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Targeted Cancer Therapies02:57

Targeted Cancer Therapies

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The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
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Inhibition of Cdk Activity02:34

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The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
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Mitogens and their receptors play a crucial role in controlling the progression of the cell cycle. However, the loss of mitogenic control over cell division leads to tumor formation. Therefore, mitogens and mitogen receptors play an important role in cancer research. For instance, the epidermal growth factor (EGF) - a type of mitogen and its transmembrane receptor (EGFR), decides the fate of the cell's proliferation. When EGF binds to EGFR, a member of the ErbB family of tyrosine kinase...
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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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Protein-protein Interfaces02:04

Protein-protein Interfaces

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Many proteins form complexes to carry out their functions, making protein-protein interactions (PPIs) essential for an organism's survival. Most PPIs are stabilized by numerous weak noncovalent chemical forces. The physical shape of the interfaces determines the way two proteins interact. Many globular proteins have closely-matching shapes on their surfaces, which form a large number of weak bonds. Additionally, many PPIs occur between two helices or between a surface cleft and a...
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An organism can have thousands of different proteins, and these proteins must cooperate to ensure the health of an organism. Proteins bind to other proteins and form complexes to carry out their functions. Many proteins interact with multiple other proteins creating a complex network of protein interactions.
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Peptide-based Identification of Functional Motifs and their Binding Partners
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Peptide inhibitors: Breaking cancer code.

Fleur Coburn1, Yanyamba Nsereko1, Amy Armstrong1

  • 1School of Pharmacy, Newcastle University, Newcastle Upon Tyne, NE1 7RU, UK.

European Journal of Medicinal Chemistry
|July 17, 2025
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Summary
This summary is machine-generated.

Peptide inhibitors offer a selective approach to target tumour signalling pathways, overcoming limitations of traditional chemotherapy. Innovations in peptide design and delivery are enhancing their efficacy against cancer, with several candidates in clinical trials.

Keywords:
CancerInhibitorsPeptidesRASSignalling pathwaysmTOR

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Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Tumour signalling pathways are crucial for cancer development and progression.
  • Conventional chemotherapy faces challenges including toxicity and drug resistance.
  • Peptide inhibitors present a targeted therapeutic strategy by disrupting oncogenic pathways.

Purpose of the Study:

  • To review strategies for enhancing the efficacy of peptide-based cancer drugs.
  • To explore the mechanisms of peptide inhibitors targeting key cancer pathways.
  • To highlight current research and clinical potential of peptide interventions.

Main Methods:

  • Review of existing literature on peptide inhibitors in cancer therapy.
  • Analysis of peptide design innovations (e.g., cyclisation, nanoparticle delivery).
  • Examination of specific peptide targeting mechanisms for rat sarcoma protein (RAS) and mammalian target of rapamycin (mTOR) pathways.

Main Results:

  • Several peptide inhibitors targeting RAS and mTOR pathways have been identified.
  • Examples include KRpep-2D, LUNA18, and a mutant KRAS peptide vaccine.
  • Mutant KRAS peptide vaccine and LUNA18 show promising clinical potential and are in trials.

Conclusions:

  • Peptide inhibitors are a promising alternative to conventional cancer treatments.
  • Ongoing research focuses on overcoming stability, delivery, and resistance challenges.
  • Advanced peptide therapeutics are advancing towards clinical application.