Julia Kalashova
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View article: Discovery of novel, potent and orally available benzoazipinone derivatives that elicit MKLP2-inhibitory phenotypes
Discovery of novel, potent and orally available benzoazipinone derivatives that elicit MKLP2-inhibitory phenotypes Open
Mitotic kinesin-like protein 2 (MKLP2/KIF20A) is a key mitotic regulator frequently overexpressed in human malignancies and its abundance is positively correlated with poor outcomes of the disease. Despite extensive research on MKLP2 as a …
View article: MYC amplifies mitotic perturbations elicited by LXY18 to enable synthetic lethality
MYC amplifies mitotic perturbations elicited by LXY18 to enable synthetic lethality Open
The MYC oncoprotein represents an intriguing target for cancer treatment, but its therapeutic potential has been hindered by the absence of specific pharmacological inhibitors. In this study, we demonstrate that the phenoxy quinoline compo…
View article: The Aurora kinase B relocation blocker LXY18 triggers mitotic catastrophe selectively in malignant cells
The Aurora kinase B relocation blocker LXY18 triggers mitotic catastrophe selectively in malignant cells Open
The mitotic regulator, Aurora kinase B (AURKB), is frequently overexpressed in malignancy and is a target for therapeutic intervention. The compound, LXY18, is a potent, orally available small molecule that inhibits the proper localization…
View article: Orally Bioavailable 4-Phenoxy-quinoline Compound as a Potent Aurora Kinase B Relocation Blocker for Cancer Treatment
Orally Bioavailable 4-Phenoxy-quinoline Compound as a Potent Aurora Kinase B Relocation Blocker for Cancer Treatment Open
We investigated a novel 4-phenoxy-quinoline-based scaffold that mislocalizes the essential mitotic kinase, Aurora kinase B (AURKB). Here, we evaluated the impact of halogen substitutions (F, Cl, Br, and I) on this scaffold with respect to …
View article: Characterization of mitotic phenotypes associated with a MYC synthetic lethal compound
Characterization of mitotic phenotypes associated with a MYC synthetic lethal compound Open
Therapeutic targeting of MYC directly has proven difficult, but several means to target MYC indirectly using a synthetic lethal drug approach have been proposed. Synthetic lethal approaches for MYC have sought to take advantage of vulnerab…
View article: An orally bioavailable 4-phenoxy-quinoline compound as a potent AURKB relocation blocker for cancer treatment
An orally bioavailable 4-phenoxy-quinoline compound as a potent AURKB relocation blocker for cancer treatment Open
We investigated a novel 4-phenoxy-quinoline-based scaffold that mislocalizes the essential mitotic kinase, AURKB. Here, we evaluated the impact of halogen substitutions (F, Cl, Br, I) on this scaffold with respect to various drug parameter…
View article: Integrating a phenotypic screening with a structural simplification strategy to identify 4-phenoxy-quinoline derivatives to potently disrupt the mitotic localization of Aurora kinase B
Integrating a phenotypic screening with a structural simplification strategy to identify 4-phenoxy-quinoline derivatives to potently disrupt the mitotic localization of Aurora kinase B Open
View article: Discovery and Optimization of Seven-Membered Lactam-Based Compounds to Phenocopy the Inhibition of the Aurora Kinase B
Discovery and Optimization of Seven-Membered Lactam-Based Compounds to Phenocopy the Inhibition of the Aurora Kinase B Open
We used mechanism-informed phenotypic screening to identify and optimize compounds that phenocopy the genetic depletion of the mitotic aurora kinase B (AURKB) kinase. After assaying nine aryl fused seven-membered lactam compounds, we ident…