Preferred Label : NMT Inhibitor PCLX-001;
NCIt synonyms : N-myristoyl Transferase Inhibitor PCLX-001;
NCIt definition : An orally bioavailable inhibitor of the enzyme N-myristoyl transferase (NMT), with
potential antineoplastic activity. Upon oral administration, NMT inhibitor PCLX-001
targets and binds to NMT, especially NMT type 2 (NMT2). This prevents NMT-mediated
signaling and myristoylation. This inhibits proliferation of certain cancer cells
in which NMT expression is lost. PCLX-001 also inhibits B-cell receptor (BCR) signaling
and reduces the levels of Src-family tyrosine kinases (SFKs). NMTs mediate myristoylation,
a key process by which the fatty acid myristate is added to proteins and allows proteins
to interact with cell membranes and become part of the cell signaling system. NMT
expression is lost in numerous cancers, such as blood cancer cells, thereby making
these cells more sensitive to PCLX-001 compared to normal cells. The loss of NMT expression
may promote tumorigenesis.;
Molecule name : PCLX-001; PCLX 001;
NCI Metathesaurus CUI : CL1662944;
Origin ID : C180576;
UMLS CUI : C5210401;
Semantic type(s)
- concept_is_in_subset
- has_target
