keyword
MENU ▼
Read by QxMD icon Read
search

Small molecule epigenetics

keyword
https://www.readbyqxmd.com/read/29236313/micrornas-and-exosomes-in-depression-potential-diagnostic-biomarkers
#1
Jahanshir Tavakolizadeh, Kambiz Roshanaei, Arash Salmaninejad, Reza Yari, Javid Sadri Nahand, Hoda Khoshdel Sarkarizi, Seyed Mojtaba Mousavi, Reza Salarinia, Majid Rahmati, Seyed Farshid Mousavi, Ryan Mokhtari, Hamed Mirzaei
Depression is known as one of important psychiatric disorders which could be associated with disability among various populations. Diagnostic and statistical manual of mental disorders, 4th edition (DSM-IV) and international statistical classification of diseases and related health problems (ICD-10) could be used as subjective diagnostic schemes for identification of mental disorders such as depression. Utilization of subjective diagnostic schemes are associated with limitations. Hence, it seems that employing of new diagnosis platforms is required...
December 13, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/29233295/novel-approaches-to-targeting-brd4
#2
REVIEW
Olesya A Kharenko, Henrik C Hansen
Inhibition of bromo and extra-terminal (BET) bromodomains, including BRD4, has emerged as a new exciting epigenetic target for oncology, in particular. Recently, novel alternatives to the traditional use of reversible small molecules have emerged, including proteolytic targeting BET agents and irreversible binding inhibitors. These alternatives to reversible inhibitors may offer some advantage and can be used as tools to further decipher the underlying biology. Supportive pre-clinical data have these novel approaches bound for clinical development in the near future...
June 2017: Drug Discovery Today. Technologies
https://www.readbyqxmd.com/read/29222300/emerging-options-in-multiple-myeloma-targeted-immune-and-epigenetic-therapies
#3
REVIEW
Shaji Kumar
Considerable progress has been made in the treatment of multiple myeloma in the past decade with median survival for the disease improving significantly. This has come through a combination of better understanding of the disease biology and coordinated research into new treatment approaches including better supportive care. However, patients eventually become refractory to available treatments and succumb to the disease, highlighting the need to develop new treatment approaches. The genetic heterogeneity in the disease and clonal evolution under treatment pressure underlie the development of resistance, underscoring the need to develop more effective therapies that can eradicate the disease at initial treatment as well as the need for new classes of drugs with varying mechanisms of action...
December 8, 2017: Hematology—the Education Program of the American Society of Hematology
https://www.readbyqxmd.com/read/29215703/design-synthesis-and-characterization-of-%C3%AE-%C3%AE-unsaturated-carboxylic-acid-and-its-urea-based-derivatives-that-explores-novel-epigenetic-modulators-in-human-non-small-cell-lung-cancer-a549-cell-line
#4
Anusha Chidambaram, S H Kavya, Ramesh Kumar Chidambaram, Rajasekaran Subbiah, John Marshal Jayaraj, Karthikeyan Muthusamy, Ravikumar Vilwanathan
Histone deacetylase inhibitors (HDACi) are a small molecule chemotherapeutics that target the chromatin remodeling through the regulation of histone and non-histone proteins. These inhibitors directed against HDAC enzymes have become an important therapeutic tool in oncology; consequently, scientific efforts have fortified the quest for newer and novel HDACi, which forces the design of structurally innovative HDACi. Various urea containing compounds exhibited admirable anticancer activity. On the basis of these observations, we design and synthesize HDAC specific blocker molecules which are specifically besieged towards class I, class II and class IV HDAC isoforms to enhance the structural assortment for HDACi...
December 7, 2017: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/29214166/mirnas-important-targets-for-oral-cancer-pain-research
#5
REVIEW
Cláudia Maria Pereira, Dayany Sehnem, Estevão Oliveira da Fonseca, Heráclito Fernando Gurgel Barboza, Antônio Carlos Pires de Carvalho, Alexandre F M DaSilva, Vivaldo Moura-Neto, Marcos F DosSantos
Pain is a symptom shared by an incredible number of diseases. It is also one of the primary conditions that prompt individuals to seek medical treatment. Head and neck squamous cell carcinoma (HNSCC) corresponds to a heterogeneous disease that may arise from many distinct structures of a large, highly complex, and intricate region. HNSCC affects a great number of patients worldwide and is directly associated with chronic pain, which is especially prominent during the advanced stages of oral squamous cell carcinoma (OSCC), an anatomical and clinical subtype that corresponds to the great majority oral cancers...
2017: BioMed Research International
https://www.readbyqxmd.com/read/29207103/epigenetic-alterations-of-the-igf2-promoter-and-the-effect-of-mir%C3%A2-483%C3%A2-5p-on-its-target-gene-expression-in-esophageal-squamous-cell-carcinoma
#6
Han Zhang, Xiaowei Shi, Weidong Chang, Yingying Li, Li Wang, Linsong Wang
Esophageal squamous cell carcinoma (ESCC) is one of the most widespread malignancies in China. MicroRNAs (miRNAs/miRs) are endogenous evolutionarily‑conserved small non‑coding RNAs that are able to regulate ESCC formation and deterioration by negatively regulating specific target genes. In the present study, the expression levels of miR‑483‑5p and its associated mRNAs were measured by quantitative polymerase chain reaction (PCR) analysis, and the methylation levels of the insulin‑like growth factor 2 (Igf2) promoter were detected via the methylation‑specific PCR method in serum and tissues from patients with ESCC...
November 22, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29193029/recent-progress-in-understanding-and-manipulating-haemoglobin-switching-for-the-haemoglobinopathies
#7
REVIEW
Divya S Vinjamur, Daniel E Bauer, Stuart H Orkin
The major β-haemoglobinopathies, sickle cell disease and β-thalassaemia, represent the most common monogenic disorders worldwide and a steadily increasing global disease burden. Allogeneic haematopoietic stem cell transplantation, the only curative therapy, is only applied to a small minority of patients. Common clinical management strategies act mainly downstream of the root causes of disease. The observation that elevated fetal haemoglobin expression ameliorates these disorders has motivated longstanding investigations into the mechanisms of haemoglobin switching...
November 28, 2017: British Journal of Haematology
https://www.readbyqxmd.com/read/29189147/disrupting-acetyl-lysine-interactions-recent-advance-in-the-development-of-bet-inhibitors
#8
Fa Zhang, Shutao Ma
BACKGROUND: Histone acetylation is an essential way of post-translational modification (PTM) and a significant component of epigenetic regulation that is mediated by Bromodomain-containing protein (BRD). In recent years, many researchers have found that a variety of malignancy, inflammatory and other diseases occurrence and development are associated with BRD4 expression disorders or dysfunction. Meanwhile, many the bromodomain inhibitors of the bromodomains and extra-terminal (BET) family is reported in many papers...
November 29, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/29189124/overview-on-anticancer-drug-design-and-development
#9
Sureyya Olgen
Many impediments of current anti-cancer therapies have urged scientists to discover new agents. As a result of growing spectrums of new targets and strategies and recent biological and biotechnological progresses, many anti-cancer agents such as monoclonal antibodies, small molecule tyrosine kinase inhibitors and epigenetic drugs have been reached to clinical trials. Addition to the traditional targets (mitosis, DNA synthesis, repairing systems, tumor growth, apoptosis, tumor vasculature and cell signaling mechanisms), other targets such as proteasome, heat shock proteins (HSPs), and epigenetics (HDACs, HATs, DNMT, PAD4, AID, and Tet1) are used to design new anti-cancer agents...
November 29, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29180474/vitamin-c-sensitizes-melanoma-to-bet-inhibitors
#10
Gaofeng Wang, Sushmita Mustafi, Vladimir Camarena, Claude-Henry Volmar, Tyler C Huff, David W Sant, Shaun P Brothers, Zhao-Jun Liu, Claes Wahlestedt
Bromodomain and extra-terminal inhibitors (BETi) are promising cancer therapies, yet prominent side effects of BETi at effective doses have been reported in Phase I clinical trials. Here we screened a panel of small molecules targeting epigenetic modulators against human metastatic melanoma cells. Cells were pretreated with or without ascorbate (vitamin C), which promotes DNA demethylation and subsequently changes the sensitivity to drugs. Top hits were structurally unrelated BETi including JQ1, I-BET151, CPI-203, and BI-2536...
November 27, 2017: Cancer Research
https://www.readbyqxmd.com/read/29179434/growth-of-malignant-extracranial-tumors-alters-micrornaome-in-the-prefrontal-cortex-of-tumorgraft-mice
#11
Anna Kovalchuk, Yaroslav Ilnytskyy, Rocio Rodriguez-Juarez, Amanda Katz, David Sidransky, Bryan Kolb, Olga Kovalchuk
A wide array of central nervous system complications, neurological deficits, and cognitive impairments occur and persist as a result of systemic cancer and cancer treatments. This condition is known as chemo brain and it affects over half of cancer survivors. Recent studies reported that cognitive impairments manifest before chemotherapy and are much broader than chemo brain alone, thereby adding in tumor brain as a component. The molecular mechanisms of chemo brain are under-investigated, and the mechanisms of tumor brain have not been analyzed at all...
October 24, 2017: Oncotarget
https://www.readbyqxmd.com/read/29174541/engineered-multivalent-sensors-to-detect-coexisting-histone-modifications-in-living-stem-cells
#12
Aurore M-F Delachat, Nora Guidotti, Andreas L Bachmann, Antonio C A Meireles-Filho, Horst Pick, Carolin C Lechner, Cédric Deluz, Bart Deplancke, David M Suter, Beat Fierz
The regulation of fundamental processes such as gene expression or cell differentiation involves chromatin states, demarcated by combinatorial histone post-translational modification (PTM) patterns. The subnuclear organization and dynamics of chromatin states is not well understood, as tools for their detection and modulation in live cells are lacking. Here, we report the development of genetically encoded chromatin-sensing multivalent probes, cMAPs, selective for bivalent chromatin, a PTM pattern associated with pluripotency in embryonic stem cells (ESCs)...
November 21, 2017: Cell Chemical Biology
https://www.readbyqxmd.com/read/29170627/combinatorial-in-silico-strategy-towards-identifying-potential-hotspots-during-inhibition-of-structurally-identical-hdac1-and-hdac2-enzymes-for-effective-chemotherapy-against-neurological-disorders
#13
Shabir Ahmad Ganai, Ehsaan Abdullah, Romana Rashid, Mohammad Altaf
Histone deacetylases (HDACs) regulate epigenetic gene expression programs by modulating chromatin architecture and are required for neuronal development. Dysregulation of HDACs and aberrant chromatin acetylation homeostasis have been implicated in various diseases ranging from cancer to neurodegenerative disorders. Histone deacetylase inhibitors (HDACi), the small molecules interfering HDACs have shown enhanced acetylation of the genome and are gaining great attention as potent drugs for treating cancer and neurodegeneration...
2017: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/29160132/active-h3k27me3-demethylation-by-kdm6b-is-required-for-normal-development-of-bovine-preimplantation-embryos
#14
Nhi Chung, Yanina S Bogliotti, Wei Ding, Marcela Vilarino, Kazuki Takahashi, James L Chitwood, Richard M Schultz, Pablo J Ross
The substantial epigenetic remodeling that occurs during early stages of mammalian embryonic development likely contributes to reprogramming the parental genomes from a differentiated to a totipotent state and activation of the embryonic genome. Trimethylation of lysine 27 of histone 3 (H3K27me3) is a repressive mark that undergoes global dynamic changes during preimplantation development of several species. To ascertain the role of H3K27me3 in bovine preimplantation development we perturbed the activity of KDM6B, which demethylates H3K27me3...
November 21, 2017: Epigenetics: Official Journal of the DNA Methylation Society
https://www.readbyqxmd.com/read/29151691/parallel-mrna-proteomics-and-mirna-expression-analysis-in-cell-line-models-of-the-intestine
#15
Finbarr O'Sullivan, Joanne Keenan, Sinead Aherne, Fiona O'Neill, Colin Clarke, Michael Henry, Paula Meleady, Laura Breen, Niall Barron, Martin Clynes, Karina Horgan, Padraig Doolan, Richard Murphy
AIM: To identify miRNA-regulated proteins differentially expressed between Caco2 and HT-29: two principal cell line models of the intestine. METHODS: Exponentially growing Caco-2 and HT-29 cells were harvested and prepared for mRNA, miRNA and proteomic profiling. mRNA microarray profiling analysis was carried out using the Affymetrix GeneChip Human Gene 1.0 ST array. miRNA microarray profiling analysis was carried out using the Affymetrix Genechip miRNA 3.0 array...
November 7, 2017: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/29146205/pax3-foxo1-zooming-in-on-an-undruggable-target
#16
REVIEW
Marco Wachtel, Beat W Schäfer
Driver oncogenes are prime targets for therapy in tumors many of which, including leukemias and sarcomas, express recurrent fusion transcription factors. One specific example for such a cancer type is alveolar rhabdomyosarcoma, which is associated in the majority of cases with the fusion protein PAX3-FOXO1. Since fusion transcription factors are challenging targets for development of small molecule inhibitors, indirect inhibitory strategies for this type of oncogenes represent a more promising approach. One can envision strategies at different molecular levels including upstream modifiers and activators, epigenetic and transcriptional co-regulators, and downstream effector targets...
November 13, 2017: Seminars in Cancer Biology
https://www.readbyqxmd.com/read/29145444/inhibition-of-the-h3k9-methyltransferase-g9a-attenuates-oncogenicity-and-activates-the-hypoxia-signaling-pathway
#17
Jolene Caifeng Ho, Lissa Nurrul Abdullah, Qing You Pang, Sudhakar Jha, Edward Kai-Hua Chow, Henry Yang, Hiroyuki Kato, Lorenz Poellinger, Jun Ueda, Kian Leong Lee
Epigenetic mechanisms play important roles in the regulation of tumorigenesis, and hypoxia-induced epigenetic changes may be critical for the adaptation of cancer cells to the hypoxic microenvironment of solid tumors. Previously, we showed that loss-of-function of the hypoxia-regulated H3K9 methyltransferase G9A attenuates tumor growth. However, the mechanisms by which blockade of G9A leads to a tumor suppressive effect remain poorly understood. We show that G9A is highly expressed in breast cancer and is associated with poor patient prognosis, where it may function as a potent oncogenic driver...
2017: PloS One
https://www.readbyqxmd.com/read/29133140/the-histone-methyltransferase-g9a-a-new-therapeutic-target-in-biliary-tract-cancer
#18
Christian Mayr, Katharina Helm, Martin Jakab, Markus Ritter, Rajeev Shrestha, Ramesh Makaju, Andrej Wagner, Martin Pichler, Marlena Beyreis, Stefan Staettner, Tarkan Jaeger, Eckhard Klieser, Tobias Kiesslich, Daniel Neureiter
The histone methyltransferase G9a (EHMT2) is a key enzyme for dimethylation of lysine 9 at histone 3 (H3K9me2), a suppressive epigenetic mark. G9a is over-expressed in tumour cells and contributes to cancer aggressiveness. Biliary tract cancer (BTC) is a rare cancer with dismal prognosis due to a lack of effective therapies. Currently, there are no data on the role of G9a in BTC carcinogenesis. We analysed G9a expression in n=68 BTC patient specimens and correlated the data with clinico-pathological and survival data...
November 10, 2017: Human Pathology
https://www.readbyqxmd.com/read/29106445/a-potent-hydroxamic-acid-based-small-molecule-inhibitor-a452-preferentially-inhibits-hdac6-activity-and-induces-cytotoxicity-toward-cancer-cells-irrespective-of-p53-status
#19
Hyun-Wook Ryu, Dong-Hee Shin, Dong Hoon Lee, Hye-Rim Won, So Hee Kwon
HDAC6-selective inhibitors are novel epigenetic anticancer agents. However, their precise mechanisms of action are incompletely understood. We investigated the anticancer mechanisms of the novel potent and selective HDAC6 inhibitor A452 compared with current clinically tested HDAC6 inhibitor ACY-1215. We demonstrate that A452 effectively inhibits the cell growth and viability of various cancer cell types, irrespective of p53 status. A452 induced apoptosis as evidenced by activated caspase 3 and PARP, increased Bak and Bax, and decreased Bcl-xL...
November 2, 2017: Carcinogenesis
https://www.readbyqxmd.com/read/29101267/identification-and-verification-of-potential-pirnas-from-domesticated-yak-testis
#20
Jishang Gong, Quanwei Zhang, Qi Wang, Youji Ma, Jiaxiang Du, Yong Zhang, Xingxu Zhao
PIWI-interacting RNAs (piRNA) are small non-coding RNA molecules expressed in animal germ cells that interact with PIWI family proteins to form RNA- protein complexes involved in epigenetic and post- transcriptional gene silencing of retrotransposons and other genetic elements in germ line cells, including reproductive stem cell self- sustainment, differentiation, meiosis and spermatogenesis. In the present study, weperformed high- throughput sequencing of piRNAs in testis samples from yaks in different stages of sexual maturity...
November 3, 2017: Reproduction: the Official Journal of the Society for the Study of Fertility
keyword
keyword
27390
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"