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Examples of Agonist

Sentences with the noun Agonist

2 examples:

Liraglutide is an agonist of glucagon-like receptor-1, which is a component of an important biological system that inhibits food intake and enhances insulin secretion from the pancreas in the presence of glucose.
(Nature Reviews Endocrinology, )

Our results show that conformational changes in transmembrane segments 5 and 6 (TM5 and TM6), which are required for the full engagement of a G protein, are almost completely dependent on the presence of both the agonist and the G protein mimetic nanobody, revealing a weak allosteric coupling between the agonist-binding pocket and the G-protein-coupling interface (TM5 and TM6), similar to that observed for the β2-adrenergic receptor.
(Nature, )

Other sentences

53 examples:

An orally available, highly selective agonist of Gpr120 is developed and tested.
(Nature Medicine, )

After agonist removal, these changes persist for longer than the direct receptor interaction.
(Nature, )

How agonist peptides initiate the T cell antigen receptor (TCR) signaling cascade is widely debated.
(Nature Immunology, )

The drug, selexipag, is a first-in-class orally available selective prostacyclin IP receptor agonist.
(Forbes - Technology, )

Importantly, mice fed a high-fat diet and treated with an A2A agonist are leaner with improved glucose tolerance.
(Nature, )

However, direct evidence that addresses how agonist binding leads to the formation of an active receptor state is scarce.
(Nature, )

In contrast, partial agonist (LUF5834) and an allosteric modulator (HMA) exclusively increase the population of the S3 state.
(Nature, )

δ activity is impaired by mutant huntingtin, and a PPAR-δ agonist attenuates disease in a mouse model of Huntington's disease.
(Nature Medicine, )

Agonist and non-nucleotide antagonist adopt different orientations in the P2Y12R, with only partially overlapped binding pockets.
(Nature, )

Weiss and Chakraborty discuss current models of the proximal signaling events that ensue upon recognition of agonist peptide–MHC complexes by TCRs.
(Nature Immunology, )

A rationally designed peptide agonist that targets three key hormone receptors reduces obesity and its complications in a manner superior to other agonists.
(Nature Medicine, )

The activity of a peptide agonist on a G protein–coupled receptor is readily modulated by altering its backbone structure without changing its side chains.
(Nature Biotechnology, )

Here the authors use a variety of structural approaches to rationally design PPARγ inverse agonist SR2595, and demonstrate its ability to promote osteogenesis.
(Nature Communications, )

Taking B2AR agonist asthma drugs during pregnancy appears to be associated with an increased risk that the child will develop autism, according to new research.
(Science Daily - News, )

We obtain spectra of the μOR in the absence of ligand, and in the presence of the high-affinity agonist BU72 alone, or with BU72 and a G protein mimetic nanobody.
(Nature, )

Here the authors describe azobenzene-triazole-glutamate ( ATG ), a new diffusible photoswitchable agonist that allows precise temporal control over NMDAR activity.
(Nature Communications, )

Our results support a general mechanism for the activation of mGluRs in which agonist binding induces closure of the LBDs, followed by dimer interface reorientation.
(Nature, )

Notably, a highly potent, selective FXR agonist obeticholic acid (INT-747) counteracted these effects, suggesting a potential new therapeutic avenue for liver disease.
(Science Daily - News, )

The GABAB receptor agonist R-baclofen (R-BAC) improves non-rapid eye movement sleep quality and alleviates cataplexy in a mouse model of narcolepsy, a new study has shown.
(Nature Reviews Neurology, )

The molecular mechanism involves the estrogen-related receptor γ (ERRγ) in the liver, which can be targeted with an inverse agonist to improve survival of infected animals.
(Nature Medicine, )

Here Wang et al. report structures of Smoothened in complex with antagonists and an agonist, and describe how mutations may result in resistance to anti-Smoothened treatment.
(Nature Communications, )

A new study reports that the oestrogen receptor beta agonist LY500307 does not improve symptoms in men with enlarged prostate secondary to benign prostatic hypertrophy (BPH).
(Nature Reviews Urology, )

New cryo-electron microscopy structures of these receptors trapped in distinct functional states provide remarkable insight into conformational changes triggered by agonist binding.
(Nature Chemical Biology , )

While investigating acupuncture mechanisms, the researchers also have determined that fenoldopam, a dopamine receptor agonist, also shows promise as a pharmaceutical sepsis treatment.
(Science Daily - News, )

The results of a futility trial, which used the PPAR-γ receptor agonist pioglitazone in an attempt to modify disease progression in Parkinson disease, do not support initiation of further trials.
(Nature Reviews Neurology, )

TAK-875, or fasiglifam, is an orally available, potent and selective partial agonist of hGPR40 receptor, which reached phase III clinical trials for the potential treatment of type-2 diabetes mellitus.
(Nature, )

Few Medicare enrollees appear to be receiving buprenorphine-naloxone, the only opioid agonist therapy for opioid addiction available through Medicare Part D prescription drug coverage, according to a study.
(Science Daily - News, )

The risk of several adverse events is higher in patients who receive gonadotropin-releasing hormone agonist (GnRHa) therapy for prostate cancer than in those who undergo orchiectomy, according to a new paper.
(Nature Reviews Urology, )

Addition of inverse agonist (ZM241385) increases the population of the inactive states, while full agonists (UK432097 or NECA) stabilize the active state, S3′, in a manner consistent with conformational selection.
(Nature, )

Although mutagenesis and modelling studies of the P2Y12R provided useful insights into ligand binding, the agonist and antagonist recognition and function at the P2Y12R remain poorly understood at the molecular level.
(Nature, )

The agonist-bound P2Y12R structure answers long-standing questions surrounding P2Y12R–agonist recognition, and reveals interactions with several residues that had not been reported to be involved in agonist binding.
(Nature, )

The β3-adrenoceptor agonist mirabegron is a novel agent, which relaxes urinary bladder smooth muscle in patients with overactive bladder syndrome (OAB); however, the exact mechanism of action of this agent remains elusive.
(Nature Reviews Urology, )

To address how agonist binding is transduced into pore opening in NMDARs, the authors manipulated the coupling between the ligand binding domain (LBD) and the ion channel and performed computational and thermodynamic analyses.
(Nature Neuroscience, )

The ability of bound ligands to dissociate from the receptor is also hindered, providing a structural explanation for the G-protein-mediated enhancement of agonist affinity, which has been observed for many GPCR–G-protein pairs.
(Nature, )

The human OX2 receptor (OX2R) belongs to the β branch of the rhodopsin family of GPCRs, and can bind to diverse compounds including the native agonist peptides orexin-A and orexin-B and the potent therapeutic inhibitor suvorexant.
(Nature, )

Here the authors report the peptide, P5, a variant of the GLP-1 receptor agonist exendin-4, with 'biased' signalling activity, and show that P5 improves glucose homeostasis in diabetic mice by increasing adipose tissue hyperplasia.
(Nature Communications, )

The initial 5α-reduced metabolite, 3-keto-5α-abiraterone, is present at higher concentrations than D4A in patients with prostate cancer taking abiraterone, and is an androgen receptor agonist, which promotes prostate cancer progression.
(Nature, )

Here the authors show PX-RICS deficient mice exhibit autism-like social behavioural abnormalities and impaired GABA A receptor trafficking, and enhancing inhibitory synaptic transmission with a GABA A receptor agonist ameliorate the behavioural deficits.
(Nature Communications, )

By combining mathematical simulation and biochemical experiments in cultured adult cardiomyocytes, Shin et al . show that the concentration of a β-adrenergic receptor agonist affects the expression of Bcl-2, influencing the balance between cell survival and death.
(Nature Communications, )

Surprisingly, the effects of G protein on the hormone-binding site can be observed in the absence of a bound agonist, where G-protein coupling driven by basal receptor activity impedes the association of agonists, partial agonists, antagonists and inverse agonists.
(Nature, )

The dopamine D1 receptor agonist fenoldopam mesylate does not prevent deterioration of renal function in patients with early acute kidney injury (AKI) after cardiac surgery, according to new findings from a randomized controlled trial (RCT) by Tiziana Bove and colleagues.
(Nature Reviews Nephrology, )

Here we report the structures of the human P2Y12R in complex with the full agonist 2-methylthio-adenosine-5′-diphosphate (2MeSADP, a close analogue of endogenous agonist ADP) at 2.5 Å resolution, and the corresponding ATP derivative 2-methylthio-adenosine-5′-triphosphate (2MeSATP) at 3.1 Å resolution.
(Nature, )

In a large phase 3 randomized clinical trial, addition of the peroxisome proliferator–activated receptor agonist aleglitazar to standard medical therapy was ineffective in protecting against cardiovascular morbidity among patients with type 2 diabetes mellitus (T2DM) who were hospitalized after an acute coronary syndrome.
(Nature Reviews Endocrinology, )

Both peptides bind with high affinity to the melanocortin-4 receptor (MC4R); existing data show that α-MSH is an agonist that couples the receptor to the Gαs signalling pathway, while AgRP binds competitively to block α-MSH binding and blocks the constitutive activity mediated by the ligand-mimetic amino-terminal domain of the receptor.
(Nature, )

In a group of young users of injection drugs, recent maintenance opioid agonist therapy with methadone or buprenorphine for opioid use disorders, such as heroin addiction, was associated with a lower incidence of hepatitis C virus infection and may be an effective strategy to reduce injection-drug use and the resulting spread of HCV, according to a study.
(Science Daily - News, )

Unexpectedly, in the presence of agonist alone, we find larger spectral changes involving intracellular loop 1 and helix 8 compared to changes in TM5 and TM6. These results suggest that one or both of these domains may play a role in the initial interaction with the G protein, and that TM5 and TM6 are only engaged later in the process of complex formation.
(Nature, )

Our data also indicate that, in contrast to agonist binding alone, coupling of a G protein in the absence of an agonist stabilizes large structural changes in a GPCR. The effects of nucleotide-free G protein on ligand-binding kinetics are shared by other members of the superfamily of GPCRs, suggesting that a common mechanism may underlie G-protein-mediated enhancement of agonist affinity.
(Nature, )

Crystallographic evidence from a prototypic GPCR, the β2-adrenergic receptor (β2AR), in complex with its cognate G protein, Gs, has provided a model for how agonist binding promotes conformational changes that propagate through the GPCR and into the nucleotide-binding pocket of the G protein α-subunit to catalyse GDP release, the key step required for GTP binding and activation of G proteins.
(Nature, )

However, there remain unanswered questions about the mechanism of channel opening and closing, the location and nature of the shut ion channel gate, the transitions between the closed/resting, open/activated and closed/desensitized states, and the mechanism by which conformational changes are coupled between the extracellular, orthosteric agonist binding domain and the transmembrane, ion channel domain.
(Nature, )

As a first example, to our knowledge, of a GPCR in which agonist access to the binding pocket requires large-scale rearrangements in the highly malleable extracellular region, the structural and docking studies will therefore provide invaluable insight into the pharmacology and mechanisms of action of agonists and different classes of antagonists for the P2Y12R and potentially for other closely related P2YRs.
(Nature, )

Here we show that, in mice, regulation of firing activity of neurons from the paraventricular nucleus of the hypothalamus (PVN) by α-MSH and AgRP can be mediated independently of Gαs signalling by ligand-induced coupling of MC4R to closure of inwardly rectifying potassium channel, Kir7.1. Furthermore, AgRP is a biased agonist that hyperpolarizes neurons by binding to MC4R and opening Kir7.1, independently of its inhibition of α-MSH binding.
(Nature, )

In 2011 our group published structures of the Caenorhabditis elegans glutamate-gated chloride channel (GluCl) in complex with the allosteric partial agonist ivermectin, which provided insights into the structure of a possibly open state of a eukaryotic Cys-loop receptor, the basis for anion selectivity and channel block, and the mechanism by which ivermectin and related molecules stabilize the open state and potentiate neurotransmitter binding.
(Nature, )

We find that the agonist isoprenaline has a 15,000-fold higher affinity for β2AR in the presence of Nb80 compared to the affinity of isoprenaline for β2AR in the presence of Nb60, highlighting the full allosteric range of a GPCR. Assessing the binding of 17 ligands of varying efficacy to the β2AR in the absence and presence of Nb60 or Nb80 reveals large ligand-specific effects that can only be explained using an allosteric model which assumes equilibrium amongst at least three receptor states.
(Nature, )

Other examples

See also examples for agonists, Co-Agonist.

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