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Related Concept Videos

Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Structure-Activity Relationships and Drug Design01:28

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Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
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Pharmacodynamic (PD) responses describe the interaction between a drug and its biological target, culminating in a physiological effect. These responses can be classified into different types: continuous variables, such as blood glucose levels; categorical outcomes, like survival rates; and time-to-event metrics, such as disease progression. Understanding and modeling PD responses are critical for optimizing drug efficacy and safety.PD models describe the relationship between drug concentration...
Transducer Mechanism: Nuclear Receptors01:31

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About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
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Indirect-acting cholinergic agonists are agents that interact with the acetylcholinesterase enzyme in the synaptic cleft, preventing the breakdown of acetylcholine into choline and acetate. Consequently, the concentration of acetylcholine in the synaptic cleft increases. These agonists can be classified into reversible and irreversible inhibitors based on their duration of action.
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[PPARs: structure, mechanisms of action and control. Note I].

Florina Filip-Ciubotaru1, Liliana Foia, Carmen Manciuc

  • 1Universitatea de Medicină Si Farmacie Gr. T. Popa Iaşi Facultatea de Medicină, Disciplina de Medicina de Familie.

Revista Medico-Chirurgicala a Societatii De Medici Si Naturalisti Din Iasi
|August 30, 2011
PubMed
Summary

Peroxisome proliferator activated receptors (PPARs) are ligand-activated transcription factors. They regulate gene expression through heterodimers with RXR, binding to DNA response elements and influencing various cellular functions.

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Area of Science:

  • Molecular Biology
  • Genetics
  • Cell Biology

Context:

  • Peroxisome proliferator-activated receptors (PPARs) are nuclear receptors that function as ligand-activated transcription factors.
  • Three main isoforms exist: PPAR-alpha, PPAR-beta/delta, and PPAR-gamma, each with distinct tissue expression and functions.
  • PPARs regulate gene expression by forming heterodimers with the retinoid X receptor (RXR) and binding to specific DNA sequences (PPREs).

Purpose:

  • To elucidate the fundamental mechanisms of PPARs as transcription factors.
  • To describe the structural and functional characteristics of PPAR isoforms.
  • To explain the process of PPAR-mediated gene regulation.

Summary:

  • PPARs are proteins that control gene activity upon binding to specific molecules (ligands).
  • They form complexes with RXR, translocate to the nucleus, and bind to DNA (PPREs) to modulate gene expression.
  • Ligand binding, cofactor recruitment, and post-translational modifications all regulate PPAR activity.

Impact:

  • Provides a foundational understanding of PPARs' role in cellular regulation.
  • Highlights the complexity of gene transcription control by nuclear receptors.
  • Establishes the basis for investigating PPARs in various physiological and pathological processes.