Cited by 27Cellular transport and secretionProtein Kinase Regulation and GTPase SignalingCancer, Hypoxia, and Metabolism

Dual blockade of macropinocytosis and asparagine bioavailability shows synergistic anti-tumor effects on KRAS-mutant colorectal cancer

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Hanada, Keita, Kawada, Kenji, Nishikawa, Gen, Toda, Kosuke, Maekawa, Hisatsugu, Nishikawa, Yasuyo, Masui, Hideyuki, Hirata, Wataru +12 more·2021·Cancer Letters

Abstract

Mutations of KRAS gene are found in various types of cancer, including colorectal cancer (CRC). Despite intense efforts, no pharmacological approaches are expected to be effective against KRAS-mutant cancers. Macropinocytosis is an evolutionarily conserved actin-dependent endocytic process that internalizes extracellular fluids into large vesicles called macropinosomes. Recent studies have revealed macropinocytosis's important role in metabolic adaptation to nutrient stress in cancer cells harboring KRAS mutations. Here we showed that KRAS-mutant CRC cells enhanced macropinocytosis for tumor growth under nutrient-depleted conditions. We also demonstrated that activation of Rac1 and phosphoinositide 3-kinase were involved in macropinocytosis of KRAS-mutant CRC cells. Furthermore, we found that macropinocytosis was closely correlated with asparagine metabolism. In KRAS-mutant CRC cells engineered with knockdown of asparagine synthetase, macropinocytosis was accelerated under glutamine-depleted condition, and albumin addition could restore the glutamine depletion-induced growth suppression by recovering the intracellular asparagine level. Finally, we discovered that the combination of macropinocytosis inhibition and asparagine depletion dramatically suppressed the tumor growth of KRAS-mutant CRC cells in vivo. These results indicate that dual blockade of macropinocytosis and asparagine bioavailability could be a novel therapeutic strategy for KRAS-mutant cancers.

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Authors
Hanada, K., Kawada, K., Nishikawa, G., Toda, K., Maekawa, H., Nishikawa, Y., Masui, H., Hirata, W., Okamoto, M., Kiyasu, Y., Honma, S., Ogawa, R., Mizuno, R., Itatani, Y., Miyoshi, H., Sasazuki, T., Shirasawa, S., Taketo, M. M., Obama, K., & Sakai, Y.
Affiliations
  • Kyoto University (JP)
  • Otsu Municipal Hospital (JP)
  • Kobe City Medical Center West Hospital (JP)
  • Uji-Tokushukai Medical Center (JP)
  • Kyoto University Hospital (JP)
  • Kyushu University (JP)
  • Fukuoka University (JP)
  • Osaka Red Cross Hospital (JP)
Corresponding author
Kawada, Kenji
Venue
Cancer Letters
Publisher
Elsevier BV
Published
2021-12
Volume
522
Pages
129-141
ISSN
0304-3835 (ISSN-L)
OpenAlex
W3199187959
Cited by
27
References
60
Citations by year
2026: 3 · 2025: 10 · 2024: 4 · 2023: 3 · 2022: 7
FWCI
1.83
Type
journal article
Language
en
Open access
Locations
  • Cancer Letters (publishedVersion)
  • PubMed (publishedVersion)
  • Kyoto University Research Information Repository (Kyoto University) (submittedVersion)
Funders
Ministry of Education, Culture, Sports, Science and Technology
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Cell Biology › Cellular transport and secretion
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Kinase Regulation and GTPase Signaling
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Cancer, Hypoxia, and Metabolism
Keywords
macropinocytosis, asparagine metabolism, KRAS-mutant colorectal cancer, asparagine synthetase, glutamine deprivation, albumin, Rac1, phosphatidylinositol 3-kinase, nutritional stress, tumor growth inhibition, combination therapy
MeSH terms
Asparagine, Aspartate-Ammonia Ligase, Humans, Mutation, Pinocytosis, Colorectal Neoplasms, Proto-Oncogene Proteins p21(ras), Phosphatidylinositol 3-Kinases, rac1 GTP-Binding Protein, Cell Line, Tumor, Cell Proliferation, Gene Knockdown Techniques

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