This Review discusses the potential advantages of allosteric ligands from a drug discovery perspective, and highlights opportunities that arise from these advantages. Here, we first provide a ...

Tremendous advances have been made in the discovery of novel ligands for G-protein-coupled receptors (GPCRs) that act at allosteric sites to regulate receptor function. Small molecules can act at ...

12月6日，国际知名期刊eLife在线发表了华中科技大学生命科学与技术学院刘剑峰教授团队题为“Allosteric ligands control the activation of a class C GPCR heterodimer by acting at the transmembrane interface”（变构配体通过跨膜相互作用界面控制C族GPCR异源二聚体激活）的最新科研成果 ...

Scientists have unlocked new details on important receptor proteins—promising targets for the creation of novel drugs for ...

The first class of drugs to demonstrate allostery were the benzodiazepines, which are allosteric ligands for a neurotransmitter γ-aminobutyric acid (GABA) receptor. Since then, many other ...

b. Two different agonists (ligands 2 and 3) promote a similar active state or conformation (R*), which binds the transducer (T1), but bias emerges through allosteric communication between the ...

But in allostery, ligands bind enzymes or receptors on sites other than the active site, and cause different effects. For example, allosteric binding can reduce or even stop the activity of a ...

Background: Many neuromuscular blockers act as negative allosteric modulators of muscarinic acetylcholine receptors by decreasing affinity and potency of acetylcholine. The neuromuscular blocker ...

Comparison of the effects of rapacuronium with those of the prototypic allosteric modulators alcuronium and gallamine (Figures eleven and twelve) on M 3 receptors shows that acceleration of ACh ...

This initiates the pathological hijacking. Such binding at a second site is called allosteric binding. In G protein-coupled receptors, allosteric ligands are known to often alter signaling of the ...

The firm claims the platform can identify orthosteric and allosteric ligands of GPCRs, including silent allosteric modulators and can address traditionally intractable targets such as orphan and p ...