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Related Concept Videos

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

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.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
Assembly of Signaling Complexes01:30

Assembly of Signaling Complexes

Multiprotein signaling complexes are formed in a dynamic process involving protein-protein interactions at the cytoplasmic domain of transmembrane receptors or enzymatic and non-enzymatic proteins associated with the receptor. These complexes ensure the activation and propagation of intracellular signals that regulate cell functions.
Interaction domains in cell signaling
Interaction domains recognize exposed features of their binding partners containing post-translationally modified sequences,...
Protein Dynamics in Living Cells01:19

Protein Dynamics in Living Cells

Different fluorescence-based techniques are used to study the protein dynamics in living cells. These techniques include FRAP, FRET, and PET.
Fluorescent recovery after photobleaching (FRAP) is a fluorescent-protein-based detection technique used to quantify protein movement rates within the cell. This method exposes a small portion of the cell to an intense laser beam. The laser beam causes permanent photobleaching of the fluorophore-tagged proteins in the exposed region. As the bleached...
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

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 cells.
Two...
Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

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.
GPCRs are also called heptahelical, 7TM, or...

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Deciphering the Structural Effects of Activating EGFR Somatic Mutations with Molecular Dynamics Simulation
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Energy landscapes as a tool to integrate GPCR structure, dynamics, and function.

Xavier Deupi1, Brian K Kobilka

  • 1Unitat de Bioestadística, Facultat de Medicina, Universitat Autònoma de Barcelona, Catalunya, Spain. xavier.deupi@psi.ch

Physiology (Bethesda, Md.)
|October 14, 2010
PubMed
Summary

G protein-coupled receptors (GPCRs) are key signaling proteins. New structural data and energy landscapes help explain how GPCR structure relates to their diverse functions in the body.

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Structural Biology

Background:

  • G protein-coupled receptors (GPCRs) are crucial cell surface receptors involved in numerous physiological processes.
  • They mediate cellular responses to a vast array of external signals, including hormones and neurotransmitters.
  • Understanding GPCR structure and dynamics is essential for deciphering their signaling mechanisms.

Purpose of the Study:

  • To explore the relationship between the structure and function of G protein-coupled receptors (GPCRs).
  • To utilize energy landscapes as a conceptual framework for understanding GPCR versatility.
  • To integrate recent high-resolution structural data with dynamic principles.

Main Methods:

  • Analysis of high-resolution structural data of GPCRs.
  • Application of energy landscape theory to model receptor dynamics.
  • Conceptualization of structure-function relationships using computational approaches.

Main Results:

  • Recent structural studies provide unprecedented detail into GPCR architecture.
  • Energy landscapes offer a framework to link static structures to dynamic functional states.
  • This approach illuminates the molecular basis for the broad signaling capabilities of GPCRs.

Conclusions:

  • The integration of structural insights and energy landscape concepts enhances our understanding of GPCR signaling.
  • GPCR versatility arises from a complex interplay of structure, dynamics, and energy states.
  • This conceptual model provides a foundation for future research into GPCR mechanisms and drug discovery.