Targeting protein kinase C in sarcoma

被引：8

作者：

Martin-Liberal, J. ^{[1
]}

Cameron, A. J. ^{[3
]}

Claus, J. ^{[4
]}

Judson, I. R. ^{[1
]}

Parker, P. J. ^{[4
,5
]}

Linch, M. ^{[2
]}

机构：

[1] Royal Marsden Hosp, Sarcoma Unit, London SW3 6JJ, England

[2] UCL, Inst Canc, Dept Oncol, London, England

[3] Queen Mary Univ London, Barts Canc Inst, London EC1M 6BQ, England

[4] Canc Res UK, London Res Inst, Prot Phosphorylat Lab, London WC2A 3LY, England

[5] Kings Coll London, Div Canc Studies, London SE1 1UL, England

来源：

BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER | 2014年 / 1846卷 / 02期

关键词：

Kinases; Protein kinase C; Sarcoma; Therapeutics; GASTROINTESTINAL STROMAL TUMORS; PHASE-II TRIAL; PKC-THETA EXPRESSION; SOFT-TISSUE SARCOMA; CELL LUNG-CANCER; NF-KAPPA-B; ANTISENSE OLIGONUCLEOTIDE; GENE-EXPRESSION; 1ST-LINE TREATMENT; CRYSTAL-STRUCTURE;

D O I：

10.1016/j.bbcan.2014.10.002

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Protein kinase C (PKC) is a family of serine/threonine tyrosine kinases that regulate many cellular processes including division, proliferation, survival, anoikis and polarity. PKC is abundant in many human cancers and aberrant PKC signalling has been demonstrated in cancer models. On this basis, PKC has become an attractive target for small molecule inhibition within oncology drug development programmes. Sarcoma is a heterogeneous group of mesenchymal malignancies. Due to their relative insensitivity to conventional chemotherapies and the increasing recognition of the driving molecular events of sarcomagenesis, sarcoma provides an excellent platform to test novel therapeutics. In this review we provide a structure-function overview of the PKC family, the rationale for targeting these kinases in sarcoma and the state of play with regard to PKC inhibition in the clinic. (C) 2014 Elsevier B.V. All rights reserved.

引用

页码：547 / 559

页数：13

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