Anti-TNFRSF10B (Conatumumab)-SPDB-DM4 ADC (ADC-W-1863)

 ADC Target

  • Name
  • TNFRSF10B
  • Alternative Names
  • TNFRSF10B; tumor necrosis factor receptor superfamily, member 10b; tumor necrosis factor receptor superfamily member 10B; CD262; DR5; KILLER; TRAIL R2; TRICK2A; TRICKB; Fas-like protein; death receptor 5; cytotoxic TRAIL receptor-2; apoptosis inducing receptor TRAIL-R2; apoptosis inducing protein TRICK2A/2B; TNF-related apoptosis-inducing ligand receptor 2; death domain containing receptor for TRAIL/Apo-2L; tumor necrosis factor receptor-like protein ZTNFR9; p53-regulated DNA damage-inducible cell death receptor(killer); TRICK2; ZTNFR9; TRAILR2; TRICK2B; TRAIL-R2; KILLER/DR5;
  • Target Entrez Gene ID
  • 8795
  • Overview
  • The protein encoded by this gene is a member of the TNF-receptor superfamily, and contains an intracellular death domain. This receptor can be activated by tumor necrosis factor-related apoptosis inducing ligand (TNFSF10/TRAIL/APO-2L), and transduces an apoptosis signal. Studies with FADD-deficient mice suggested that FADD, a death domain containing adaptor protein, is required for the apoptosis mediated by this protein. Two transcript variants encoding different isoforms and one non-coding transcript have been found for this gene.

 ADC Antibody

  • Overview
  • Human Anti-TNFRSF10B IgG1-kappa antibody, Conatumumab
  • Generic name
  • Conatumumab
  • Host animal
  • Human

 ADC Linker

  • Name
  • SPDB (N-succinimidyl-4-(2-pyridyldithio)butyrate)
  • Description
  • Disulfide Linkers, are extensively exploited as a chemically labile linkage. Since the release of disulfide-linked drugs requires a cytoplasmic thiol cofactor, such as glutathione (GSH). Disulfides maintain stable at physiological pH and only when ADCs are internalized inside cells, the cytosol provides reducing environment including intracellular enzyme protein disulfide isomerase, or similar enzymes, drugs can be released.

 ADC payload drug

  • Name
  • DM4 (N2'-Deacetyl-N2'-(4-mercapto-4-methyl-1-oxopentyl)maytansine)
  • Description
  • Derived from Maytansinoid,a group of cytotoxins structurally similar to rifamycin, geldanamycin, and ansatrienin. The eponymous natural cytotoxic agent maytansine is a 19-member lactam (ansa macrolide) structure originally isolated from the Ethiopian shrub Maytenus ovatus. Maytansinoids can bind to tubulin at or near the vinblastine-binding site, which interfere the formation of microtubules and depolymerize already formed microtubules, inducing mitotic arrest in the intoxicated cells.

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