Targeting transcription cycles in cancer
Accurate control of gene expression is essential for normal development and dysregulation
of transcription underpins cancer onset and progression. Similar to cell cycle regulation …
of transcription underpins cancer onset and progression. Similar to cell cycle regulation …
An atlas of substrate specificities for the human serine/threonine kinome
Protein phosphorylation is one of the most widespread post-translational modifications in
biology,. With advances in mass-spectrometry-based phosphoproteomics, 90,000 sites of …
biology,. With advances in mass-spectrometry-based phosphoproteomics, 90,000 sites of …
From structure modification to drug launch: A systematic review of the ongoing development of cyclin-dependent kinase inhibitors for multiple cancer therapy
Z Shi, L Tian, T Qiang, J Li, Y **ng, X Ren… - Journal of medicinal …, 2022 - ACS Publications
Herein, we discuss more than 50 cyclin-dependent kinase (CDK) inhibitors that have been
approved or have undergone clinical trials and their therapeutic application in multiple …
approved or have undergone clinical trials and their therapeutic application in multiple …
SPT5 stabilizes RNA polymerase II, orchestrates transcription cycles, and maintains the enhancer landscape
Transcription progression is governed by multitasking regulators including SPT5, an
evolutionarily conserved factor implicated in virtually all transcriptional steps from enhancer …
evolutionarily conserved factor implicated in virtually all transcriptional steps from enhancer …
Pre-mRNA splicing and its cotranscriptional connections
Transcription of eukaryotic genes by RNA polymerase II (Pol II) yields RNA precursors
containing introns that must be spliced out and the flanking exons ligated together. Splicing …
containing introns that must be spliced out and the flanking exons ligated together. Splicing …
Discovery of SY-5609: a selective, noncovalent inhibitor of CDK7
JJ Marineau, KB Hamman, S Hu… - Journal of Medicinal …, 2021 - ACS Publications
CDK7 has emerged as an exciting target in oncology due to its roles in two important
processes that are misregulated in cancer cells: cell cycle and transcription. This report …
processes that are misregulated in cancer cells: cell cycle and transcription. This report …
Oncogenic CDK13 mutations impede nuclear RNA surveillance
RNA surveillance pathways detect and degrade defective transcripts to ensure RNA fidelity.
We found that disrupted nuclear RNA surveillance is oncogenic. Cyclin-dependent kinase …
We found that disrupted nuclear RNA surveillance is oncogenic. Cyclin-dependent kinase …
Transcription associated cyclin-dependent kinases as therapeutic targets for prostate cancer
TA Constantin, KK Greenland, A Varela-Carver… - Oncogene, 2022 - nature.com
Transcriptional deregulation has emerged as a hallmark of several cancer types. In
metastatic castration-resistant prostate cancer, a stage in which systemic androgen …
metastatic castration-resistant prostate cancer, a stage in which systemic androgen …
Novel covalent CDK7 inhibitor potently induces apoptosis in acute myeloid leukemia and synergizes with Venetoclax
T Gaur, R Poddutoori, L Khare, B Bagal… - Journal of Experimental …, 2023 - Springer
Introduction The emergence of resistance to the highly successful BCL2-directed therapy is
a major unmet need in acute myeloid leukemia (AML), an aggressive malignancy with poor …
a major unmet need in acute myeloid leukemia (AML), an aggressive malignancy with poor …
Insights into the structural and functional activities of forgotten Kinases: PCTAIREs CDKs
In cells, signal transduction heavily relies on the intricate regulation of protein kinases, which
provide the fundamental framework for modulating most signaling pathways. Dysregulation …
provide the fundamental framework for modulating most signaling pathways. Dysregulation …