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1 eliciting ligand-specific responses ("biased agonism").
2 suggesting potential SERCA block and/or RyR agonism.
3 abinoids which had been associated with CB1R agonism.
4 ling contribute to the pharmacology of super agonism.
5 DCD lungs, which are further reduced by A2AR agonism.
6 ypes using Wnt, FGF, cAMP and glucocorticoid agonism.
7 a novel analytical method to quantify biased agonism.
8 apo-GHSR1a and DRD1 that is enhanced by DRD1 agonism.
9 y with regard to agonism but also to inverse agonism.
10 ls and suppresses IL-1beta release after TLR agonism.
11 erve cognitive enhancement through PPARgamma agonism.
12 d in addition may allow for designed partial agonism.
13 ing the molecular basis for dual GP-BAR1/FXR agonism.
14 ing pathways normally activated by full PAR1 agonism.
15 otypes have been found to show S1P1 receptor agonism.
16 fold beta1-AR vs beta2-AR selectivity and no agonism.
17 xtremely valuable method of quantifying drug agonism.
18 ysteines in TRPA1 resulted in a loss of DNCB agonism.
19 or their retinoid X receptor (RXR) selective agonism.
20 pathways, a phenomenon referred to as biased agonism.
21 4(+) DC deficiency can be rescued by LTbetaR agonism.
22 ut enhanced weight loss stimulated by GLP1-R agonism.
23 esidues into dTRPA1 recapitulates anesthetic agonism.
24 o isomer 6 (MRS5701) displayed mixed A1/A3AR agonism.
25 o improve affinity, selectivity, and partial agonism.
26 discovered it possessed significant partial agonism.
27 ist at the M3 receptor without measurable M2 agonism.
28 osiglitazone, implying gene-specific partial agonism.
29 behavioral insensitivity to ghrelin receptor agonism.
30 the induction of oxidative genes by beta-AR agonism.
31 to a mature-like locomotor pattern by D(4)R agonism.
32 at the biological effects were due to GPR119 agonism.
33 ed to a mature-like pattern via spinal D(4)R agonism.
34 ns in G-protein interaction underpin partial agonism.
35 ontrol signaling, a phenomenon termed biased agonism.
36 says, SARs were different, indicating biased agonism.
37 selectivity in promoting delta-OR over mu-OR agonism.
38 ioprotection primarily arises from PPARalpha agonism.
39 epresent a novel approach to achieve protean agonism.
40 ing bias, constitutive activity, and inverse agonism.
41 perates through a mechanism involving GPR120 agonism.
42 tin, a concept known as beta-arrestin-biased agonism.
43 ssed for selective retinoid X receptor (RXR) agonism.
44 g epithelial cells in a manner devoid of S1P agonism.
45 sting a mechanism for tissue specific biased agonism.
46 ngated aryl-ethynyl groups, exhibited biased agonism.
47 ivation and the mechanistic basis for biased agonism.
48 sign and interpretation of studies of biased agonism.
49 s by immunogold electron microscopy, and its agonism 1) increased cAMP, 2) activated PKA, 3) phosphor
53 ceptor to incorporate concepts of allosteric agonism, allosteric modulation, signaling bias, constitu
55 to the still enigmatic phenomenon of protean agonism and a rationale for the design of such compounds
56 e MOR/KOR dual-selective ligand 10 showed no agonism and acted as a potent antagonist in the tail-fli
57 ing of properly designed dose-dependent GPCR agonism and allosterism data permits the determination o
59 egration of these NMR studies with the known agonism and antagonism profiles of these peptides in Agr
60 a previously unrecognized convergence of Shh agonism and cyclin-dependent kinase inhibition as potent
61 uence can decide between agonism and inverse agonism and have a major impact on the biological activi
63 ds, 2 and 4, showed dual PPARalpha/PPARgamma agonism and interesting food intake reduction in rats.
64 s in the peptide sequence can decide between agonism and inverse agonism and have a major impact on t
65 eature of the GPCR system is known as biased agonism and is subject to various interpretations, inclu
66 f CB1 allosteric modulators that show biased agonism and potentially antiobesity behavior via a new m
68 basis and are likely to involve both biased agonism and the many mu opioid receptor subtypes that ha
69 thered ligand that triggers biased G-protein agonism and thus predisposes platelets to full activatio
71 mine D3 antagonism, serotonin 5-HT1A partial agonism, and antagonism at 5-HT2A leads to a novel appro
72 n functional assays, did not exhibit inverse agonism, and behaved as a robust positive allosteric mod
73 aling amplitudes varied from full to minimal agonism, and structures of these DA/EpoR complexes diffe
74 onist receptor selectivity, bias, cell-based agonism, and the effects of receptor mutation on signali
75 oop family, reveals novel aspects of partial agonism, and unmasks molecular actions of classically de
79 inhibition of protein-protein interactions, agonism/antagonism of GPCR ligands, and anti-angiogenic
81 a few specific residues are associated with agonism/antagonism, affinity, and selectivity, and sugge
83 disease-relevant phenotype often require an agonism approach to up-regulate or re-establish the acti
84 concepts of allosteric modulation and biased agonism are revolutionizing modern approaches to drug di
87 er, these results provide evidence for TAAR1 agonism as a novel pharmacological treatment for compuls
88 pport the concept of GLP-1 and glucagon dual agonism as a possible treatment for obesity and diabetes
89 -like activity of BuTAC and implicate M4AChR agonism as a potential novel therapeutic mechanism for a
90 acute intestinal injury and highlights C3aR agonism as a potential treatment option for acute, neutr
93 The recent pharmacological concept of biased agonism asserts that highly selective agonists can prefe
94 5beta2,3gamma2S and rho1 GABAARs and partial agonism at alpha6beta2,3delta GABAARs expressed in Xenop
98 the decrease in respiratory rate, indicating agonism at GABA(B) receptors to be primarily responsible
100 ion-promoting compound, indicate that biased agonism at MC receptors is an innovative, viable approac
101 us mGluR1 activator (i.e., endogenous biased agonism at mGluR1) and changes in spinal dynorphin/KOR s
103 number of studies have suggested that biased agonism at the dopamine D2 receptor (D2R) may be advanta
105 crystal structures, the mechanism of partial agonism at the glycine-binding site is thought to be med
106 ontinence (SUI) and no measurable functional agonism at the key selectivity targets 5-HT2A and 5-HT2B
107 hin dualsteric compounds that elicit protean agonism at the muscarinic M2 acetylcholine receptor.
108 lor, inhibition of platelet ENT1 and inverse agonism at the P2Y12R that contribute to its effective i
111 receptor (GPCR) signaling and ligand-biased agonism, at least three dimensional spaces must be consi
112 onstrated that adenosine A2A receptor (A2AR) agonism attenuates lung ischemia-reperfusion injury.
114 e a complete allosteric framework for biased agonism based on alternative preexisting conformations t
115 f bitopic ligands and in coordinating biased agonism between intracellular calcium mobilization and E
116 nd that NOP receptor antagonism, rather than agonism, blocks nicotine self-administration, which stro
119 ed version of ZnTerp that showed no inherent agonism but maintained positive allosteric modulation of
120 AM activity, those that showed no detectable agonism but robust PAM activity and ligands that display
122 ues without destroying mu-, delta-, or kappa-agonism, but the antinociceptive activity after i.v. adm
124 litated anti-OX40 antibody to have increased agonism by promoting the clustering of OX40 receptors wi
126 e have demonstrated that efficacy and biased agonism can be finely tuned by minor structural modifica
127 eptor states (closed versus open) and how co-agonism can be readily understood as simply addition of
129 control physiologic processes through biased agonism can reveal vital information required to enable
131 ile potent and selective partial alpha4beta2 agonism characterizes the hydroxybenzodioxane derivative
132 ls as valid frameworks for understanding the agonism, coagonism, and modulation of ligand-gated ion c
133 ith the operational model of pharmacological agonism confirmed that endomorphin-2 had a much lower op
136 an individual sensitivity to GLP-1 receptor agonism could predict metabolic benefits of surgeries as
143 expressed in Xenopus oocytes, the pronounced agonism exhibited by the compound at alpha4beta1delta an
144 ciated in Tg2576 in vivo, and that PPARgamma agonism facilitated recruitment of PPARgamma to pERK dur
145 n and the pharmacological response to GPR119 agonism, findings that may inform the lack of robust eff
146 EGF receptor ligands may result from partial agonism for dimer formation, differences in the kinetic
149 tency at the CB1 receptor and high levels of agonism, good physical and pharmacokinetic properties, a
150 in mice and rats, we evaluated whether TAAR1 agonism had beneficial effects in two mouse models of na
154 ly, coagonist peptides that include glucagon agonism have emerged as promising therapeutic candidates
159 c series of mGlu5 PAMs exhibiting allosteric agonism in addition to positive allosteric modulation (a
160 the paradoxical effects of beta2AR and PAR2 agonism in asthma is that the beneficial and harmful eff
167 gest parallels between partial and/or biased agonism in RTKs and G-protein-coupled receptors, as well
168 o rigorously assess the potential for biased agonism in the actions of endogenous opioids at the MOP
170 ~ 3.0), was selected as a potent PAM with no agonism in the in vitro system used for compound charact
171 nce by selective 5-HT(3) receptor antagonism/agonism in the posterior (granular) region of the IC and
176 ping a systems-level understanding of biased agonism in vivo, with the overall goal of overcoming cur
178 increases wakefulness, whereas TAAR1 partial agonism increases wakefulness and also reduces NREM and
180 the peptide behavior from inverse agonism to agonism, indicating the importance of this sequence.
181 bility of tBPC to selectively potentiate Y4R agonism initiated by PP was confirmed in mouse descendin
186 tory properties of tapinarof derive from AhR agonism is conclusively demonstrated using the mouse mod
193 inimally invoking adipogenesis and classical agonism, is indeed a valid framework to develop improved
194 phaIIbbeta3 have been shown to cause partial agonism, leading to the opposite pharmacological effect.
196 r beta1-adrenoceptor selectivity and partial agonism (log KD of -7.75 and -5.15 as an antagonist of f
197 s, combining muscarinic antagonism and beta2-agonism (MABA) in a single molecule, potentially provide
198 pain, and it is believed that selective CB2 agonism may afford a superior analgesic agent devoid of
206 conformational selection model, the partial agonism of cAMP arises from the sampling of a third, par
207 lude blockade of co-stimulation pathways and agonism of coinhibitory pathways, in order to achieve th
210 bile acids and their conjugates resulting in agonism of FXR in intestine and liver resulting in a sma
216 would have to be consumed to sustain chronic agonism of Gpr120 is too high to be practical, and, thus
217 nist-mediated, glutamate-independent inverse agonism of group II and III metabotropic glutamate (mGlu
220 -FRET activation reporter assay demonstrated agonism of PPARgamma by all three compounds (EC(50) of 4
225 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
233 First, the selective blockade or inverse agonism of the type 1 cannabinoid receptor has been test
235 olitary tract known to be targeted by GLP-1R agonism, offering a potential mechanism for the interact
238 tested Pen derivatives displayed mild to no agonism on RyRs, SR Ca(2+) leak, or [(3)H]ryanodine bind
240 GPCRs now extends beyond simple competitive agonism or antagonism by ligands interacting with the or
241 on through selective GLP-1 receptor (GLP-1R) agonism or by prevention of enzymatic degradation by inh
243 increases habituation, whereas serotonergic agonism or DRN activation with ChR2 reduces habituation.
244 the molecular mechanisms of TLR4 activation (agonism) or inhibition (antagonism) by small organic mol
245 ulations directs cell fate, with chronic AhR agonism permissive to erythroid differentiation and acut
246 duction by iNKT cells after IR and that A2AR agonism prevents IR injury by blocking NOX2 activation i
248 ibility that direct activation by allosteric agonism, rather than allosteric modulation, could be res
249 al sphingosine 1-phosphate receptor 3 (S1P3) agonism recruits anti-inflammatory monocytes to remodeli
255 n and primarily targets T cells and that its agonism represents a potential novel therapeutic approac
256 the compounds, using an operational model of agonism, revealed a global signaling signature for all o
257 proliferator-activated receptor (PPAR) gamma agonism reversed TNFalpha-induced insulin resistance.
259 ext set out to determine whether IP receptor agonism similarly affects nephrin phosphorylation in pod
260 Local CCL4, a chemokine liberated by TLR7 agonism, similarly enhances central memory T cell functi
261 d to be a nonselective S1P receptor agonist, agonism specifically of S1P1 is responsible for the peri
264 specific signaling patterns, known as biased agonism, that produce distinct functional outputs by the
265 In concordance with its alpha6beta2,3delta agonism, Thio-THIP evoked robust currents through extras
266 r, like other class B GPCRs, displays biased agonism, though the physiologic significance of this is
267 dentify compounds that likely mediated their agonism through an irreversible interaction with the A1A
268 we elucidate the mechanism for cAMP partial agonism through the comparative NMR analysis of the apo,
269 t can swap the peptide behavior from inverse agonism to agonism, indicating the importance of this se
271 nd the basis for ligand selectivity and BTLA agonism to develop novel anti-inflammatory agonists.
273 layed intrinsic activities ranging from full agonism to partial agonism with low intrinsic activity.
274 contribution of cooperativity and allosteric agonism to the adverse effect liability and neurotoxicit
275 therapeutics that attempt to restrict 4-1BB agonism to the tumor microenvironment and minimize syste
276 erine 273 (S273) in the absence of classical agonism, to derive insulin-sensitizing efficacy with imp
277 red the sensitivity of these synapses to KOR agonism (U50488) or antagonism (norbinaltorphimine [norB
281 tructure-activity relationship of allosteric agonism was examined within an acetylenic series of mGlu
286 investigate the structural basis of partial agonism, we performed comparative microsecond-scale mole
287 21680) demonstrated sustained wash-resistant agonism, where residual receptor activation continued af
291 the inflammasome by Toll-like receptor (TLR) agonism with bacterial lipopolysaccharide (LPS) and the
294 xyphenyl)-N-arylhydantoins displayed partial agonism with nanomolar in vitro potency in transactivati
295 analgesic combining mu-opioid receptor (MOR) agonism with norepinephrine reuptake inhibition (NRI), m
297 residues involved in peptide-mediated biased agonism, with R2.60(190), N3.43(240), and Q7.49(394) pre
298 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
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