May 2024
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2 Reads
SLAS DISCOVERY Advancing the Science of Drug Discovery
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Publications (5)
April 2024
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6 Reads
SLAS DISCOVERY Advancing the Science of Drug Discovery
December 2023
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46 Reads
SLAS DISCOVERY Advancing the Science of Drug Discovery
February 2022
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44 Reads
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21 Citations
Journal of Medicinal Chemistry
October 2021
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36 Reads
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16 Citations
Drug Discovery Today
Dysregulation of the epigenome is associated with the onset and progression of several diseases, including cancer, autoimmune, cardiovascular, and neurological disorders. Members from the three families of epigenetic proteins (readers, writers, and erasers) have been shown to be druggable using small-molecule inhibitors. Increasing knowledge of the role of epigenetics in disease and the reversibility of these modifications explain why pharmacological intervention is an attractive strategy for tackling epigenetic-based disease. In this review, we provide an overview of epigenetics drug targets, focus on approaches used for initial hit identification, and describe the subsequent role of structure-guided chemistry optimisation of initial hits to clinical candidates. We also highlight current challenges and future potential for epigenetics-based therapies.
Citations (2)
... [5] The importance of nitrogen heterocycles has meant that synthetic routes making these accessible by simple means have attracted widespread attention. [6] Purine bioisosteres, such as 1,2,4-triazolo- [4,3-a]pyrazine, have demonstrated clinical applications in blood pressure medication, [7] anti-cancer, [8][9][10] anti-malarial, [11] anti-viral, [12] and anti-microbial [13,14] drugs and as A 2a adenosine receptor (AR) specific antagonists. [15,16] A 2a AR is one of the 4 types of adenosine receptors (A 1 , A 2a , A 2b , A 3 ) and has garnered attention for drug design. ...
- Citing Article
February 2022
Journal of Medicinal Chemistry
... In the field of the discovery of epigenetic target inhibitors, in silico methods are utilized as an indispensable tool and constitute the current research hotspot [17]. The crystal structures of human DNMT enzymes have created new perspectives to build up potent in silico screening approaches to reveal novel specific epigenetic inhibitors [18]. ...
- Citing Article
October 2021
Drug Discovery Today