Understand KRAS and the Quest for Anti-Cancer Drugs
Chang Woo Han1, Mi Suk Jeong2, Se Bok Jang3
1Institute of Systems Biology, Pusan National University, Jangjeon-dong, Geumjeong-gu, Busan 46241, Korea.
Abstract:
The KRAS oncogene is mutated in approximately ~30% of human cancers, and the targeting of KRAS has long been highlighted in many studies. Nevertheless, attempts to target KRAS directly have been ineffective. This review provides an overview of the structure of KRAS and its characteristic signaling pathways. Additionally, we examine the problems associated with currently available KRAS inhibitors and discuss promising avenues for drug development.
Insights
Targeting the KRAS oncogene in cancer has been challenging due to ineffective direct inhibitors. This review explores KRAS structure, signaling, current drug limitations, and future therapeutic strategies for cancer treatment.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- The KRAS oncogene is frequently mutated in human cancers (~30%).
- Direct targeting of KRAS has historically proven ineffective.
- Understanding KRAS structure and signaling is crucial for cancer therapy development.
Purpose of the Study:
- To review the structural and signaling characteristics of KRAS.
- To analyze the challenges and limitations of current KRAS inhibitors.
- To explore novel strategies for effective KRAS-targeted drug development.
Main Methods:
- Literature review of KRAS structure and function.
- Analysis of existing KRAS inhibitor studies.
- Discussion of emerging drug development approaches.
Main Results:
- KRAS mutations are prevalent in various human cancers.
- Direct inhibition of KRAS has faced significant obstacles.
- Current inhibitors exhibit limitations in efficacy and specificity.
Conclusions:
- Despite challenges, KRAS remains a critical target in oncology.
- Further research into KRAS pathways and inhibitor design is essential.
- Promising new avenues for KRAS-targeted cancer therapies are emerging.
More Related Videos
Related Concept Videos
The Ras Gene
Ras is a...
Targeted Cancer Therapies
There are several types of targeted therapies against...
mTOR Signaling and Cancer Progression
The mTOR pathway or the...
Small GTPases - Ras and Rho
Three regulatory proteins control their activity:
Inhibition of Cdk Activity
Cancer-Critical Genes I: Proto-oncogenes
When the function of certain critical genes, especially those involved in cell cycle regulation and cell growth signaling cascades, gets disrupted, it upsets the cell cycle progression. Such cells with unchecked cell cycles start proliferating uncontrollably and eventually develop into tumors.
Such genes that act...


