Universität zu Köln

Becker, Christian, Oecal, Sinan, Nguyen, Hoang D., Keul, Marina, Simard, Jeffrey R. and Rauh, Daniel ORCID: 0000-0002-1970-7642 (2016). Monitoring Conformational Changes in the Receptor Tyrosine Kinase EGFR. ChemBioChem, 17 (11). S. 990 - 995. WEINHEIM: WILEY-V C H VERLAG GMBH. ISSN 1439-7633

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Abstract

The receptor tyrosine kinase EGFR is regulated by complex conformational changes, and this conformational control is disturbed in certain types of cancer. Many ligands are known to bind EGFR in its active conformation, thereby preventing ATP from binding. Only a few ligands are known to stabilize EGFR in its inactive conformation, thus providing novel strategies for perturbing EGFR activity. We report a direct binding assay that enables the identification of novel ligands that bind to and stabilize the inactive conformation of EGFR.

Item Type:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Becker, Christian UNSPECIFIED UNSPECIFIED UNSPECIFIED Oecal, Sinan UNSPECIFIED UNSPECIFIED UNSPECIFIED Nguyen, Hoang D. UNSPECIFIED UNSPECIFIED UNSPECIFIED Keul, Marina UNSPECIFIED UNSPECIFIED UNSPECIFIED Simard, Jeffrey R. UNSPECIFIED UNSPECIFIED UNSPECIFIED Rauh, Daniel UNSPECIFIED orcid.org/0000-0002-1970-7642 UNSPECIFIED
URN:	urn:nbn:de:hbz:38-272526
DOI:	10.1002/cbic.201600115
Journal or Publication Title:	ChemBioChem
Volume:	17
Number:	11
Page Range:	S. 990 - 995
Date:	2016
Publisher:	WILEY-V C H VERLAG GMBH
Place of Publication:	WEINHEIM
ISSN:	1439-7633
Language:	English
Faculty:	Unspecified
Divisions:	Unspecified
Subjects:	no entry
Uncontrolled Keywords:	Keywords Language GROWTH-FACTOR RECEPTOR; CELL LUNG-CANCER; INHIBITOR SELECTIVITY; DRUG-RESISTANCE; MUTATIONS; GEFITINIB; DOMAIN; ERLOTINIB; AZD9291; ACTIVATION Multiple languages Biochemistry & Molecular Biology; Chemistry, Medicinal Multiple languages
Refereed:	Yes
URI:	http://kups.ub.uni-koeln.de/id/eprint/27252