Haspin inhibitor

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August undefined, 2024

WebSep 3, 2024 · Background: HASPIN, a mitotic kinase for Histone H3, is a promising target for anti-cancer therapy. However, as HASPIN is an atypical kinase with low similarity to … WebAug 30, 2024 · Haspin is required for chromosomal stability; hence, treatment with the haspin inhibitor CHR-6494 has been identified to induce apoptosis in cancer cells by inducing genomic instability (Quadri et al., 2024). Our data suggest that prolonged nuclear accumulation of fascin in response to haspin inhibition may also contribute to these …

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WebOct 10, 2012 · Here, we further investigated the role of Haspin in the regulation of the CPC by means of a small-molecule ATP-competitive Haspin inhibitor, 5-iodotubercidin (5-Iodo-7-β-d-ribofuranosyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine, abbreviated as 5-ITu). 5-ITu was originally characterized as an inhibitor of adenosine kinase (Wotring and Townsend, … WebDec 1, 2024 · Haspin is a promising target for the design of inhibitors as potent anticancer drugs for cancer therapy [10], [11]. CHR6494 (3-(1H-indazol-5-yl)-N-propylimidazo[1,2-b]pyridazin-6-amine) is a novel Haspin inhibitor that targets the component of the mitotic machinery other than the microtubule [12]. CHR6494 inhibited cell proliferation and ... naismith award vs wooden award

Haspin: a promising target for the design of inhibitors as potent ...

WebApr 15, 2024 · Only a few preclinical studies of monovalent Haspin kinase inhibitors have been reported by 2024. For instance, CHR-6494 (62) (Table 3), containing an indazolyl-imidazo [1,2-b]pyridazine scaffold, exhibited high inhibitory potency toward Haspin (IC 50 = 2 nM) and showed a broad spectrum of anticancer effects. WebLDN-192960 is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively. - Mechanism of Action & Protocol. From 11:00 pm to 12:00 pm EST ( 8:00 … WebJun 1, 2024 · Novel 7-azaindole derivatives were investigated as potential inhibitors of selected protein kinases. • The most potent inhibitor (8l) exhibits an IC 50 value of 14 nM for Haspin, • Two other active compounds (8g and 8h) are dual inhibitors of CDK9/CyclinT and Haspin. • These compounds have potential as starting points for design of potent ... medline hoyer lift weight scale

Function and inhibition of Haspin kinase: targeting …

Abstract 3949: Identification of a novel HASPIN inhibitor and the ...

WebFeb 1, 2024 · Haspin is a serine/threonine kinase that associates with chromosome and phosphorylates threonine 3 of histone 3 during mitosis. Haspin overexpression or … WebFeb 16, 2024 · HASPIN is a serine/threonine kinase that is expressed in various cells. To examine whether HASPIN is involved in the onset of Alzheimer’s disease through tau … naismith award watch listWebSep 14, 2024 · HASPIN plays an important role in the regulation of normal mitosis of cells through the regulation of H3 histones. It has been shown that HASPIN inhibitors have potent anti-tumoral effects . HASPIN inhibition leads to the dephosphorylation of the third threonine of H3 histones, which in turn affects the binding of CPC components to … naismith ball

"WebDec 1, 2009 · Here we report structures of human haspin in complex with ATP and the inhibitor iodotubercidin. These structures reveal a constitutively active kinase … " - Haspin inhibitor

Haspin inhibitor

Haspin: a promising target for the design of inhibitors as potent ...

WebJun 15, 2024 · HASPIN, a mitotic kinase to phosphorylate Histone H3 at centromere, has been studied as a promising target for anti-cancer therapy. However, as HASPIN … WebJun 15, 2024 · Abstract. HASPIN, a mitotic kinase to phosphorylate Histone H3 at centromere, has been studied as a promising target for anti-cancer therapy. However, as HASPIN belongs to atypical kinase, lacking the Asp-Phe-Gly (DFG) motif, development from the chemical library of kinase inhibitors with conventional pharmacophore, would be …

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WebJul 1, 2024 · Haspin RNAi, inhibitors, or CRISPR/Cas9 targeting all remove mitotic H3T3ph in cultured mammalian cells, supporting the view that this is a critical kinase for H3T3ph during cell division 9,11,12 ... WebAug 25, 2024 · Methods: Anti-tumor activities of the haspin inhibitor CHR-6494 were tested in a number of melanoma cell lines either as a single agent or in combination with the MEK inhibitor Trametinib (GSK1120242). Experiments are based on: 1) Cell viability determined by the crystal violet staining assay; 2) apoptotic responses measured by the caspase 3/7 ...

WebSep 14, 2024 · We investigated the synergistic effect of a combination of mTOR and HASPIN inhibitors on cell viability, cell cycle, cell apoptosis, DNA damage, and mitotic … WebApr 14, 2024 · HASPIN is a serine/threonine kinase that regulates mitosis by phosphorylating histone H3 at threonine 3. The expression levels of HASPIN in various cancers are associated with tumor malignancy and …

WebNational Center for Biotechnology Information WebOct 1, 2024 · However, no inhibitors targeting haspin have entered clinical trials presently. 5-iTU (5-iodotubercidin) is a useful and classical chemical probe for the investigation of haspin activity, but its ...

WebHere, we further investigated the role of Haspin in the regulation of the CPC by means of a small-molecule ATP-competitive Haspin inhibitor, 5-iodotubercidin (5-Iodo-7-β-d-ribofuranosyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine, abbreviated as 5-ITu). 5-ITu was originally characterized as an inhibitor of adenosine kinase (Wotring and Townsend, 1979 ...

WebAug 1, 2011 · From the cellular standpoint, the identified small-molecule Haspin inhibitor causes arrest in G2/M and subsequently apoptosis. … naismith basketball player of the yearWebFeb 7, 2011 · Potent and selective haspin inhibitor: 4828: LDN 209929 dihydrochloride: Potent and selective haspin inhibitor: Related Targets. Cell Cycle; Mitosis; Haspin (histone H3 associated protein kinase), EC 2.7.11.1, is a serine/threonine kinase that has a critical function in mitosis. The enzyme is localized to chromosomes and phosphorylates ... naismith bowls clubWebFunction and inhibition of Haspin kinase: targeting multiple cancer therapies by antimitosis Here our perspective includes a comprehensive review of the roles and structure of … medline hybrid 2 transport chairWebDec 1, 2009 · Indeed, haspin-selective inhibitors have been identified by high-throughput screening of chemical libraries , and screening using 88 Ser/Thr kinases showed that the inhibitor iodotubercidin bound to only one other kinase with low nM affinity . Iodotubercidin's high potency, cell permeability, and selectivity for haspin make this compound an ... naismith camp naismith bidenWebHASPIN kinase inhibitors were recently isolated, and their antitumor activity reported. Colorectal cancer occurs with high incidence worldwide. In this study, we examined whether HASPIN inhibitor CHR-6494 suppresses cancer progression in Apc Min/+ mice, a familial colon tumor disease model. Mice were treated by intraperitoneal injection of CHR ... medline hybrid wheelchairWebMay 22, 2024 · The 7-azaindole scaffold attracts attention due to its value in the design of inhibitors of diseases related protein kinases. However, this scaffold has not been evaluated against Haploid germ cell-specific nuclear protein kinase (Haspin). Herein, we report the synthesis of a select set of 7-azaindole derivatives and their evaluation against … naismith basketball coach of the year