Targeting Peroxisome Proliferator-Activated Receptor-β/δ (PPARβ/δ) for Cancer Chemoprevention

Jeffrey M. Peters, Pei Li Yao, Frank J. Gonzalez

Research output: Contribution to journalReview article

14 Citations (Scopus)

Abstract

The role of peroxisome proliferator-activated receptor-β/δ (PPARβ/δ) in cancer remains contentious due in large part to divergent publications indicating opposing effects in different rodent and human cell culture models. During the past 10 years, some facts regarding PPARβ/δ in cancer have become clearer, while others remain uncertain. For example, it is now well accepted that (1) expression of PPARβ/δ is relatively lower in most human tumors as compared to the corresponding non-transformed tissue, (2) PPARβ/δ promotes terminal differentiation, and (3) PPARβ/δ inhibits pro-inflammatory signaling in multiple in vivo models. However, whether PPARβ/δ is suitable to target with natural and/or synthetic agonists or antagonists for cancer chemoprevention is hindered because of the uncertainty in the mechanism of action and role in carcinogenesis. Recent findings that shed new insight into the possibility of targeting this nuclear receptor to improve human health will be discussed.

Original languageEnglish (US)
Pages (from-to)121-128
Number of pages8
JournalCurrent Pharmacology Reports
Volume1
Issue number2
DOIs
StatePublished - Apr 1 2015

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Peroxisome Proliferator-Activated Receptors
Chemoprevention
Neoplasms
Cytoplasmic and Nuclear Receptors
Cell culture
Uncertainty
Publications
Tumors
Rodentia
Carcinogenesis
Cell Culture Techniques
Health
Tissue

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Genetics
  • Pharmacology
  • Drug Discovery

Cite this

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title = "Targeting Peroxisome Proliferator-Activated Receptor-β/δ (PPARβ/δ) for Cancer Chemoprevention",
abstract = "The role of peroxisome proliferator-activated receptor-β/δ (PPARβ/δ) in cancer remains contentious due in large part to divergent publications indicating opposing effects in different rodent and human cell culture models. During the past 10 years, some facts regarding PPARβ/δ in cancer have become clearer, while others remain uncertain. For example, it is now well accepted that (1) expression of PPARβ/δ is relatively lower in most human tumors as compared to the corresponding non-transformed tissue, (2) PPARβ/δ promotes terminal differentiation, and (3) PPARβ/δ inhibits pro-inflammatory signaling in multiple in vivo models. However, whether PPARβ/δ is suitable to target with natural and/or synthetic agonists or antagonists for cancer chemoprevention is hindered because of the uncertainty in the mechanism of action and role in carcinogenesis. Recent findings that shed new insight into the possibility of targeting this nuclear receptor to improve human health will be discussed.",
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Targeting Peroxisome Proliferator-Activated Receptor-β/δ (PPARβ/δ) for Cancer Chemoprevention. / Peters, Jeffrey M.; Yao, Pei Li; Gonzalez, Frank J.

In: Current Pharmacology Reports, Vol. 1, No. 2, 01.04.2015, p. 121-128.

Research output: Contribution to journalReview article

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N2 - The role of peroxisome proliferator-activated receptor-β/δ (PPARβ/δ) in cancer remains contentious due in large part to divergent publications indicating opposing effects in different rodent and human cell culture models. During the past 10 years, some facts regarding PPARβ/δ in cancer have become clearer, while others remain uncertain. For example, it is now well accepted that (1) expression of PPARβ/δ is relatively lower in most human tumors as compared to the corresponding non-transformed tissue, (2) PPARβ/δ promotes terminal differentiation, and (3) PPARβ/δ inhibits pro-inflammatory signaling in multiple in vivo models. However, whether PPARβ/δ is suitable to target with natural and/or synthetic agonists or antagonists for cancer chemoprevention is hindered because of the uncertainty in the mechanism of action and role in carcinogenesis. Recent findings that shed new insight into the possibility of targeting this nuclear receptor to improve human health will be discussed.

AB - The role of peroxisome proliferator-activated receptor-β/δ (PPARβ/δ) in cancer remains contentious due in large part to divergent publications indicating opposing effects in different rodent and human cell culture models. During the past 10 years, some facts regarding PPARβ/δ in cancer have become clearer, while others remain uncertain. For example, it is now well accepted that (1) expression of PPARβ/δ is relatively lower in most human tumors as compared to the corresponding non-transformed tissue, (2) PPARβ/δ promotes terminal differentiation, and (3) PPARβ/δ inhibits pro-inflammatory signaling in multiple in vivo models. However, whether PPARβ/δ is suitable to target with natural and/or synthetic agonists or antagonists for cancer chemoprevention is hindered because of the uncertainty in the mechanism of action and role in carcinogenesis. Recent findings that shed new insight into the possibility of targeting this nuclear receptor to improve human health will be discussed.

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