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Chapter 4: Pyrrolobenzodiazepines as Transcription Factor Inhibitors: An Overview

Research output: Chapter in Book/Report/Conference proceedingChapter

Original languageEnglish
Title of host publicationTherapies for Retinal Degeneration
Subtitle of host publicationTargeting Common Processes
PublisherRoyal Society of Chemistry
Pages81-124
Number of pages44
Edition65
DOIs
StatePublished - 1 Jan 2019

Publication series

NameRSC Drug Discovery Series
Number65
Volume2019-January
ISSN (Print)2041-3203
ISSN (Electronic)2041-3211

King's Authors

Abstract

Since their discovery in Streptomyces bacteria over half a century ago, pyrrolobenzodiazepines (PBDs) have generated significant interest as potential chemotherapeutic agents due to their sequence-selective DNA alkylating capacity. The development of synthetic PBD compounds from their naturally derived bacterial counterparts has enhanced both the potency and safety profiles of PBDs. Interestingly, such modifications of traditional PBD cores have sometimes led to an expansion of the mechanism of action of these compounds from simple DNA alkylation. This review documents one such change in mechanism of action of the PBDs, which has been engineered through chemical modifications of traditional PBD structures: the inhibition of transcription factor activity.

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