6N3N

Identification of novel, potent and selective GCN2 inhibitors as first-in-class anti-tumor agents

Summary for 6N3N

• Entry DOI: 10.2210/pdb6n3n/pdb
• Descriptor: eIF-2-alpha kinase GCN2,eIF-2-alpha kinase GCN2, N-{3-[(2-aminopyrimidin-5-yl)ethynyl]-2,4-difluorophenyl}-2,5-dichloro-3-(hydroxymethyl)benzene-1-sulfonamide (2 entities in total)
• Functional Keywords: gcn2, kinase, inhibitor, anti-tumor, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (Human); More
• Total number of polymer chains: 1
• Total formula weight: 36697.06

Authors

Hoffman, I.D.,Fujimoto, J.,Kurasawa, O.,Takagi, T.,Klein, M.G.,Kefala, G.,Ding, S.C.,Cary, D.R.,Mizojiri, R. (deposition date: 2018-11-15, release date: 2019-10-09, Last modification date: 2024-03-13)

• Primary citation: Fujimoto, J.,Kurasawa, O.,Takagi, T.,Liu, X.,Banno, H.,Kojima, T.,Asano, Y.,Nakamura, A.,Nambu, T.,Hata, A.,Ishii, T.,Sameshima, T.,Debori, Y.,Miyamoto, M.,Klein, M.G.,Tjhen, R.,Sang, B.C.,Levin, I.,Lane, S.W.,Snell, G.P.,Li, K.,Kefala, G.,Hoffman, I.D.,Ding, S.C.,Cary, D.R.,Mizojiri, R.; Identification of Novel, Potent, and Orally Available GCN2 Inhibitors with Type I Half Binding Mode.; Acs Med.Chem.Lett., 10:1498-1503, 2019; PubMed: 31620240; DOI: 10.1021/acsmedchemlett.9b00400

Experimental method

X-RAY DIFFRACTION (3.01 Å)