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PDBsum entry 3eta
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Signaling protein, transferase
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PDB id
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3eta
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Contents |
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* Residue conservation analysis
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PDB id:
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| Name: |
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Signaling protein, transferase
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Title:
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Kinase domain of insulin receptor complexed with a pyrrolo pyridine inhibitor
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Structure:
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Insulin receptor, kinase domain. Chain: a, b. Fragment: kinase domain. Synonym: ir, insulin receptor subunit alpha, insulin receptor subunit beta. Engineered: yes
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Source:
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Homo sapiens. Human. Organism_taxid: 9606. Gene: insr. Expressed in: spodoptera frugiperda. Expression_system_taxid: 7108.
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Resolution:
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2.60Å
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R-factor:
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0.203
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R-free:
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0.232
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Authors:
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S.Patnaik,K.Stevens,R.Gerding,F.Deanda,B.Shotwell,J.Tang,T.Hamajima, H.Nakamura,A.Leesnitzer,A.Hassell,L.Shewchuk,R.Kumar,H.Lei, S.Chamberlain
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Key ref:
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S.Patnaik
et al.
(2009).
Discovery of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines as potent inhibitors of the insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase.
Bioorg Med Chem Lett,
19,
3136-3140.
PubMed id:
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Date:
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07-Oct-08
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Release date:
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26-May-09
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PROCHECK
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Headers
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References
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P06213
(INSR_HUMAN) -
Insulin receptor from Homo sapiens
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Seq:
Struc:
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1382 a.a.
293 a.a.
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Key: |
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PfamA domain |
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Secondary structure |
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CATH domain |
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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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Bioorg Med Chem Lett
19:3136-3140
(2009)
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PubMed id:
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Discovery of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines as potent inhibitors of the insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase.
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S.Patnaik,
K.L.Stevens,
R.Gerding,
F.Deanda,
J.B.Shotwell,
J.Tang,
T.Hamajima,
H.Nakamura,
M.A.Leesnitzer,
A.M.Hassell,
L.M.Shewchuck,
R.Kumar,
H.Lei,
S.D.Chamberlain.
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ABSTRACT
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Exploration of the SAR around a series of
3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines led to the discovery of novel
pyrrolopyridine inhibitors of the IGF-1R tyrosine kinase. Several compounds
demonstrated nanomolar potency in enzyme and cellular mechanistic assays.
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Links
