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- W2799448290 abstract "Protein kinase CK2, formerly referred to as casein kinase II, is a serine/threonine kinase often found overexpressed in solid tumors and hematologic malignancies that phosphorylates many substrates integral to the hallmarks of cancer. CK2 has emerged as a viable oncology target having been experimentally validated with different kinase inhibitors, including small molecule ATP-competitors, synthetic peptides, and antisense oligonucleotides. To date only two CK2 inhibitors, CIGB-300 and CX-4945, have entered the clinic in phase 1-2 trials. This review provides information on CIGB-300, a cell-permeable cyclic peptide that inhibits CK2-mediated phosphorylation by targeting the substrate phosphoacceptor domain. We review data that support the concept of CK2 as an anticancer target, address the mechanism of action, and summarize preclinical studies showing antiangiogenic and antimetastatic effects as well as synergism with anticancer drugs in preclinical models. We also summarize early clinical research (phase 1/2 trials) of CIGB-300 in cervical cancer, including data in combination with chemoradiotherapy. The clinical data demonstrate the safety, tolerability, and clinical effects of intratumoral injections of CIGB-300 and provide the foundation for future phase 3 clinical trials in locally advanced cervical cancer in combination with standard chemoradiotherapy." @default.
- W2799448290 created "2018-05-17" @default.
- W2799448290 creator A5004701925 @default.
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- W2799448290 creator A5028868174 @default.
- W2799448290 creator A5075408516 @default.
- W2799448290 date "2018-01-01" @default.
- W2799448290 modified "2023-09-23" @default.
- W2799448290 title "CIGB-300: A peptide-based drug that impairs the Protein Kinase CK2-mediated phosphorylation" @default.
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- W2799448290 doi "https://doi.org/10.1053/j.seminoncol.2018.04.006" @default.
- W2799448290 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30318085" @default.
- W2799448290 hasPublicationYear "2018" @default.
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