Transferase(Phosphotransferase); domain 1
Non-specific serine/threonine protein kinase
Regulation of ack-family nonreceptor tyrosine kinases.
SUBUNIT, SUBCELLULAR LOCATION, PHOSPHORYLATION AT TYR-284, DOMAIN SAM-LIKE.
Regulation of Ack1 localization and activity by the amino-terminal SAM domain.
Cancer-associated mutations activate the nonreceptor tyrosine kinase Ack1.
PHOSPHORYLATION AT TYR-284, INTERACTION WITH SRC.
The Cdc42-associated kinase ACK1 is not autoinhibited but requires Src for activation.
Structure of the small G protein Cdc42 bound to the GTPase-binding domain of ACK.
Biochemical properties of the Cdc42-associated tyrosine kinase ACK1. Substrate specificity, authphosphorylation, and interaction with Hck.
X-RAY CRYSTALLOGRAPHY (2.0 ANGSTROMS) OF 107-395, PHOSPHORYLATION AT TYR-284.
Crystal structures of the phosphorylated and unphosphorylated kinase domains of the Cdc42-associated tyrosine kinase ACK1.
X-RAY CRYSTALLOGRAPHY (2.0 ANGSTROMS) OF 117-392 IN COMPLEX WITH INHIBITOR, CATALYTIC ACTIVITY.
Identification and optimization of N3,N6-diaryl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamines as a novel class of ACK1 inhibitors.
Synthesis and optimization of substituted furo[2,3-d]-pyrimidin-4-amines and 7H-pyrrolo[2,3-d]pyrimidin-4-amines as ACK1 inhibitors.
This enzyme belongs to Ack (activated Cdc42-associated kinase) nonreceptor tyrosine kinase family (see [8]). This enzyme is composed of N-terminal sterile alpha motif (SAM) domain, kinase domain, SH3 domain, Cdc42/Rac-interactive domain (CRIB), Clathrin binding motif, region that shares a high homology with Mitogen induced gene6 (Mig6), and C-terminal ubiquitin associated (UBA) domain. The catalytic domain of this enzyme is homologous to that of proto-oncogene tyrosine-protein kinase ABL1 (M00130 in EzCatDB).