5AA8

Structure of C1156Y,L1198F Mutant Human Anaplastic Lymphoma Kinase in Complex with PF-06463922 ((10R)-7-amino-12-fluoro-2,10,16-trimethyl- 15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo(4,3-h)(2,5,11) benzoxadiazacyclotetradecine-3-carbonitrile).

Summary for 5AA8

• Entry DOI: 10.2210/pdb5aa8/pdb
• Related: 5A9U 5AA9 5AAA 5AAB 5AAC
• Descriptor: ALK TYROSINE KINASE RECEPTOR, (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile (3 entities in total)
• Functional Keywords: transferase, receptor tyrosine kinase, inhibitor, mutant
• Biological source: HOMO SAPIENS (HUMAN)
• Cellular location: Cell membrane ; Single-pass type I membrane protein : Q9UM73
• Total number of polymer chains: 1
• Total formula weight: 37409.82

Authors

McTigue, M.,Deng, Y.-L.,Liu, W.,Brooun, A.,Stewart, A. (deposition date: 2015-07-23, release date: 2016-06-08, Last modification date: 2024-01-10)

• Primary citation: Shaw, A.T.,Friboulet, L.,Leshchiner, I.,Gainor, J.F.,Bergqvist, S.,Brooun, A.,Burke, B.J.,Deng, Y.,Liu, W.,Dardaei, L.,Frias, R.L.,Schultz, K.R.,Logan, J.,James, L.P.,Smeal, T.,Timofeevski, S.,Katayama, R.,Iafrate, A.J.,Le, L.,Mctigue, M.,Getz, G.,Johnson, T.W.,Engelman, J.A.; Resensitization to Crizotinib by the Lorlatinib Alk Resistance Mutation L1198F.; N.Engl.J.Med., 374:54-, 2016; PubMed: 26698910; DOI: 10.1056/NEJMOA1508887

Experimental method

X-RAY DIFFRACTION (1.86 Å)