Results 51 to 60 of about 6,513 (167)

Epigenetic polypharmacology: from combination therapy to multitargeted drugs [PDF]

, 2016
The modern drug discovery process has largely focused its attention in the so-called magic bullets, single chemical entities that exhibit high selectivity and potency for a particular target.
A Anighoro, A Dey, A Ganesan, A Mai, A Nudelman, AF Fliri, B Al-Lazikani, B Knoechel, B Meunier, BC Smith, BC Smith, BC Smith, BE Gryder, C Choudhary, C Corminboeuf, C Liu, C Qian, C Tang, C Yu, C Zwergel, C-W Chen, CM Fillmore, CM Grozinger, CY Fong, D Bixby, D Gallenkamp, D Matei, D Passarella, D Rotili, D Sharma, DA Mele, E Bicaku, E Borretto, E Nicodeme, F Sun, F-W Peng, G Zhang, G-L Chen, GE Winter, GL Verdine, H Patel, HS Bandukwala, HS Takhar, J Fischer, J Lu, J Schneider, J Zhao, J Zuber, J-B Chen, J-F Couture, J-PJ Issa, JC Culhane, JL Avalos, JM Burg, JS Kirk, K Agger, K Chen, K K-p, K Pruitt, K Zhao, KB Daniel, KT Thurn, L Chen, L Chen, LK Gediya, M Buchwald, M De los Santos, M Yang, M Zuo, MA Dawson, MA Dawson, MA Park, MB Poulin, MC Chen, MJ Keiser, MM Singh, MS Finnin, N Geva-Zatorsky, OW Rokhlin, P Anand, P Bamborough, P Filippakopoulos, P Hu, P Hu, P Jones, P Rathert, PA Marks, PK Mazur, PN Munster, Q Wang, R Anand, R Morphy, R Morphy, R Nimmanapalli, R Pereira, R Pili, R Álvarez, RA Copeland, RA Juergens, RL Momparler, S Daujat, S Klimasauskas, S Mahboobi, S Mahboobi, S Zhao, SC Hodawadekar, SJ Atkinson, SS Ng, T Beckers, T Finkel, T Kokkola, T Qiu, T Vaissiere, T-G Lee, TH Luu, TJ Galloway, TM Pitts, W Guerrant, WF Hawse, X Cai, X Cheng, X Sun, X Zhang, Y Ling, Y Zhang, Z Chen   +125 more
core   +1 more source

A potential common role of the Jumonji C domain‑containing 1A histone demethylase and chromatin remodeler ATRX in promoting colon cancer

Oncology Letters, 2018
Jumonji C domain-containing 1A (JMJD1A) is a histone demethylase and epigenetic regulator that has been implicated in cancer development. In the current study, its mRNA and protein expression was analyzed in human colorectal tumors. It was demonstrated that JMJD1A levels were increased and correlated with a more aggressive phenotype.
Li, Xiaomeng, Oh, Sangphil, Song, Hoogeun, Shin, Sook, Zhang, Bin, Freeman, Willard M., Janknecht, Ralf   +6 more
openaire   +3 more sources

Role of enhancer of zeste homolog 2 polycomb protein and its significance in tumor progression and cell differentiation [PDF]

, 2013
Epigenetics is a branch of genetics that focuses on the heritable changes of DNA or associated proteins, other than DNA sequence variations, which carry information content during cell division [1,2].
Bagella, Luigi Marco, Marchesi, Irene
core   +2 more sources

Histone Lysine Demethylase JMJD2D/KDM4D and Family Members Mediate Effects of Chronic Social Defeat Stress on Mouse Hippocampal Neurogenesis and Mood Disorders

Brain Sciences, 2020
Depression, anxiety and related mood disorders are major psychiatric illnesses worldwide, and chronic stress appears to be one of the primary underlying causes.
Swati Maitra, Nitin Khandelwal, Scherazad Kootar, Pooja Sant, Salil S. Pathak, Sujatha Reddy, Annapoorna P. K., Upadhyayula Suryanarayana Murty, Sumana Chakravarty, Arvind Kumar   +9 more
doaj   +1 more source

A New Family of Jumonji C Domain-Containing KDM Inhibitors Inspired by Natural Product Purpurogallin

Frontiers in Chemistry, 2020
Aberrant epigenetic modifications are involved in cancer development. Jumonji C domain-containing histone lysine demethylases (KDMs) are found mainly up-regulated in breast, prostate, and colon cancer.
José A. Souto, Federica Sarno, Angela Nebbioso, Chiara Papulino, Rosana Álvarez, Jessica Lombino, Ugo Perricone, Alessandro Padova, Lucia Altucci, Ángel R. de Lera   +9 more
doaj   +1 more source

Functional Crosstalk between Lysine Methyltransferases on Histone Substrates: The Case of G9A/GLP and Polycomb Repressive Complex 2 [PDF]

, 2015
Significance: Methylation of histone H3 on lysine 9 and 27 (H3K9 and H3K27) are two epigenetic modifications that have been linked to several crucial biological processes, among which are transcriptional silencing and cell differentiation.
Ait Si Ali, Slimane, Mozzetta, Chiara, Pontis, Julien   +2 more
core   +2 more sources

Identification of MEF2A, MEF2C, and MEF2D interactomes in basal and Fsk‐stimulated mouse MA‐10 Leydig cells

Andrology, EarlyView.
Abstract Background Myocyte enhancer factor 2 transcription factors regulate essential transcriptional programs in various cell types. The activity of myocyte enhancer factor 2 factors is modulated through interactions with cofactors, chromatin remodelers, and other regulatory proteins, which are dependent on cell context and physiological state.
Karine de Mattos, Marie‐Pier Scott‐Boyer, Arnaud Droit, Robert S. Viger, Jacques J. Tremblay   +4 more
wiley   +1 more source

Multi-dimensional histone methylations for coordinated regulation of gene expression under hypoxia [PDF]

, 2017
Hypoxia increases both active and repressive histone methylation levels via decreased activity of histone demethylases. However, how such increases coordinately regulate induction or repression of hypoxia-responsive genes is largely unknown.
Chae, Sehyun, Hwang, Daehee, Lee, Ho-Youl, Lee, Jieon, Lee, Seongyeol, Moon, Yunwon, Park, Bongju, Park, Hyunsung, Yang, Eun Gyeong   +8 more
core   +2 more sources

Selective small molecule targeting of KDM4 as a therapeutic strategy to reduce proliferation of acute myeloid leukaemia

British Journal of Haematology, EarlyView.
Summary Acute myeloid leukaemia (AML) is an aggressive disease with poor survival and high relapse rates. Coupled with the complex mutational burden observed, there is an unmet clinical need for more targeted therapies. Epigenetic therapies have shown promise both as monotherapy and in combination strategies and specifically histone lysine demethylase,
Laura Monaghan, Roderick P. Bunschoten, Joana Bittencourt‐Silvestre, Taeju Park, Susan Gannon, Petrisor Alin Pirvan, Alex Hoose, Helen Wheadon, Robert M. J. Liskamp, Xu Huang, Heather G. Jørgensen   +10 more
wiley   +1 more source

Vitamin D and the Epigenome

Frontiers in Physiology, 2014
Epigenetic mechanisms play a crucial role in regulating gene expression. The main mechanisms involve methylation of DNA and covalent modifications of histones by methylation, acetylation, phosphorylation, or ubiquitination.
Irfete S. Fetahu, Julia eHöbaus, Enikö eKallay   +2 more
doaj   +1 more source