Highly Specific, Bi-substrate-Competitive Src Inhibitors from DNA-Templated Macrocycles [PDF]
, 2014 Protein kinases are attractive therapeutic targets, but their high sequence and structural conservation complicates the development of specific inhibitors.
Georghiou, George +4 more
core +1 more source
SRC: A Century of Science Brought to the Clinic
Neoplasia: An International Journal for Oncology Research, 2010 The SRC family kinases are the largest family of norreceptor tyrosine kinases and one of the best-studied targets for cancer therapy. SRC, arguably the oldest oncogene, has been implicated in pathways regulating proliferation, angiogenesis, invasion and ...
Alexey Aleshin, Richard S. Finn
doaj +1 more source
Nef alleles from all major HIV-1 clades activate Src-family kinases and enhance HIV-1 replication in an inhibitor-sensitive manner. [PDF]
PLoS ONE, 2012 The HIV-1 accessory factor Nef is essential for high-titer viral replication and AIDS progression. Nef function requires interaction with many host cell proteins, including specific members of the Src kinase family.
Purushottam S Narute, Thomas E Smithgall
doaj +1 more source
Activation of tyrosine kinases by mutation of the gatekeeper threonine. [PDF]
, 2008 Protein kinases targeted by small-molecule inhibitors develop resistance through mutation of the gatekeeper threonine residue of the active site. Here we show that the gatekeeper mutation in the cellular forms of c-ABL, c-SRC, platelet-derived growth ...
Azam, Mohammad +4 more
core +1 more source
A role for the protein tyrosine phosphatase CD45 in macrophage adhesion through the regulation of paxillin degradation. [PDF]
PLoS ONE, 2013 CD45 is a protein tyrosine phosphatase expressed on all cells of hematopoietic origin that is known to regulate Src family kinases. In macrophages, the absence of CD45 has been linked to defects in adhesion, however the molecular mechanisms involved ...
Joëlle St-Pierre, Hanne L Ostergaard
doaj +1 more source
FUS-CHOP promotes invasion in myxoid liposarcoma through a SRC/FAK/RHO/ROCK-dependent pathway [PDF]
, 2017 Deregulated SRC/FAK signaling leads to enhanced migration and invasion in many types of tumors. In myxoid and round cell liposarcoma (MRCLS), an adipocytic tumor characterized by the expression of the fusion oncogene FUS-CHOP, SRC have been found as one ...
González, M. Victoria +3 more
core +2 more sources
Deletion within the Src homology domain 3 of Bruton's tyrosine kinase resulting in X-linked agammaglobulinemia (XLA). [PDF]
, 1994 The gene responsible for X-linked agammaglobulinemia (XLA) has been recently identified to code for a cytoplasmic tyrosine kinase (Bruton's agammaglobulinemia tyrosine kinase, BTK), required for normal B cell development. BTK, like many other cytoplasmic
Chen, SH +11 more
core +1 more source
Prion-associated Increases in Src-family Kinases [PDF]
Journal of Biological Chemistry, 2005 The prion diseases result from the generation and propagation of an abnormal conformer of the prion protein. It is unclear how this molecular event disrupts neuronal function and viability. Current evidence argues it is not due to loss of normal prion protein activity or direct toxic effects of the abnormal conformer. Both the normal and abnormal prion
openaire +2 more sources
PLoS ONE, 2018 Studies have demonstrated that the solute carrier family 11 member 1 (SLC11A1) is heavily glycosylated and phosphorylated in macrophages. However, the mechanisms of SLC11A1 phosphorylation, and the effects of phosphorylation on SLC11A1 activity remain ...
Yong Zhong Xu +4 more
doaj +1 more source
Real-time analysis of imatinib- and dasatinib-induced effects on chronic myelogenous leukemia cell interaction with fibronectin. [PDF]
PLoS ONE, 2014 Attachment of stem leukemic cells to the bone marrow extracellular matrix increases their resistance to chemotherapy and contributes to the disease persistence.
Adam Obr +3 more
doaj +1 more source