bims-ectoca Biomed News
on Epigenetic control of tolerance in cancer
Issue of 2022‒09‒25
seven papers selected by
Ankita Daiya, Birla Institute of Technology and Science



  1. Chem Asian J. 2022 Sep 18.
      Histone deacetylases (HDACs) play critical roles in epigenetic modification. These enzymes can remove acetyl groups from the N -terminal lysine residues of histones, thereby regulating gene expression. Because of their great relevance to various diseases, numerous HDAC inhibitors have been developed. In this context, assays for HDAC activity are prerequisite. Due to the advantages of small-molecule fluorescent probes, researchers have developed many probes to detect HDAC activity for developing HDAC inhibitors. Based on the mechanism of action, two main types of small-molecule fluorescent probes are known. One type is based on binding affinity that are generally HDAC inhibitor-fluorophore conjugates. The other one is enzyme-activated probes, which act as HDAC substrates and show fluorogenic or ratiometric response after being deacetylated by HDACs.
    Keywords:  HDAC, enzymatic activity, fluorescent probe, inhibitor, fluorescence imaging
    DOI:  https://doi.org/10.1002/asia.202200835
  2. Epigenomes. 2022 Sep 06. pii: 28. [Epub ahead of print]6(3):
      The polycomb group (PcG) proteins are a subset of transcription regulators highly conserved throughout evolution. Their principal role is to epigenetically modify chromatin landscapes and control the expression of master transcriptional programs to determine cellular identity. The two mayor PcG protein complexes that have been identified in mammals to date are Polycomb Repressive Complex 1 (PRC1) and 2 (PRC2). These protein complexes selectively repress gene expression via the induction of covalent post-translational histone modifications, promoting chromatin structure stabilization. PRC2 catalyzes the histone H3 methylation at lysine 27 (H3K27me1/2/3), inducing heterochromatin structures. This activity is controlled by the formation of a multi-subunit complex, which includes enhancer of zeste (EZH2), embryonic ectoderm development protein (EED), and suppressor of zeste 12 (SUZ12). This review will summarize the latest insights into how PRC2 in mammalian cells regulates transcription to orchestrate the temporal and tissue-specific expression of genes to determine cell identity and cell-fate decisions. We will specifically describe how PRC2 dysregulation in different cell types can promote phenotypic plasticity and/or non-mutational epigenetic reprogramming, inducing the development of highly aggressive epithelial neuroendocrine carcinomas, including prostate, small cell lung, and Merkel cell cancer. With this, EZH2 has emerged as an important actionable therapeutic target in such cancers.
    Keywords:  Merkel cell cancer (MCC); polycomb group (PcG); polycomb repressive complex 2 (PRC2); prostate cancer (PCa); small cell lung cancer (SCLC); the enhancer of zeste (EZH2)
    DOI:  https://doi.org/10.3390/epigenomes6030028
  3. Front Mol Biosci. 2022 ;9 977653
      For certain inducible genes, the rate and molecular mechanism of transcriptional activation depends on the prior experiences of the cell. This phenomenon, called epigenetic transcriptional memory, accelerates reactivation and requires both changes in chromatin structure and recruitment of poised RNA Polymerase II (RNAPII) to the promoter. Forms of epigenetic transcriptional memory have been identified in S. cerevisiae, D. melanogaster, C. elegans, and mammals. A well-characterized model of memory is found in budding yeast where memory of inositol starvation involves a positive feedback loop between gene-and condition-specific transcription factors, which mediate an interaction with the nuclear pore complex and a characteristic histone modification: histone H3 lysine 4 dimethylation (H3K4me2). This histone modification permits recruitment of a memory-specific pre-initiation complex, poising RNAPII at the promoter. During memory, H3K4me2 is essential for recruitment of RNAPII and faster reactivation, but RNAPII is not required for H3K4me2. Unlike the RNAPII-dependent H3K4me2 associated with active transcription, RNAPII-independent H3K4me2 requires Nup100, SET3C, the Leo1 subunit of the Paf1 complex and can be inherited through multiple cell cycles upon disrupting the interaction with the Nuclear Pore Complex. The H3K4 methyltransferase (COMPASS) physically interacts with the potential reader (SET3C), suggesting a molecular mechanism for the spreading and re-incorporation of H3K4me2 following DNA replication. Thus, epigenetic transcriptional memory is a conserved adaptation that utilizes a heritable chromatin state, allowing cells and organisms to alter their gene expression programs in response to recent experiences over intermediate time scales.
    Keywords:  S. cerevisiae; chromatin; chromosomes; epigentics; heritable histones; nuclear pore; transcriptional memory
    DOI:  https://doi.org/10.3389/fmolb.2022.977653
  4. Cancers (Basel). 2022 Sep 08. pii: 4375. [Epub ahead of print]14(18):
      Non-coding segments of the human genome are enriched in cis-regulatory modules that constitute functional elements, such as transcriptional enhancers and Super-enhancers. A hallmark of cancer pathogenesis is the dramatic dysregulation of the "archetype" gene expression profiles of normal human cells. Genomic variations can promote such deficiencies when occurring across enhancers and Super-enhancers, since they affect their mechanistic principles, their functional capacity and specificity, and the epigenomic features of the chromatin microenvironment across which these regulatory elements reside. Here, we comprehensively describe: fundamental mechanisms of gene expression dysregulation in cancers that involve genomic abnormalities within enhancers' and Super-enhancers' (SEs) sequences, which alter the expression of oncogenic transcription factors (TFs); cutting-edge technologies applied for the analysis of variation-enriched hotspots of the cancer genome; and pharmacological approaches for the treatment of Super-enhancers' aberrant function. Finally, we provide an intratumor meta-analysis, which highlights that genomic variations in transcription-factor-driven tumors are accompanied overexpression of genes, a portion of which encodes for additional cancer-related transcription factors.
    Keywords:  Next-Generation Sequencing (NGS); Super-enhancers (SEs); cancer; chromatin; enhancers; epigenetics; gene expression programs; genomic variations; oncogenes; transcription factors (TFs); tumorigenesis
    DOI:  https://doi.org/10.3390/cancers14184375
  5. Biochim Biophys Acta Mol Basis Dis. 2022 Sep 17. pii: S0925-4439(22)00223-X. [Epub ahead of print] 166552
      The critical role of dysregulated epigenetic pathways in cancer genesis, development, and therapy has typically been established as a result of scientific and technical innovations in next generation sequencing. RNA interference, histone modification, DNA methylation and chromatin remodelling are epigenetic processes that control gene expression without causing mutations in the DNA. Although epigenetic abnormalities are thought to be a symptom of cell tumorigenesis and malignant events that impact tumor growth and drug resistance, physicians believe that related processes might be a key therapeutic target for cancer treatment and prevention due to the reversible nature of these processes. A plethora of novel strategies for addressing epigenetics in cancer therapy for immuno-oncological complications are currently available - ranging from basic treatment to epigenetic editing. - and they will be the subject of this comprehensive review. In this review, we cover most of the advancements made in the field of targeting epigenetics with special emphasis on microbiology, plasma science, biophysics, pharmacology, molecular biology, phytochemistry, and nanoscience.
    Keywords:  Epigenetics; Nanomedicines; Therapeutic targets; cancer
    DOI:  https://doi.org/10.1016/j.bbadis.2022.166552
  6. Bioinformatics. 2022 Sep 20. pii: btac642. [Epub ahead of print]
      MOTIVATION: Multiomic profiling data, such as The Cancer Genome Atlas (TCGA) and pharmacogenomic data, facilitate research into cancer mechanisms and drug development. However, it is not easy for researchers to connect, integrate, and analyze huge and heterogeneous data, which is a major obstacle to the utilization of cancer genomic data.RESULTS: We developed Cancer Genome Viewer (CGV), a user-friendly web service that provides functions to integrate and visualize cancer genome data and pharmacogenomic data. Users can easily select and customize the samples to be analyzed with the pre-defined selection options for patients' clinic-pathological features from multiple data sets. Using the customized data set, users can perform subsequent data analyses comprehensively, including gene set analysis, clustering, or survival analysis. CGV also provides pre-calculated drug response scores from pharmacogenomic data, which may facilitate the discovery of new cancer targets and therapeutics.
    AVAILABILITY AND IMPLEMENTATION: CGV web service is implemented with the R Shiny application at http://cgv.sysmed.kr and the source code is freely available at https://git.sysmed.kr/sysmed_public/cgv.
    SUPPLEMENTARY INFORMATION: Supplementary data are available at Bioinformatics online.
    DOI:  https://doi.org/10.1093/bioinformatics/btac642
  7. Cell Mol Bioeng. 2022 Aug;15(4): 313-330
      Introduction-Local hemodynamics impact the mechanotransduction in endothelial cells (ECs) lining the vascular network. On the other hand, cancer cells are shown to influence the local hemodynamics in their vicinity, in microvasculature. The first objective of present study is to explore how cancer cell-induced changes in local hemodynamics can impact the forces experienced by intra/inter-cellular organelles of ECs that are believed to play important roles in mechanotransduction. Moreover, extracellular matrix (ECM) stiffening has been shown to correlate with progression of most cancer types. However, it is still not well understood how ECM stiffness impacts ECs mechanosensors. The second objective of this study is to elucidate the role of ECM stiffness on mechanotransduction in ECs. Methods-A three-dimensional, multiscale, multicomponent, viscoelastic model of focally adhered ECs is developed to simulate the force transmission through ECs mechanosensors [actin cortical layer, nucleus, cytoskeleton, focal adhesions (FAs), and adherens junctions (ADJs)]. Results-Our results show that cancer cell-altered hemodynamics results in significantly high forces transmitted to subcellular organelles of ECs which are in vicinity of cancer cells. This impact is more drastic on stress fibers (SFs) both centrally located and peripheral ones. Furthermore, we demonstrate that ADJs, FAs, and SFs experience higher stresses in ECs attached to stiffer ECM. Impact of ECM stiffness is particularly significant in ECs exposed to fluid shear stresses of 2 Pa or lower. This finding reveals the role of organ-specific stiffness in promoting cancer cell transmigration even in capillaries larger than cancer cell diameter. Conclusions-ÊCancer cell-induced-changes in ECs mechanotransduction represents an important potential mechanism for cancer cell transmigration in the microvasculature particularly with stiffer ECM. The identification of ECs mechanosensors involved in early stages of EC-cancer cell interaction will help with developing more efficient therapeutic interventions to suppress cancer cell transmigration in the microvasculature.
    Keywords:  Cancer cells; Endothelial Cells; Extracellular matrix; Mechanosensors; Mechanotransduction
    DOI:  https://doi.org/10.1007/s12195-022-00728-w