3en4 Summary

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Targeted polypharmacology: crystal structure of the c-Src kinase domain in complex with PP121, a multitargeted kinase inhibitor

The structure was published by Apsel, B., Blair, J.A., Gonzalez, B., et al., Williams, R.L., Shokat, K.M., and Knight, Z.A., in 2008 in a paper entitled "Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases." (abstract).

This crystal structure was determined using X-ray diffraction at a resolution of 2.55 Å and deposited in 2008.

The experimental data on which the structure is based was also deposited.

This PDB entry contains multiple copies of the structure of Proto-oncogene tyrosine-protein kinase Src.

It also contains one or more heterogenic compounds (e.g., ligands, co-factors, ions, modified amino acids, etc.); see here for a complete list.

The molecule has more than one probable quaternary state observed. For more details see the quaternary structure page.

The following tables show cross-reference information to other databases (to obtain a list of all PDB entries sharing the same property or classification, click on the magnifying glass icon):


Chain Name UniProt Name of source organism % of UniProt sequence present in the sample Residues in the sample molecules % of residues observed
A Proto-oncogene tyrosine-protein kinase Src P00523 (251-533) (SRC_CHICK)search Gallus gallussearch < 90% 286 93%
B Proto-oncogene tyrosine-protein kinase Src P00523 (251-533) (SRC_CHICK)search Gallus gallussearch < 90% 286 93%


This entry contains 1 unique UniProt protein:

UniProt accession Name Organism PDB
P00523 (251 - 533) Proto-oncogene tyrosine-protein kinase Src Gallus gallus

Chain Structural classification (CATH) Sequence family (Pfam)
A, B Phosphorylase Kinase; domain 1search, Transferase(Phosphotransferase) domain 1search Protein tyrosine kinasesearch

Chain ID Molecular function (GO) Biological process (GO)
A, B (P00523) protein tyrosine kinase activitysearch protein kinase activitysearch ATP bindingsearch transferase activity, transferring phosphorus-containing groupssearch protein phosphorylationsearch

Chain InterPro annotation
A, B Protein kinase domainsearch Serine-threonine/tyrosine-protein kinase catalytic domainsearch Tyrosine-protein kinase, active sitesearch Protein kinase-like domainsearch Protein kinase, ATP binding sitesearch Tyrosine-protein kinase, catalytic domainsearch