7E5N
crystal structure of cis assembled TROP-2
Summary for 7E5N
| Entry DOI | 10.2210/pdb7e5n/pdb |
| Descriptor | Tumor-associated calcium signal transducer 2 (1 entity in total) |
| Functional Keywords | trop-2, crystal, sacituzumab, assembly, tumor, antitumor protein |
| Biological source | Homo sapiens (Human) |
| Total number of polymer chains | 4 |
| Total formula weight | 143057.86 |
| Authors | |
| Primary citation | Sun, M.,Zhang, H.,Jiang, M.,Chai, Y.,Qi, J.,Gao, G.F.,Tan, S. Structural insights into the cis and trans assembly of human trophoblast cell surface antigen 2. Iscience, 24:103190-103190, 2021 Cited by PubMed Abstract: Human trophoblast cell surface antigen 2 (TROP-2) is an important target of tumor therapy, and antibody-drug conjugates with sacituzumab targeting TROP-2 have been approved for the treatment of triple-negative breast cancer. Here, we report the crystal structures of TROP-2-ECD, which can be either or dimers depending on which distinct but overlapping interfaces is used to engage with monomers. The or -tetrameric forms of TROP-2 can also be assembled with a non-overlapping interface with either - or dimerization, suggesting that - and dimers cluster on the cell surface. The binding site of sacituzumab on TROP-2 is mapped to be located on a stretched polypeptide in CPD (Q237-Q252), which is not involved in either or interactions. The present findings will improve understanding of the molecular assembly of TROP-2 on tumor cells and shed light on future design of biologics for tumor therapy. PubMed: 34693228DOI: 10.1016/j.isci.2021.103190 PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (3.2 Å) |
Structure validation
Download full validation report
