Global and focused transcriptional profiling of small molecule aminopeptidase N inhibitor reveals its mechanism of angiogenesis inhibition

Joong Sup Shim, Hyo Mi Park, Jiyong Lee, Ho Jeong Kwon

Research output: Contribution to journalArticle

6 Citations (Scopus)

Abstract

We recently developed a specific small molecule inhibitor of aminopeptidase N (APN), named as HNSA, through a high throughput screening. In the present study, we investigated the major cellular phenotypes of HNSA in comparison with those of APN knock-down in human fibrosarcoma cells and the mechanism of angiogenesis inhibition by the compound using DNA microarray analyses. Global gene expression analyses showed that HNSA signatures are significantly correlated with those of APN knock-down in HT1080 cells, suggesting that APN is a primary target of HNSA in the cells. Using the angiogenesis-focused DNA microarrays, nine of angiogenesis-related genes were identified as crucial mediators of angiogenesis inhibition by HNSA. These data demonstrate that HNSA can be used as a valuable tool to decipher the APN function in angiogenesis.

Original languageEnglish
Pages (from-to)99-103
Number of pages5
JournalBiochemical and Biophysical Research Communications
Volume371
Issue number1
DOIs
Publication statusPublished - 2008 Jun 20

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CD13 Antigens
Molecules
Microarrays
Oligonucleotide Array Sequence Analysis
Fibrosarcoma
DNA
Microarray Analysis
Gene expression
Screening
Genes
Throughput
Phenotype
Gene Expression

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Biophysics
  • Molecular Biology

Cite this

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abstract = "We recently developed a specific small molecule inhibitor of aminopeptidase N (APN), named as HNSA, through a high throughput screening. In the present study, we investigated the major cellular phenotypes of HNSA in comparison with those of APN knock-down in human fibrosarcoma cells and the mechanism of angiogenesis inhibition by the compound using DNA microarray analyses. Global gene expression analyses showed that HNSA signatures are significantly correlated with those of APN knock-down in HT1080 cells, suggesting that APN is a primary target of HNSA in the cells. Using the angiogenesis-focused DNA microarrays, nine of angiogenesis-related genes were identified as crucial mediators of angiogenesis inhibition by HNSA. These data demonstrate that HNSA can be used as a valuable tool to decipher the APN function in angiogenesis.",
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Global and focused transcriptional profiling of small molecule aminopeptidase N inhibitor reveals its mechanism of angiogenesis inhibition. / Shim, Joong Sup; Park, Hyo Mi; Lee, Jiyong; Kwon, Ho Jeong.

In: Biochemical and Biophysical Research Communications, Vol. 371, No. 1, 20.06.2008, p. 99-103.

Research output: Contribution to journalArticle

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