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The Ras Gene

The Ras Gene

The Ras-gene-encoded proteins are regulators of signaling pathways controlling cell proliferation, differentiation, or cell survival. The Ras-gene family in humans constitutes three primary members—the HRas, NRas, and KRas. These genes code for four functionally distinct yet closely related proteins—the HRas, NRas, KRas4A, and KRas4B. The involvement of mutant Ras genes in human cancer was first discovered in 1982 and is among the most common causes of human tumorigenesis.
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Feedback Inhibition

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Enzyme Inhibition

Enzyme Inhibition

Inhibitors are molecules that reduce enzyme activity by binding to the enzyme. In a normally functioning cell, enzymes are regulated by a variety of inhibitors. Drugs and other toxins can also inhibit enzymes. Some inhibitors bind to the enzyme’s active site, while others inhibit enzymatic activity by binding to other sites on the protein structure.

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Related Experiment Video

Updated: Feb 14, 2026

Identification of EGFR and RAS Inhibitors using Caenorhabditis elegans

Identification of EGFR and RAS Inhibitors using Caenorhabditis elegans

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Blocking Ras inhibition as an antitumor strategy.

Nagore I Marín-Ramos¹, Silvia Ortega-Gutiérrez², María L López-Rodríguez²

¹Department of Neurosurgery, Keck School of Medicine, University of Southern California, Los Angeles, CA, United States.

Seminars in Cancer Biology

|February 8, 2018

Summary

Targeting Ras proteins, crucial in cancer, is challenging. This review details recent small molecule inhibitors, focusing on direct binders and post-translational modification inhibitors, advancing cancer therapy.

Keywords:

Cancer GEF Inhibitor Ras Ras-effector interaction Small GTPase

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Area of Science:

Oncology
Molecular Biology
Drug Discovery

Background:

Ras proteins are frequently mutated in human cancers, acting as key drivers of tumorigenesis.
Despite their importance, Ras proteins remain difficult pharmaceutical targets.
Understanding Ras structure, signaling, and modifications is crucial for developing effective inhibitors.

Purpose of the Study:

To review recent advances in small molecule inhibitors targeting Ras proteins.
To discuss two main strategies: direct Ras binding and inhibition of post-translational modifications.
To highlight promising molecules in medicinal chemistry and drug development pipelines.

Main Methods:

Literature review of recent studies on Ras inhibitors.
Categorization of inhibitors based on their mechanism of action (direct binding vs. modification inhibition).
Analysis of compounds progressing in drug development and clinical trials.

Main Results:

Small molecules targeting Ras directly include nucleotide exchange inhibitors, allosteric compounds, and effector interaction inhibitors.
Inhibitors targeting Ras post-translational modifications offer another therapeutic avenue.
Several Ras inhibitors have shown significant progress in medicinal chemistry and preclinical/clinical development.

Conclusions:

Targeting Ras proteins with small molecules is a rapidly advancing field in cancer therapy.
Dual approaches, direct inhibition and modification targeting, offer diverse strategies.
Ongoing clinical trials and future research hold promise for overcoming challenges in Ras-targeted drug development.