MLchartDataset catalogue

FR Alpha/TRPV6 bispecific ligand drug conjugate CBP-1008

Term · Oncology and biomedicine · MLC-T-ONC-013775

A bispecific ligand drug conjugate targeting both human folate receptor alpha (FR alpha; FOLR1) and transient receptor potential cation channel subfamily V member 6 (TRPV6; CaT1; CATL) and conjugated to monomethyl auristatin E (MMAE), an auristatin derivative and potent microtubule disrupting agent, with potential antineoplastic activity. Upon administration of FR alpha/TRPV6 bispecific ligand drug conjugate CBP-1008, the bispecific ligand moiety targets and binds to FR alpha and/or TRPV6, which are overexpressed in certain tumor types. After internalization of the agent, the MMAE moiety is released and binds to tubulin and inhibits its polymerization, which results in G2/M phase arrest and apoptosis. This inhibits the proliferation of tumor cells expressing FR alpha and/or TRPV6. FR alpha is a high-affinity folate-binding protein and a member of the folate receptor family; it is overexpressed in certain tumor types. The TRPV6 ion channel plays a key role in calcium homeostasis and is highly selective for calcium compared to other cations; it is overexpressed in a variety of tumors and initiates tumor cell growth, proliferation and metastases.

Table 1. Record
IdentifierMLC-T-ONC-013775
FieldOncology and biomedicine
SynonymsFR alpha/TRPV6 bi-specific ligand drug conjugate CBP-1008; FR Alpha/TRPV6-targeted MMAE conjugate CBP-1008
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-013775",
  "term": "FR Alpha/TRPV6 bispecific ligand drug conjugate CBP-1008",
  "field": "Oncology and biomedicine",
  "definition": "A bispecific ligand drug conjugate targeting both human folate receptor alpha (FR alpha; FOLR1) and transient receptor potential cation channel subfamily V member 6 (TRPV6; CaT1; CATL) and conjugated to monomethyl auristatin E (MMAE), an auristatin derivative and potent microtubule disrupting agent, with potential antineoplastic activity. Upon administration of FR alpha/TRPV6 bispecific ligand drug conjugate CBP-1008, the bispecific ligand moiety targets and binds to FR alpha and/or TRPV6, which are overexpressed in certain tumor types. After internalization of the agent, the MMAE moiety is released and binds to tubulin and inhibits its polymerization, which results in G2/M phase arrest and apoptosis. This inhibits the proliferation of tumor cells expressing FR alpha and/or TRPV6. FR alpha is a high-affinity folate-binding protein and a member of the folate receptor family; it is overexpressed in certain tumor types. The TRPV6 ion channel plays a key role in calcium homeostasis and is highly selective for calcium compared to other cations; it is overexpressed in a variety of tumors and initiates tumor cell growth, proliferation and metastases.",
  "synonyms": [
    "FR alpha/TRPV6 bi-specific ligand drug conjugate CBP-1008",
    "FR Alpha/TRPV6-targeted MMAE conjugate CBP-1008"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/fr-alpha-trpv6-bispecific-ligand-drug-conjugate-cbp-1008/"
}

Record 7,601 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.