Preferred Name

p97 Inhibitor CB-5339 Tosylate

ID

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C167262

code

C167262

Concept_In_Subset

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C116977

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

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C177537

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

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C116978

Contributing_Source

CTRP

GDC

DEFINITION

The tosylate salt of CB-5339, an orally bioavailable, selective, second-generation inhibitor of valosin-containing protein (VCP)/p97, with potential antineoplastic activity. Upon oral administration, p97 inhibitor CB-5339 binds to and inhibits the activity of p97. This prevents ubiquitin-dependent protein degradation and causes cellular accumulation of poly-ubiquitinated proteins. The inhibition of endoplasmic reticulum (ER)-associated protein degradation activates the ER-dependent stress response pathway, and leads to both an induction of apoptosis and the inhibition of cell proliferation in susceptible tumor cells. VCP/p97, a type II AAA+ ATPase, plays a key role in cellular protein homeostasis processes including endoplasmic reticulum associated degradation (ERAD), chromatin associated degradation (CAD) and the DNA damage response (DDR). Its overexpression in many tumor cell types is associated with increased tumor cell proliferation and survival.

Display_Name

p97 Inhibitor CB-5339 Tosylate

FULL_SYN

CB-5339 Tosylate

p97 Inhibitor CB-5339 Tosylate

CB5339 Tosylate

CB 5339 Tosylate

Has_Free_Acid_Or_Base_Form

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C167257

Is_Value_For_GDC_Property

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C1909

label

p97 Inhibitor CB-5339 Tosylate

Maps_To

p97 Inhibitor CB-5339 Tosylate

NCI_Drug_Dictionary_ID

800450

NCI_META_CUI

CL972249

PDQ_Closed_Trial_Search_ID

800450

PDQ_Open_Trial_Search_ID

800450

Preferred_Name

p97 Inhibitor CB-5339 Tosylate

prefixIRI

Thesaurus:C167262

prefLabel

p97 Inhibitor CB-5339 Tosylate

Semantic_Type

Pharmacologic Substance

subClassOf

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C471

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