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Anti-HLA-DRB1 (Apolizumab)-MC-MMAF ADC (ADC-W-1204)

This ADC product is comprised of an anti-HLA-DRB1 monoclonal antibody conjugated via a MC linker to MMAF. The MMAF is targeted to certain cancers by immunerecognition and delivered into cancer cells via receptor mediated endocytosis. Within the cell, MMAF binds to tubulins, interrupts microtubule dynamics, and subsequently, induces cell death.

 ADC Target

  • Name
  • HLA-DRB1
  • Alternative Names
  • HLA-DRB1; major histocompatibility complex, class II, DR beta 1; HLA DR1B; DW2.2/DR2.2; MHC class II antigen; lymphocyte antigen DRB1; MHC class II HLA-DRw10-beta; human leucocyte antigen DRB1; MHC class II HLA-DR beta 1 chain; MHC class II HLA-DR-beta cell surface glycoprotein; HLA class II histocompatibility antigen, DR-1 beta chain; SS1; DRB1; DRw10; HLA-DRB; HLA-DR1B; FLJ75017; FLJ76359;
  • Target Entrez Gene ID
  • 3123
  • Overview
  • HLA-DRB1 belongs to the HLA class II beta chain paralogs. The class II molecule is a heterodimer consisting of an alpha (DRA) and a beta chain (DRB), both anchored in the membrane. It plays a central role in the immune system by presenting peptides derived from extracellular proteins. Class II molecules are expressed in antigen presenting cells (APC: B lymphocytes, dendritic cells, macrophages). The beta chain is approximately 26-28 kDa. It is encoded by 6 exons. Exon one encodes the leader peptide; exons 2 and 3 encode the two extracellular domains; exon 4 encodes the transmembrane domain; and exon 5 encodes the cytoplasmic tail. Within the DR molecule the beta chain contains all the polymorphisms specifying the peptide binding specificities. Hundreds of DRB1 alleles have been described and typing for these polymorphisms is routinely done for bone marrow and kidney transplantation. DRB1 is expressed at a level five times higher than its paralogs DRB3, DRB4 and DRB5. DRB1 is present in all individuals. Allelic variants of DRB1 are linked with either none or one of the genes DRB3, DRB4 and DRB5. There are 4 related pseudogenes: DRB2, DRB6, DRB7, DRB8 and DRB9.

 ADC Antibody

  • Overview
  • Human Anti-HLA-DRB1 IgG1 antibody, Apolizumab
  • Generic name
  • Apolizumab
  • Host animal
  • Mouse

 ADC Linker

  • Name
  • MC (maleimidocaproyl)
  • Description
  • Noncleavable linkers, is considered noncleavable-meaning linker cleavage, and payload release does not depend on the differential properties between the plasma and some cytoplasmic compartments. Instead, the release of the cytotoxic drug is postulated to occur after internalization of the ADC via antigen-mediated endocytosis and delivery to lysosomal compartment, where the antibody is degraded to the level of amino acids through intracellular proteolytic degradation.

 ADC payload drug

  • Name
  • MMAF
  • Description
  • Derived from Auristatin,are water-soluble dolastatin analogs of dolastatin 10. Dolastatin 10 belongs to dolastatin family and it can powerfully bind to tubulin, thus inhibiting polymerization mediated through the binding to the vinca alkaloid binding domain, and causes cell to accumulate in metaphase arrest.

For Research Use Only. NOT FOR CLINICAL USE.

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