Targeting cyclin-dependent kinase 9 in cancer therapy
Nov 22, 2021 · The novel CDK9 inhibitor, XPW1, alone and in combination with BRD4 inhibitor JQ1, for the treatment of clear cell renal cell carcinoma. Cyclin-dependent kinase (CDK) 9 associates mainly with ...
CDK9: A Comprehensive Review of Its Biology, and Its Role as a ...
May 9, 2021 · Inhibition of CDK9 by selective inhibitors (e.g., AZ5576) or by genetic knockdown negatively regulated MYC and MCL-1 expression, and induced apoptosis in primary and transformed cells from this lymphoma, providing an attractive therapeutic strategy (139, 140).
CDK inhibitors in cancer therapy, an overview of recent ... - PMC
Several CDK9 inhibitors have been developed, and their significant anti-tumor activity has been demonstrated in preclinical studies, such as Fadraciclib, AZD-4573, CDKI-73, MC180295, etc. In addition, Fadraciclib combined with temozolomide can effectively suppress MYCN-amplified neuroblastoma long-term [ 65 ].
Targeting CDK9 with selective inhibitors or degraders in tumor …
As a catalytic subunit of the positive transcription elongation factor b (P-TEFb), cyclin-dependent kinase 9 (CDK9) has been demonstrated to contribute to carcinogenesis. This review focuses on the development of selective CDK9 inhibitors and ...
VIP152 is a selective CDK9 inhibitor with pre-clinical in ...
Nov 14, 2022 · VIP152 kinome profiling revealed CDK9 as the main enzyme inhibited at 100 nM, with over a 10-fold increase in potency compared with other inhibitors currently in development for this target.
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy
Oct 10, 2016 · Cyclin dependent kinase (CDK) inhibitors have been the topic of intense research for nearly 2 decades due to their widely varied and critical functions within the cell. Recently CDK9 has emerged as a druggable target for the development of cancer therapeutics. CDK9 plays a crucial role in transcription regulation; specifically, CDK9 mediated ...
CDK9 inhibition constrains multiple oncogenic transcriptional and ...
Aug 8, 2024 · The orally bioavailable CDK9 inhibitor CDKI-73 has a multipronged mode of action, suppressing oncogenic transcriptional programs driven by AR, MYC, and BRD4 as well as suppressing critical anti...
Recent Discovery and Development of Inhibitors that Target CDK9 …
Apr 2, 2024 · In this perspective, we present a comprehensive overview of the structural characteristics, biological functions, and preclinical status of CDK9 inhibitors. Our focus extends to various types of inhibitors, including pan-inhibitors, selective inhibitors, dual-target inhibitors, degraders, PPI inhibitors, and natural products.
Full article: Targeting CDK9 with selective inhibitors or degraders …
This review focuses on the development of selective CDK9 inhibitors and proteolysis-targeting chimera (PROTAC) degraders. Twenty selective CDK9 inhibitors and degraders are introduced along with their structures, IC50 values, in vitro and in vivo experiments, mechanisms underlying their inhibitory effects, and combination regimens.
AZD4573 Is a Highly Selective CDK9 Inhibitor That ...
Feb 14, 2020 · This work describes the novel CDK9 inhibitor, AZD4573, that was optimized for high selectivity and potency against CDK9 as well as physicochemical properties enabling intravenous infusion and a short PK half-life.