Preferred Label : Zelenirstat;
NCIt synonyms : N-myristoyl Transferase Inhibitor PCLX-001; NMT Inhibitor PCLX-001;
NCIt definition : An orally bioavailable inhibitor of the enzyme N-myristoyl transferase (NMT), with
potential antineoplastic activity. Upon oral administration, zelenirstat 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. Zelenirstat 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 zelenirstat compared to normal cells. The loss of NMT expression may
promote tumorigenesis.;
UNII : 5HY8BYC3Q6;
CAS number : 1215011-08-7;
Molecule name : PCLX-001; PCLX 001; DDD-86481; DDD 86481;
NCI Metathesaurus CUI : CL1662944;
Origin ID : C180576;
UMLS CUI : C5210401;
Semantic type(s)
concept_is_in_subset
has_target