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1 eliciting ligand-specific responses ("biased agonism").
2 oid receptor agonism) and tizanidine (alpha2 agonism).
3 beta4 selectivity to the alpha4beta2 partial agonism.
4 in the lungs of infected mice following S1PR agonism.
5 exacerbates MI/R injury, irrespective of EP4 agonism.
6 fold beta1-AR vs beta2-AR selectivity and no agonism.
7 abinoids which had been associated with CB1R agonism.
8 ls and suppresses IL-1beta release after TLR agonism.
9 ing pathways normally activated by full PAR1 agonism.
10 xtremely valuable method of quantifying drug agonism.
11 esidues into dTRPA1 recapitulates anesthetic agonism.
12 behavioral insensitivity to ghrelin receptor agonism.
13 ns in G-protein interaction underpin partial agonism.
14 ontrol signaling, a phenomenon termed biased agonism.
15 says, SARs were different, indicating biased agonism.
16 selectivity in promoting delta-OR over mu-OR agonism.
17 ioprotection primarily arises from PPARalpha agonism.
18 epresent a novel approach to achieve protean agonism.
19 ing bias, constitutive activity, and inverse agonism.
20 perates through a mechanism involving GPR120 agonism.
21 tin, a concept known as beta-arrestin-biased agonism.
22 ssed for selective retinoid X receptor (RXR) agonism.
23 g epithelial cells in a manner devoid of S1P agonism.
24 sting a mechanism for tissue specific biased agonism.
25 ngated aryl-ethynyl groups, exhibited biased agonism.
26 ivation and the mechanistic basis for biased agonism.
27 sign and interpretation of studies of biased agonism.
28 suggesting potential SERCA block and/or RyR agonism.
29 ling contribute to the pharmacology of super agonism.
30 DCD lungs, which are further reduced by A2AR agonism.
31 ypes using Wnt, FGF, cAMP and glucocorticoid agonism.
32 a novel analytical method to quantify biased agonism.
33 apo-GHSR1a and DRD1 that is enhanced by DRD1 agonism.
34 y with regard to agonism but also to inverse agonism.
35 erve cognitive enhancement through PPARgamma agonism.
36 inding free energies of PFASs relate to hPXR agonism.
37 eta(2)AR and provide a mechanism for inverse agonism.
38 or future in vitro and in vivo testing of ER agonism.
39 ammatory potential of GLP-1 receptor (Glp1r) agonism.
40 ide effects characteristic of balanced NTSR1 agonism.
41 signaling and the kinetic context of biased agonism.
42 e correspond to different degrees of inverse agonism.
43 ion and propose a mechanism for I942 partial agonism.
44 the ligand specificity toward HER4-dominant agonism.
45 th agonist efficacy, consistent with partial agonism.
46 ve an enhanced inflammatory response to TLR9 agonism.
47 (METx) would lead to selective AVP receptor agonism.
48 ctional profile of CB2 antagonism versus CB1 agonism.
49 s by immunogold electron microscopy, and its agonism 1) increased cAMP, 2) activated PKA, 3) phosphor
50 ther G proteins or arrestins-known as biased agonism(3)-is important in drug development, because the
53 ceptor to incorporate concepts of allosteric agonism, allosteric modulation, signaling bias, constitu
54 therapy or glucagon-like peptide 1 receptor agonism alone or in combination with sodium/glucose cotr
57 to the still enigmatic phenomenon of protean agonism and a rationale for the design of such compounds
58 potent purine scaffold TLR7 agonist to lose agonism and acquire antagonist activity, which could fur
59 ing of properly designed dose-dependent GPCR agonism and allosterism data permits the determination o
60 e develop and validate operational models of agonism and allosterism for receptors with multiple orth
63 a previously unrecognized convergence of Shh agonism and cyclin-dependent kinase inhibition as potent
66 ds, 2 and 4, showed dual PPARalpha/PPARgamma agonism and interesting food intake reduction in rats.
67 eature of the GPCR system is known as biased agonism and is subject to various interpretations, inclu
69 f CB1 allosteric modulators that show biased agonism and potentially antiobesity behavior via a new m
72 u, showed a balanced dual profile (i.e., MOR agonism and sigma antagonism) and a potent analgesic act
74 These results provide evidence that dual MOR agonism and sigma(1)R antagonism may be a useful strateg
75 oxycodone, providing evidence that dual MOR agonism and sigma(1)R antagonism may be a useful strateg
76 thered ligand that triggers biased G-protein agonism and thus predisposes platelets to full activatio
78 cing mouse hypothermia, despite mA(1)AR full agonism and variable mA(3)AR efficacy, but strong hypoth
81 n functional assays, did not exhibit inverse agonism, and behaved as a robust positive allosteric mod
82 may be a novel antifibrotic mechanism of FXR agonism, and EDP-305 could be used to treat renal fibros
84 aling amplitudes varied from full to minimal agonism, and structures of these DA/EpoR complexes diffe
85 onist receptor selectivity, bias, cell-based agonism, and the effects of receptor mutation on signali
86 oop family, reveals novel aspects of partial agonism, and unmasks molecular actions of classically de
90 disease-relevant phenotype often require an agonism approach to up-regulate or re-establish the acti
91 d on application of the operational model of agonism are frequently confounded by failure to consider
93 concepts of allosteric modulation and biased agonism are revolutionizing modern approaches to drug di
95 er, these results provide evidence for TAAR1 agonism as a novel pharmacological treatment for compuls
96 by donor apoptotic cells and implicate MerTK agonism as a promising target for promoting transplantat
97 ts highlight the potential of short-term Wnt agonism as a therapeutic target and establish a platform
99 orepressor associations, implicating partial agonism as the main driver of its dissociative propertie
100 range, we observed full, partial, and biased agonism as well as stage-selective effects on hematopoie
101 The recent pharmacological concept of biased agonism asserts that highly selective agonists can prefe
105 ion-promoting compound, indicate that biased agonism at MC receptors is an innovative, viable approac
106 us mGluR1 activator (i.e., endogenous biased agonism at mGluR1) and changes in spinal dynorphin/KOR s
108 crystal structures, the mechanism of partial agonism at the glycine-binding site is thought to be med
109 hin dualsteric compounds that elicit protean agonism at the muscarinic M2 acetylcholine receptor.
110 lor, inhibition of platelet ENT1 and inverse agonism at the P2Y12R that contribute to its effective i
111 SEP-363856, a novel psychotropic agent with agonism at trace amine receptor 1 (TAAR1) and 5-HT(1A) r
112 receptor (GPCR) signaling and ligand-biased agonism, at least three dimensional spaces must be consi
113 onstrated that adenosine A2A receptor (A2AR) agonism attenuates lung ischemia-reperfusion injury.
115 resence of "receptor reserve" and/or partial agonism, (b) multiple responses assessed at different va
116 e a complete allosteric framework for biased agonism based on alternative preexisting conformations t
117 improves and simplifies assessment of biased agonism because the same assay modality is used to compa
118 nd that NOP receptor antagonism, rather than agonism, blocks nicotine self-administration, which stro
121 ed version of ZnTerp that showed no inherent agonism but maintained positive allosteric modulation of
122 AM activity, those that showed no detectable agonism but robust PAM activity and ligands that display
123 ues without destroying mu-, delta-, or kappa-agonism, but the antinociceptive activity after i.v. adm
125 litated anti-OX40 antibody to have increased agonism by promoting the clustering of OX40 receptors wi
127 , Byun et al. demonstrate that the extent of agonism by these cGMP derivatives relates to the degree
128 control physiologic processes through biased agonism can reveal vital information required to enable
129 ile potent and selective partial alpha4beta2 agonism characterizes the hydroxybenzodioxane derivative
135 in vivo, and here we show that chronic GIPR agonism desensitizes GIPR activity in primary adipocytes
138 icient to overcome LID-resistance, and Nurr1 agonism exacerbated LID severity in dyskinetic rats.
139 iferation, and combined EP2 and EP4 receptor agonism exhibited positive cooperativity in both chronic
140 ses estradiol hypersensitivity and tamoxifen agonism, explaining the poor prognosis associated with n
141 n and the pharmacological response to GPR119 agonism, findings that may inform the lack of robust eff
143 1/2 phosphorylation, but it displays partial agonism for betaarr recruitment and receptor endocytosis
147 in mice and rats, we evaluated whether TAAR1 agonism had beneficial effects in two mouse models of na
149 t, glucagon-like peptide 1 receptor (GLP-1R) agonism has emerged as a preferred treatment for diabete
161 ity and possibly directly through PPAR-gamma agonism in patients ofT2DM with hypertriglyceridemia.
164 gest parallels between partial and/or biased agonism in RTKs and G-protein-coupled receptors, as well
166 Thus, we developed operational models of agonism in systems with cooperative agonist binding and
167 o rigorously assess the potential for biased agonism in the actions of endogenous opioids at the MOP
173 ping a systems-level understanding of biased agonism in vivo, with the overall goal of overcoming cur
176 increases wakefulness, whereas TAAR1 partial agonism increases wakefulness and also reduces NREM and
177 bility of tBPC to selectively potentiate Y4R agonism initiated by PP was confirmed in mouse descendin
178 previously undescribed mechanism for inverse agonism involving an omega loop to helix switch which in
181 perational model (OM) of functional receptor agonism is a useful means for the determination of agoni
182 tory properties of tapinarof derive from AhR agonism is conclusively demonstrated using the mouse mod
192 phaIIbbeta3 have been shown to cause partial agonism, leading to the opposite pharmacological effect.
193 s, combining muscarinic antagonism and beta2-agonism (MABA) in a single molecule, potentially provide
194 cotine withdrawal and suggest that PPARgamma agonism may represent a promising treatment to aid smoki
196 oncept of functional selectivity (aka biased agonism) might be useful for amplifying beneficial actio
197 sequencing analyses demonstrated that GPBAR1 agonism modulated the expression of multiple pathways, i
201 conformational selection model, the partial agonism of cAMP arises from the sampling of a third, par
202 lude blockade of co-stimulation pathways and agonism of coinhibitory pathways, in order to achieve th
205 d analyzed for in vitro bioactivities (e.g., agonism of ER, GR, and PPARgamma) and BC concentrations;
206 bile acids and their conjugates resulting in agonism of FXR in intestine and liver resulting in a sma
207 tinal crypt proliferation can be promoted by agonism of Fzd5 and/or Fzd8 receptors, while a broad spe
212 nist-mediated, glutamate-independent inverse agonism of group II and III metabotropic glutamate (mGlu
214 mpetition, but also suggest that the partial agonism of I942 arises from its ability to stabilize an
215 ith other actions (e.g., activation of ACE2, agonism of MAS1 receptors, beta-arrestin-based Angiotens
216 biological response is attained by selective agonism of MC(1), not shared by non-selective ligands, a
218 al cells, and in retinal pigment epithelium; agonism of PPARalpha with genetic or pharmacological too
221 coculture systems, we demonstrated that the agonism of the 41BB-41BBL axis enhanced costimulatory si
227 gammaRIIB can lead to a further boost of the agonism of the anti-OX40 antibody with IgG1 Fc but not w
229 long-term fear memories, and pharmacological agonism of the ghrelin receptor during the memory consol
231 vitro and in vivo effects of pharmacological agonism of the prostaglandin I2 (IP) receptor in pancrea
232 First, the selective blockade or inverse agonism of the type 1 cannabinoid receptor has been test
235 CR) for medium and long-chained fatty acids, agonism of which can regulate a myriad of metabolic, sen
236 We review the allosteric modulation, biased agonism, oligomerization, and compartmentalized signalin
237 perational model of allosterically-modulated agonism (OMAM) including modulation by allosteric agonis
238 trates that mediate the effects of PPARgamma agonism on alcohol drinking and seeking in msP rats.
240 ur dual agonist lead compound exhibited weak agonism on FXR and PPARdelta and was structurally refine
241 es of the drug comprising selective and dual agonism on RXRs and PPARs that may serve as superior pha
244 GPCRs now extends beyond simple competitive agonism or antagonism by ligands interacting with the or
245 on through selective GLP-1 receptor (GLP-1R) agonism or by prevention of enzymatic degradation by inh
246 increases habituation, whereas serotonergic agonism or DRN activation with ChR2 reduces habituation.
248 as signal bias, allosteric modulation, dual agonism, polymorphic receptor variants, spatial compartm
249 duction by iNKT cells after IR and that A2AR agonism prevents IR injury by blocking NOX2 activation i
253 ibility that direct activation by allosteric agonism, rather than allosteric modulation, could be res
256 proliferator-activated receptor (PPAR) gamma agonism reversed TNFalpha-induced insulin resistance.
257 ion is attributed to mild mu-opioid receptor agonism, serotonin and norepinephrine mediated nocicepti
258 detectable MAPK signaling activities, C5aR2 agonism significantly dampened C5aR1-, C3aR-, and chemok
259 ext set out to determine whether IP receptor agonism similarly affects nephrin phosphorylation in pod
260 d to be a nonselective S1P receptor agonist, agonism specifically of S1P1 is responsible for the peri
261 t was evoked by exogenous adenosine receptor agonism, suggesting upstream impairment, likely astrocyt
262 r, like other class B GPCRs, displays biased agonism, though the physiologic significance of this is
263 Overall, our findings show a novel mode of agonism through an allosteric site in the extracellular
264 dentify compounds that likely mediated their agonism through an irreversible interaction with the A1A
265 we elucidate the mechanism for cAMP partial agonism through the comparative NMR analysis of the apo,
266 and in derivatives of 1 by Trp turned Y(4)R agonism to antagonism, giving Y(4)R antagonists with pK(
267 nd the basis for ligand selectivity and BTLA agonism to develop novel anti-inflammatory agonists.
268 nhibitor Entinostat (MS-275) enhances GLP-1R agonism to potentiate glucose-stimulated insulin secreti
269 therapeutics that attempt to restrict 4-1BB agonism to the tumor microenvironment and minimize syste
270 erine 273 (S273) in the absence of classical agonism, to derive insulin-sensitizing efficacy with imp
271 e following the in vitro evaluation of H(3)R agonism using a cyclic adenosine monophosphate response
272 neurons (ChIs) by dopamine D2 receptor (D2R) agonism using ex vivo slice electrophysiology in Dyt1 (D
273 ferator-activated receptor-gamma (PPARgamma) agonism using thiazolidinediones has potent podocyte cyt
274 rovide insights into the structural basis of agonism versus antagonism in steroid receptors with pote
279 imilarly, in mice with advanced tumors, GITR agonism was not sufficient to activate cytolytic T cells
281 Thus, the anti-inflammatory action of Glp1r agonism was tested in a nondiabetic, T-cell-mediated mur
284 investigate the structural basis of partial agonism, we performed comparative microsecond-scale mole
285 ct system for the mechanistic study of CD11b agonism, we present in this study, to our knowledge, a n
286 21680) demonstrated sustained wash-resistant agonism, where residual receptor activation continued af
289 s that are synergistic or antagonistic to M1 agonism, which we have prospectively experimentally veri
290 plex) DCyFIR modes, recapitulated known GPCR agonism with 100% accuracy, and identified unexpected in
293 the inflammasome by Toll-like receptor (TLR) agonism with bacterial lipopolysaccharide (LPS) and the
294 clinical evidence to rationally combine GITR agonism with checkpoint blockade in future clinical tria
296 ctly promoted the integrated use of glucagon agonism with other hormones in a manner that runs counte
297 ted the first in-human phase 1 trial of GITR agonism with the anti-GITR antibody TRX518 ( NCT01239134
298 residues involved in peptide-mediated biased agonism, with R2.60(190), N3.43(240), and Q7.49(394) pre
299 vation, extends the novel concept of partial agonism within the Cys-loop family, reveals novel aspect
300 = 6.6 x 10(-7)), liver X receptor alpha/beta agonism (z = 2.1, P = 2.8 x 10(-7)), and inhibition of l