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G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...
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Cyclic Adenosine Monophosphate (cAMP) is an essential second messenger that activates protein kinase A (PKA) and regulates various biological processes. A single epinephrine molecule binds to GPCR and activates several heterotrimeric G proteins, each stimulating multiple adenylyl cyclase, amplifying the signal, and synthesizing large numbers of cAMP molecules. Small changes in cAMP concentration affect PKA activity. The binding of four cAMP molecules induces a conformational change in PKA,...
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Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
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Preclinical development consists of a series of tests that ensure the safety and efficacy of a new therapeutic compound before it is tested in humans. There are four main phases to this process. First, safety pharmacology tests are conducted to ensure the drug does not produce any acutely harmful effects. These tests examine parameters such as bronchoconstriction, cardiac dysrhythmias, blood pressure changes, and ataxia. Next, preliminary toxicological testing is performed to determine the...
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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.
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N/C-degron pathways and inhibitor development for PROTAC applications.

Zhibin Wu1, Yunyuan Huang1, Ke Liu1

  • 1Hubei Key Laboratory of Genetic Regulation and Integrative Biology, School of Life Sciences, Central China Normal University, Wuhan 430079, PR China.

Biochimica Et Biophysica Acta. Gene Regulatory Mechanisms
|June 1, 2023
PubMed
Summary

This review details E3 ubiquitin ligases and ubiquitination mechanisms, focusing on N/C-degron pathways. It also explores targeted inhibitors and PROteolysis TArgeting Chimeras (PROTACs) for therapeutic applications.

Keywords:
DegronE3 ubiquitin ligaseProteolysis-targeting chimera (PROTAC)Ubiquitination

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Cell Biology

Background:

  • Ubiquitination is a crucial post-translational modification regulating numerous cellular processes.
  • E3 ubiquitin ligases play a central role in determining substrate specificity.
  • Understanding ubiquitination pathways is vital for deciphering cellular functions and disease mechanisms.

Purpose of the Study:

  • To provide a comprehensive overview of E3 ubiquitin ligases and ubiquitination.
  • To examine N/C-degron mediated ubiquitination pathways and their mechanisms.
  • To discuss the therapeutic potential of targeting these pathways, including inhibitors and PROTACs.

Main Methods:

  • Literature review of ubiquitination pathways.
  • Analysis of E3 ubiquitin ligase classification and function.
  • Examination of N/C-degron mechanisms and substrate recognition.
  • Review of current developments in N/C-degron inhibitors and PROTACs.

Main Results:

  • Detailed classification and mechanistic insights into E3 ubiquitin ligases.
  • Elucidation of unique features and substrate recognition of N/C-degron pathways.
  • Overview of emerging therapeutic strategies targeting ubiquitination.

Conclusions:

  • Ubiquitin biology is a rapidly advancing field with significant therapeutic implications.
  • Targeting N/C-degron pathways offers promising avenues for drug development.
  • PROteolysis TArgeting Chimeras (PROTACs) represent a novel therapeutic modality in ubiquitin-mediated protein degradation.