2ZM3

Complex Structure of Insulin-like Growth Factor Receptor and Isoquinolinedione Inhibitor

Summary for 2ZM3

• Entry DOI: 10.2210/pdb2zm3/pdb
• Related: 1JQH
• Descriptor: Insulin-like growth factor 1 receptor, (4Z)-6-bromo-4-({[4-(pyrrolidin-1-ylmethyl)phenyl]amino}methylidene)isoquinoline-1,3(2H,4H)-dione (3 entities in total)
• Functional Keywords: igfr, protein-inhibitor complex, tyrosine kinase, atp-binding, cleavage on pair of basic residues, disease mutation, glycoprotein, membrane, nucleotide-binding, phosphoprotein, polymorphism, receptor, transferase, transmembrane, tyrosine-protein kinase
• Biological source: Homo sapiens (Human)
• Cellular location: Membrane; Single-pass type I membrane protein: P08069
• Total number of polymer chains: 4
• Total formula weight: 143073.80

Authors

Xu, W.,Mayer, S.C.,Boschelli, F.,Johnson, M.,Dwyer, B. (deposition date: 2008-04-10, release date: 2008-06-10, Last modification date: 2023-11-15)

• Primary citation: Mayer, S.C.,Banker, A.L.,Boschelli, F.,Di, L.,Johnson, M.,Kenny, C.H.,Krishnamurthy, G.,Kutterer, K.,Moy, F.,Petusky, S.,Ravi, M.,Tkach, D.,Tsou, H.R.,Xu, W.; Lead identification to generate isoquinolinedione inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment; Bioorg.Med.Chem.Lett., 18:3641-3645, 2008; PubMed: 18501599; DOI: 10.1016/j.bmcl.2008.04.044

Experimental method

X-RAY DIFFRACTION (2.5 Å)