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1 hich other triggers for drug use become more potent.
2 erved with lorcaserin, a 5-HT2C agonist with potent 5-HT2B and 5-HT2A agonist activities, which is ap
4 we show that the XPC DNA repair complex is a potent accelerator of global and locus-specific DNA deme
7 ound binding to the Sirt6 catalytic core and potent activation of Sirt6-dependent deacetylation of pe
8 e identified tacrolimus (FK-506) as the most potent activator of ALK1 signaling in BMP9-challenged C2
10 ven that TGF-beta1 and myocardin (MYOCD) are potent activators for VSMC differentiation, we screened
12 the new complexes are phototoxic and display potent activity against chemotherapeutically resistant c
14 ailable, with no overt signs of toxicity and potent activity in both murine xenograft and patient-der
19 h IC50 values of less than 20 nM, is <100 nM potent against JAK2 and HDAC11, and is selective for the
21 ive significant clinical benefit from a more potent ALK inhibitor after failure of crizotinib, and es
25 onstrained derivative 36 emerged as the most potent analogue with a KD of 76 nM against BioA and a mi
26 its D-enantiomer, D-RR4, emerged as the most potent analogues with a more than 32-fold improvement in
27 es in identification of donors with the most potent and broad anti-HIV serum neutralizing responses w
28 elicit distinct antibody specificities with potent and broad neutralizing activity against all seven
30 compound 27 (DNS-8254), was identified as a potent and highly selective PDE2a enzyme inhibitor with
31 uin rearranging ligands (SirReals) as highly potent and isotype-selective Sirt2 inhibitors with thali
32 oparticle (NP; PC7A), in human PBMCs induces potent and long-acting antiretroviral response against s
34 Oligomeric proanthocyanidins (OPACs) are potent and renewable natural bioactives possible to be r
35 on led to identification of compound 25 as a potent and selective A2A adenosine receptor (A2AAdoR) an
38 perspectives in the development of new more potent and selective arsenical drugs against solid tumor
39 sing SBDD culminated in the discovery of the potent and selective Brr2 inhibitor 9 with helicase inhi
42 as found to be sufficient to explain Pre1a's potent and selective inhibitory effect on the fast inact
43 4A-activating C-DIM compounds may serve as a potent and selective means to enhance memory and synapti
45 against pathogens that can also result in a potent and sometimes pathological inflammatory response.
46 , our study supports that 38u might act as a potent and specific AEP inhibitor useful for cancer trea
48 n, butanol also enhanced fusion but was less potent, and low doses of methanol mildly inhibited fusio
49 forward in the search of chemically simple, potent, and selective antagonists for the hA3AR, and exe
52 , HDAC2 represses thrombospondin-1 (TSP1), a potent angiogenesis inhibitor, through epigenetic regula
55 pholide (ANDRO), a botanical compound, has a potent anti-inflammatory activity due to its ability to
56 s corticosteroids) are steroid hormones with potent anti-inflammatory and immune modulatory profiles.
57 cialized proresolving mediator (SPM) hosting potent anti-inflammatory and proresolving properties wit
60 tion is showcased by the construction of the potent antibacterial marine natural product bromophycoic
61 polyketide/fatty acid backbones and exhibit potent antibiotic activity against methicillin-resistant
62 a global threat as the clinically available potent antibiotic drugs are becoming exceedingly scarce.
63 winian process in which B lymphocytes evolve potent antibodies to encountered antigens and generate i
64 ne therapy (ET) with trastuzumab or with the potent antibody-cytotoxic, anti-HER2 compound trastuzuma
65 romising combinations of approved drugs with potent anticancer activity for further mechanistic study
66 of hydroxy fatty acids (FAHFAs), lipids with potent antidiabetic and anti-inflammatory activities, in
67 n (4-hydroxy-N-desmethyltamoxifen), the most potent antiestrogenic metabolite, are reduced in women w
74 -alkynyl-1,2,3-triazole family that exhibits potent antileukemic effects on several hematologic malig
77 vancomycin disaccharide to provide even more potent antimicrobial agents [VRE minimum inhibitory conc
78 isting mainly of monoterpenes, including the potent antimicrobial and insecticidal monoterpene 3-care
79 stems, chemical defence systems comprised of potent antimicrobial compounds released by prospective h
81 .11) mg GAEg(-1) respectively, and exhibited potent antioxidant activity (from 0.28+/-0.01 to 5.34+/-
82 Our results demonstrate that 5-HT acts as a potent antioxidant and binds with a superior affinity to
84 odocytes and that NAC (N-acetyl-cysteine), a potent antioxidant, significantly eliminated the excessi
85 ed to compare clopidogrel with ticagrelor, a potent antiplatelet agent, in patients with peripheral a
87 have resulted in compounds with moderate to potent antitubercular activity and improved physicochemi
88 d inspired the discovery of a novel class of potent antitubercular agents that unexpectedly possessed
90 agellin derivatives, have been shown to have potent antitumor and metastasis-suppressive effects in m
92 V-1 integrase strand transfer inhibitor with potent antiviral activity and a long half-life when admi
93 Taken together, these data suggest that the potent antiviral capacity of some HIV-specific CD8(+) T
95 of arenavirus nucleoproteins and uncovers a potent antiviral host protein that is neutralized during
97 nd aroma extract dilution analysis, the most potent aroma components include: dipropyl disulfide, S-p
98 at the African ZIKV isolate (MR-766) is more potent at causing brain damage and postnatal lethality t
99 several models of inflammation yet was less potent at inhibiting chemotaxis in vitro with an IC50 of
100 e now show that ANI-7 is up to 263-fold more potent at inhibiting the growth of breast cancer cell li
101 show that HLA-B*14-EL9 is substantially more potent at inhibiting viral replication than HLA-B*14-DA9
105 for a variety of GPCRs with a propensity for potent binding across therapeutically relevant adenosine
107 l design parameters for the creation of more potent biological delivery agents for research and biome
108 ndent growth rates of two algae that produce potent biotoxins, Alexandrium fundyense and Dinophysis a
111 30 and rLmI/h30 vaccines were generally more potent booster vaccines than r30 with an adjuvant and a
113 pproach we discovered a highly selective and potent BTK kinase inhibitor (CHMFL-BTK-11) which exerted
115 rapy in that it facilitates the emergence of potent CD8(+) T-cell immunity able to durably suppress v
116 fter prolonged exposure to the selective and potent CDK4/6 inhibitor LY2835219, clones emerged and se
117 mportant attribute to consider for obtaining potent cell-based inhibition of this cancer metabolism t
120 ive neurobiological mechanism underlying the potent combination of psychotherapy and somatic stimulat
123 we here identify arylmethylamino steroids as potent compounds and characterize more than 60 derivativ
124 The previously identified selective and potent CYP11B1 inhibitor 5-((5-methylpyridin-3-yl)methyl
128 s of ternary complex formation and were more potent degraders than tetrahydroquinoline compounds, whi
129 uggest that hepsin, like matriptase, induces potent destruction of the extracellular matrix whilst di
131 colibactins) are unsaturated imines that are potent DNA damaging agents, thereby confirming an earlie
132 3'-telomeric overhang of telomeres, elicits potent DNA-damage responses in melanoma cells; however,
133 aneous administration of ALN-GO1 resulted in potent, dose-dependent, and durable silencing of the mRN
134 r and BTB domain-containing 7b (Zbtb7b) as a potent driver of brown fat development and thermogenesis
138 Consequently, Lp/OVA/StII induced a more potent effector function, as shown by CTLs, in vivo assa
140 mbined SFK/FAK inhibition exhibited the most potent effects on growth inhibition, induction of apopto
142 ne of the challenges these species face is a potent environmental source of DNA double-strand breaks,
144 immunogenic, but it is expected that a more potent formulation will be required to establish antibod
146 onin containing fraction-4 (F4) was the most potent fraction based on its ability to inhibit ROS prod
148 starting from the structural similarity of a potent G4 ligand previously discovered by our group and
155 ologous transactivation domains can act as a potent guide RNA sequence-directed inducer or repressor
157 ich we obtained X-ray structures of the most potent hit (compound 19, IC50 = 2.9 muM) in complex with
160 lent safety profile and property of inducing potent immune responses against recombinant (r) antigens
162 s vaccination strategies to elicit broad and potent immune responses based on the immunomodulatory pr
163 ent pathogen Streptococcus pyogenes secretes potent immunomodulatory proteins known as superantigens
164 Among them, ginsenoside Ro was the most potent in inhibiting embryonic implantation within non-c
165 ession of the wild-type PDGFRA was even more potent in promoting transformation than the mutant PDGFR
168 ocally acting SGLT1 inhibitor that is highly potent in vitro and delays intestinal glucose absorption
169 er of the vitamin E family of compounds with potent in vitro anti-cancer properties, is limited by it
171 d to have limited brain penetrance, elicited potent in vitro CB1R antagonist activities and iNOS inhi
172 proliferation of cSCC cells and resulted in potent inhibition of extracellular signal-regulated kina
176 ed compared with soluble protein, leading to potent inhibition of wound closure following PMN-MP bind
177 l acetamide, has been identified as a novel, potent inhibitor against human 11beta-hydroxysteroid deh
178 exemplifies as a cautionary tale how a more potent inhibitor does not necessarily generate more pote
179 action assay, was less cytotoxic, and a more potent inhibitor of alpha-smooth muscle actin protein ex
180 inhibitory assays demonstrated that it was a potent inhibitor of human cathepsins B, K, and L ( Ki =
181 ive E2f-mediated transactivation of Socs3, a potent inhibitor of Jak2 signaling, in cycling HSCs.
182 eoxyriboside triphosphate, in vivo creates a potent inhibitor of several human DNA polymerases that c
183 Here, we describe the discovery of the most potent inhibitor of sirtuin 5 (SIRT5) reported to date.
186 ng cells (IC50 = 230 nM), providing the most potent inhibitor of the sonic hedgehog/patched interacti
188 e SET8-NQO1/TRXR1 axis with its specific and potent inhibitors could lead to promising host-directed
189 tetrazole-containing derivatives were highly potent inhibitors in both assays, with complete inhibiti
190 In particular, compounds 13 and 14 are very potent inhibitors in that they demonstrated the lowest I
191 er exhibit poor amyloid formation and act as potent inhibitors in trans of simple polyQ peptide aggre
192 tial, we targeted our efforts at identifying potent inhibitors of FXIa with a focus on discovering an
193 This work identifies TGF-beta1 and BMP-2 as potent inhibitors of IL-34 expression in RA synovial fib
195 ludes lipid substrates for enzymatic assays, potent inhibitors, and chemical probes to detect, track,
197 G505 SOSIP, have improved the elicitation of potent isolate-specific antibody responses in rabbits an
198 orum-sensing (QS) apparatus have a rapid and potent killing phenotype following microinjection into a
201 s study, we demonstrate that GA101 is a more potent mediator of trogocytosis than RTX in vitro in bot
203 rain penetrating PDE1B enzyme inhibitor with potent memory-enhancing effects in a rat model of object
206 on will enable the structure-based design of potent modulators of these clinically relevant enzymes.
208 F-GCN4t was also shown to bind D25, a highly potent monoclonal antibody specific for the pre-F confor
214 Methylmercury (MeHg(+) ) is one of the most potent neurotoxins, which damages the brain and nervous
215 active breadth for sera identified as having potent neutralization activity based on initial screenin
216 spread in fibroblasts, including those with potent neutralizing activity against fibroblast entry, w
219 tes, and Proteobacteria phyla, we found that potent Nod-like receptor-stimulating bacteria in the upp
220 The design and synthesis of a new series of potent non-prostanoid IP receptor agonists that showed o
221 itis B patients under long-term therapy with potent nucleos(t)ide analogues is currently unclear.
223 result in altered on-target sites and novel potent off-target sites, which can predispose patients t
224 munocytokines that are up to 1,000-fold more potent on target cells, allowing specific signaling in s
225 Administration of bictegravir, a novel, potent, once-daily INSTI designed to improve on existing
227 ane proteins SUN1/UNC84A and SUN2/UNC84B are potent or modest inhibitors of HIV-1 infection, respecti
228 fragment-derived lead resulting in AT-IAP, a potent, orally bioavailable, dual antagonist of XIAP and
230 with inhaled or topical delivery resulted in potent pan-JAK inhibitor 2 (PF-06263276), which was adva
231 y of PDE2A inhibition, we sought to identify potent PDE2A inhibitors with improved brain penetration
234 whereas Pt-G4K(+)B hydrogels exhibited more potent photocytotoxicity (IC50 3 muM, blue light) with a
235 ation of all-trans retinoic acid (ATRA) as a potent Pin1 inhibitor provides a promising candidate for
238 d incorporation assays: TGFbeta1 delivered a potent pro-fibrotic stimulus, which was reduced by TGFbe
239 inhibitor does not necessarily generate more potent PROTACs and underscores the key roles played by t
240 ed that these viral vectors can mediate more potent protection against influenza virus infection in a
241 atase 1 regulatory subunit 1A (PPP1R1A) is a potent protein phosphatase 1 (PP1) inhibitor; however, i
242 e results suggest a novel role for EMCN as a potent regulator of angiogenesis and point to its potent
243 mation, our data demonstrate that IL-27 is a potent regulator of ROS induction and may be a novel the
244 and bryostatin-1 could thus be considered as potent regulators of BBB permeability and inflammation t
245 l, strains carrying the pocR gene locus were potent reuterin producers, with L. reuteri 17938 inhibit
247 IL-7-immunized mice promptly produced a more potent secondary anti-RABV neutralizing antibody respons
248 of rapid ecological change, one of the most potent selective forces, sexual selection, remains curio
250 e-based drug design has resulted in a highly potent, selective, brain penetrant compound 71 (PF-05085
252 ed ascarosides, which include several highly potent signals in intra and interspecies communication a
253 pore-forming protein Perfringolysin O (PFO), potent silencing was achieved in vitro with no detectabl
255 these data demonstrate that 6E11 is a novel potent small molecular inhibitor of RIPK1-driven necropt
256 oji berries therefore might represent a more potent source of macular pigments than green leafy veget
257 P1B inhibitor trodusquemine (MSI-1436), is a potent, specific, and orally bioavailable inhibitor of P
258 cutaneous leishmaniasis, identifying several potent structures that exhibited EC50 values of <100 nM.
259 nyl))I](+) (where p-cym=para-cymene) exhibit potent sub-micromolar antiproliferative activity towards
261 0 overexpression, we identified miR-100 as a potent suppressor of endothelial adhesion molecule expre
262 which encodes an H3K36 methyltransferase, as potent suppressors of morc-1(-) and nuclear RNAi mutant
263 atabase indicates that the structure of most potent sweeteners combines a hydrophobic scaffold functi
264 bination and PARP-mediated DNA repair yields potent synthetic lethality in triple-negative breast tum
267 s scFvFITC:sTRAIL and scFvFITC:sFasL induced potent target antigen-restricted apoptosis in a panel of
269 lin-36-[L28C(30kDa-PEG)] is 10,000-fold less potent than apelin-36 at activating the APJ receptor but
270 rogenic effects to BPA and that BPAF is more potent than BPA, further highlighting health concerns re
272 system, Proxison is orders of magnitude more potent than natural flavonoids at protecting neural cell
273 inhibition of Notch signaling that was more potent than pharmacologic blockage of Notch activation v
274 ll receptor coregulatory molecule GITR exert potent therapeutic activities in preclinical tumor model
275 cles such as cyclosporine are among the most potent therapeutics identified to date, but there is cur
278 all changes in arterial CO2 are particularly potent to change CBF (1 mmHg variation in arterial CO2 c
279 Thus, R. typhi(GFPuv) bacteria are a novel, potent tool to study infection with the pathogen in vitr
283 of the UPR, cleaves Xbp1 mRNA to generate a potent transcription factor adaptive toward ER stress.
288 , Ace-DEX MP-encapsulated cGAMP represents a potent vaccine adjuvant of humoral and cellular immunity
290 Justicidin B is structurally similar to more potent vacuolar-type H(+)-ATPase inhibitors, which all i
292 c oxide synthase (eNOS), which generates the potent vasodilator nitric oxide (NO), is decreased.
294 (APOBEC) 3 proteins have been identified as potent viral DNA mutators and have broad antiviral activ
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