a-amanitin

alpha-Amanitin (alpha-Amanitin) is the lethal toxin in Trichoderma viride and acts in vivo via the enterohepatic circulation and transport system. alpha-Amanitin induces cell death and can be used in the synthesis of ADCs. alpha-Amanitin has been shown to induce cell death and can be used in the synthesis of ADCs.

MC-VC-PABC-C6-alpha-Amanitin is an antibody-drug conjugate that combines the anticancer toxin alpha-Amanitin with the monoclonal antibody MC-VC-PABC-C6. Alpha-Amanitin, a potent inhibitor of RNA polymerase IIα, enables the conjugate to selectively target and recognize HER2-positive tumor cells, making it a valuable research tool in the study of breast and gastric cancers [1].

β-Amanitin, a cyclic peptide toxin found in the poisonous Amanita phalloides mushroom, inhibits eukaryotic RNA polymerase II and III, thereby disrupting protein synthesis.

Mal-C6-α-Amanitin, an ADC (antibody-drug conjugate) linker drug, incorporates the powerful antitumor agent α-Amanitin, an inhibitor of RNA polymerase II, through the Mal-C6 linker, showcasing potent antitumor activity.

γ-Amanitin, an ADC (antibody-drug conjugate) cytotoxin isolated from mushrooms, inhibits RNA polymerase II, disrupting mRNA synthesis. It exhibits effects akin to those of α-Amanitin and β-Amanitin.

Alamethicin is a channel-forming antibiotic peptide isolated from Trichoderma viride with potential antimicrobial activity, inhibits methanogenesis and promotes acetogenesis in bioelectrochemical systems. alpha-Amanitin (BI-9627) is a channel-forming antibiotic peptide isolated from Trichoderma viride.

ε-Amanitin is a cyclic peptide obtained from various mushroom species. It exhibits a strong affinity for RNA polymerase II and effectively inhibits its activity.

RNA polymerase II-IN-2 (compound 20iii), a potent inhibitor of RNA polymerase II (Pol II) with a K i value of 9.5 nM, exhibits cytotoxicity against cancer cells, demonstrating toxicity levels 2 and 5 times higher than α-amanitin in CHO and HEK293 cells, respectively [1].

Dideoxy-amanitin (compound 2), a derivative of α-Amanitin, functions as a potent, selective allosteric inhibitor of RNA polymerase II, demonstrating an inhibition concentration (IC50) of 74.2 nM [1].

Fmoc-L-Asn(EDA-N3)-OH is a chemical compound equipped with an azide group used in click chemistry. Reports in the literature have demonstrated its application in the modification of α-amanitin, the deadliest member of the amatoxin peptide family produced by the death cap mushroom. α-Amanitin is a highly lethal natural compound (LD50=50-100 µg/kg), an orally ingested rigid bicyclic octapeptide, acting as a highly selective conformational inhibitor of RNA polymerase II.

MGTA-117 is a humanized monoclonal antibody that targets CD117. It carries an amanitin payload and is used to synthesize antibody-drug conjugates (ADC). MGTA-117 demonstrates potent antitumor activity, enhancing survival in three acute myeloid leukemia (AML) xenograft models [Kasumi-1, AML PDX 1, and AML PDX 2]. It is applicable for AML, myelodysplastic syndromes with excess blasts (MDS-EB), and preconditioning for hematopoietic stem cell transplantation (HSCT) in gene therapy.