Further evaluation of this role has been hampered by the lack of selective pharmacological inhibitors. Herein, we provide a comprehensive overview about the therapeutic potential of targeting CDK3 in cancer.

over 2 years ago

Review • Journal

EGFR (Epidermal growth factor receptor) • CDK4 (Cyclin-dependent kinase 4) • CDK6 (Cyclin-dependent kinase 6) • CDK2 (Cyclin-dependent kinase 2) • E2F1 (E2F transcription factor 1)

tamoxifen • fadraciclib (CYC065) • zotiraciclib (TG02) • AT7519 • roniciclib (BAY1000394)

over3years

CDK inhibitors in cancer therapy, an overview of recent development. (PubMed, Am J Cancer Res)

We reviewed first-generation pan-CDKIs Flavopiridol and Roscovitine, and second-generation CDKIs Dinaciclib, P276-00, AT7519, TG02, Roniciclib, RGB-286638 by focusing on their developing stages, clinical trials and targeting cancers. These CDKIs include CDK4/6, CDK7, CDK9, and CDK12/13 inhibitors. Finally, the efficacy and discrepancy of combination therapy with CDK inhibitors and PD1/PDL1 antibodies were analyzed, which might give insights into the development of promising strategy for cancer treatment.

over 3 years ago

Review • Journal

CDK12 (Cyclin dependent kinase 12) • CDK7 (Cyclin Dependent Kinase 7) • CDK9 (Cyclin Dependent Kinase 9)

HR positive

alvocidib (DSP-2033) • dinaciclib (MK-7965) • zotiraciclib (TG02) • AT7519 • RGB-286638 • riviciclib (P27600) • roniciclib (BAY1000394)

almost4years

Roniciclib down-regulates stemness and inhibits cell growth by inducing nucleolar stress in neuroblastoma. (PubMed, Sci Rep)

Furthermore, we found that high expression of Nucleophosmin-1 correlates with patients' short survival. The co-expression of several stem cell surface antigens such as CD44v6 and CD114, together with the nucleolar markers here described, extends new possibilities to isolate undifferentiated subpopulations from neuroblastoma and identify new targets for the treatment of this childhood malignancy.

almost 4 years ago

Journal

NPM1 (Nucleophosmin 1) • CSF3R (Colony Stimulating Factor 3 Receptor) • CD44 (CD44 Molecule) • CD14 (CD14 Molecule)

roniciclib (BAY1000394)

over6years

Japanese BAY1000394 Monotherapy Phase I Study (clinicaltrials.gov)

P1; N=12; Completed; Sponsor: Bayer; Active, not recruiting --> Completed; Trial completion date: Apr 2019 --> Jul 2018

over 6 years ago

Trial completion date • Trial completion

roniciclib (BAY1000394)