Target Information
| Target General Information | Top | |||||
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| Target ID |
T57001
(Former ID: TTDR00892)
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| Target Name |
Cell surface A33 antigen (GPA33)
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| Synonyms |
GPA33; A33 cognate antigen; A33 antigen
Click to Show/Hide
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| Gene Name |
GPA33
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Colorectal cancer [ICD-11: 2B91] | |||||
| Function |
May play a role in cell-cell recognition and signaling.
Click to Show/Hide
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| BioChemical Class |
Immunoglobulin
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| UniProt ID | ||||||
| Sequence |
MVGKMWPVLWTLCAVRVTVDAISVETPQDVLRASQGKSVTLPCTYHTSTSSREGLIQWDK
LLLTHTERVVIWPFSNKNYIHGELYKNRVSISNNAEQSDASITIDQLTMADNGTYECSVS LMSDLEGNTKSRVRLLVLVPPSKPECGIEGETIIGNNIQLTCQSKEGSPTPQYSWKRYNI LNQEQPLAQPASGQPVSLKNISTDTSGYYICTSSNEEGTQFCNITVAVRSPSMNVALYVG IAVGVVAALIIIGIIIYCCCCRGKDDNTEDKEDARPNREAYEEPPEQLRELSREREEEDD YRQEEQRSTGRESPDHLDQ Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| Drugs and Modes of Action | Top | |||||
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| Clinical Trial Drug(s) | [+] 4 Clinical Trial Drugs | + | ||||
| 1 | KRN-330 | Drug Info | Phase 1/2 | Colorectal cancer | [1] | |
| 2 | MGD007 | Drug Info | Phase 1/2 | Colorectal cancer | [2] | |
| 3 | HuA33 | Drug Info | Phase 1 | Colorectal cancer | [3], [4] | |
| 4 | Radiolabelled-huA33 | Drug Info | Phase 1 | Colorectal cancer | [5] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Modulator | [+] 1 Modulator drugs | + | ||||
| 1 | MGD007 | Drug Info | [6] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Similarity Proteins
Human Tissue Distribution
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Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
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| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| References | Top | |||||
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| REF 1 | Phase 1/2 study of KRN330, a fully human anti-A33 monoclonal antibody, plus irinotecan as second-line treatment for patients with metastatic colorectal cancer. Invest New Drugs. 2014 Aug;32(4):682-90. | |||||
| REF 2 | ClinicalTrials.gov (NCT03531632) MGD007 Combined With MGA012 in Relapsed/Refractory Metastatic Colorectal Cancer. U.S. National Institutes of Health. | |||||
| REF 3 | ClinicalTrials.gov (NCT00199797) Phase I Trial of huA33 Plus Chemotherapy in Patients With Metastatic Colorectal Cancer. U.S. National Institutes of Health. | |||||
| REF 4 | Phase I trial of 131I-huA33 in patients with advanced colorectal carcinoma. Clin Cancer Res. 2005 Jul 1;11(13):4818-26. | |||||
| REF 5 | ClinicalTrials.gov (NCT00291486) Capecitabine and 131I-huA33 in Patients With Metastatic Colorectal Cancer. U.S. National Institutes of Health. | |||||
| REF 6 | Bispecific antibodies rise again. Nat Rev Drug Discov. 2014 Nov;13(11):799-801. | |||||
| REF 7 | (124)I-huA33 antibody PET of colorectal cancer. J Nucl Med. 2011 Aug;52(8):1173-80. | |||||
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