Signal transduction pathway targets for anticancer drug discovery
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Updated: Oct 16, 2026

Mimicking the Function of Signaling Proteins: Toward Artificial Signal Transduction Therapy
Published on: September 29, 2016
1Mayo Clinic, Division of Medical Oncology, 200 First Street S. W., Rochester, MN 55905, USA. adjie.alex@mayo.edu
Abstract:
There are currently over 80 agents officially approved for the treatment of cancer world-wide. However, the most common epithelial cancers, which cause greater than 75% of cancer deaths, remain incurable. Most drugs have been developed empirically by testing large numbers of chemicals on rapidly growing transplantable rodent tumors, and more recently, human tumor xenografts. This approach has identified prodeminantly DNA-active drugs that are considerably toxic and have limited efficacy. Novel molecular targets, which are selective for neoplastic cells, are needed for chemotherapeutic agents to improve cure rates of epithelial malignancies, with acceptable toxicity. In recent years, agents inhibiting signal transduction pathway molecules have entered clinical trials. These include antibodies and small molecules, which inhibit growth factor receptors and their receptor tyrosine kinases, inhibitors of cytoplasmic second messengers such as ras, raf and MEK, inhibitors of protein trafficking, and inhibitors of protein degradation.
Insights
Targeting novel molecular pathways is crucial for developing effective cancer chemotherapeutics. New agents inhibiting signal transduction molecules show promise for treating incurable epithelial cancers with reduced toxicity.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- Over 80 cancer agents exist, yet common epithelial cancers causing most deaths remain incurable.
- Traditional drug development relies on empirical screening, yielding toxic, DNA-active agents with limited efficacy.
- Novel molecular targets selective for cancer cells are needed to improve epithelial cancer cure rates and reduce toxicity.
Purpose of the Study:
- To highlight the need for novel molecular targets in cancer chemotherapy.
- To discuss the potential of signal transduction pathway inhibitors for treating epithelial malignancies.
Main Methods:
- Review of current cancer treatment landscape and drug development approaches.
- Analysis of emerging therapeutic strategies targeting signal transduction pathways.
- Identification of key molecular targets within these pathways.
Main Results:
- Empirical drug development has led to toxic agents with limited efficacy against epithelial cancers.
- Signal transduction pathway inhibitors are entering clinical trials.
- These inhibitors target growth factor receptors, kinases, and protein regulation pathways.
Conclusions:
- Novel molecular targets are essential for advancing cancer chemotherapy.
- Signal transduction inhibitors represent a promising new class of anti-cancer agents.
- Targeted therapies may offer improved efficacy and reduced toxicity for epithelial cancers.
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