Reference SummaryLee SH, Cancers (Basel) 2020 May 28;12(6):

Title

The Combination of Loss of ALDH1L1 Function and Phenformin Treatment Decreases Tumor Growth in KRAS-Driven Lung Cancer.

Authors

Lee SH; Jeon Y; Kang JH; Jang H; Lee H; Kim SY

Journal

Cancers (Basel)

Volume

12

Issue

6

Year

2020

Pages

Abstract

Lung adenocarcinoma cells express high levels of ALDH1L1, an enzyme of the one-carbon pathway that catalyzes the conversion of 10-formyltetrahydrofolate into tetrahydrofolate and NAD(P)H. In this study, we evaluated the potential of ALDH1L1 as a therapeutic target by deleting the Aldh1l1 gene in Kras(LA2) mice, a model of spontaneous non-small cell lung cancer (NSCLC). Reporter assays revealed KRAS-mediated upregulation of the ALDH1L1 promoter in human NSCLC cells. Aldh1l1(-/-) mice exhibited a normal phenotype, with a 10% decrease in Kras-driven lung tumorigenesis. By contrast, the inhibition of oxidative phosphorylation inhibition using phenformin in Aldh1l1(-/-); Kras(LA2) mice dramatically decreased the number of tumor nodules and tumor area by up to 50%. Furthermore, combined treatment with pan-ALDH inhibitor and phenformin showed a decreased number and area of lung tumors by 70% in the Kras(LA2) lung cancer model. Consistent with this, previous work showed that the combination of ALDH1L1 knockdown and phenformin treatment decreased ATP production by as much as 70% in NSCLS cell lines. Taken together, these results suggest that the combined inhibition of ALDH activity and oxidative phosphorylation represents a promising therapeutic strategy for NSCLC.

Links

J:294979 – MGI References
32481524 – National Library of Medicine/PubMed

Models

Strain Model Name Treatment Agent(s) Organ Affected Frequency Model Details
C57BL/6-Krastm3Tyj/+ Lung adenocarcinoma Lung

0

C57BL/6-Krastm3Tyj/+ Lung adenocarcinoma
  • phenformin
  • gossypol
Lung

0

C57BL/6-Krastm3Tyj/+ Lung adenoma Lung

observed

C57BL/6-Krastm3Tyj/+ Lung adenoma Lung

observed

C57BL/6-Krastm3Tyj/+ Lung adenoma
  • phenformin
Lung

observed

C57BL/6-Aldh1l1tm1b(KOMP)Wtsi Krastm3Tyj/+ Lung adenoma Lung

observed

C57BL/6-Aldh1l1tm1b(KOMP)Wtsi Krastm3Tyj/+ Lung adenoma
  • phenformin
Lung

observed

C57BL/6-Krastm3Tyj/+ Lung adenoma
  • phenformin
  • gossypol
Lung

observed

C57BL/6-Krastm3Tyj/+ Lung hyperplasia Lung

observed

C57BL/6-Krastm3Tyj/+ Lung hyperplasia Lung

observed

C57BL/6-Krastm3Tyj/+ Lung hyperplasia
  • phenformin
Lung

observed

C57BL/6-Aldh1l1tm1b(KOMP)Wtsi Krastm3Tyj/+ Lung hyperplasia Lung

observed

C57BL/6-Aldh1l1tm1b(KOMP)Wtsi Krastm3Tyj/+ Lung hyperplasia
  • phenformin
Lung

observed

C57BL/6-Krastm3Tyj/+ Lung hyperplasia
  • phenformin
  • gossypol
Lung

observed

C57BL/6-Krastm3Tyj/+ Lung tumor Lung

observed - 100

C57BL/6-Krastm3Tyj/+ Lung tumor Lung

observed - 100

C57BL/6-Krastm3Tyj/+ Lung tumor
  • phenformin
Lung

observed - 100

C57BL/6-Aldh1l1tm1b(KOMP)Wtsi Krastm3Tyj/+ Lung tumor Lung

observed - 100

C57BL/6-Aldh1l1tm1b(KOMP)Wtsi Krastm3Tyj/+ Lung tumor
  • phenformin
Lung

observed - 100