Aug 2026· Nature reviews. Drug discovery· 0 citations· 260 references
Medicine
TL;DR
This Review examines how transcriptional or co-transcriptional processes become dysregulated in cancer cells, and how this dysfunction might create targetable vulnerabilities, and summarizes advances in therapeutic strategies targeting transcriptional CDKs.
This review critically evaluates recent mechanistic advances in CDK/cyclin biology and their pathological dysregulation across malignancies and highlights emerging approaches including proteolysis‐targeting chimeras, HSP90‐mediated targeting chimeras, hydrophobic tagging, molecular glues, and autophagy‐tethering compou...
The molecular functions of the CDK9/positive transcription elongation factor b (P-TEFb) axis, its role in super-enhancer-driven oncogenic programs, and the mechanisms by which CDK9 inhibition promotes apoptosis, epigenetic derepression, and tumor microenvironment remodeling are summarized.
Ti-Yao Liu, Zhongran Liu, Wen-Jing Wei et al.· Expert opinion on therapeuti...· 0 citations
Transcriptional cyclin-dependent kinases (tCDKs) are master regulators of gene expression, controlling RNAPII activity and RNA synthesis across multiple phases of the transcription cycle. While highly controlled transcription is essential for all cellular processes and functions, aberrant gene expression or corrupted a...
J. Devlin, Salla Kyheröinen, Ricky W. Johnstone· The FEBS Journal· 0 citations
Global upregulation of transcription, or hypertranscription, is observed in most human cancers, driven by the action of oncogene-encoded transcription factors (TFs). TF interactions with RNA Polymerase II (Pol II) are mediated by kinases that phosphorylate the Pol II C-terminal domain (CTD) to drive productive elonga...
S. Henikoff, Robert N. Eisenman, K. Ahmad· Epigenetics & Chromatin· 0 citations
TEgment, a TE-centric RNA-sequencing analysis pipeline, provides a versatile framework for resolving TE transcriptional modalities at locus and structural levels, enabling precise interpretation of TE-derived transcripts in cancer and other contexts.
D. Prokopov, A. Moussa, Hale Tunbak et al.· bioRxiv· 0 citations
This work highlights non-canonical transcriptional kinases that could operate alongside and beyond CDKs to modulate transcription by RNAPII, and discusses how these kinases could introduce context-specific CTD modifications that enable transcriptional plasticity, facilitate rapid loci-specific activation, and integrate...
David D. Lowe, A. Shilatifard· Molecules and Cells· 0 citations
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