PMID- 10360180
OWN - NLM
STAT- MEDLINE
DCOM- 19990617
LR  - 20190915
IS  - 1097-2765 (Print)
IS  - 1097-2765 (Linking)
VI  - 3
IP  - 5
DP  - 1999 May
TI  - Crystal structure of Hck in complex with a Src family-selective tyrosine kinase
      inhibitor.
PG  - 639-48
AB  - The crystal structure of the autoinhibited form of Hck has been determined at 2.0
      A resolution, in complex with a specific pyrazolo pyrimidine-type inhibitor, PP1.
      The activation segment, a key regulatory component of the catalytic domain, is
      unphosphorylated and is visualized in its entirety. Tyr-416, the site of
      activating autophosphorylation in the Src family kinases, is positioned such that
      access to the catalytic machinery is blocked. PP1 is bound at the ATP-binding
      site of the kinase, and a methylphenyl group on PP1 is inserted into an adjacent 
      hydrophobic pocket. The enlargement of this pocket in autoinhibited Src kinases
      suggests a route toward the development of inhibitors that are specific for the
      inactive forms of these proteins.
FAU - Schindler, T
AU  - Schindler T
AD  - Laboratories of Molecular Biophysics, Rockefeller University, New York, New York 
      10021, USA.
FAU - Sicheri, F
AU  - Sicheri F
FAU - Pico, A
AU  - Pico A
FAU - Gazit, A
AU  - Gazit A
FAU - Levitzki, A
AU  - Levitzki A
FAU - Kuriyan, J
AU  - Kuriyan J
LA  - eng
SI  - PDB/1QCF
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - United States
TA  - Mol Cell
JT  - Molecular cell
JID - 9802571
RN  - 0 (Proto-Oncogene Proteins)
RN  - EC 2.7.10.1 (Protein-Tyrosine Kinases)
RN  - EC 2.7.10.2 (Proto-Oncogene Proteins c-hck)
RN  - EC 2.7.10.2 (Proto-Oncogene Proteins pp60(c-src))
SB  - IM
MH  - Animals
MH  - Binding Sites
MH  - Cells, Cultured
MH  - Crystallography
MH  - Insecta
MH  - Molecular Sequence Data
MH  - Phosphorylation
MH  - Protein Binding/physiology
MH  - Protein Structure, Secondary
MH  - Protein Structure, Tertiary
MH  - Protein-Tyrosine Kinases/*chemistry/metabolism
MH  - Proto-Oncogene Proteins/*chemistry/metabolism
MH  - Proto-Oncogene Proteins c-hck
MH  - Proto-Oncogene Proteins pp60(c-src)/*antagonists &
      inhibitors/*chemistry/metabolism
MH  - Sequence Homology, Amino Acid
MH  - Substrate Specificity
MH  - src Homology Domains/physiology
EDAT- 1999/06/09 00:00
MHDA- 1999/06/09 00:01
CRDT- 1999/06/09 00:00
PHST- 1999/06/09 00:00 [pubmed]
PHST- 1999/06/09 00:01 [medline]
PHST- 1999/06/09 00:00 [entrez]
AID - S1097-2765(00)80357-3 [pii]
AID - 10.1016/s1097-2765(00)80357-3 [doi]
PST - ppublish
SO  - Mol Cell. 1999 May;3(5):639-48. doi: 10.1016/s1097-2765(00)80357-3.