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Targeted Cancer Therapies02:57

Targeted Cancer Therapies

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 specific...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

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:
Amplifying Signals via Enzymatic Cascade01:22

Amplifying Signals via Enzymatic Cascade

When a ligand binds to a cell-surface receptor, the receptor's intracellular domain changes shape, which may either activate its enzyme function or allow its binding to other molecules. The initial signal is amplified by most signal transduction pathways. This means that a single ligand molecule can activate multiple molecules of a downstream target. Proteins that relay a signal are most commonly phosphorylated at one or more sites, activating or inactivating the protein. Kinases catalyze the...
Combination Therapies and Personalized Medicine02:50

Combination Therapies and Personalized Medicine

Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
In-vitro Mutagenesis01:16

In-vitro Mutagenesis

To learn more about the function of a gene, researchers can observe what happens when the gene is inactivated or “knocked out,” by creating genetically engineered knockout animals. Knockout mice have been particularly useful as models for human diseases such as cancer, Parkinson’s disease, and diabetes.
Mitogens and the Cell Cycle02:38

Mitogens and the Cell Cycle

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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Castration Resistance Accelerates Prostate Cancer Kinetics.

The Prostate·2026
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WOMBAT (ANZUP 2201): A Phase 2, Single-arm Study of Bipolar Androgen Therapy in Patients with Nonmetastatic Castration-resistant Prostate Cancer with Prostate-specific Antigen Progression on Darolutamide.

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CRM1 regulates androgen receptor stability and impacts DNA repair pathways in prostate cancer, independent of the androgen receptor.

FASEB journal : official publication of the Federation of American Societies for Experimental Biology·2025
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Updated: May 20, 2026

Genome-Wide CRISPR Screen for Unveiling Radiosensitive and Radioresistant Genes
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Engineering enzymatically activated "molecular grenades" for cancer.

Samuel R Denmeade, John T Isaacs

    Oncotarget
    |July 28, 2012
    PubMed
    Summary

    The novel drug G202, a PSMA-activated thapsigargin, shows promise in cancer treatment due to its non-myelosuppressive nature. It may enhance therapies by reducing androgen and estrogen receptors, suggesting synergistic potential in prostate and breast cancers.

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    Area of Science:

    • Oncology
    • Pharmacology
    • Molecular Biology

    Background:

    • G202, a Prostate-Specific Membrane Antigen (PSMA)-activated thapsigargin drug, has demonstrated non-myelosuppressive properties in preclinical and Phase I clinical trials.
    • Its non-myelosuppressive profile allows for flexible combination therapies with existing treatments.

    Discussion:

    • Thapsigargin's capacity to induce endoplasmic reticulum (ER) stress suggests potential synergistic effects when G202 is combined with radiation or cytotoxic chemotherapies.
    • G202 administration leads to a significant decrease in androgen receptor (AR) expression in prostate cancer cells and estrogen receptor (ER) protein in breast cancer cells.

    Key Insights:

    • G202's lack of myelosuppression supports its use in combination cancer treatment strategies.
    • G202 effectively targets AR in prostate cancer and ER in breast cancer, indicating potential for hormone-driven cancer therapies.

    Outlook:

    • Combination therapy involving G202 with anti-androgens or anti-estrogens presents a promising synergistic approach for treating prostate and breast cancers.
    • These combination strategies are currently undergoing preclinical validation.