关于蛋白激酶C调节剂的最新专利。

Sonia Sanchez-Bautista, Francisco E Nicolas
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引用次数: 10

摘要

蛋白激酶C (PKC)由10个丝氨酸/苏氨酸激酶家族组成,分为3个亚家族:经典、新型和非典型。这些同工酶是信号转导的主要介质之一,大多数可能与多种致病过程有关,包括恶性转化或癌症和转移。此外,一些活化的同工酶还参与其他疾病,如梗死、器官移植组织相容性不完全引起的排斥反应、疼痛、糖尿病性黄斑水肿等。在这里,我们回顾了几个与PKC抑制剂相关的专利,它们代表了预防和治疗这些疾病的一种新的有前途的策略。在这些抑制剂中,我们纳入了反义寡核苷酸作为治疗与PKC和肿瘤坏死因子α (TNF-α)表达失调相关的感染性和自身免疫性疾病的另一种有效策略。另一方面,本文也综述了PKC的两种不同的激活剂及其在神经退行性疾病中的应用。
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Recent patents concerning modulators of protein kinase C.

Protein kinase C (PKC) comprises a family of 10 serine/threonine kinases divided into 3 subfamilies: classical, novel and atypical. These isoenzymes represent one of the major mediators of signal transduction, and most may be associated with several pathogenic processes including malignant transformation or cancer and metastasis. Moreover, some activated isoenzymes are also involved in other diseases such as infarct, rejection due to incomplete histocompatibility in organ transplantation, pain, diabetic macular edema, etc. Here, we review several patents related to inhibitors of PKC that represent a new and promising strategy for the prevention and treatment of these illnesses. Among these inhibitors, we included antisense oligonucleotides as another useful strategy to treat infectious and autoimmune diseases associated with misregulated expression of PKC and tumour necrosis factor alpha (TNF-α). On the other hand, two different activators of PKC and their applications related to neurodegenerative diseases have also been reviewed in this work.

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