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Related Concept Videos

Covalently Linked Protein Regulators02:04

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Proteins can undergo many types of post-translational modifications, often in response to changes in their environment. These modifications play an important role in the function and stability of these proteins. Covalently linked molecules include functional groups, such as methyl, acetyl, and phosphate groups, and also small proteins, such as ubiquitin. There are around 200 different types of covalent regulators that have been identified.
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Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
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The gene expression in cells is regulated at different stages: (i) transcription, (ii) RNA processing, (iii) RNA localization, and (iv) translation. Transcriptional regulation is mediated by regulatory proteins such as transcription factors, activators, or repressors—these control gene expression by initiating or inhibiting the transcription of genes. Once a precursor or pre-mRNA is produced, it undergoes post-transcriptional modification, including 5' capping, splicing, and the...
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Pharmaceutical substances known as xenobiotics are predominantly lipophilic and nonionized. This enables them to permeate lipid bilayers, such as cell membranes, and interact with intracellular target receptors. Lipophilic drugs have an advantage in crossing biological barriers and reaching their intended sites of action. However, lipophilic drugs often have a restricted capacity for renal expulsion or elimination from the body. When these drugs enter the kidneys and undergo glomerular...
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A gene is a stretch of DNA that serves as the blueprint for functional RNAs and proteins. Since DNA is comprised  of nucleotides and proteins are comprised of amino acids, a mediator is required to convert the information encoded in DNA into proteins. This mediator is the messenger RNA (mRNA). mRNA copies the blueprint from DNA by a process called transcription. In eukaryotes, transcription occurs in the nucleus by complementary base-pairing with the DNA template. The mRNA is then...
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Updated: Aug 25, 2025

High-throughput Screening for Chemical Modulators of Post-transcriptionally Regulated Genes
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Minor structural changes, major functional impacts: posttranslational modifications and drug targets.

Hyo Jung Kim1

  • 1College of Pharmacy, Woosuk University, 55338, Wanju, Republic of Korea. hyojungkim@woosuk.ac.kr.

Archives of Pharmacal Research
|October 17, 2022
PubMed
Summary

Posttranslational modifications (PTMs) add chemical diversity to proteins, impacting crucial biological processes. Understanding PTMs

Keywords:
Biological functionDrug targetsPTMPTM-disease associationPosttranslational modificationProtein structure

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Proteomics

Background:

  • Posttranslational modifications (PTMs) enhance protein functional and structural diversity beyond the primary amino acid sequence.
  • PTMs regulate vital cellular processes such as signaling, metabolism, and protein degradation, influencing macromolecular interactions.
  • Defects in PTMs are associated with numerous diseases, making them significant therapeutic targets.

Purpose of the Study:

  • To review major well-studied protein PTMs and their associated drug targets.
  • To highlight the structural changes induced by PTMs.
  • To explore the implications of PTMs for drug development and understanding disease mechanisms.

Main Methods:

  • Literature review of major protein PTMs.
  • Analysis of structural and functional impacts of PTMs.
  • Identification of PTMs as drug targets and disease markers.

Main Results:

  • PTMs significantly expand protein functionality and structural complexity.
  • Characterization of PTMs' structural signatures has been historically challenging.
  • PTMs play critical roles in various physiological and pathological conditions.

Conclusions:

  • Understanding PTM-induced structural changes offers new avenues for drug development.
  • PTMs are crucial for detailed mechanistic insights into biological processes and diseases.
  • Targeting PTMs and their enzymes holds promise for therapeutic interventions.