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Related Concept Videos

The Ras Gene02:38

The Ras Gene

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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.
Ras is a...
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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.
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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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Small GTPases - Ras and Rho01:24

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Ras and Rho are small monomeric GTPases that act downstream of receptor tyrosine kinase (RTK) and regulate various cellular processes. These GTPases switch between active and inactive states by binding to guanine nucleotides.
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Under normal conditions, most adult cells remain in a non-proliferative state unless stimulated by internal or external factors to replace lost cells. Abnormal cell proliferation is a condition in which the cell's growth exceeds and is uncoordinated with normal cells. In such situations, cell division persists in the same excessive manner even after cessation of the stimuli, leading to persistent tumors. The tumor arises from the damaged cells that replicate to pass the damage to the...
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Updated: Nov 9, 2025

Utilizing 18F-FDG PET/CT Imaging and Quantitative Histology to Measure Dynamic Changes in the Glucose Metabolism in Mouse Models of Lung Cancer
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Targeting mutant KRAS.

Daniel A Erlanson1, Kevin R Webster1

  • 1Frontier Medicines Corporation, 151 Oyster Point Blvd., 2nd Floor, South San Francisco, CA, 94080, USA.

Current Opinion in Chemical Biology
|April 10, 2021
PubMed
Summary
This summary is machine-generated.

Targeting KRAS G12C mutations in cancer has yielded five clinical compounds since 2018. Further research aims to develop inhibitors for broader KRAS mutations and prevent drug resistance.

Keywords:
Covalent drugsFragment-based drug discoveryG12CG12DKRASPrecision oncology

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Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • The KRAS protein is a key target in cancer drug discovery, historically considered undruggable.
  • Specific KRAS mutations, like G12C, are implicated in various cancers.

Purpose of the Study:

  • To review existing and emerging therapeutic strategies targeting KRAS mutations.
  • To identify challenges and future directions in KRAS-targeted cancer therapy.

Main Methods:

  • Review of clinical compounds targeting KRAS G12C.
  • Analysis of additional approaches for targeting other KRAS mutants.
  • Discussion of resistance mechanisms and inhibitor development.

Main Results:

  • Five compounds targeting KRAS G12C have been approved for clinical use since 2018.
  • Various other strategies are being explored for different KRAS mutations.

Conclusions:

  • Targeting KRAS G12C represents a significant advancement in cancer therapy.
  • Future efforts must focus on developing inhibitors for a wider range of KRAS mutations and overcoming resistance.