1 min read

ID: 804412

Short Link: https://gregory-ms.com/articles/804412/

Discovery Date: 01 August 2022, 23:41:14 UTC

Published Date: 2022-07-31 23:00:00

Source: BioMedCentral

Link: https://clinicalepigeneticsjournal.biomedcentral.com/articles/10.1186/s13148-022-01305-8

Manual Selection: true

Machine Learning Gaussian Naive Bayes Model: false

Abstract

jats:titleAbstract</jats:title>jats:pHistone 3 lysine 27 (H3K27) demethylation constitutes an important epigenetic mechanism of gene activation. It is mediated by the Jumonji C domain-containing lysine demethylases KDM6A and KDM6B, both of which have been implicated in a wide myriad of diseases, including blood and solid tumours, autoimmune and inflammatory disorders, and infectious diseases. Here, we review and summarise the pre-clinical evidence, both in vitro and in vivo, in support of the therapeutic potential of inhibiting H3K27-targeting demethylases, with a focus on the small-molecule inhibitor GSK-J4. In malignancies, KDM6A/B inhibition possesses the ability to inhibit proliferation, induce apoptosis, promote differentiation, and heighten sensitivity to currently employed chemotherapeutics. KDM6A/B inhibition also comprises a potent anti-inflammatory approach in inflammatory and autoimmune disorders associated with inappropriately exuberant inflammatory and autoimmune responses, restoring immunological homeostasis to inflamed tissues. With respect to infectious diseases, KDM6A/B inhibition can suppress the growth of infectious pathogens and attenuate the immunopathology precipitated by these pathogens. The pre-clinical in vitro and in vivo data, summarised in this review, suggest that inhibiting H3K27 demethylases holds immense therapeutic potential in many diseases.</jats:p>

Noun Phrases in Title

  • Therapeutic potential
  • histone
  • 3 lysine 27 demethylases
  • a review
  • the literature
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