Hypoxia-inducible factor 2α: A novel target in gliomas

Jaclyn J. Renfrow; Michael H. Soike; Waldemar Debinski; Shakti H. Ramkissoon; Ryan T. Mott; Mark B. Frenkel; Jann N. Sarkaria; Glenn J. Lesser; Roy E. Strowd

doi:10.4155/fmc-2018-0163

Hypoxia-inducible factor 2α: A novel target in gliomas

Jaclyn J. Renfrow, Michael H. Soike, Waldemar Debinski, Shakti H. Ramkissoon, Ryan T. Mott, Mark B. Frenkel, Jann N. Sarkaria, Glenn J. Lesser, Roy E. Strowd

Radiation Oncology

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

13 Scopus citations

Abstract

Hypoxia is an important contributor to aggressive behavior and resistance mechanisms in glioblastoma. Upregulation of hypoxia inducible transcription factors (HIFs) is the primary adaptive cellular response to a hypoxic environment. While HIF1α has been widely studied in cancer, HIF2α offers a potentially more specific and appealing target in glioblastoma given expression in glioma stem cells and not normal neural progenitors, activation in states of chronic hypoxia and expression that correlates with glioma patient survival. A first-in-class HIF2α inhibitor, PT2385, is in clinical trials for renal cell carcinoma, and provides the first opportunity to therapeutically target this important pathway in glioma biology.

Original language	English (US)
Pages (from-to)	2227-2236
Number of pages	10
Journal	Future Medicinal Chemistry
Volume	10
Issue number	18
DOIs	https://doi.org/10.4155/fmc-2018-0163
State	Published - Sep 2018

Keywords

cancer
glioblastoma
hypoxia
hypoxia-inducible factors

ASJC Scopus subject areas

Molecular Medicine
Pharmacology
Drug Discovery

Access to Document

10.4155/fmc-2018-0163

Cite this

@article{7bfda852aec0424cbdd528a48df08fce,

title = "Hypoxia-inducible factor 2α: A novel target in gliomas",

abstract = "Hypoxia is an important contributor to aggressive behavior and resistance mechanisms in glioblastoma. Upregulation of hypoxia inducible transcription factors (HIFs) is the primary adaptive cellular response to a hypoxic environment. While HIF1α has been widely studied in cancer, HIF2α offers a potentially more specific and appealing target in glioblastoma given expression in glioma stem cells and not normal neural progenitors, activation in states of chronic hypoxia and expression that correlates with glioma patient survival. A first-in-class HIF2α inhibitor, PT2385, is in clinical trials for renal cell carcinoma, and provides the first opportunity to therapeutically target this important pathway in glioma biology.",

keywords = "cancer, glioblastoma, hypoxia, hypoxia-inducible factors",

author = "Renfrow, {Jaclyn J.} and Soike, {Michael H.} and Waldemar Debinski and Ramkissoon, {Shakti H.} and Mott, {Ryan T.} and Frenkel, {Mark B.} and Sarkaria, {Jann N.} and Lesser, {Glenn J.} and Strowd, {Roy E.}",

note = "Publisher Copyright: {\textcopyright} 2018 Newlands Press.",

year = "2018",

month = sep,

doi = "10.4155/fmc-2018-0163",

language = "English (US)",

volume = "10",

pages = "2227--2236",

journal = "Future Medicinal Chemistry",

issn = "1756-8919",

publisher = "Future Science",

number = "18",

}

TY - JOUR

T1 - Hypoxia-inducible factor 2α

T2 - A novel target in gliomas

AU - Renfrow, Jaclyn J.

AU - Soike, Michael H.

AU - Debinski, Waldemar

AU - Ramkissoon, Shakti H.

AU - Mott, Ryan T.

AU - Frenkel, Mark B.

AU - Sarkaria, Jann N.

AU - Lesser, Glenn J.

AU - Strowd, Roy E.

PY - 2018/9

Y1 - 2018/9

N2 - Hypoxia is an important contributor to aggressive behavior and resistance mechanisms in glioblastoma. Upregulation of hypoxia inducible transcription factors (HIFs) is the primary adaptive cellular response to a hypoxic environment. While HIF1α has been widely studied in cancer, HIF2α offers a potentially more specific and appealing target in glioblastoma given expression in glioma stem cells and not normal neural progenitors, activation in states of chronic hypoxia and expression that correlates with glioma patient survival. A first-in-class HIF2α inhibitor, PT2385, is in clinical trials for renal cell carcinoma, and provides the first opportunity to therapeutically target this important pathway in glioma biology.

AB - Hypoxia is an important contributor to aggressive behavior and resistance mechanisms in glioblastoma. Upregulation of hypoxia inducible transcription factors (HIFs) is the primary adaptive cellular response to a hypoxic environment. While HIF1α has been widely studied in cancer, HIF2α offers a potentially more specific and appealing target in glioblastoma given expression in glioma stem cells and not normal neural progenitors, activation in states of chronic hypoxia and expression that correlates with glioma patient survival. A first-in-class HIF2α inhibitor, PT2385, is in clinical trials for renal cell carcinoma, and provides the first opportunity to therapeutically target this important pathway in glioma biology.

KW - cancer

KW - glioblastoma

KW - hypoxia

KW - hypoxia-inducible factors

UR - http://www.scopus.com/inward/record.url?scp=85052883641&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=85052883641&partnerID=8YFLogxK

U2 - 10.4155/fmc-2018-0163

DO - 10.4155/fmc-2018-0163

M3 - Article

C2 - 30089425

AN - SCOPUS:85052883641

SN - 1756-8919

VL - 10

SP - 2227

EP - 2236

JO - Future Medicinal Chemistry

JF - Future Medicinal Chemistry

IS - 18

ER -

Hypoxia-inducible factor 2α: A novel target in gliomas

Abstract

Keywords

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this