and validates druggable targets for treatment.

247 Such studies may yield druggable targets for weight loss therapies.

248 However, no druggable targets have been identified to potentiate act

249 tic ligands, represent the largest family of druggable targets in the human genome.

250 of host cellular machineries are potentially druggable targets in the search for therapeutic options

251 These results suggest specific druggable targets in the structural motifs of alpha-synu

252 ther, they help define rules for identifying druggable targets in the transcriptome.

253 ally, using molecular profiling, we identify druggable targets in these neurons and show that local i

254 Protein kinases (PKs) are a class of druggable targets in Trypanosoma brucei, the causative a

255 The major druggable targets of SARS-CoV-2 include 3-chymotrypsin-l

256 However, druggable targets that could modulate microglial TREM2 s

257 onditions and consider possible pathways and druggable targets that may be suitable for this objectiv

258 umours for immunoevasion and point to common druggable targets that may enhance immunotherapy.

259 ere is urgent need for the identification of druggable targets that mediate the reinforcing action of

260 cal mechanism without hypoxia provides novel druggable targets to ameliorate and, perhaps, reverse th

261 d plasma membrane L-type calcium channels as druggable targets to intercept mitochondrial calcium ove

262 A large number of potential druggable targets was thus chemically interrogated, but

263 four families, representing the most common druggable targets with an emphasis on understudied prote

264 patients will depend on the discovery of new druggable targets with improved therapeutic efficacy.

265 e in glaucoma treatment has been to identify druggable targets within the conventional aqueous humor

266 e disease, augment current therapies, expand druggable targets, and minimize morbidity.

267 al genes per disease and 4000 genes encoding druggable targets, examining the effect of varying the p

268 Despite substantial efforts to define druggable targets, there are no therapeutic options that

269 To identify novel druggable targets, we carried out an unbiased high-throu

270 pathways required for HIV-1 reactivation as druggable targets.

271 t novel biomarker candidates and potentially druggable targets.

272 hind the disease, and consequently a lack of druggable targets.

273 apid identification of involved pathways and druggable targets.

274 uble minute (MDM)2/p53 complex represent two druggable targets.

275 arked by the realization that they represent druggable targets.

276 their biological functions and potential as druggable targets.

277 ical probes and lead compounds for novel and druggable targets.

278 f these developmental pathways could lead to druggable targets.

279 nd support further exploration of LIMK1/2 as druggable targets.

280 ation will help identify and validate novel "druggable" targets and optimize therapeutic strategies.

281 n interactions (PPIs) are considered poorly "druggable" targets requiring case-by-case validation.

282 tin signatures that can be used to identify "druggable" targets to counter human aging and age-relate

283 mited to a small subset of disease-relevant 'druggable' targets.

284 the pursuit of targets considered to be less druggable that offer potential for development of promis

285 This work validates RET receptor as a druggable therapeutic target and provides for potential

286 novel diagnostic and prognostic markers and druggable therapeutic targets for GBM.

287 lator of EMT, and provides new insights into druggable therapeutic targets that may limit cancer meta

288 RDEB tissue becomes malignant and offer new druggable therapeutic targets to prevent cSCC onset.

289 Our findings designate NR0B1 as a druggable transcriptional regulator that supports NRF2-d

290 CtBP2 is thus a druggable transforming oncoprotein critical for the evol

291 ainable by genomic analysis, suggesting that druggable translational and/or post-translational regula

292 he serine/threonine-specific kinase p38 as a druggable upstream regulator of FOXC2 stability and func

293 allenge by developing a two-armed screen for druggable upstream regulatory kinases in the PAX3/7-FOXO

294 To identify additional druggable vulnerabilities in Wnt-driven pancreatic cance

295 mens identifies RPS6KB1 and PIM1 as emerging druggable vulnerabilities predictive of poor outcome in

296 ncer metabolic alterations that might unveil druggable vulnerabilities, systematic characterizations

297 To reveal its druggable vulnerabilities, we perform kinase-focused RNA

298 mmon in several cancers, but may also expose druggable vulnerabilities.

299 zygous deletions on chromosome 16q present a druggable vulnerability for targeting MYC protein throug

300 dentification of new cancer targets that are druggable with conventional approaches.