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Related Concept Videos

Allosteric Regulation01:08

Allosteric Regulation

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Allosteric regulation of enzymes occurs when the binding of an effector molecule to a site that is different from the active site causes a change in the enzymatic activity. This alternate site is called an allosteric site, and an enzyme can contain more than one of these sites. Allosteric regulation can either be positive or negative, resulting in an increase or decrease in enzyme activity. Most enzymes that display allosteric regulation are metabolic enzymes involved in the degradation or...
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Transducer Mechanism: G Protein–Coupled Receptors01:30

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G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
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Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of...
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G Protein-coupled Receptors01:15

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G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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Functional and structural perspectives on allosteric modulation of GPCRs.

Christopher J Langmead1, Arthur Christopoulos1

  • 1Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Department of Pharmacology, Monash University, 399 Royal Parade, Parkville 3052, Victoria, Australia.

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Summary

Allosteric sites on G protein-coupled receptors (GPCRs) offer new avenues for drug selectivity and pathway bias. Novel analytical methods are advancing the study of allosteric modulation in GPCRs.

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Area of Science:

  • Pharmacology
  • Molecular Biology
  • Biochemistry

Background:

  • G protein-coupled receptors (GPCRs) are key drug targets.
  • Orthosteric site modulation is the traditional approach for GPCR drug discovery.
  • GPCRs also feature allosteric sites that modulate receptor activity.

Purpose of the Study:

  • To explore the potential of allosteric sites for achieving GPCR subtype selectivity.
  • To highlight the advantages of allosteric modulation, including fine-tuning physiological responses and signal pathway bias.
  • To discuss the challenges and advancements in detecting and quantifying allosteric drug candidates.

Main Methods:

  • Review of recent breakthroughs in structural biology of GPCRs.
  • Application of computational biology approaches to GPCRs.
  • Development of novel analytical methods for quantifying allosteric modulation.

Main Results:

  • Allosteric sites present greater opportunities for receptor subtype selectivity compared to orthosteric sites.
  • Allosteric modulation allows for fine-tuning of physiological responses and signal pathway bias.
  • Advancements in analytical techniques are improving structure-activity and structure-function studies of allosteric modulation.

Conclusions:

  • Allosteric modulation of GPCRs offers significant therapeutic potential.
  • Understanding the molecular mechanisms of allosteric modulation is crucial for drug development.
  • Continued development of analytical and computational tools will accelerate the discovery of allosteric modulators.