HS-173, a novel phosphatidylinositol 3-kinase (PI3K) inhibitor, has anti-tumor activity through promoting apoptosis and inhibiting angiogenesis

Hyunseung Lee; Kyung Hee Jung; Yujeong Jeong; Sungwoo Hong; Soon Sun Hong

doi:10.1016/j.canlet.2012.08.020

HS-173, a novel phosphatidylinositol 3-kinase (PI3K) inhibitor, has anti-tumor activity through promoting apoptosis and inhibiting angiogenesis

Hyunseung Lee, Kyung Hee Jung, Yujeong Jeong, Sungwoo Hong, Soon Sun Hong

Research output: Contribution to journal › Article › peer-review

47 Scopus citations

Abstract

We synthesized a novel imidazopyridine analogue, a PI3Kα inhibitor HS-173 and investigated anti-cancer capacity in human cancer cells. HS-173 inhibited the PI3K signaling pathway, and showed anti-proliferative effects on cancer cells. Also, HS-173 induced cell cycle arrest at the G₂/M phase and apoptosis. In addition, HS-173 decreased the expression HIF-1α and VEGF which play an important role in angiogenesis. This effect was confirmed by the suppression of tube formation and migration assay in vitro. Furthermore, HS-173 diminished blood vessel formation in the Matrigel plug assay in mice. Therefore, HS-173 is considered as a novel drug candidate to treat cancer patients.

Original language	English
Pages (from-to)	152-159
Number of pages	8
Journal	Cancer Letters
Volume	328
Issue number	1
DOIs	https://doi.org/10.1016/j.canlet.2012.08.020
State	Published - 1 Jan 2013
Externally published	Yes

Bibliographical note

Funding Information:
This work was supported by the National R&D Program for Cancer Control (1020250), Ministry of Health & Welfare, and National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science and Technology (2012-0002988, 2012-0003009, 2011-0016436 and 2011-0020322) and Inha University Grant.

Keywords

Angiogenesis
Anti-cancer drug
Apoptosis
PI3K inhibitor

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.canlet.2012.08.020

Cite this

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title = "HS-173, a novel phosphatidylinositol 3-kinase (PI3K) inhibitor, has anti-tumor activity through promoting apoptosis and inhibiting angiogenesis",

abstract = "We synthesized a novel imidazopyridine analogue, a PI3Kα inhibitor HS-173 and investigated anti-cancer capacity in human cancer cells. HS-173 inhibited the PI3K signaling pathway, and showed anti-proliferative effects on cancer cells. Also, HS-173 induced cell cycle arrest at the G2/M phase and apoptosis. In addition, HS-173 decreased the expression HIF-1α and VEGF which play an important role in angiogenesis. This effect was confirmed by the suppression of tube formation and migration assay in vitro. Furthermore, HS-173 diminished blood vessel formation in the Matrigel plug assay in mice. Therefore, HS-173 is considered as a novel drug candidate to treat cancer patients.",

keywords = "Angiogenesis, Anti-cancer drug, Apoptosis, PI3K inhibitor",

author = "Hyunseung Lee and Jung, {Kyung Hee} and Yujeong Jeong and Sungwoo Hong and Hong, {Soon Sun}",

note = "Funding Information: This work was supported by the National R&D Program for Cancer Control (1020250), Ministry of Health & Welfare, and National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science and Technology (2012-0002988, 2012-0003009, 2011-0016436 and 2011-0020322) and Inha University Grant.",

year = "2013",

month = jan,

day = "1",

doi = "10.1016/j.canlet.2012.08.020",

language = "English",

volume = "328",

pages = "152--159",

journal = "Cancer Letters",

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AU - Lee, Hyunseung

AU - Jung, Kyung Hee

AU - Jeong, Yujeong

AU - Hong, Sungwoo

AU - Hong, Soon Sun

N1 - Funding Information: This work was supported by the National R&D Program for Cancer Control (1020250), Ministry of Health & Welfare, and National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science and Technology (2012-0002988, 2012-0003009, 2011-0016436 and 2011-0020322) and Inha University Grant.

PY - 2013/1/1

Y1 - 2013/1/1

N2 - We synthesized a novel imidazopyridine analogue, a PI3Kα inhibitor HS-173 and investigated anti-cancer capacity in human cancer cells. HS-173 inhibited the PI3K signaling pathway, and showed anti-proliferative effects on cancer cells. Also, HS-173 induced cell cycle arrest at the G2/M phase and apoptosis. In addition, HS-173 decreased the expression HIF-1α and VEGF which play an important role in angiogenesis. This effect was confirmed by the suppression of tube formation and migration assay in vitro. Furthermore, HS-173 diminished blood vessel formation in the Matrigel plug assay in mice. Therefore, HS-173 is considered as a novel drug candidate to treat cancer patients.

AB - We synthesized a novel imidazopyridine analogue, a PI3Kα inhibitor HS-173 and investigated anti-cancer capacity in human cancer cells. HS-173 inhibited the PI3K signaling pathway, and showed anti-proliferative effects on cancer cells. Also, HS-173 induced cell cycle arrest at the G2/M phase and apoptosis. In addition, HS-173 decreased the expression HIF-1α and VEGF which play an important role in angiogenesis. This effect was confirmed by the suppression of tube formation and migration assay in vitro. Furthermore, HS-173 diminished blood vessel formation in the Matrigel plug assay in mice. Therefore, HS-173 is considered as a novel drug candidate to treat cancer patients.

KW - Angiogenesis

KW - Anti-cancer drug

KW - Apoptosis

KW - PI3K inhibitor

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U2 - 10.1016/j.canlet.2012.08.020

DO - 10.1016/j.canlet.2012.08.020

M3 - Article

C2 - 22929971

AN - SCOPUS:84868484417

SN - 0304-3835

VL - 328

SP - 152

EP - 159

JO - Cancer Letters

JF - Cancer Letters

IS - 1

ER -

HS-173, a novel phosphatidylinositol 3-kinase (PI3K) inhibitor, has anti-tumor activity through promoting apoptosis and inhibiting angiogenesis

Abstract

Bibliographical note

Keywords

UN SDGs

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