10 papers · ranked by Valyu relevance
James P. Higham, David Colquhoun
A fundamental mistake in receptor theory has led to an enduring misunderstanding of how to estimate the affinity and efficacy of an agonist. These properties are inextricably linked and cannot be easily separated in any case where the binding of a ligand induces a conformation change in its receptor. Consequently…
Yoonji Lee, Sun Choi, Changbong Hyeon
Dynamics and functions of G-protein coupled receptors (GPCRs) are accurately regulated by the type of ligands that bind to the orthosteric or allosteric binding sites. To glean the structural and dynamical origin of ligand-dependent modulation of GPCR activity, we performed total ∼ 5 µsec molecular dynamics simulations…
Yuya Koga, Kento Kawaharazuka, Moritaka Onitsuka, Tasuku Makabe + 5 more
'Kei Tsuzuki' 'Yusuke Omura' 'Yuki Asano' 'Kei Okada' 'Masayuki Inaba'] Abstract— In recent years, some research on musculoskeletal humanoids is in progress. However, there are some challenges such as unmeasurable transformation of body structure and muscle path, and difficulty in measuring own motion because of lack…
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Targeting retinoic acid-related orphan receptor γ (RORγ) with inverse agonists presents a promising therapeutic strategy for treating autoimmune diseases, including psoriasis, rheumatoid arthritis, and multiple sclerosis. Through structure-based virtual screening, we identified a lupane-type pentacyclic triterpenoid…
Sabine Willems, Romy Busch, Felix Nawa, Marco Ballarotto + 12 more
Nuclear receptor related 1 (Nurr1, NR4A2) is a ligand-sensing transcription factor with neuroprotective and anti-inflammatory roles widely distributed in the CNS. Pharmacological Nurr1 modulation is considered a promising experimental strategy in Parkinson's and Alzheimer's disease but target validation is incomplete.…
Laura Riccetti, Romain Yvinec, Danièle Klett, Nathalie Gallay + 5 more
'Yves Combarnous' 'Éric Reiter' 'Manuela Simoni' 'Livio Casarini' 'Mohammed Akli Ayoub'] Human luteinizing hormone (LH) and chorionic gonadotropin (hCG) have been considered biologically equivalent because of their structural similarities and their binding to the same receptor; the LH/CGR. However, accumulating…
Spencer Kim, Dylan Gray, Michelle Shanguhyia, Rachel Steinhardt
Recreating the signaling profile a chemical synapse to analyze serotonin receptor activation is a challenge. This is due in part to the kinetics of the synapse, where neurotransmitters are rapidly released and quickly cleared by active reuptake machinery. One strategy to produce a rapid rise in a bio-orthogonally…
Ranjita Dutta-Roy, Christian Rosenmund, Stuart J. Edelstein, Nicolas Le Novère
'Nicolas Le Novère'] Modulation of the properties of AMPA receptors at the post-synaptic membrane is one of the main suggested mechanisms underlying fast synaptic transmission in the central nervous system of vertebrates. Electrophysiological recordings of single channels stimulated with agonists showed that both…
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GPR3 belongs to the protein superfamily of G protein-coupled receptors (GPCRs) and plays a central role in both benign and malignant physiological processes, such as energy expenditure in adipocytes and Alzheimer’s disease pathology, respectively. Despite the therapeutic potential of both receptor agonists and inverse…
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Allosteric modulators offers a promising approach for targeting receptor function in pathological contexts. Although numerous orthosteric ligands have been developed, the discovery of allosteric inhibitors remains limited, hindered by challenges with identifying modulators and the perceived lower druggability of…