Perspectives of protein kinase C (PKC) inhibitors as anti-cancer agents

A. Gonelli, C. Mischiati, R. Guerrini, R. Voltan, S. Salvadori, Giorgo Zauli

Research output: Contribution to journalArticle

Abstract

Although the role of serine/threonine protein kinase C (PKC) in malignant transformation is known from decades, an anti-PKC based approach in cancer therapy was hampered for the difficulties in developing pharmacological compounds able to selectively inhibit specific PKC isoforms. In this review, the role of PKC-ε and PKC-δ in promoting and counteracting tumor progression in different types of cancer, respectively, will be discussed in relationship with promising therapeutic perspectives based either on small molecule inhibitors or on natural compounds. Among a miriad of molecules able to modulate PKC activity, we will focus on the role of the enzastaurin and briostatin-1, which already entered clinical trials for several human cancers.

Original languageEnglish
Pages (from-to)498-509
Number of pages12
JournalMini-Reviews in Medicinal Chemistry
Volume9
Issue number4
DOIs
Publication statusPublished - 2009

Fingerprint

Protein C Inhibitor
Protein Kinase Inhibitors
Protein Kinase C
Neoplasms
Protein-Serine-Threonine Kinases
Protein Isoforms
Clinical Trials
Pharmacology
Therapeutics

Keywords

  • Apoptosis
  • Differentiation
  • PKC
  • Tumorigenesis

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmacology

Cite this

Gonelli, A., Mischiati, C., Guerrini, R., Voltan, R., Salvadori, S., & Zauli, G. (2009). Perspectives of protein kinase C (PKC) inhibitors as anti-cancer agents. Mini-Reviews in Medicinal Chemistry, 9(4), 498-509. https://doi.org/10.2174/138955709787847967

Perspectives of protein kinase C (PKC) inhibitors as anti-cancer agents. / Gonelli, A.; Mischiati, C.; Guerrini, R.; Voltan, R.; Salvadori, S.; Zauli, Giorgo.

In: Mini-Reviews in Medicinal Chemistry, Vol. 9, No. 4, 2009, p. 498-509.

Research output: Contribution to journalArticle

Gonelli, A, Mischiati, C, Guerrini, R, Voltan, R, Salvadori, S & Zauli, G 2009, 'Perspectives of protein kinase C (PKC) inhibitors as anti-cancer agents', Mini-Reviews in Medicinal Chemistry, vol. 9, no. 4, pp. 498-509. https://doi.org/10.2174/138955709787847967
Gonelli, A. ; Mischiati, C. ; Guerrini, R. ; Voltan, R. ; Salvadori, S. ; Zauli, Giorgo. / Perspectives of protein kinase C (PKC) inhibitors as anti-cancer agents. In: Mini-Reviews in Medicinal Chemistry. 2009 ; Vol. 9, No. 4. pp. 498-509.
@article{6d0cc15fa2f5435182d52f0fb550971e,
title = "Perspectives of protein kinase C (PKC) inhibitors as anti-cancer agents",
abstract = "Although the role of serine/threonine protein kinase C (PKC) in malignant transformation is known from decades, an anti-PKC based approach in cancer therapy was hampered for the difficulties in developing pharmacological compounds able to selectively inhibit specific PKC isoforms. In this review, the role of PKC-ε and PKC-δ in promoting and counteracting tumor progression in different types of cancer, respectively, will be discussed in relationship with promising therapeutic perspectives based either on small molecule inhibitors or on natural compounds. Among a miriad of molecules able to modulate PKC activity, we will focus on the role of the enzastaurin and briostatin-1, which already entered clinical trials for several human cancers.",
keywords = "Apoptosis, Differentiation, PKC, Tumorigenesis",
author = "A. Gonelli and C. Mischiati and R. Guerrini and R. Voltan and S. Salvadori and Giorgo Zauli",
year = "2009",
doi = "10.2174/138955709787847967",
language = "English",
volume = "9",
pages = "498--509",
journal = "Mini-Reviews in Medicinal Chemistry",
issn = "1389-5575",
publisher = "Bentham Science Publishers B.V.",
number = "4",

}

TY - JOUR

T1 - Perspectives of protein kinase C (PKC) inhibitors as anti-cancer agents

AU - Gonelli, A.

AU - Mischiati, C.

AU - Guerrini, R.

AU - Voltan, R.

AU - Salvadori, S.

AU - Zauli, Giorgo

PY - 2009

Y1 - 2009

N2 - Although the role of serine/threonine protein kinase C (PKC) in malignant transformation is known from decades, an anti-PKC based approach in cancer therapy was hampered for the difficulties in developing pharmacological compounds able to selectively inhibit specific PKC isoforms. In this review, the role of PKC-ε and PKC-δ in promoting and counteracting tumor progression in different types of cancer, respectively, will be discussed in relationship with promising therapeutic perspectives based either on small molecule inhibitors or on natural compounds. Among a miriad of molecules able to modulate PKC activity, we will focus on the role of the enzastaurin and briostatin-1, which already entered clinical trials for several human cancers.

AB - Although the role of serine/threonine protein kinase C (PKC) in malignant transformation is known from decades, an anti-PKC based approach in cancer therapy was hampered for the difficulties in developing pharmacological compounds able to selectively inhibit specific PKC isoforms. In this review, the role of PKC-ε and PKC-δ in promoting and counteracting tumor progression in different types of cancer, respectively, will be discussed in relationship with promising therapeutic perspectives based either on small molecule inhibitors or on natural compounds. Among a miriad of molecules able to modulate PKC activity, we will focus on the role of the enzastaurin and briostatin-1, which already entered clinical trials for several human cancers.

KW - Apoptosis

KW - Differentiation

KW - PKC

KW - Tumorigenesis

UR - http://www.scopus.com/inward/record.url?scp=67549115857&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=67549115857&partnerID=8YFLogxK

U2 - 10.2174/138955709787847967

DO - 10.2174/138955709787847967

M3 - Article

C2 - 19356127

AN - SCOPUS:67549115857

VL - 9

SP - 498

EP - 509

JO - Mini-Reviews in Medicinal Chemistry

JF - Mini-Reviews in Medicinal Chemistry

SN - 1389-5575

IS - 4

ER -