Gα Protein Signaling Bias at Serotonin 1A Receptor. [PDF]
Mol Pharmacol, 2023 Serotonin 1A receptor (5-HT1AR) is a clinically relevant target because of its involvement in several central and peripheral functions, including sleep, temperature homeostasis, processing of emotions, and response to stress.
Alabdali R, Franchini L, Orlandi C.
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Structures of atypical chemokine receptor 3 reveal the basis for its promiscuity and signaling bias. [PDF]
Sci Adv, 2022 Both CXC chemokine receptor 4 (CXCR4) and atypical chemokine receptor 3 (ACKR3) are activated by the chemokine CXCL12 yet evoke distinct cellular responses. CXCR4 is a canonical G protein–coupled receptor (GPCR), whereas ACKR3 is intrinsically biased for
Yen YC +10 more
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Optimization of a Series of Mu Opioid Receptor (MOR) Agonists with High G Protein Signaling Bias. [PDF]
J Med Chem, 2018 While mu opioid receptor (MOR) agonists are especially effective as broad-spectrum pain relievers, it has been exceptionally difficult to achieve a clear separation of analgesia from many problematic side effects.
Kennedy NM +8 more
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Computationally designed GPCR quaternary structures bias signaling pathway activation
Nature Communications, 2022 Computational modeling and design of G Protein-Coupled Receptor quaternary structures reveals a signaling bias switch at the receptor dimer interface that selectively controls G protein vs β-arrestin activation.
Justine S. Paradis +12 more
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Is the Quest for Signaling Bias Worth the Effort? [PDF]
Molecular Pharmacology, 2018 The question of whether signaling bias is a viable discovery strategy for drug therapy is discussed as a value proposition. On the positive side, bias is easily identified and quantified in simple in vitro functional assays with little resource expenditure.
T. Kenakin
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Structurally Related Kappa Opioid Receptor Agonists with Substantial Differential Signaling Bias: Neuroendocrine and Behavioral Effects in C57BL6 Mice. [PDF]
Int J Neuropsychopharmacol, 2018 Background The kappa opioid receptor system has been revealed as a potential pharmacotherapeutic target for the treatment of addictions to substances of abuse.
Dunn AD +5 more
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Overconfidence is a Social Signaling Bias [PDF]
SSRN Electronic Journal, 2010 Evidence from psychology and economics indicates that many individuals overestimate their ability, both absolutely and relatively. We test three different theories about observed relative overconfidence. The first theory notes that simple statistical comparisons (for example, whether the fraction of individuals rating own skill above the median value ...
Burks, Stephen V. +3 more
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Fine Tuning Muscarinic Acetylcholine Receptor Signaling Through Allostery and Bias
Frontiers in Pharmacology, 2021 The M1 and M4 muscarinic acetylcholine receptors (mAChRs) are highly pursued drug targets for neurological diseases, in particular for Alzheimer’s disease and schizophrenia.
Emma T. van der Westhuizen +7 more
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The adenosine metabolite inosine is a functional agonist of the adenosine A2A receptor with a unique signaling bias. [PDF]
Cell Signal, 2016 Inosine is an endogenous purine nucleoside that is produced by catabolism of adenosine. Adenosine has a short half-life (approximately 10 s) and is rapidly deaminated to inosine, a stable metabolite with a half-life of approximately 15 h.
Welihinda AA +4 more
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Evaluating signaling bias for synthetic cannabinoid receptor agonists at the cannabinoid CB2 receptor [PDF]
Pharmacology Research & Perspectives, 2023 The rapid structural evolution and emergence of novel synthetic cannabinoid receptor agonists (SCRAs) in the recreational market remains a key public health concern.
Monica Patel +4 more
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