Article
Biochemistry & Molecular Biology
Anil Kumar Yadav, Byeong-Churl Jang
Summary: The CK2 inhibitor CX-4945 has strong anti-adipogenic and pro-lipolytic effects on 3T3-L1 cells, by reducing lipid droplet accumulation, triglyceride content, and controlling the expression and phosphorylation levels of various proteins.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biology
Katrina Kildey, Neha S. Gandhi, Katherine B. Sahin, Esha T. Shah, Eric Boittier, Pascal H. G. Duijf, Christopher Molloy, Joshua T. Burgess, Sam Beard, Emma Bolderson, Amila Suraweera, Derek J. Richard, Kenneth J. O'Byrne, Mark N. Adams
Summary: Platinum-based chemotherapy is the mainstay of treatment for NSCLC, but resistance is a major issue. Research shows that CDCA3 levels correlate with sensitivity to platinum agents in NSCLC tumors, and inhibition of CK2 can increase CDCA3 levels and enhance sensitivity to platinum agents.
COMMUNICATIONS BIOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Anne S. Boewe, Silke Wemmert, Philipp Kulas, Bernhard Schick, Claudia Goetz, Selina Wrublewsky, Mathias Montenarh, Michael D. Menger, Matthias W. Laschke, Emmanuel Ampofo
Summary: The inhibition of CK2 may represent a promising therapeutic approach for the treatment of NG2-expressing juvenile angiofibroma, as it can significantly reduce NG2 expression and suppress the proliferation and migration of JA cells.
Article
Cell Biology
Mauro Salvi, Christian Borgo, Lorenzo A. Pinna, Maria Ruzzene
Summary: The newly developed compound SGC-CK2-1, which is more selective than other CK2 inhibitors, has shown poor efficacy in reducing cell growth in different cancer cell lines, raising questions about the anticancer efficacy of CX-4945, the commonly used clinical-grade CK2 inhibitor.
CELL DEATH DISCOVERY
(2021)
Article
Oncology
Da Sol Lee, Seonmin Lee, Chorong Kim, Danbee Kim, Kyu-Pyo Kim, Changhoon Yoo
Summary: This study found that the CK2 inhibitor CX-4945 can induce cell cycle arrest and cell death in cholangiocarcinoma cells through the regulation of PLK1 and p53. This provides a novel therapeutic strategy for the treatment of advanced cholangiocarcinoma.
ANTICANCER RESEARCH
(2022)
Article
Biochemistry & Molecular Biology
Saini Wang, Anil Kumar Yadav, Jin-Yi Han, Keun Soo Ahn, Byeong-Churl Jang
Summary: This study found that CX-4945 has anti-growth, anti-angiogenic, and proapoptotic effects on HuCCT-1 cells, which are mediated through the control of CK2, caspase-9/3, DR-4, STAT-3/5, Mcl-1, eIF-2 alpha, and HIF-1 alpha.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Lucia Villamanan, Laura Martinez-Escardo, Carles Arus, Victor J. Yuste, Ana P. Candiota
Summary: In vitro experiments demonstrated that combined treatment may simultaneously release two potent immunogenic signals, potentially explaining its superior performance over single treatments in vivo.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Rulin Sun, Xujun He, Xiaoting Jiang, Houquan Tao
Summary: Pancreatic cancer is often diagnosed at an advanced stage, making chemotherapy the best treatment option. Research suggests that Riluzole may have potential in inhibiting tumors, including pancreatic cancer. Further experiments are needed to confirm the reliability of these findings, but data indicates Riluzole may offer promise for future treatments.
JOURNAL OF CELLULAR BIOCHEMISTRY
(2021)
Article
Cell Biology
Mauro Rosales, Arielis Rodriguez-Ulloa, Vladimir Besada, Ailyn C. Ramon, George V. Perez, Yassel Ramos, Osmany Guirola, Luis J. Gonzalez, Katharina Zettl, Jacek R. Wisniewski, Yasser Perera, Silvio E. Perea
Summary: This study investigated the impact of CK2 inhibitor CX-4945 on the phosphoproteome of two cell lines representing major AML subtypes. The findings suggest that CX-4945 significantly alters phosphorylation levels in HL-60 and OCI-AML3 cells, mainly through direct CK2 inhibition rather than off-target effects. Additionally, CK2 substrates regulated by CX-4945 are primarily involved in mRNA processing, translation, DNA repair, and the cell cycle.
Article
Oncology
Mingyang Song, Qin Lu, Min Xu, Yajie Li, Yawen Zhao, Chen Gong, Xilong Ou
Summary: This study conducted a bibliometric analysis on literature related to autophagy of pancreatic cancer to present the global research features and hotspots, and forecast the emerging trends. China and the United States were the most frequent publishers and collaborators in this field. The research hotspots focused on autophagy mechanisms in tumor onset and progression, the role of autophagy in tumor apoptosis, and autophagy-related drugs in treating pancreatic cancer.
FRONTIERS IN ONCOLOGY
(2022)
Article
Chemistry, Medicinal
Yuanjiang Wang, Zhaodan Lv, Feihong Chen, Xing Wang, Shaohua Gou
Summary: The synthesized molecule 1c has strong CK2 inhibitory activity and high selectivity, as well as the ability to modulate key signaling pathways and inhibit the expression of stem markers, showing potent inhibitory activity against cancer stem cells, making it a potential candidate for cancer treatment.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Multidisciplinary Sciences
Katsutoshi Sato, Amol A. Padgaonkar, Stacey J. Baker, Stephen C. Cosenza, Olga Rechkoblit, D. R. C. Venkata Subbaiah, Josep Domingo-Domenech, Alison Bartkowski, Elisa R. Port, Aneel K. Aggarwal, M. V. Ramana Reddy, Hanna Y. Irie, E. Premkumar Reddy
Summary: Finding therapeutic strategies for aggressive triple negative breast cancer (TNBC) is an important challenge in clinical practice. Here, the authors identify a multi-kinase inhibitor with antitumor activity and able overcome chemotherapy resistance of TNBC in vivo.
NATURE COMMUNICATIONS
(2021)
Article
Biochemistry & Molecular Biology
Laszlo Gyenis, Daniel Menyhart, Edward S. Cruise, Kristina Jurcic, Scott E. Roffey, Darren B. Chai, Flaviu Trifoi, Sam R. Fess, Paul J. Desormeaux, Teresa Nunez de Villavicencio Diaz, Adam J. Rabalski, Stephanie A. Zukowski, Jacob P. Turowec, Paula Pittock, Gilles Lajoie, David W. Litchfield
Summary: In this study, a strategy combining chemical genetics and quantitative phosphoproteomics was used to identify and validate CSNK2 substrates. The approach successfully overcame the limitations of ATP-competitive inhibitors and provided a more specific and feasible method for kinase-substrate assignment.
FRONTIERS IN MOLECULAR BIOSCIENCES
(2022)
Article
Oncology
Morgann Klink, Mohammad Atiqur Rahman, Chunhua Song, Pavan Kumar Dhanyamraju, Melanie Ehudin, Yali Ding, Sadie Steffens, Preeti Bhadauria, Soumya Iyer, Cesar Aliaga, Dhimant Desai, Suming Huang, David Claxton, Arati Sharma, Chandrika Gowda
Summary: The study reveals that inhibition of CK2 kinase can enhance the efficacy of chemotherapy drugs in patients with acute myeloid leukemia, especially when used in combination with CX-4945 inhibitor. Additionally, CK2 inhibition can also restore the function of the IKAROS tumor suppressor, increasing the sensitivity of AML cells to apoptosis.
Article
Chemistry, Medicinal
Przemyslaw Grygier, Katarzyna Pustelny, Jakub Nowak, Przemyslaw Golik, Grzegorz M. Popowicz, Oliver Plettenburg, Grzegorz Dubin, Filipe Menezes, Anna Czarna
Summary: CX-4945 is a clinical casein kinase 2 inhibitor that has significant affinity towards DYRK1A and GSK3fi kinases, which are involved in various diseases. The crystal structures of DYRK1A and GSK3fi with CX-4945 were solved and analyzed, and a model was built to rationalize the compound affinity for CK2a, DYRK1A, and GSK3fi kinases. The inhibitor limits the activity of these kinases and shows potential for application in additional disease areas.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)