Anti-FOLH1 (Capromab)-SMCC-DM1 ADC (ADC-W-1160)

 ADC Target

  • Name
  • FOLH1
  • Alternative Names
  • FOLH1; folate hydrolase (prostate-specific membrane antigen) 1; FOLH; glutamate carboxypeptidase 2; GCP2; GCPII; glutamate carboxylase II; glutamate carboxypeptidase II; NAALAD1; NAALAdase; PSM; PSMA; NAALADase I; membrane glutamate carboxypeptidase; cell growth-inhibiting gene 27 protein; folylpoly-gamma-glutamate carboxypeptidase; prostate specific membrane antigen variant F; pteroylpoly-gamma-glutamate carboxypeptidase; N-acetylated alpha-linked acidic dipeptidase 1; N-acetylated-alpha-linked acidic dipeptidase I; FGCP; mGCP;
  • Target Entrez Gene ID
  • 2346
  • Overview
  • This gene encodes a type II transmembrane glycoprotein belonging to the M28 peptidase family. The protein acts as a glutamate carboxypeptidase on different alternative substrates, including the nutrient folate and the neuropeptide N-acetyl-l-aspartyl-l-glutamate and is expressed in a number of tissues such as prostate, central and peripheral nervous system and kidney. A mutation in this gene may be associated with impaired intestinal absorption of dietary folates, resulting in low blood folate levels and consequent hyperhomocysteinemia. Expression of this protein in the brain may be involved in a number of pathological conditions associated with glutamate excitotoxicity. In the prostate the protein is up-regulated in cancerous cells and is used as an effective diagnostic and prognostic indicator of prostate cancer. This gene likely arose from a duplication event of a nearby chromosomal region. Alternative splicing gives rise to multiple transcript variants encoding several different isoforms.

 ADC Antibody

  • Overview
  • Humanized Anti-FOLH1 IgG1-kappa antibody, Capromab
  • Generic name
  • Capromab
  • Host animal
  • Mouse

 ADC Linker

  • Name
  • SMCC (N-succinimidyl 4-(Nmaleimidomethyl)cyclohexane-1-carboxylate)
  • 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
  • DM1 (N2'-Deacetyl-N2'-(3-mercapto-1-oxopropyl)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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