Article ; Online: Selectively targeting individual bromodomain: Drug discovery and molecular mechanisms.
2021 Volume 172, Page(s) 105804
Abstract: Bromodomain-containing proteins include bromodomain and extra-terminal (BET) and non-BET families. Due to the conserved bromodomain (BD) module between BD-containing proteins, and especially BETs with each member having two BDs (BD1 and BD2), the high ... ...
Abstract | Bromodomain-containing proteins include bromodomain and extra-terminal (BET) and non-BET families. Due to the conserved bromodomain (BD) module between BD-containing proteins, and especially BETs with each member having two BDs (BD1 and BD2), the high degree of structural similarity makes BD-selective inhibitors much difficult to be designed. However, increasing evidences emphasized that individual BDs had distinct functions and different cellular phenotypes after pharmacological inhibition, and selectively targeting one of the BDs could result in a different efficacy and tolerability profile. This review is to summarize the pioneering progress of BD-selective inhibitors targeting BET and non-BET proteins, focusing on their structural features, biological activity, therapeutic application and experimental/theoretical mechanisms. The present proteolysis targeting chimeras (PROTAC) degraders targeting BDs, and clinical status of BD-selective inhibitors were also analyzed, providing a new insight into future direction of bromodomain-selective drug discovery. |
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MeSH term(s) | Animals ; Drug Discovery ; Humans ; Peptides/pharmacology ; Protein Domains ; Proteins/antagonists & inhibitors ; Proteins/chemistry |
Chemical Substances | Peptides ; Proteins ; bromodomain and extra-terminal domain protein, human |
Language | English |
Publishing date | 2021-08-25 |
Publishing country | Netherlands |
Document type | Journal Article ; Research Support, Non-U.S. Gov't ; Review |
ZDB-ID | 1003347-6 |
ISSN | 1096-1186 ; 0031-6989 ; 1043-6618 |
ISSN (online) | 1096-1186 |
ISSN | 0031-6989 ; 1043-6618 |
DOI | 10.1016/j.phrs.2021.105804 |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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