tigatuzumab   Click here for help

GtoPdb Ligand ID: 9334

Synonyms: CS-1008 | humanized LM1 TRA-8
Compound class: Antibody
Comment: Tigatuzumab (CS-1008) is an investigational, humanized agonistic monoclonal antibody directed against human death receptor 5 (TNFRSF10B; a TNF family catalytic receptor for TRAIL), which is expressed on the surface of many types of cancer cells. DR5 contains an intracellular death domain and interacts with FADD (Fas-associated protein with death domain) to mediate apoptisis.
Peptide sequences and structural information for this antibody are available from its IMGT/mAb-DB record. Peptide sequences matching the heavy and light chain variable regions of tigatuzumab are claimed in patent WO2001083560 [1], but this does not provide an affinity value for the antibody vs. DR5. The antibodies described in the patent were tetsed for their ability to induce apoptosis in cells expressing DR5.
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
Bioactivity Comments
The affinity of the humanized antibody is not provided in [1], however the affinity of the original mouse anti-DR5 antibody (TRA-8) from which tigatuzumab is derived provides an approximate affinity (provided in the interaction table below).
Selectivity at catalytic receptors
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
death receptor 5 Primary target of this compound Hs Antibody Agonist ~8.5 pKd - 1
⤷ pKd ~8.5 (Kd ~3x10-9 M) [1]