磷脂酶D和胆碱激酶:它们在癌症发展中的作用及其作为药物靶点的潜力。

Progress in cell cycle research Pub Date : 2003-01-01
Agustín Rodríguez-González, Ana Ramírez de Molina, Joaquín Benítez-Rajal, Juan Carlos Lacal
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引用次数: 0

摘要

恶性细胞是由于基因改变的积累而形成的,这些改变影响了控制细胞生长、分化和凋亡的信号转导通路的组成部分。其中一个关键途径与磷脂稳态的调节有关。鉴定在转化过程中改变的正常细胞生长调节的分子成分是开发针对转化细胞的化疗干预措施所必需的。发现新的化疗药物是提高我们抗癌成功率的最有希望的方法之一,而合理的药物设计是实现这一目标的关键因素。证据支持胆碱激酶和磷脂酶D作为这样的新靶点提供。
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Phospholipase D and choline kinase: their role in cancer development and their potential as drug targets.

Malignant cells result from the accumulation of genetic alterations that impinge into the components of signal transduction pathways controlling cell growth, differentiation and apoptosis. One of the critical pathways is related to the regulation of the phospholipid homeostasis. The identification of the molecular components involved in normal cell growth regulation altered upon transformation is required for the development of chemotherapeutic interventions against transformed cells. Discovery of new chemotherapeutic agents is one of the most promising ways to improve our success against cancer, and rational drug design is a key factor to achieve this goal. Evidence supporting choline kinase and phospholipase D as such novel targets is provided.

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The contemporary drug development process: advances and challenges in preclinical and clinical development. Yeast genomics and proteomics in drug discovery and target validation. Proteomic approaches for the identification of cell cycle-related drug targets. Mining the NCI screening database: explorations of agents involved in cell cycle regulation. The role of cytosolic phospholipase A2 in cell cycle progression.
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