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Related Concept Videos

Transducer Mechanism: Nuclear Receptors01:31

Transducer Mechanism: Nuclear Receptors

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Nuclear receptors, or NRs, are unique transcription factors that regulate gene transcription and affect the cellular pathways involved in reproduction, development, or metabolism. Their ability to be stimulated by small lipophilic ligands and control vital cellular processes makes them ideal drug targets. Nearly 10-15% of currently prescribed drugs target these receptors.
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
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Drug Metabolism: Phase I Reactions01:17

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A phase I reaction is a biochemical process that introduces a functionally reactive polar group to a substance. This transformation predominantly occurs in the liver, facilitated by the cytochrome P450 system of hemoproteins situated in the lipophilic endoplasmic reticulum of cells. The metabolite generated through this process can have varying polarities. If it is sufficiently polar, it can be easily excreted in the urine due to its water compatibility. However, if the metabolite is nonpolar,...
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Regulation of Nuclear Protein Sorting01:45

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Nuclear protein sorting regulates nucleus composition and gene expression, crucial for determining the fate of a eukaryotic cell. Hence, the entry and exit of molecules across the nuclear envelope is a tightly controlled process. Nuclear protein sorting can be inhibited by one of the following ways: 1) masking cargo signal sequences, 2) modifying the nuclear receptor's affinity for cargo, 3) controlling the nuclear pore size, 4) retaining the cargo during its transit to the cytosol or the...
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Overview of Fatty Acid Metabolism01:28

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Lipids also are sources of energy that power cellular processes. Like carbohydrates, lipids are composed of carbon, hydrogen, and oxygen, but these atoms are arranged differently. Most lipids are nonpolar and hydrophobic. Major types include fats and oils, waxes, phospholipids, and steroids.
Fatty acids are catabolized in a process called beta-oxidation, which takes place in the matrix of the mitochondria and converts their fatty acid chains into two-carbon units of acetyl groups. The acetyl...
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Smooth Endoplasmic Reticulum01:21

Smooth Endoplasmic Reticulum

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Smooth endoplasmic reticulum or smooth ER is a sub-organelle with specialized functions in animal cells and plant cells. It is often associated with the tubule morphology of the endoplasmic reticulum.
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Intracellular Hormone Receptors

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Lipid-soluble hormones diffuse across the plasma and nuclear membrane of target cells to bind to their specific intracellular receptors. These receptors act as transcription factors that regulate gene expression and protein synthesis in the target cell
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Updated: Nov 11, 2025

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
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Steroidogenic cytochrome P450 17A1 structure and function.

Sarah D Burris-Hiday1, Emily E Scott2

  • 1Department of Medicinal Chemistry, University of Michigan, Ann Arbor, MI, USA.

Molecular and Cellular Endocrinology
|March 30, 2021
PubMed
Summary
This summary is machine-generated.

Cytochrome P450 17A1 (CYP17A1) is key for hormone production. Understanding its dual reactions and disease links can improve treatments for cancers and endocrine disorders.

Keywords:
CancerCrystallographyCushing's syndromeCytochrome P450 17A1MechanismProstate

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Area of Science:

  • Biochemistry
  • Endocrinology
  • Enzymology

Background:

  • Cytochrome P450 17A1 (CYP17A1) is a vital enzyme in steroidogenesis.
  • It produces essential glucocorticoids and sex hormones through complex chemical reactions.

Purpose of the Study:

  • To review the intricate functions of CYP17A1.
  • To explore its roles in classical and backdoor steroidogenic pathways.
  • To detail its hydroxylation and lyase activities.

Main Methods:

  • Functional and structural investigations of CYP17A1.
  • Focus on reaction intermediates, reaction coordination, cytochrome b5 effects, and conformational selection.

Main Results:

  • Detailed understanding of CYP17A1's dual catalytic mechanism.
  • Elucidation of factors influencing its activity, including cytochrome b5.
  • Insights into conformational selection in enzyme function.

Conclusions:

  • Enhanced comprehension of CYP17A1's physiological roles.
  • Potential for improved therapeutic strategies targeting CYP17A1.
  • Applications in treating steroidogenic diseases like prostate cancer and Cushing's syndrome.