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Related Concept Videos

Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

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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.
Major types that are helpful drug targets include:
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Mitogens and the Cell Cycle02:38

Mitogens and the Cell Cycle

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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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Role of Ephrin-Eph Signalling in Intestinal Stem Cell Renewal01:22

Role of Ephrin-Eph Signalling in Intestinal Stem Cell Renewal

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Erythropoietin-producing hepatocellular carcinoma receptor (Eph) and its ligand, Eph receptor-interacting protein (Ephrin) were first discovered in the human carcinoma cell line, hence the name. Ephrin-Eph interaction guides cells to reach their appropriate location in adult tissues. They also play an essential role in the immune system by helping in immune cell migration, adhesion, and activation. Based on their structure and function, Eph is divided into two classes — EphA and EphB.
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Receptor Downregulation in MVBs01:15

Receptor Downregulation in MVBs

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Multivesicular bodies (MVBs) are mature endosomes that sort ubiquitinated proteins and then fuse with lysosomes to degrade the sorted proteins. Epidermal growth factor (EGF) and its receptor (EGFR) form a complex that can be internalized through endocytosis, sorted into an MVB, and later degraded.
The EGFR can initiate signaling pathways that  lead to cell proliferation, migration, and differentiation. Overexpression of EGFR  stimulates cells to proliferate. Excessive  EGFR...
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ER Retrieval Pathway01:45

ER Retrieval Pathway

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In the secretory pathway, vesicles transport proteins from one cellular compartment to another in forward transport to deliver the protein to its correct location. Occasionally, misfolded proteins and incorrect proteins escape their original compartments, and a retrieval pathway is used to return the escaped proteins to their original compartment.
The ER uses many checkpoints to prevent the entry of incorrectly folded or a resident protein as cargo onto a transport vesicle. These mechanisms...
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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.
There are several types of targeted therapies against...
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Related Experiment Video

Updated: Oct 16, 2025

Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
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Bicyclic Peptide Makes Targeting EphA2 Possible

    Cancer Discovery
    |October 20, 2021
    PubMed
    Summary

    A novel bicyclic peptide, BT5528, shows promise for cancer treatment by targeting EphA2. Early trials indicate clinical responses in ovarian and urothelial cancers without significant toxicity.

    Area of Science:

    • Oncology
    • Molecular Biology
    • Drug Development

    Background:

    • EphA2 receptor tyrosine kinase is a promising cancer target.
    • Previous EphA2-directed therapies faced toxicity challenges.
    • Tumor-penetrating peptides offer a novel delivery mechanism.

    Purpose of the Study:

    • To evaluate the safety and efficacy of BT5528, a novel bicyclic peptide targeting EphA2.
    • To assess the therapeutic potential of BT5528 in patients with advanced cancers.

    Main Methods:

    • Phase I clinical trial.
    • Administration of BT5528 to patients with ovarian and urothelial cancers.
    • Monitoring for clinical responses and toxicity.

    Main Results:

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    Related Experiment Videos

    Last Updated: Oct 16, 2025

    Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
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    Bacterial Peptide Display for the Selection of Novel Biotinylating Enzymes
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    • BT5528 demonstrated clinical responses in three patients.
    • The therapeutic candidate showed an acceptable safety profile.
    • No significant toxicity issues were observed, unlike previous EphA2-directed agents.

    Conclusions:

    • BT5528 represents a potential breakthrough in targeting EphA2 for cancer therapy.
    • The drug's tumor-penetrating capabilities and favorable safety profile warrant further investigation.