bs-181 and Triple-Negative-Breast-Neoplasms

bs-181 has been researched along with Triple-Negative-Breast-Neoplasms* in 1 studies

Other Studies

1 other study(ies) available for bs-181 and Triple-Negative-Breast-Neoplasms

Article	Year
Discovery of Potent and Selective CDK9 Degraders for Targeting Transcription Regulation in Triple-Negative Breast Cancer. Journal of medicinal chemistry, 2021, 10-14, Volume: 64, Issue:19 Triple-negative breast cancer (TNBC) is highly aggressive with very limited treatment options due to the lack of efficient targeted therapies and thus still remains clinically challenging. Targeting transcription-associated cyclin-dependent kinases to remodel transcriptional regulation shows great promise in cancer therapy. Herein, we report the synthesis, optimization, and evaluation of new series of heterobifunctional molecules as highly selective and efficacious CDK9 degraders, enabling potent inhibition of TNBC cell growth and rapidly targeted degradation of CDK9. Moreover, the most potent CDK9 degrader (compound Topics: Animals; Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Cyclin-Dependent Kinase 9; Drug Discovery; Gene Expression Regulation, Neoplastic; Humans; Ligands; Mice; Protein Kinase Inhibitors; Transcription, Genetic; Triple Negative Breast Neoplasms; Xenograft Model Antitumor Assays	2021

Article

Year

Discovery of Potent and Selective CDK9 Degraders for Targeting Transcription Regulation in Triple-Negative Breast Cancer.

Journal of medicinal chemistry, 2021, 10-14, Volume: 64, Issue:19

Triple-negative breast cancer (TNBC) is highly aggressive with very limited treatment options due to the lack of efficient targeted therapies and thus still remains clinically challenging. Targeting transcription-associated cyclin-dependent kinases to remodel transcriptional regulation shows great promise in cancer therapy. Herein, we report the synthesis, optimization, and evaluation of new series of heterobifunctional molecules as highly selective and efficacious CDK9 degraders, enabling potent inhibition of TNBC cell growth and rapidly targeted degradation of CDK9. Moreover, the most potent CDK9 degrader (compound

Topics: Animals; Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Cyclin-Dependent Kinase 9; Drug Discovery; Gene Expression Regulation, Neoplastic; Humans; Ligands; Mice; Protein Kinase Inhibitors; Transcription, Genetic; Triple Negative Breast Neoplasms; Xenograft Model Antitumor Assays

2021