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1 ) GBS67 protein antigen with the CpGODN TLR9 agonist.
2 upled to GPR52 in the absence of an external agonist.
3 by intraplantar paw administration of a C3aR agonist.
4 th both heterotrimeric Gi protein and MP1104 agonist.
5 a nonamphiphilic control and the native TLR agonist.
6 NFkappaB activation in response to a TLR7/8 agonist.
7 llosterically elicited by the binding of the agonist.
8 nonbiased agonists and to the TRV130 biased agonist.
9 of small molecules (Q compounds) acts as RET agonists.
10 severity and may impair response to beta-AR agonists.
11 the context of receptor selectivity of such agonists.
12 2+ influx in response to all tested platelet agonists.
13 r the structure-based discovery of selective agonists.
14 ubunits which are differentially promoted by agonists.
15 frequency following delivery of serotonergic agonists.
16 rect neuronal target for histamine and Mrgpr agonists.
17 NBC cell lines were hyperresponsive to STING agonists.
18 itory actions of endogenous opioids and DOPr agonists.
19 nists, structurally unrelated to the natural agonists.
20 ally stable, highly potent and selective Kv7 agonists.
22 onse to maximally effective concentration of agonist 4-fold, and the racemate is brain-penetrant.
25 g them, compound 51 emerged as a potent CB2R agonist able to reduce pain in rats carrying OA induced
26 monocyte-derived macrophages, using a C5aR2 agonist (Ac-RHYPYWR-OH; P32) to selectively activate the
27 he presence of PES, the M1 and M4 helices of agonist-activated receptor rearrange, forming a tighter
28 ded chemokine structure but diminished CXCR4 agonist activity as measured by ERK phosphorylation, che
29 oes not act on dopamine D2 receptors but has agonist activity at trace amine-associated receptor 1 (T
30 mpounds 3b and 3e with mu-OR (MOR) selective agonist activity in the moderate range (EC(50) = 1-100 n
31 ic analogue 2-fluoro-ATP, and to confirm its agonist activity on rat P2X2 receptors expressed in huma
34 s the affinity and potency of the endogenous agonist alpha-melanocyte-stimulating hormone at the MC4R
36 ed by co-administration of the CB(2) inverse agonist AM630 (5 mg/kg, IP), but not the CB(1) inverse a
38 ta2 nicotinic acetylcholine receptor partial agonist and alpha7 receptor full agonist varenicline in
40 data to construct mathematical models of ER agonist and antagonist pathways to prioritize chemicals
41 man tryptases, protease activated receptor 2 agonist and antagonist peptides, and a tryptase-neutrali
43 ey establish RR-RJW100 as the stronger LRH-1 agonist and identify a potential for optimizing the SS-R
44 perimental data demonstrating the effects of agonists and allosteric modulators at receptors where ag
45 ota characteristics related to use of opioid agonists and antagonists among people receiving outpatie
46 uss current therapeutic strategies utilizing agonists and antagonists targeting nucleic acid sensors
48 s), glucagon-like peptide-1 (GLP-1) receptor agonists and dipeptidyl peptidase 4 (DPP4) inhibitors, w
49 This effect is mirrored by subunit-selective agonists and heteromeric receptors that contain binding-
50 ed unforeseen binding sites for both cooling agonists and membrane lipid phosphatidylinositol 4,5-bis
51 lective nucleosides are low efficacy partial agonists and novel, nuanced modulators of the A(3)AR, a
52 luence of CXCR1 and CXCR2 chemokine receptor agonists and other chemotactic factors produced by tumor
54 as these complexes are stabilized by inverse agonists and receptor mutations that favor the inactive
56 ts highlight the value of receptor-selective agonists and the importance of appropriately interpretin
59 oupled serotonin receptors, protein kinase C agonists, and a microbial metabolite not previously know
60 s TLR-MyD88 signaling independent of foreign agonists, and is further enhanced by CD40-CD40L interact
66 nation of anti-PD-1 inhibitory and anti-OX40 agonist antibodies reduces the proportion of T-regulator
67 el, activation by orthosteric and allosteric agonists appeared as openings in quick succession (burst
68 nd Selective Human Estrogen-Receptor Partial Agonists are being evaluated in endocrine-resistant BC c
70 ironment and suggests use of a synthetic LXR agonist as a novel therapeutic strategy to stimulate ant
71 ted in an efficacious, brain-penetrant GPR52 agonist as a valuable pharmacological tool for investiga
73 dition to TLR9 agonists, TLR2, TLR3, or TLR4 agonists, as well as TNF-alpha, IL-6, or IL-17A, but not
74 h B12 and FA blunt the effect of natural AhR agonists at baseline to prevent the symptoms that arise
75 to ATP, including the previously identified agonists ATPgammaS and ATPalphaS, we were also able to i
76 e used to monitor equilibrium binding of the agonist, ATR, as well as the noncovalent binding of beta
77 d whether a single 10 mg dose of the GABA(B) agonist baclofen impaired motor sequence learning and vi
78 a novel chemical series of non-bile acid FXR agonists based on a tricyclic dihydrochromenopyrazole co
80 netriol] (OCH), a T(H)2-polarizing iNKT cell agonist, before they received alpha-galactosylceramide.
83 ed the idea that this monovalent ion reduces agonist binding by stabilizing the receptor inactive sta
84 and allosteric modulators at receptors where agonist binding follows hyperbolic (M(4) muscarinic acet
86 and observation of allosteric regulation by agonist binding with MD remains difficult due to the tim
87 he unliganded (4.1- angstrom resolution) and agonist-bound (3.3 angstrom) states using single-particl
88 microscopy to elucidate the structure of an agonist-bound activated DRD2-G(i) complex reconstituted
89 In this issue of Cell, two papers report agonist-bound cryo-EM structures of the cannabinoid rece
91 This study validates the suitability of the agonist-bound orthosteric pocket in the MT receptor stru
92 same scheme that includes transitions of the agonist-bound receptor to closed intermediate states bef
93 ches containing a single NMDAR, we find that agonist-bound receptors transition to the open state via
96 s of the channel in the presence of the full agonist cAMP, but not with the partial agonist cGMP.
97 injection of 20E or the application of a 20E agonist can significantly impact Plasmodium infection ou
98 increasingly clear that chemically distinct agonists can produce different receptor-based effects.
101 g candidates yielded the discovery of 10 new agonist chemotypes with sub-micromolar potency at MT rec
103 P), an MC3R/MC4R antagonist and MC4R inverse agonist, contains an exposed beta-hairpin loop composed
106 e effects of systemic injections of the CB1r agonist (CP55940) on the balanced activity of the direct
108 ASOs can be selected to synergize with TLR8 agonists currently under investigation as immunotherapie
109 ose that G protein-biased mu opioid receptor agonists, currently in development as analgesics, should
110 P(2) We further show that a selective S1P(2) agonist, CYM-5478, reduces allodynia in a rat model of c
111 unstable series of mu-opioid receptor (MOR) agonist/delta-opioid receptor (DOR) antagonist bicyclic
113 he most potent and selective LPA(1) receptor agonist described so far (E(max) = 118%, EC(50) = 0.24 m
114 anism, the structural basis of CB2-selective agonists design, and the unexpected interaction of chole
115 nsciousness (LOC) with the alpha2-adrenergic agonist dexmedetomidine and return of consciousness (ROC
116 LAT-1 inhibitor), we showed that the efflux agonist did not inhibit the uptake of extracellular leuc
118 arinic M(3) receptor antagonists and inverse agonists displaying high affinity and subtype selectivit
121 k the development of promising CB2-selective agonist drugs for treating inflammatory and neuropathic
122 dified tirofiban are as effective as partial agonist drugs in inhibiting vascular thrombosis in human
124 romising anticancer activity induced by CB2R agonists due to their ability to reduce inflammation and
125 Glucagon-like peptide 1 receptor (GLP-1R) agonists effectively improve glycemia and body weight in
126 RAMP control mG(s) coupling and defined how agonist engagement of the CLR extracellular and transmem
127 subcellular calcium events as well as strong agonist-evoked calcium activation and cytoplasmic secret
128 and non-noxious general anesthetics inhibit agonist-evoked transient receptor potential ankyrin type
129 r (GLP-1R)-positive lesions, using the GLP-1 agonist exendin-4 labeled with IRDye 800CW, was examined
130 ystemic administration of the GLP-1 receptor agonist exendin-4 reduced oxycodone self-administration
131 ation and proliferation and suggest that PKC agonists exhibit potential as an antifibrotic treatment.
133 isomal proliferated activated receptor alpha agonist, fenofibrate, on liver and kidney autophagy and
134 have shown previously that the S1P receptor agonist fingolimod (FTY720) attenuates psychosine-induce
135 -(3,4-dichlorobenzyl)oxime (CITCO) is a dual agonist for human constitutive androstane receptor (hCAR
136 es of two magic methyl substrates-an inverse agonist for the nuclear receptor RORc and an antagonist
137 Measuring the apparent affinities of the agonists for the mG(s)-coupled receptors and of mG(s) fo
139 that longer term treatment with alpha7 nAChR agonists for these deficits in SCZ may be promising.
140 w synthetic trifluorinated chalcone and Nrf2 agonist, for targeted pulmonary inhalation aerosol drug
141 ramuscularly with the potent GPR30-selective agonist G-1 at 0 or 1 mug/day and fed a lithogenic diet
142 reat BC is potentially superior to a partial agonist given BPTPE's delayed induction of UPR and apopt
144 of these findings, we demonstrate that a 20E agonist, halofenozide, is able to induce anti-Plasmodium
148 ibitors and glucagon-like peptide 1 receptor agonists have consistently shown safety and reduction in
150 gh previous studies have shown that mGluR2/3 agonists have no effect on dopamine (DA) in wild type ra
151 tivation via administration of the selective agonist imiquimod (5.0 mg/kg) induces a phenotype in off
152 pically with the Toll-like receptor 7 (TLR7) agonist imiquimod (IMQ) to activate IFN-sensitive gene (
153 rophobic small-molecule toll-like receptor 7 agonist, imiquimod (IMD), and a hydrophilic macromolecul
154 we demonstrate that nicotinic acid receptor agonists impair cardiac contractility associated with a
157 dy, we investigated whether beta2-adrenergic agonists improve both neurotransmission and structural i
159 n deprotection afforded 10, which was a full agonist in Ca(2+)-release assays; its potency and bindin
160 ons, chronic administration of a D1 receptor agonist in conjunction with fluoxetine restores the effi
161 d chemokine (C-X-C motif) receptor 4 (CXCR4) agonists in a rat acute respiratory distress syndrome (A
167 ion function-2 (AF-2) helix 12 mechanism for agonist-induced coactivator interaction and NR transcrip
175 nistically novel, extremely G protein-biased agonists is in question, as is the underlying assumption
178 f the response by CB(2) receptors, the CB(2) agonist JWH133 (0.3, 1 and 3 mg/kg, IP) also produced an
179 tigate the effect of ICS/long-acting beta(2)-agonist (LABA) treatment on both lung function measures
186 chronic administration of the approved beta3 agonist mirabegron to human subjects was without effect
188 rein, we investigate the effects of a KISS1R agonist, MVT-602, in healthy women and in women with rep
190 o elevated glucose and the selective P2Y(11) agonist NF546 is blocked by disruption of A-kinase ancho
191 ion of human brain endothelial cells by NMDA agonists (NMDA or glycine) and the serine protease tissu
192 Compared to 31 participants who used neither agonists nor antagonists, 5 participants who used opioid
193 herapies for NASH, the bile acid-derived FXR agonist obeticholic acid (OCA; 6-ethyl chenodeoxycholic
194 mG(s)-coupled receptors and of mG(s) for the agonist-occupied receptors revealed that both ligand and
196 and the soy isoflavone genistein, a natural agonist of peroxisome proliferator-activated receptor ga
197 drug for treating multiple sclerosis, is an agonist of sphingosine-1-phosphate receptor (S1PR), whic
200 hosphate-adenosine monophosphate (cGAMP), an agonist of the interferon gene inducer STING (stimulator
202 several highly potent and selective inverse agonists of GHSR based on the 1,2,4-triazole scaffold.
204 onists: they are among the least efficacious agonists of Ins(1,4,5)P(3)R yet identified, providing ne
205 in, fargesin, and delta-sanshool as putative agonists of PPARG, along with previously identified agon
208 at mediate the suppressive effects of GLP-1R agonists on cocaine-seeking behavior are largely unknown
209 cinogen studies, the effects of kappa-opioid agonists on human brain function are not well-understood
210 microglia ablation, the effects of NF-kappaB-agonists on MGPC-formation are reversed, suggesting that
213 at the CB2R, compounds able to act either as agonists or as inverse agonists/antagonists were discove
214 were injected with viral (Imiquimod, a TLR7 agonist) or bacterial (ODN 2395, a TLR9 agonist) surroga
215 nt analgesic activity, comparable to the MOR agonist oxycodone in the paw pressure test in mice.
216 the lipopeptide Toll-like receptor (TLR)2/6 agonist, Pam2Cys (P2C), and the synthetic MR1 ligand, 5-
217 tide library derived from the canonical PAR4-agonist peptide, AYPGKF-NH(2), and we monitored activati
218 ort our discovery of a bi-directional ephrin agonist peptide, BIDEN-AP which, when selectively intern
220 determined in complex with their orthosteric agonist peptides, however, little is known about their e
221 eptide-1 (GLP-1) receptor by the non-peptide agonist PF 06882961 and GLP-1 that was not observed for
223 effects of a novel ghrelin receptor inverse agonist, PF-5190457, when co-administered with alcohol.
224 whose signaling activation by the selective agonist pioglitazone reduces alcohol drinking and alcoho
226 tabotropic glutamate receptor 2/3 (mGluR2/3) agonists (pomaglumetad [POMA] and TS-134) were assessed
227 We used [(11)C]carfentanil, a selective MOR agonist positron emission tomography (PET) radioligand,
232 lls expanded in vivo by one of the surrogate agonists preserved the typical VAT-Treg transcriptional
234 lic acid (4-Cl-3-HAA), a suppressor of NMDAR agonist quinolinic acid (QUIN), is a promising potential
237 roterenol (ISO) and related beta2-adrenergic agonists reacidify lysosomes in PSEN1 Knock out (KO) cel
239 mpact of three different doses of a novel D1 agonist (relative to placebo) on reactivity to reward-pr
242 f rats with PTOA treated with liposomal A2AR agonist revealed downregulation of genes associated with
244 ver therapy with as-needed short-acting beta-agonists (SABAs), while anti-inflammatory maintenance wi
246 ration of new synthetic cannabinoid receptor agonists (SCRAs) has initiated considerable interest in
250 uced a larger increase in basal activity and agonist sensitivity at room temperature than the Pro to
252 f these six ERalpha genotypes to a set of ER agonists showed that both steric and electrostatic facto
253 ineages, matched differentiation programs of agonist-signaled cells to their MHC specificity, and ide
257 espective families and represent novel hMC1R agonists, structurally unrelated to the natural agonists
258 The approaches involved in delivery of TLR2 agonists such as lipidation of antigen, conjugation to p
259 th the efficacy and potency of partial kappa agonists, such as the benzomorphans, and the classic mu
260 poRon, a small-molecule adiponectin receptor agonist, suppress colon cancer risk in part by reducing
264 ling topographical cues with the profibrotic agonist, TGFbeta (transforming growth factor beta), addi
266 erator-activated receptor-alpha (PPAR-alpha) agonist that exerts profound anti-inflammatory effects i
267 lar domain of PC-1 functions as an intrinsic agonist that is necessary and sufficient for channel act
268 ML417 is a novel and uniquely selective D3R agonist that may serve as both a research tool and a the
269 isome proliferator-activated receptor gamma) agonist that stimulates mitochondrial activity, ameliora
272 lphaS, we were also able to identify a novel agonist, the synthetic analogue 2-fluoro-ATP, and to con
273 riptional activation by gmAhr's with various agonists, the distinct binding properties with TCDD and
274 it is crucial to effectively scale-up opioid agonist therapy (OAT), such as methadone or buprenorphin
276 , both l-glucose-derived ligands are partial agonists: they are among the least efficacious agonists
278 Our work concludes that the use of a full agonist to treat BC is potentially superior to a partial
279 gn and chemistry for the conjugation of TLR2 agonists to antigens, carbohydrates, polymers, and fluor
281 These data show for the first time that GnRH agonist treatment after puberty onset exerts sex-specifi
284 ic inhibition of dopamine release by the KOR agonist U69,593 was not blocked by in vivo pretreatment
285 tor partial agonist and alpha7 receptor full agonist varenicline in rats that self-administered nicot
294 48) is a toll-like receptor 7 and 8 (TLR7/8) agonist with potent antitumor and immunostimulatory acti
297 e converted into potent FcgammaR-independent agonists with remarkable antitumor activity by isotype s
299 antagonists, 5 participants who used opioid agonists (without antagonists) had lower microbiota dive