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Fragment‐Based Drug Discovery in the Bromodomain and Extra‐Terminal Domain Family
Author(s) -
Radwan Mostafa,
Serya Rabah
Publication year - 2017
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201700147
Subject(s) - bromodomain , drug discovery , computational biology , drug , brd4 , bet inhibitor , pharmacology , medicine , bioinformatics , biology , epigenetics , biochemistry , gene
Bromodomain and extra‐terminal domain (BET) inhibition has emerged recently as a potential therapeutic target for the treatment of many human disorders such as atherosclerosis, inflammatory disorders, chronic obstructive pulmonary disease (COPD), some viral infections, and cancer. Since the discovery of the two potent inhibitors, I‐BET762 and JQ1, different research groups have used different techniques to develop novel potent and selective inhibitors. In this review, we will be concerned with the trials that used fragment‐based drug discovery (FBDD) approaches to discover or optimize BET inhibitors, also showing fragments that can be further optimized in future projects to reach novel potent BET inhibitors.