Photoaffinity labeling in target- and binding-site identification
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Smith, E., Collins, I.
(2015)
Photoaffinity labeling in target- and binding-site identification.
FUTURE MEDICINAL CHEMISTRY, 7 (2).
pp. 159-183.
ISSN 1756-8919
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Abstract
Photoaffinity labeling (PAL) using a chemical probe to covalently bind its target in response to activation by light has become a frequently used tool in drug discovery for identifying new drug targets and molecular interactions, and for probing the location and structure of binding sites. Methods to identify the specific target proteins of hit molecules from phenotypic screens are highly valuable in early drug discovery. In this review, we summarize the principles of PAL including probe design and experimental techniques for in vitro and live cell investigations. We emphasize the need to optimize and validate probes and highlight examples of the successful application of PAL across multiple disease areas.
| Item Type: | Review Article |
|---|---|
| Authors (ICR Faculty only): | Collins, Ian |
| All Authors: | Smith, E., Collins, I. |
| Additional Information: | ISI Document Delivery No.: CT5YY Times Cited: 1 Cited Reference Count: 81 Smith, Ewan Collins, Ian Wellcome Trust; Institute of Cancer Research The authors acknowledge financial support for this work from the Wellcome Trust (studentship to ES) and The Institute of Cancer Research. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed. 1 2 3 Future sci ltd London 1756-8927 |
| Uncontrolled Keywords: | nicotinic acetylcholine-receptor cell-adhesion molecule-1 drug discovery cotranslational translocation lysine acetyltransferases friedreichs-ataxia mass-spectrometry chemical probes inhibitor proteins Pharmacology & Pharmacy |
| Research teams: | ICR divisions > Cancer Therapeutics > Medicinal Chemistry 2 |
| Depositing User: | Franziska Noessig |
| Date Deposited: | 09 Nov 2015 16:08 |
| Last Modified: | 11 Nov 2015 10:42 |
| URI: | http://publications.icr.ac.uk/id/eprint/14511 |
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