Targeting CDK9 with selective inhibitors or degraders in tumor therapy: an overview of recent developments

L Xiao, Y Liu, H Chen, L Shen - Cancer Biology & Therapy, 2023 - Taylor & Francis
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 …

CDK9 inhibitors in cancer research

Z Huang, T Wang, C Wang, Y Fan - RSC Medicinal Chemistry, 2022 - pubs.rsc.org
Cyclin dependent kinase 9 (CDK9) plays an essential role in regulating transcriptional
elongation. Aberrations in CDK9 activity have been observed in various cancers, which …

A rohitukine derivative IIIM‐290 induces p53 dependent mitochondrial apoptosis in acute lymphoblastic leukemia cells

M Mintoo, S Khan, A Wani, S Malik… - Molecular …, 2021 - Wiley Online Library
Rohitukine, a chromone alkaloid extracted from Dysoxylum binectariferum, has a propitious
anticancer activity. Our previous study shows that a new Rohitukine derivative IIIM‐290 …

VEGFC/FLT4-induced cell-cycle arrest mediates sprouting and differentiation of venous and lymphatic endothelial cells

A Jerafi-Vider, I Bassi, N Moshe, Y Tevet, G Hen… - Cell reports, 2021 - cell.com
The formation of new vessels requires a tight synchronization between proliferation,
differentiation, and sprouting. However, how these processes are differentially activated …

RNF43 inhibits WNT5A-driven signaling and suppresses melanoma invasion and resistance to the targeted therapy

T Radaszkiewicz, M Nosková, K Gömöryová… - Elife, 2021 - elifesciences.org
RNF43 is an E3 ubiquitin ligase and known negative regulator of WNT/β-catenin signaling.
We demonstrate that RNF43 is also a regulator of noncanonical WNT5A-induced signaling …

Genome-wide identification of cyclin-dependent kinase (CDK) genes affecting adipocyte differentiation in cattle

C Pan, Z Lei, S Wang, X Wang, D Wei, X Cai… - BMC genomics, 2021 - Springer
Abstract Background Cyclin-dependent kinases (CDKs) are protein kinases regulating
important cellular processes such as cell cycle and transcription. Many CDK genes also play …

Targeting strategies for modulating pre-mRNA splicing with small molecules: recent advances

SJ Barraza, A Bhattacharyya, CR Trotta, MG Woll - Drug Discovery Today, 2023 - Elsevier
Highlights•Modulation of pre-mRNA splicing is an effective alternative to the direct targeting
of proteins.•Insight into pre-mRNA splicing biology offers practical targeted strategies to …

Inhibition of CDK12 elevates cancer cell dependence on P-TEFb by stimulation of RNA polymerase II pause release

Z Wang, SV Himanen, HM Haikala… - Nucleic Acids …, 2023 - academic.oup.com
P-TEFb and CDK12 facilitate transcriptional elongation by RNA polymerase II. Given the
prominence of both kinases in cancer, gaining a better understanding of their interplay could …

Targeting cyclin-dependent kinase 9 in cancer therapy

Y Shen, Y Wang, Y Zhang, S Ma, L Yang… - Acta Pharmacologica …, 2022 - nature.com
Abstract Cyclin-dependent kinase (CDK) 9 associates mainly with cyclin T1 and forms the
positive transcription elongation factor b (p-TEFb) complex responsible for transcriptional …

Targeting the heterogeneous genomic landscape in triple-negative breast cancer through inhibitors of the transcriptional machinery

VE van der Noord, B van de Water, SE Le Dévédec - Cancers, 2022 - mdpi.com
Simple Summary Triple-negative breast cancer (TNBC) is the most aggressive subtype of
breast cancer with limited options for therapy. Cancer development and maintenance is …