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Title: Crystal Structures of PRK1 in Complex with the Clinical Compounds Lestaurtinib and Tofacitinib Reveal Ligand Induced Conformational Changes

Journal Article · · PLoS ONE
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Research Organization:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Organization:
INDUSTRY
OSTI ID:
1497111
Journal Information:
PLoS ONE, Vol. 9, Issue 8; ISSN 1932-6203
Publisher:
Public Library of Science
Country of Publication:
United States
Language:
ENGLISH

References (34)

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Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders journal June 2008
Structural and Thermodynamic Characterization of the TYK2 and JAK3 Kinase Domains in Complex with CP-690550 and CMP-6 journal July 2010
A novel inducible transactivation domain in the androgen receptor: implications for PRK in prostate cancer journal January 2003
Virtual Screening of PRK1 Inhibitors: Ensemble Docking, Rescoring Using Binding Free Energy Calculation and QSAR Model Development journal December 2013
The hallmark of AGC kinase functional divergence is its C-terminal tail, a cis-acting regulatory module journal January 2007
Identification of a Putative Target for Rho as the Serine-Threonine Kinase Protein Kinase N journal February 1996
A quantitative analysis of kinase inhibitor selectivity journal January 2008
Mechanism for activation of the growth factor-activated AGC kinases by turn motif phosphorylation journal April 2007
Coot model-building tools for molecular graphics journal November 2004
Translocation of PKN from the cytosol to the nucleus induced by stresses. journal September 1996
Discovery of CP-690,550: A Potent and Selective Janus Kinase (JAK) Inhibitor for the Treatment of Autoimmune Diseases and Organ Transplant Rejection journal December 2010
REFMAC 5 for the refinement of macromolecular crystal structures journal March 2011
Comparative Effects of GTPγS and Insulin on the Activation of Rho, Phosphatidylinositol 3-Kinase, and Protein Kinase N in Rat Adipocytes: RELATIONSHIP TO GLUCOSE TRANSPORT journal March 1998
Activation of PRK1 by Phosphatidylinositol 4,5-Bisphosphate and Phosphatidylinositol 3,4,5-Trisphosphate: A COMPARISON WITH PROTEIN KINASE C ISOTYPES journal September 1995
Catalytic Domain Crystal Structure of Protein Kinase C-θ (PKCθ) journal September 2004
PRK1 distribution in normal tissues and carcinomas: overexpression and activation in ovarian serous carcinoma journal October 2009
A FLT3-targeted tyrosine kinase inhibitor is cytotoxic to leukemia cells in vitro and in vivo journal June 2002
A binary complex of the catalytic subunit of cAMP-dependent protein kinase and adenosine further defines conformational flexibility journal July 1997
A phase 2 trial of the FLT3 inhibitor lestaurtinib (CEP701) as first-line treatment for older patients with acute myeloid leukemia not considered fit for intensive chemotherapy journal November 2006
Protein kinase C-related kinase targets nuclear localization signals in a subset of class IIa histone deacetylases journal February 2010
Crystal Structure of the Catalytic Domain of Human Atypical Protein Kinase C-iota Reveals Interaction Mode of Phosphorylation Site in Turn Motif journal September 2005
Phase 2 study of CEP-701, an orally available JAK2 inhibitor, in patients with primary or post-polycythemia vera/essential thrombocythemia myelofibrosis journal February 2010
Protein kinase N1, a cell inhibitor of Akt kinase, has a central role in quality control of germinal center formation journal December 2012
Lestaurtinib Inhibits Histone Phosphorylation and Androgen-Dependent Gene Expression in Prostate Cancer Cells journal April 2012
Proteolytic activation of PKN by caspase-3 or related protease during apoptosis journal September 1998
High resolution crystal structure of the human PDK1 catalytic domain defines the regulatory phosphopeptide docking site journal August 2002
Sequence and structural analysis of kinase ATP pocket residues journal October 2004
A 3-Phosphoinositide-dependent Protein Kinase-1 (PDK1) Docking Site Is Required for the Phosphorylation of Protein Kinase Cζ (PKCζ) and PKC-related Kinase 2 by PDK1 journal April 2000
[20] Processing of X-ray diffraction data collected in oscillation mode book January 1997
Posttranslational Modifications of the Histone 3 Tail and Their Impact on the Activity of Histone Lysine Demethylases In Vitro journal July 2013
Phaser crystallographic software journal July 2007
The Structural Basis of Rho Effector Recognition Revealed by the Crystal Structure of Human RhoA Complexed with the Effector Domain of PKN/PRK1 journal November 1999

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