2Z8C

Phosphorylated insulin receptor tyrosine kinase in complex with (4-{[5-carbamoyl-4-(3-methylanilino)pyrimidin-2-yl]amino}phenyl)acetic acid

Summary for 2Z8C

• Entry DOI: 10.2210/pdb2z8c/pdb
• Related: 2Z7L
• Descriptor: Insulin receptor, 6-mer peptide from Insulin receptor substrate 1, [4-({5-(AMINOCARBONYL)-4-[(3-METHYLPHENYL)AMINO]PYRIMIDIN-2-YL}AMINO)PHENYL]ACETIC ACID (3 entities in total)
• Functional Keywords: transferase, alternative splicing, atp-binding, carbohydrate metabolism, cleavage on pair of basic residues, diabetes mellitus, disease mutation, glycoprotein, kinase, membrane, nucleotide-binding, phosphorylation, polymorphism, receptor, transmembrane, tyrosine-protein kinase, transducer
• Biological source: Homo sapiens (Human); More
• Cellular location: Cell membrane; Single-pass type I membrane protein: P06213
• Total number of polymer chains: 2
• Total formula weight: 35826.57

Authors

Katayama, N.,Kurihara, H. (deposition date: 2007-09-05, release date: 2008-08-12, Last modification date: 2024-11-20)

Primary citation

Katayama, N.,Orita, M.,Yamaguchi, T.,Hisamichi, H.,Kuromitsu, S.,Kurihara, H.,Sakashita, H.,Matsumoto, Y.,Fujita, S.,Niimi, T.
Identification of a key element for hydrogen-bonding patterns between protein kinases and their inhibitors.
Proteins, 73:795-801, 2008

PubMed Abstract: In this article, we report crystal structures for inhibitor-kinase complexes in which the inhibitor has different binding orientations and hydrogen-bonding patterns with extracellular-signal regulated kinase 2 and insulin receptor tyrosine kinase. Our crystallographic studies, and sequence and structural analyses of 532 coordinates of kinases held in the Protein Data Bank, suggest that the length of the "specificity linker" described here is a key structural element of the hydrogen-bonding patterns between protein kinases and their inhibitors.

PubMed: 18767165
DOI: 10.1002/prot.22207

Experimental method

X-RAY DIFFRACTION (3.25 Å)