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Article

Protein kinase inhibitor design by targeting the Asp-Phe-Gly (DFG) motif: the role of the DFG motif in the design of epidermal growth factor receptor inhibitors.

Journal of medicinal chemistry - 23 May 2013

Peng Yi-Hui, Shiao Hui-Yi, Tu Chih-Hsiang, Liu Pang-Min, Hsu John Tsu-An, Amancha Prashanth Kumar, Wu Jian-Sung, Coumar Mohane Selvaraj, Chen Chun-Hwa, Wang Sing-Yi, Lin Wen-Hsing, Sun Hsu-Yi, Chao Yu-Sheng, Lyu Ping-Chiang, Hsieh Hsing-Pang, Wu Su-Ying

Abstract excerpt

The Asp-Phe-Gly (DFG) motif plays an important role in the regulation of kinase activity. Structure-based drug design was performed to design compounds able to interact with the DFG motif; epidermal growth factor receptor (EGFR) was selected as an example. Structural insights obtained from the EGFR/2a complex suggested that an extension from the meta-position on the phenyl group (ring-5) would improve...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Identifiers

PMID: 23611691
DOI: 10.1021/jm400072p

Genes

EGFR

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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