Preferred Label : MARCKS Protein Inhibitor BIO-11006;
NCIt synonyms : Aerosolized BIO-11006; Myristoylated Alanine Rich C Kinase Substrate Inhibitor BIO-11006; BIO-11006 Peptide;
NCIt related terms : BIO-11006;
NCIt definition : An aerosolized 10-amino acid peptide that inhibits the myristoylated alanine rich
protein kinase C substrate (MARCKS) protein, with potential immunomodulating and antineoplastic
activities. Upon inhalation, the MARCKS protein inhibitor BIO-11006 targets, binds
to and inhibits the phosphorylation of MARCKS (P-MARCKS). This prevents MARCKS-mediated
signaling, thereby preventing the release of phosphatidylinositol 4,5-bisphosphate
(PIP2) from the cell membrane upon MARCKS binding. This prevents the PIP2-mediated
activation of focal adhesion kinase (FAK) and the FAK-mediated activation of the PI3K/AKT
pathway and the activation of integrins, talin, vinculin and paxillin. This leads
to an inhibition of tumor cell proliferation, migration, metastasis and survival.
In addition, inhibition of MARCKS prevents mucin granule release and reduces the overproduction
of mucus in the lungs. This may abrogate airway obstruction, impaired lung function,
airway inflammation and bacterial infections associated with overproduction of mucus
in the lungs. The MARCKS protein, a filamentous actin crosslinking protein and substrate
for protein kinase C (PKC) is localized on the plasma membrane. Upon phosphorylation
by PKC or binding to the calcium-calmodulin complex, the association of MARCKS with
actin and with the plasma membrane is blocked, leading to its presence in the cytoplasm.
The MARCKS protein plays a key role in the exocytosis of a number of vesicles and
granules, cell movement, mitogenesis and membrane trafficking.;
UNII : 609AWV0US2;
CAS number : 901117-03-1; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 901117-03-1
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G-SRS /a ;
Molecule name : BIO-11006; BIO 11006;
NCI Metathesaurus CUI : CL935857;
Origin ID : C156733;
UMLS CUI : C4745025;
Semantic type(s)
- concept_is_in_subset
