Acylfulvene-derived Prodrug LP-184

Preferred Label : Acylfulvene-derived Prodrug LP-184;

NCIt synonyms : Alkylating Agent Prodrug LP-184;

NCIt related terms : LP-184;

NCIt definition : A tumor-site activated acylfulvene-derived prodrug and alkylating agent, with potential antineoplastic activity. Upon administration, acylfulvene-derived prodrug LP-184 becomes activated by prostaglandin reductase 1 (PTGR1), an oxidoreductase that is specifically upregulated in certain tumor cell types. The active form of LP-184 covalently binds to and alkylates DNA at N3-adenine, thereby causing double strand breaks. As tumor cells often carry DNA damage repair (DDR) mutations and are therefore deficient in DDR pathways, the DNA damage cannot be repaired. In turn, the damaged DNA causes apoptosis and inhibits proliferation in susceptible DDR mutated tumor cells. PTGR1 is often elevated in solid tumors but not in normal tissues.;

UNII : L683VC69K8;

CAS number : 924835-67-6;

Molecule name : LP 184; LP-184;

NCI Metathesaurus CUI : CL1922476;

Détails

Origin ID

C203657;

UMLS CUI

C5853897;

Semantic type(s)
- Organic Chemical [UMLS semantic type]
- Pharmacologic Substance [UMLS semantic type]
chemical_or_drug_has_mechanism_of_action
- DNA Intercalation [NCIt concept]
chemical_or_drug_has_physiologic_effect
- DNA Crosslinking [NCIt concept]
- DNA Replication Inhibition [NCIt concept]
- Positive Regulation of Apoptosis [NCIt concept]
concept_is_in_subset
- CTRP Agent Terminology [NCIt concept]
- CTRP Terminology [NCIt concept]
- FDA Established Names and Unique Ingredient Identifier Codes Terminology [NCIt concept]
- GDC Therapeutic Agent Terminology [NCIt concept]
- NCI Drug Dictionary Terminology [NCIt concept]
- NCIt Antineoplastic Agent Terminology [NCIt concept]

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