Selective Fragments for the CREBBP Bromodomain Identified from an Encoded Self‐assembly Chemical Library
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Date
2020-09-16
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Journal Article
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Abstract
DNA‐encoded chemical libraries (DECLs) are collections of chemical moieties individually coupled to distinctive DNA barcodes. Compounds can be displayed either at the end of a single DNA strand (i. e., single‐pharmacophore libraries) or at the extremities of two complementary DNA strands (i. e., dual‐pharmacophore libraries). In this work, we describe the use of a dual‐pharmacophore encoded self‐assembly chemical (ESAC) library for the affinity maturation of a known 4,5‐dihydrobenzodiazepinone ring (THBD) acetyl‐lysine (KAc) mimic for the cyclic‐AMP response element binding protein (CREB) binding protein (CREBBP or CBP) bromodomain. The new pair of fragments discovered from library selection showed a sub‐micromolar affinity for the CREBBP bromodomain in fluorescence polarization and ELISA assays, and selectivity against BRD4(1). © 2020 Wiley-VCH GmbH.
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published
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Journal / series
Volume
15 (18)
Pages / Article No.
1752 - 1756
Publisher
Wiley
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Date collected
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Subject
CREBBP bromodomain; DNA-encoded chemical library; Encoded self-assembly chemical library; Inhibitors; Medicinal chemistry
Organisational unit
03463 - Neri, Dario (ehemalig) / Neri, Dario (former)
08641 - Scheuermann, Jörg (Tit.-Prof.) / Scheuermann, Jörg (Tit.-Prof.)
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Funding
182003 - Understanding and Exploiting the Molecular Targeting of Tumor Neo-vasculature (SNF)
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