Bridging the gap: bitopic ligands of G-protein-coupled receptors.
about
Multiple protein stationary phases: a reviewMuscarinic acetylcholine receptor X-ray structures: potential implications for drug developmentA new mechanism of allostery in a G protein-coupled receptor dimerWhat can crystal structures of aminergic receptors tell us about designing subtype-selective ligands?Disruption of the Na+ ion binding site as a mechanism for positive allosteric modulation of the mu-opioid receptor.Reversible inhibitors of regulators of G-protein signaling identified in a high-throughput cell-based calcium signaling assay.Investigation of the binding and functional properties of extended length D3 dopamine receptor-selective antagonistsReceptor, Ligand and Transducer Contributions to Dopamine D2 Receptor Functional Selectivity.Computational Advances for the Development of Allosteric Modulators and Bitopic Ligands in G Protein-Coupled ReceptorsDevelopment of M1 mAChR allosteric and bitopic ligands: prospective therapeutics for the treatment of cognitive deficitsMolecular Pharmacology of δ-Opioid Receptors.A synthetic bivalent ligand of CXCR4 inhibits HIV infectionSeparation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonistBiased agonism at G protein-coupled receptors: the promise and the challenges--a medicinal chemistry perspective.Muscarinic acetylcholine receptors: novel opportunities for drug development.Insights into the structural biology of G-protein coupled receptors impacts drug design for central nervous system neurodegenerative processes.GPR40 agonists for the treatment of type 2 diabetes: life after 'TAKing' a hit.New approaches in the design and development of cannabinoid receptor ligands: multifunctional and bivalent compounds.Ethyl Vanillin Activates TRPA1.Quantitative analysis of receptor allosterism and its implication for drug discovery.Rational Modification of the Biological Profile of GPCR Ligands through Combination with Other Biologically Active Moieties.On the 'micro'-pharmacodynamic and pharmacokinetic mechanisms that contribute to long-lasting drug action.The Pharmacology and Function of Receptors for Short-Chain Fatty Acids.On the different experimental manifestations of two-state 'induced-fit' binding of drugs to their cellular targetsMultivalent approaches and beyond: novel tools for the investigation of dopamine D2 receptor pharmacology.High performance enzyme kinetics of turnover, activation and inhibition for translational drug discovery.Pharmacologically distinct phenotypes of α1B -adrenoceptors: variation in binding and functional affinities for antagonists.'Partial' competition of heterobivalent ligand binding may be mistaken for allosteric interactions: a comparison of different target interaction models.Pharmacological properties of acid N-thiazolylamide FFA2 agonists.Molecular mechanism of allosteric modulation at GPCRs: insight from a binding kinetics study at the human A1 adenosine receptor.Avidity and positive allosteric modulation/cooperativity act hand in hand to increase the residence time of bivalent receptor ligands.Simplified models for heterobivalent ligand binding: when are they applicable and which are the factors that affect their target residence time.A Photoswitchable Dualsteric Ligand Controlling Receptor Efficacy.Synthesis of novel and functionally selective non-competitive muscarinic antagonists as chemical probes.The E2.65A mutation disrupts dynamic binding poses of SB269652 at the dopamine D2 and D3 receptors.Synthesis and Pharmacological Characterization of Novel trans-Cyclopropylmethyl-Linked Bivalent Ligands That Exhibit Selectivity and Allosteric Pharmacology at the Dopamine D3 Receptor (D3R).Bitopic muscarinic agonists and antagonists and uses thereof: a patent evaluation of US20160136145A1.Ligands at the Free Fatty Acid Receptors 2/3 (GPR43/GPR41).Prediction of consensus binding mode geometries for related chemical series of positive allosteric modulators of adenosine and muscarinic acetylcholine receptors.Heterodimerization of Dibenzodiazepinone-Type Muscarinic Acetylcholine Receptor Ligands Leads to Increased M2R Affinity and Selectivity.
P2860
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P2860
Bridging the gap: bitopic ligands of G-protein-coupled receptors.
description
2012 nî lūn-bûn
@nan
2012年の論文
@ja
2012年学术文章
@wuu
2012年学术文章
@zh-cn
2012年学术文章
@zh-hans
2012年学术文章
@zh-my
2012年学术文章
@zh-sg
2012年學術文章
@yue
2012年學術文章
@zh
2012年學術文章
@zh-hant
name
Bridging the gap: bitopic ligands of G-protein-coupled receptors.
@en
type
label
Bridging the gap: bitopic ligands of G-protein-coupled receptors.
@en
prefLabel
Bridging the gap: bitopic ligands of G-protein-coupled receptors.
@en
P2093
P50
P1476
Bridging the gap: bitopic ligands of G-protein-coupled receptors
@en
P2093
Arthur Christopoulos
J Robert Lane
Patrick M Sexton
P356
10.1016/J.TIPS.2012.10.003
P577
2012-11-20T00:00:00Z