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Related Concept Videos

G-protein Coupled Receptors01:21

G-protein Coupled Receptors

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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.
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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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Structural Protein Function01:56

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Structural proteins are a category of proteins responsible for functions ranging from cell shape and movement to providing support to major structures such as bones, cartilage, hair, and muscles. This group includes proteins such as collagen, actin, myosin, and keratin.
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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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Protein and Protein Structure02:15

Protein and Protein Structure

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Proteins are one of the most abundant organic molecules in living systems and have the most diverse range of functions of all macromolecules. Proteins may be structural, regulatory, contractile, or protective. They may serve in transport, storage, or membranes; or they may be toxins or enzymes. Their structures, like their functions, vary greatly. They are all, however, amino acid polymers arranged in a linear sequence.
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Quantifying Agonist Activity at G Protein-coupled Receptors
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Quantifying Agonist Activity at G Protein-coupled Receptors

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Reprogramming G protein coupled receptor structure and function.

D Keri1, P Barth2

  • 1Swiss Federal Institute of Technology (EPFL), Interfaculty Institute of Bioengineering, 1015 Lausanne, Switzerland.

Current Opinion in Structural Biology
|July 29, 2018
PubMed
Summary
This summary is machine-generated.

G protein-coupled receptors (GPCRs) are crucial drug targets, but studying them is difficult. This review covers engineering methods to overcome challenges in GPCR characterization and understand their function.

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • G protein-coupled receptors (GPCRs) are the largest human gene family and a major focus for drug discovery due to their roles in physiology and disease.
  • Over 800 GPCRs exist in the human genome, making them a significant target for therapeutic interventions.
  • Challenges in GPCR research include low expression, instability outside native lipid environments, and complexities in studying in vivo signaling.

Purpose of the Study:

  • To review current and emerging engineering methods for GPCR characterization.
  • To address the challenges hindering GPCR research, including expression, stability, and functional studies.
  • To enhance the understanding of GPCR functional roles through improved characterization techniques.

Main Methods:

  • Summarizing existing GPCR engineering techniques.
  • Highlighting novel approaches in receptor stabilization and functional analysis.
  • Discussing strategies for spatiotemporal control of GPCR activation in functional studies.

Main Results:

  • Engineering methods can overcome low expression and stability issues.
  • Advanced techniques facilitate better structural characterization of GPCRs.
  • Improved methods allow for more precise in vivo functional studies of GPCR signaling.

Conclusions:

  • GPCR engineering is vital for advancing drug discovery and structural biology.
  • Overcoming technical hurdles through engineering enhances our understanding of GPCRs.
  • Future research will benefit from continued development of innovative GPCR engineering strategies.