loading...| Preferred Name |
Niclosamide |
|
| Synonyms |
|
|
| Definitions |
An orally bioavailable chlorinated salicylanilide, with anthelmintic and potential antineoplastic activity. Upon oral administration, niclosamide specifically induces degradation of the androgen receptor (AR) variant V7 (AR-V7) through the proteasome-mediated pathway. This downregulates the expression of the AR variant, inhibits AR-V7-mediated transcriptional activity, and reduces AR-V7 recruitment to the prostate-specific antigen (PSA) gene promoter. Niclosamide also prevents AR-V7-mediated STAT3 phosphorylation and activation. This inhibits AR/STAT3-mediated signaling and prevents expression of STAT3 target genes. Altogether, this may inhibit growth of AR-V7-overexpressing cancer cells. The AR-V7 variant, which is encoded by contiguous splicing of AR exons 1/2/3/CE3, is upregulated in a variety of cancer cell types, and is associated with both cancer progression and resistance to AR-targeted therapies. |
|
| ID |
http://purl.obolibrary.org/obo/NCIT_C66240 |
|
| CAS_Registry |
50-65-7 |
|
| Chemical_Formula |
C13H8Cl2N2O4 |
|
| code |
C66240 |
|
| Contributing_Source |
CTRP FDA |
|
| definition |
An orally bioavailable chlorinated salicylanilide, with anthelmintic and potential antineoplastic activity. Upon oral administration, niclosamide specifically induces degradation of the androgen receptor (AR) variant V7 (AR-V7) through the proteasome-mediated pathway. This downregulates the expression of the AR variant, inhibits AR-V7-mediated transcriptional activity, and reduces AR-V7 recruitment to the prostate-specific antigen (PSA) gene promoter. Niclosamide also prevents AR-V7-mediated STAT3 phosphorylation and activation. This inhibits AR/STAT3-mediated signaling and prevents expression of STAT3 target genes. Altogether, this may inhibit growth of AR-V7-overexpressing cancer cells. The AR-V7 variant, which is encoded by contiguous splicing of AR exons 1/2/3/CE3, is upregulated in a variety of cancer cell types, and is associated with both cancer progression and resistance to AR-targeted therapies. |
|
| Display_Name |
Niclosamide |
|
| FDA_UNII_Code |
8KK8CQ2K8G |
|
| in_subset |
http://purl.obolibrary.org/obo/NCIT_C63923 http://purl.obolibrary.org/obo/NCIT_C173383 http://purl.obolibrary.org/obo/NCIT_C173381 http://purl.obolibrary.org/obo/NCIT_C177537 http://purl.obolibrary.org/obo/NCIT_C176424 http://purl.obolibrary.org/obo/NCIT_C116977 http://purl.obolibrary.org/obo/NCIT_C116978 http://purl.obolibrary.org/obo/NCIT_C128784 |
|
| Is_Value_For_GDC_Property | ||
| label |
Niclosamide |
|
| Legacy Concept Name |
Niclosamide |
|
| Maps_To |
Niclosamide |
|
| NCI_Drug_Dictionary_ID |
775866 |
|
| PDQ_Closed_Trial_Search_ID |
775866 |
|
| PDQ_Open_Trial_Search_ID |
775866 |
|
| Preferred_Name |
Niclosamide |
|
| prefixIRI |
NCIT:C66240 |
|
| prefLabel |
Niclosamide |
|
| Semantic_Type |
Pharmacologic Substance |
|
| UMLS_CUI |
C0699963 |
|
| subClassOf |