IC261 suppresses progression of hepatocellular carcinoma in a casein kinase 1 δ/ε independent manner

Yuan, Feifei; Li, Donghe; Guo, Mengzhou; Fang, Tingting; Sun, Jialei; Feng, Qi; Rao, Qianwen; Zhao, Zhiying; Huang, Peixin; Yang, Biwei; Xia, Jinglin

doi:10.1016/j.bbrc.2019.12.105

Cited by 9 publications

(7 citation statements)

References 25 publications

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“…Consequently, the cytotoxicity of IC261 can be attributed to the direct inhibition of microtubule polymerization rather than to the specific inhibition of CK1δ and ε [ 156 ]. These findings are supported by another study demonstrating that IC261-induced centrosome fragmentation during mitosis is independent of CK1δ [ 157 ]. Microtubule depolymerization by IC261 can furthermore be antagonized by pretreatment of cells with the stabilizing agent paclitaxel.…”

Section: Addressing Inhibition Of Cell Division In Cancer Therapysupporting

confidence: 78%

CK1 Is a Druggable Regulator of Microtubule Dynamics and Microtubule-Associated Processes

Roth

Gihring

Bischof

et al. 2022

Cancers

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Protein kinases of the Casein Kinase 1 family play a vital role in the regulation of numerous cellular processes. Apart from functions associated with regulation of proliferation, differentiation, or apoptosis, localization of several Casein Kinase 1 isoforms to the centrosome and microtubule asters also implicates regulatory functions in microtubule dynamic processes. Being localized to the spindle apparatus during mitosis Casein Kinase 1 directly modulates microtubule dynamics by phosphorylation of tubulin isoforms. Additionally, site-specific phosphorylation of microtubule-associated proteins can be related to the maintenance of genomic stability but also microtubule stabilization/destabilization, e.g., by hyper-phosphorylation of microtubule-associated protein 1A and RITA1. Consequently, approaches interfering with Casein Kinase 1-mediated microtubule-specific functions might be exploited as therapeutic strategies for the treatment of cancer. Currently pursued strategies include the development of Casein Kinase 1 isoform-specific small molecule inhibitors and therapeutically useful peptides specifically inhibiting kinase-substrate interactions.

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Section: Addressing Inhibition Of Cell Division In Cancer Therapysupporting

confidence: 78%

CK1 Is a Druggable Regulator of Microtubule Dynamics and Microtubule-Associated Processes

Roth

Gihring

Bischof

et al. 2022

Cancers

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“… 352 , 354 In an in vitro study, IC261 induced centrosome fragmentation during mitosis independent of CK1δ. 355 Other CK1 inhibitors include PF670 and PF480 that do not kill cancer cells.…”

Section: Promising Preclinical Targeted Therapiesmentioning

confidence: 99%

Wnt/β-catenin signaling in cancers and targeted therapies

Chen

et al. 2021

Sig Transduct Target Ther

277

160

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Wnt/β-catenin signaling has been broadly implicated in human cancers and experimental cancer models of animals. Aberrant activation of Wnt/β-catenin signaling is tightly linked with the increment of prevalence, advancement of malignant progression, development of poor prognostics, and even ascendence of the cancer-associated mortality. Early experimental investigations have proposed the theoretical potential that efficient repression of this signaling might provide promising therapeutic choices in managing various types of cancers. Up to date, many therapies targeting Wnt/β-catenin signaling in cancers have been developed, which is assumed to endow clinicians with new opportunities of developing more satisfactory and precise remedies for cancer patients with aberrant Wnt/β-catenin signaling. However, current facts indicate that the clinical translations of Wnt/β-catenin signaling-dependent targeted therapies have faced un-neglectable crises and challenges. Therefore, in this study, we systematically reviewed the most updated knowledge of Wnt/β-catenin signaling in cancers and relatively targeted therapies to generate a clearer and more accurate awareness of both the developmental stage and underlying limitations of Wnt/β-catenin-targeted therapies in cancers. Insights of this study will help readers better understand the roles of Wnt/β-catenin signaling in cancers and provide insights to acknowledge the current opportunities and challenges of targeting this signaling in cancers.

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“…–Inhibition of tumor growth in mice bearing HCC tumor xenografts –Reduction in both tumor volume and weight. HCC cell lines and BALB/c nude mice bearing HCC tumor xenografts Hepatocellular carcinoma 167 PF-670462 CK1ε and CK1δ Inhibitor –Reduction in chemotaxis, invasion and communication with stromal cells in primary CLL cells and in all major subtypes of CLL. –Decrease in the leukemic cell’s accumulation in the peripheral blood and spleen.…”

Section: Time As a Crucial Dimension To Medicinementioning

confidence: 99%

Molecular regulations of circadian rhythm and implications for physiology and diseases

Fagiani

Marino

Romagnoli

et al. 2022

Sig Transduct Target Ther

130

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The term “circadian rhythms” describes endogenous oscillations with ca. 24-h period associated with the earth’s daily rotation and light/dark cycle. Such rhythms reflect the existence of an intrinsic circadian clock that temporally orchestrates physiological processes to adapt the internal environment with the external cues. At the molecular level, the circadian clock consists of multiple sets of transcription factors resulting in autoregulatory transcription-translation feedback loops. Notably, in addition to their primary role as generator of circadian rhythm, the biological clock plays a key role in controlling physiological functions of almost all tissues and organs. It regulates several intracellular signaling pathways, ranging from cell proliferation, DNA damage repair and response, angiogenesis, metabolic and redox homeostasis, to inflammatory and immune response. In this review, we summarize findings showing the crosstalk between the circadian molecular clock and some key intracellular pathways, describing a scenario wherein their reciprocal regulation impinges upon several aspects of mammalian physiology. Moreover, based on evidence indicating that circadian rhythms can be challenged by environmental factors, social behaviors, as well as pre-existing pathological conditions, we discuss implications of circadian misalignment in human pathologies, such as cancer and inflammatory diseases. Accordingly, disruption of circadian rhythm has been reported to affect several physiological processes that are relevant to human diseases. Expanding our understanding of this field represents an intriguing and transversal medicine challenge in order to establish a circadian precision medicine.

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IC261 suppresses progression of hepatocellular carcinoma in a casein kinase 1 δ/ε independent manner

Cited by 9 publications

References 25 publications

CK1 Is a Druggable Regulator of Microtubule Dynamics and Microtubule-Associated Processes

CK1 Is a Druggable Regulator of Microtubule Dynamics and Microtubule-Associated Processes

Wnt/β-catenin signaling in cancers and targeted therapies

Molecular regulations of circadian rhythm and implications for physiology and diseases

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