Article ; Online: Multiple conformational states of the HPK1 kinase domain in complex with sunitinib reveal the structural changes accompanying HPK1 trans-regulation.
The Journal of biological chemistry
2019 Volume 294, Issue 23, Page(s) 9029–9036
Abstract: Hematopoietic progenitor kinase 1 (HPK1 or MAP4K1) is a Ser/Thr kinase that operates via the c-Jun N-terminal kinase (JNK) and extracellular signal-regulated kinase (ERK) signaling pathways to dampen the T-cell response and antitumor immunity. ... ...
Abstract | Hematopoietic progenitor kinase 1 (HPK1 or MAP4K1) is a Ser/Thr kinase that operates via the c-Jun N-terminal kinase (JNK) and extracellular signal-regulated kinase (ERK) signaling pathways to dampen the T-cell response and antitumor immunity. Accordingly, selective HPK1 inhibition is considered a means to enhance antitumor immunity. Sunitinib, a multi-receptor tyrosine kinase (RTK) inhibitor approved for the management of gastrointestinal stromal tumors (GISTs), renal cell carcinoma (RCC), and pancreatic cancer, has been reported to inhibit HPK1 |
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MeSH term(s) | Adenosine Triphosphate/chemistry ; Adenosine Triphosphate/metabolism ; Binding Sites ; Crystallography, X-Ray ; Dimerization ; Humans ; Interleukin-2/metabolism ; Molecular Dynamics Simulation ; Mutagenesis, Site-Directed ; Phosphorylation ; Protein Structure, Tertiary ; Protein-Serine-Threonine Kinases/antagonists & inhibitors ; Protein-Serine-Threonine Kinases/genetics ; Protein-Serine-Threonine Kinases/metabolism ; Recombinant Proteins/biosynthesis ; Recombinant Proteins/chemistry ; Recombinant Proteins/genetics ; Sunitinib/chemistry ; Sunitinib/metabolism ; Sunitinib/pharmacology ; T-Lymphocytes/cytology ; T-Lymphocytes/drug effects ; T-Lymphocytes/metabolism |
Chemical Substances | Interleukin-2 ; Recombinant Proteins ; Adenosine Triphosphate (8L70Q75FXE) ; hematopoietic progenitor kinase 1 (EC 2.7.1.11) ; Protein-Serine-Threonine Kinases (EC 2.7.11.1) ; Sunitinib (V99T50803M) |
Language | English |
Publishing date | 2019-04-24 |
Publishing country | United States |
Document type | Journal Article |
ZDB-ID | 2997-x |
ISSN | 1083-351X ; 0021-9258 |
ISSN (online) | 1083-351X |
ISSN | 0021-9258 |
DOI | 10.1074/jbc.AC119.007466 |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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