PTEN modulators: a patent review.
PTEN modulators: a patent review.
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DOI：
10.1517/13543776.2013.768985
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发表时间：
2013-05
影响因子：
6.6
通讯作者：
Agrawal DK
中科院分区：
文献类型：
--
作者：
Boosani CS;Agrawal DK
PTEN（phosphatase and tensin homolog deleted on chromosome 10）通过抑制PI 3 K/Akt通路在控制细胞存活和增殖的细胞内信号传导中起关键作用，并且其功能障碍与多种肿瘤性疾病相关。PTEN在许多病理条件下经常发生突变，突出了其在正常生理功能中的重要性。与通过磷酸化激活的几种细胞蛋白不同，PTEN在通过使其C-末端区域中的丝氨酸和苏氨酸残基磷酸化的特异性激酶磷酸化后失活。因此，开发特异性靶向影响PTEN的激酶和含激酶结构域的蛋白质的治疗剂将导致治疗PTEN相关疾病。随着越来越多的证据表明，在许多人类疾病中的作用，本审查的重点是临床相关的PTEN与一个全面的清单，目前已确定的调节剂的PTEN，并提出潜在的新的分子靶点，可以帮助开发候选药物治疗的PTEN相关的疾病，如心血管疾病，糖尿病，肥胖症，癌症，自闭症，帕金森氏症和阿尔茨海默氏症。这篇综述描述了几个靶点，可以帮助开发新的候选药物来调节或恢复PTEN的正常生理功能，并且在治疗人类疾病中PTEN起着关键作用。
PTEN (phosphatase and tensin homolog deleted on chromosome 10) plays a pivotal role in controlling intracellular signaling for cell survival and proliferation by inhibiting the PI3K/Akt pathway, and its dysfunction is associated with several neoplastic diseases. PTEN is frequently found mutated in many pathological conditions highlighting its importance in normal physiological function. Unlike several cellular proteins which are activated by phosphorylation, PTEN is inactivated upon phosphorylation by specific kinases which phosphorylate serine and threonine residues in its C-terminal region. Therefore, development of therapeutic agents that specifically target kinases and kinase-domain-containing proteins affecting PTEN would lead to the treatment of PTEN-related diseases. With increasing evidence on the role of PTEN in many human diseases, the present review focuses on the clinical relevance of PTEN with a comprehensive list of currently identified modulators of PTEN, and proposes potentially novel molecular targets which could aid in the development of drug candidates for the treatment of PTEN-related diseases such as cardiovascular diseases, diabetes, obesity, cancer, autism, Parkinson’s and Alzheimer’s diseases. This review describes several target sites that could help in the development of novel drug candidates to regulate or restore the normal physiological functions of PTEN and are essential in the treatment of human diseases where PTEN plays a pivotal role.
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影响因子：
3.9
作者：
Abouantoun, Thamara J.;Castellino, Robert C.;MacDonald, Tobey J.
通讯作者：
MacDonald, Tobey J.
亚硒酸钠在DU-145前列腺癌细胞中增加了肿瘤抑制蛋白PTEN的活性。
DOI：
10.1080/01635580802521338
发表时间：
2009
期刊：
Nutrition and cancer
影响因子：
--
作者：
Berggren M;Sittadjody S;Song Z;Samira JL;Burd R;Meuillet EJ
通讯作者：
Meuillet EJ
影响因子：
3.7
作者：
Giagulli C;Marsico S;Magiera AK;Bruno R;Caccuri F;Barone I;Fiorentini S;Andò S;Caruso A
通讯作者：
Caruso A
影响因子：
8.8
作者：
Frattini, M;Saletti, P;Romagnani, E;Martin, V;Molinari, F;Ghisletta, M;Camponovo, A;Etienne, L L;Cavalli, F;Mazzucchelli, L
通讯作者：
Mazzucchelli, L
影响因子：
4.8
作者：
Gustin, JA;Maehama, T;Donner, DB
通讯作者：
Donner, DB