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PDBsum entry 8a2d
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PDB id:
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Transferase
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Title:
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Egfr kinase domain (l858r/v948r) in complex with 2-[4- (difluoromethyl)-6-[2-[4-[[4-(hydroxymethyl)-1- piperidyl]methyl]phenyl]ethynyl]-7-methyl-indazol-2-yl]-2-spiro[6,7- dihydropyrrolo[1,2-c]imidazole-5,1'-cyclopropane]-1-yl-n-thiazol-2- yl-acetamide
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Structure:
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Epidermal growth factor receptor. Chain: a. Synonym: proto-oncogenE C-erbb-1,receptor tyrosine-protein kinase erbb-1. Engineered: yes. Mutation: yes
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Source:
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Homo sapiens. Human. Organism_taxid: 9606. Gene: egfr, erbb, erbb1, her1. Expressed in: spodoptera frugiperda. Expression_system_taxid: 7108
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Resolution:
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1.11Å
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R-factor:
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0.164
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R-free:
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0.179
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Authors:
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A.Kuglstatter,A.Ehler
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Key ref:
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U.Obst-Sander
et al.
(2022).
Discovery of novel allosteric egfr l858r inhibitors f treatment of non-Small-Cell lung cancer as a single a in combination with osimertinib..
J.Med.Chem.,
65,
13052.
PubMed id:
DOI:
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Date:
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03-Jun-22
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Release date:
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19-Oct-22
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PROCHECK
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Headers
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References
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P00533
(EGFR_HUMAN) -
Epidermal growth factor receptor from Homo sapiens
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Seq:
Struc:
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1210 a.a.
281 a.a.*
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Key: |
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PfamA domain |
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Secondary structure |
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*
PDB and UniProt seqs differ
at 7 residue positions (black
crosses)
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Enzyme class:
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E.C.2.7.10.1
- receptor protein-tyrosine kinase.
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Reaction:
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L-tyrosyl-[protein] + ATP = O-phospho-L-tyrosyl-[protein] + ADP + H+
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L-tyrosyl-[protein]
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+
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ATP
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=
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O-phospho-L-tyrosyl-[protein]
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+
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ADP
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+
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H(+)
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Molecule diagrams generated from .mol files obtained from the
KEGG ftp site
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Links
