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Epigenetic drugs- from chemistry via biology to medicine and back

Edited by: Professor Lucia Altucci & Professor Marianne Rots

The last decade has seen a growing awareness of epigenetic deregulations underlying cancer and many other diseases. This awareness is paralleled by intensive research activities to identify inhibitors for epigenetic writers and erasers (and even readers) associated with such epigenetic dysregulations. In this review series, we provide insights into the current status of the early epigenetic drugs, while also addressing upcoming new classes of drugs. 

All new therapeutic targets face challenges when tested in biological systems, but for epigenetic enzymes this is even more complex. Altogether, various aspects of genome-wide acting epigenetic enzyme modulators require more in depth investigations to fully fulfil the promise of clinically reversing epigenetic mutations. Despite such awareness, the current epi-drug era has opened novel therapeutic avenues for various diseases beyond cancer.

The work in this series was supported by the COST action CM1406- Epigenetic Chemical Biology.  

Collection published: 23 May 2016 

  1. Ageing is the main risk factor for human neurological disorders. Among the diverse molecular pathways that govern ageing, epigenetics can guide age-associated decline in part by regulating gene expression and ...

    Authors: Raúl Delgado-Morales, Roberto Carlos Agís-Balboa, Manel Esteller and María Berdasco
    Citation: Clinical Epigenetics 2017 9:67
  2. Multiple myeloma (MM) is a hematological malignancy, which remains incurable because most patients eventually relapse or become refractory to current treatments. Due to heterogeneity within the cancer cell mic...

    Authors: Mark E. Issa, Farnaz Sedigheh Takhsha, Chandra Sekhar Chirumamilla, Claudina Perez-Novo, Wim Vanden Berghe and Muriel Cuendet
    Citation: Clinical Epigenetics 2017 9:17
  3. A myriad of diseases is caused or characterized by alteration of epigenetic patterns, including changes in DNA methylation, post-translational histone modifications, or chromatin structure. These changes of th...

    Authors: René A. M. Dirks, Hendrik G. Stunnenberg and Hendrik Marks
    Citation: Clinical Epigenetics 2016 8:122
  4. In the presence of different environmental cues that are able to trigger specific responses, a given genotype has the ability to originate a variety of different phenotypes. This property is defined as plastic...

    Authors: T. A. L. Brevini, G. Pennarossa, E. F. M. Manzoni, C. E. Gandolfi, A. Zenobi and F. Gandolfi
    Citation: Clinical Epigenetics 2016 8:119
  5. SETD8/SET8/Pr-SET7/KMT5A is the only known lysine methyltransferase (KMT) that monomethylates lysine 20 of histone H4 (H4K20) in vivo. Lysine residues of non-histone proteins including proliferating cell nucle...

    Authors: Ciro Milite, Alessandra Feoli, Monica Viviano, Donatella Rescigno, Agostino Cianciulli, Amodio Luca Balzano, Antonello Mai, Sabrina Castellano and Gianluca Sbardella
    Citation: Clinical Epigenetics 2016 8:102
  6. Prostate cancer is one of the most common non-cutaneous malignancies among men worldwide. Epigenetic aberrations, including changes in DNA methylation patterns and/or histone modifications, are key drivers of ...

    Authors: Inês Graça, Eva Pereira-Silva, Rui Henrique, Graham Packham, Simon J. Crabb and Carmen Jerónimo
    Citation: Clinical Epigenetics 2016 8:98
  7. The azanucleosides azacitidine and decitabine are currently used for the treatment of acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS) in patients not only eligible for intensive chemotherapy b...

    Authors: Jeannine Diesch, Anabel Zwick, Anne-Kathrin Garz, Anna Palau, Marcus Buschbeck and Katharina S. Götze
    Citation: Clinical Epigenetics 2016 8:71
  8. When assembled in multiprotein polycomb repressive complexes (PRCs), highly evolutionary conserved polycomb group (PcG) proteins epigenetically control gene activity. Although the composition of PRCs may vary ...

    Authors: Koraljka Gall Trošelj, Renata Novak Kujundzic and Djurdjica Ugarkovic
    Citation: Clinical Epigenetics 2016 8:55
  9. Sirtuins are NAD+-dependent histone deacetylases regulating important metabolic pathways in prokaryotes and eukaryotes and are involved in many biological processes such as cell survival, senescence, proliferatio...

    Authors: Vincenzo Carafa, Dante Rotili, Mariantonietta Forgione, Francesca Cuomo, Enrica Serretiello, Gebremedhin Solomon Hailu, Elina Jarho, Maija Lahtela-Kakkonen, Antonello Mai and Lucia Altucci
    Citation: Clinical Epigenetics 2016 8:61