Therapeutic targeting of Notch signaling in cancer

被引：4

作者：

Brahmi, Mehdi ^{[1
]}

Bally, Olivia ^{[1
]}

Eberst, Lauriane ^{[1
]}

Cassier, Philippe ^{[1
]}

机构：

[1] Ctr Leon Berard, Dept Cancerol Med, 28 Rue Laennec, F-69373 Lyon 08, France

来源：

BULLETIN DU CANCER | 2017年 / 104卷 / 10期

关键词：

Notch; Cancer; Targeted therapy; Gamma-secretase inhibitor; GAMMA-SECRETASE INHIBITOR; CELL-CYCLE ARREST; PHASE-I; BREAST-CANCER; MONOCLONAL-ANTIBODY; RO4929097; DLL4; BLOCKADE; PATHWAY; GENE;

D O I：

10.1016/j.bulcan.2017.07.007

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

The Notch pathway plays an essential role during embryonal development and tissue in adults. Notch signaling occurs through transmembrane receptors which undergo several proteolytic cleavages that lead to the release of the Notch intracytoplasmic domain (NICD), which in turn activates the transcription of target genes. Oncogenic alterations of Notch receptors were first identified in T acute lymphoblastic leukemia and subsequently in solid tumors and other hematological malignancies. The important role of Notch signaling in cancer makes it an interesting target for drug development. Several classes of compounds targeting Notch signaling are currently in clinical development. However, the complexity of Notch signaling as well as its importance in tissue homeostasis makes the clinical development of these therapies more complex than anticipated. Additional clinical and preclinical investigations are needed to adequately target Notch signaling in cancer therapy.

引用

页码：883 / 891

页数：9

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