Emerging roles of Aurora-A kinase in cancer therapy resistance
2023年7月1日 · Aurora kinase A (Aurora-A), a serine/threonine kinase, plays a pivotal role in various cellular processes, including mitotic entry, centrosome maturation and spindle formation. Overexpression or gene-amplification/mutation of Aurora-A kinase occurs in different types of cancer, including lung cancer, colorectal cancer, and breast cancer.
A new wave of innovations within the DNA damage response
2023年9月8日 · ATR-CHK1-WEE1 axis, ATM-CHK2-p53 axis, PKMYT1, and DNA-PK are the best-known DNA damage checkpoint. PLK1 and aurora kinase A (Aurora-A) are also involved in damage checkpoint regulation.
Safety, tolerability, and pharmacokinetics of Aurora kinase B
2023年3月4日 · Drug exposure was sustained for several days post-dose. The most common AZD2811-related adverse events (AEs) were fatigue (27.3%) at ≤200 mg/cycle and neutropenia (37.9%) at ≥400 mg/cycle.
Aurora A kinase inhibition compromises its antitumor efficacy by ...
Three aurora kinase inhibitors, the selective Aurora A inhibitor alisertib, the selective Aurora B inhibitor AZD1152, and the pan-Aurora inhibitor tozasertib, were found to enhance IFN-γ–induced PD-L1 expression (Supplemental Figure 1B and Supplemental Table 1).
Aurora Kinase Inhibitors in Oncology Clinical Trials: Current State …
The main side effects include febrile neutropenia, stomatitis, gastrointestinal toxicity, hypertension, and fatigue. Responses including complete remissions have been described in diverse, advanced malignancies, most notably ovarian cancer and acute myelogenous leukemia.
Aurora Kinases and Potential Medical Applications of Aurora …
The most frequently encountered serious side effects were leukopenia, neutropenia, febrile neutropenia, neutropenic infections, azotemia and pyrexia. They concluded that their results provide ample justification for further clinical trials . Danusertib related renal side effects have been investigated in rats and dogs.
Nuclear localisation of Aurora-A: its regulation and ... - Nature
2021年5月13日 · Although the well-known mitotic roles of Aurora-A point at chromosomal instability, a hallmark of cancer, as a major link between Aurora-A overexpression and disease, recent evidence highlights...
Revisiting Aurora Kinase B: A promising therapeutic target for …
Aurora Kinase B inhibitors show promising biological results in in-vitro and in-vivo experiments. However, there are no inhibitors approved yet for clinical use, primarily because of the side effects associated with Aurora B inhibitors.
Aurora Kinase B Inhibition: A Potential Therapeutic Strategy for …
Deregulation of AURKB is observed in several tumors and its overexpression is frequently linked to tumor cell invasion, metastasis and drug resistance. AURKB has emerged as an attractive drug target leading to the development of small molecule inhibitors.
Aurora Kinase Inhibitors: Current Status and Outlook
2015年12月20日 · These observations led to a number of programs among academic and pharmaceutical organizations to discovering small molecule Aurora kinase inhibitors as anti-cancer drugs. This review will summarize the known Aurora kinase inhibitors currently in the clinic, and discuss the current and future directions.