Preferred Name

NMT Inhibitor PCLX-001

ID

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C180576

code

C180576

Concept_In_Subset

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C157712

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C157711

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C176424

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C128784

Contributing_Source

GDC

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.

FULL_SYN

PCLX-001

PCLX001

NMT Inhibitor PCLX-001

N-myristoyl Transferase Inhibitor PCLX-001

PCLX 001

Has_Target

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C19421

label

NMT Inhibitor PCLX-001

NCI_Drug_Dictionary_ID

805501

NCI_META_CUI

CL1662944

Preferred_Name

NMT Inhibitor PCLX-001

prefixIRI

Thesaurus:C180576

prefLabel

NMT Inhibitor PCLX-001

Semantic_Type

Pharmacologic Substance

subClassOf

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C1404

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