What are Aurora kinase inhibitors?

What are Aurora kinase inhibitors?

Furthermore, Aurora kinases are known to be oncogenic and overexpressed in various forms of cancerous growth, including leukemia, colon cancer, prostate cancer and breast cancer tumors. So far three Aurora-kinase inhibitors have been described: ZM447439, hesperadin and VX-680.

What does Aurora kinase do?

Aurora kinases are enzymes that help the cell cycle through the regulation of mitotic spindles. Mutations in this enzyme lead to aneuploidy or genomic instability. The increased expression of aurora kinases has been found in breast cancer, colon cancer, and neural malignancies.

Which drugs are protein kinase inhibitors?

bosutinib, crizotinib, dasatinib, erlotinib, gefitinib, lapatinib, pazopanib, ruxolitinib, sunitinib, and vemurafenib. Apart from the large-scale clinical success, Type I kinase inhibitors also come with adverse side-effects.

What is a cell cycle?

A cell cycle is a series of events that takes place in a cell as it grows and divides. A cell spends most of its time in what is called interphase, and during this time it grows, replicates its chromosomes, and prepares for cell division. The cell then leaves interphase, undergoes mitosis, and completes its division.

Is Alisertib FDA approved?

However, alisertib is not currently approved by the Food and Drug Administration (FDA) in the United States for lymphoma. With regard to pralatrexate, which is FDA approved for relapsed or refractory PTCL, the phase 1 and 2 trials cumulatively included 3 subjects with ATLL.

What is protein kinase and why are they important?

Protein kinases (PTKs) are enzymes that regulate the biological activity of proteins by phosphorylation of specific amino acids with ATP as the source of phosphate, thereby inducing a conformational change from an inactive to an active form of the protein.

Which stage is the fastest in the cell cycle?

For the characteristic cell cycle time of 20 hours in a HeLa cell, almost half is devoted to G1 (BNID 108483) and close to another half is S phase (BNID 108485) whereas G2 and M are much faster at about 2-3 hours and 1 hour, respectively (BNID 109225, 109226).

How are Aurora kinases used to treat cancer?

Aurora kinases are strongly expressed in a broad range of cancer types. Aurora A expression in tumors is often associated with gene amplification, genetic instability, poor histologic differentiation, and poor prognosis.

How are serine threonine kinases related to cancer?

The human aurora family of serine-threonine kinases comprises three members, which act in concert with many other proteins to control chromosome assembly and segregation during mitosis. Aurora dysfunction can cause aneuploidy, mitotic arrest, and cell death. Aurora kinases are strongly expressed in a broad range of cancer types.

Where are the execution points of Aurora kinases?

Fig. 1. Cell cycle execution points and targets of aurora A and B kinases. Substrates phosphorylated in each phase of the cell cycle by each kinase are detailed, with orange circles denoting targets of aurora A and green circles denoting targets of aurora B. Orange/green line, known substrates of the single yeast aurora kinase IpI1p.