Inhibitors of phosphoinositide 3-kinase (PI3K) and phosphoinositide 3-kinase-related protein kinase family (PIKK)
AbstractPhosphoinositide 3-kinases (PI3K) and phosphoinositide 3-kinase-related protein kinases (PIKK) are two structurally related families of kinases that play vital roles in cell growth and DNA damage repair. Dysfunction of PIKK members and aberrant stimulation of the PI3K/AKT/mTOR signalling pat...
| Main Authors: | , , , , , , , , , , , |
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2023-12-01
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| Series: | Journal of Enzyme Inhibition and Medicinal Chemistry |
| Subjects: | |
| Online Access: | https://www.tandfonline.com/doi/10.1080/14756366.2023.2237209 |
| _version_ | 1797400995203907584 |
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| author | Xueqin Huang Li You Eugenie Nepovimova Miroslav Psotka David Malinak Marian Valko Ladislav Sivak Jan Korabecny Zbynek Heger Vojtech Adam Qinghua Wu Kamil Kuca |
| author_facet | Xueqin Huang Li You Eugenie Nepovimova Miroslav Psotka David Malinak Marian Valko Ladislav Sivak Jan Korabecny Zbynek Heger Vojtech Adam Qinghua Wu Kamil Kuca |
| author_sort | Xueqin Huang |
| collection | DOAJ |
| description | AbstractPhosphoinositide 3-kinases (PI3K) and phosphoinositide 3-kinase-related protein kinases (PIKK) are two structurally related families of kinases that play vital roles in cell growth and DNA damage repair. Dysfunction of PIKK members and aberrant stimulation of the PI3K/AKT/mTOR signalling pathway are linked to a plethora of diseases including cancer. In recent decades, numerous inhibitors related to the PI3K/AKT/mTOR signalling have made great strides in cancer treatment, like copanlisib and sirolimus. Notably, most of the PIKK inhibitors (such as VX-970 and M3814) related to DNA damage response have also shown good efficacy in clinical trials. However, these drugs still require a suitable combination therapy to overcome drug resistance or improve antitumor activity. Based on the aforementioned facts, we summarised the efficacy of PIKK, PI3K, and AKT inhibitors in the therapy of human malignancies and the resistance mechanisms of targeted therapy, in order to provide deeper insights into cancer treatment. |
| first_indexed | 2024-03-09T02:02:31Z |
| format | Article |
| id | doaj.art-2625c42c0d07439f92419713efaf92ad |
| institution | Directory Open Access Journal |
| issn | 1475-6366 1475-6374 |
| language | English |
| last_indexed | 2024-03-09T02:02:31Z |
| publishDate | 2023-12-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Journal of Enzyme Inhibition and Medicinal Chemistry |
| spelling | doaj.art-2625c42c0d07439f92419713efaf92ad2023-12-08T03:24:20ZengTaylor & Francis GroupJournal of Enzyme Inhibition and Medicinal Chemistry1475-63661475-63742023-12-0138110.1080/14756366.2023.2237209Inhibitors of phosphoinositide 3-kinase (PI3K) and phosphoinositide 3-kinase-related protein kinase family (PIKK)Xueqin Huang0Li You1Eugenie Nepovimova2Miroslav Psotka3David Malinak4Marian Valko5Ladislav Sivak6Jan Korabecny7Zbynek Heger8Vojtech Adam9Qinghua Wu10Kamil Kuca11College of Life Science, Yangtze University, Jingzhou, ChinaCollege of Physical Education and Health, Chongqing College of International Business and Economics, Chongqing, ChinaDepartment of Chemistry, Faculty of Science, University of Hradec Kralove, Czech RepublicDepartment of Chemistry, Faculty of Science, University of Hradec Kralove, Czech RepublicDepartment of Chemistry, Faculty of Science, University of Hradec Kralove, Czech RepublicFaculty of Chemical and Food Technology, Slovak University of Technology in Bratislava, Bratislava, SlovakiaDepartment of Chemistry and Biochemistry, Mendel University in Brno, Brno, Czech RepublicBiomedical Research Center, University Hospital Hradec Kralove, Hradec Kralove, Czech RepublicDepartment of Chemistry and Biochemistry, Mendel University in Brno, Brno, Czech RepublicDepartment of Chemistry and Biochemistry, Mendel University in Brno, Brno, Czech RepublicCollege of Life Science, Yangtze University, Jingzhou, ChinaDepartment of Chemistry, Faculty of Science, University of Hradec Kralove, Czech RepublicAbstractPhosphoinositide 3-kinases (PI3K) and phosphoinositide 3-kinase-related protein kinases (PIKK) are two structurally related families of kinases that play vital roles in cell growth and DNA damage repair. Dysfunction of PIKK members and aberrant stimulation of the PI3K/AKT/mTOR signalling pathway are linked to a plethora of diseases including cancer. In recent decades, numerous inhibitors related to the PI3K/AKT/mTOR signalling have made great strides in cancer treatment, like copanlisib and sirolimus. Notably, most of the PIKK inhibitors (such as VX-970 and M3814) related to DNA damage response have also shown good efficacy in clinical trials. However, these drugs still require a suitable combination therapy to overcome drug resistance or improve antitumor activity. Based on the aforementioned facts, we summarised the efficacy of PIKK, PI3K, and AKT inhibitors in the therapy of human malignancies and the resistance mechanisms of targeted therapy, in order to provide deeper insights into cancer treatment.https://www.tandfonline.com/doi/10.1080/14756366.2023.2237209PI3KPIKKAKTinhibitorsanticancer therapy |
| spellingShingle | Xueqin Huang Li You Eugenie Nepovimova Miroslav Psotka David Malinak Marian Valko Ladislav Sivak Jan Korabecny Zbynek Heger Vojtech Adam Qinghua Wu Kamil Kuca Inhibitors of phosphoinositide 3-kinase (PI3K) and phosphoinositide 3-kinase-related protein kinase family (PIKK) Journal of Enzyme Inhibition and Medicinal Chemistry PI3K PIKK AKT inhibitors anticancer therapy |
| title | Inhibitors of phosphoinositide 3-kinase (PI3K) and phosphoinositide 3-kinase-related protein kinase family (PIKK) |
| title_full | Inhibitors of phosphoinositide 3-kinase (PI3K) and phosphoinositide 3-kinase-related protein kinase family (PIKK) |
| title_fullStr | Inhibitors of phosphoinositide 3-kinase (PI3K) and phosphoinositide 3-kinase-related protein kinase family (PIKK) |
| title_full_unstemmed | Inhibitors of phosphoinositide 3-kinase (PI3K) and phosphoinositide 3-kinase-related protein kinase family (PIKK) |
| title_short | Inhibitors of phosphoinositide 3-kinase (PI3K) and phosphoinositide 3-kinase-related protein kinase family (PIKK) |
| title_sort | inhibitors of phosphoinositide 3 kinase pi3k and phosphoinositide 3 kinase related protein kinase family pikk |
| topic | PI3K PIKK AKT inhibitors anticancer therapy |
| url | https://www.tandfonline.com/doi/10.1080/14756366.2023.2237209 |
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