Target validation: switching domains

Alessio Ciulli

doi:10.1038/nchembio.2154

Target validation: switching domains

Alessio Ciulli (Lead / Corresponding author)

Biological Chemistry and Drug Discovery

Research output: Contribution to journal › Short survey › peer-review

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Abstract

Chemical probes and drugs often bind to functional domains on disease-relevant proteins. A study suggests a chemical genetic approach to establish on-target effects by swapping the targeted domain, affording resistance to pharmacological inhibition while retaining functionality.

Original language	English
Pages (from-to)	659-660
Number of pages	2
Journal	Nature Chemical Biology
Volume	12
Issue number	9
Early online date	18 Aug 2016
DOIs	https://doi.org/10.1038/nchembio.2154
Publication status	Published - Sep 2016

Keywords

Cancer therapy
Chemical genetics
Small molecules
Target validation
Transcription

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1038/nchembio.2154

Author Accepted ManuscriptAccepted author manuscript, 173 KB

2 Finished

Dissecting and Exploiting Molecular Recognition at Protein-Protein Interfaces (David Phillips Fellowship)
Ciulli, A.
Biotechnology and Biological Sciences Research Council
8/04/13 → 7/07/15
Project: Research
A Systems Approach for the Fragment-based Development of Selective Chemical Probes of Bromodomain Function (joint with University of Oxford)
Ciulli, A.
Biotechnology and Biological Sciences Research Council
8/04/13 → 7/06/15
Project: Research

Cite this

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title = "Target validation: switching domains",

abstract = "Chemical probes and drugs often bind to functional domains on disease-relevant proteins. A study suggests a chemical genetic approach to establish on-target effects by swapping the targeted domain, affording resistance to pharmacological inhibition while retaining functionality.",

keywords = "Cancer therapy, Chemical genetics, Small molecules, Target validation, Transcription",

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AB - Chemical probes and drugs often bind to functional domains on disease-relevant proteins. A study suggests a chemical genetic approach to establish on-target effects by swapping the targeted domain, affording resistance to pharmacological inhibition while retaining functionality.

KW - Cancer therapy

KW - Chemical genetics

KW - Small molecules

KW - Target validation

KW - Transcription

U2 - 10.1038/nchembio.2154

DO - 10.1038/nchembio.2154

M3 - Short survey

C2 - 27538023

VL - 12

SP - 659

EP - 660

JO - Nature Chemical Biology

JF - Nature Chemical Biology

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Target validation: switching domains

Abstract

Keywords

UN SDGs

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Projects

Dissecting and Exploiting Molecular Recognition at Protein-Protein Interfaces (David Phillips Fellowship)

A Systems Approach for the Fragment-based Development of Selective Chemical Probes of Bromodomain Function (joint with University of Oxford)

Cite this