Target Information
| Target General Information | Top | |||||
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| Target ID |
T43115
(Former ID: TTDR00611)
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| Target Name |
Leukocyte common antigen (PTPRC)
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| Synonyms |
T200; Receptor-type tyrosine-protein phosphatase C; L-CA; CD45 antigen; CD45
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| Gene Name |
PTPRC
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Acute myeloid leukaemia [ICD-11: 2A60] | |||||
| 2 | Transplanted organ/tissue [ICD-11: QB63] | |||||
| Function |
Acts as a positive regulator of T-cell coactivation upon binding to DPP4. The first PTPase domain has enzymatic activity, while the second one seems to affect the substrate specificity of the first one. Upon T-cell activation, recruits and dephosphorylates SKAP1 and FYN. Dephosphorylates LYN, and thereby modulates LYN activity. Protein tyrosine-protein phosphatase required for T-cell activation through the antigen receptor.
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| BioChemical Class |
Phosphoric monoester hydrolase
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| UniProt ID | ||||||
| EC Number |
EC 3.1.3.48
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| Sequence |
MTMYLWLKLLAFGFAFLDTEVFVTGQSPTPSPTGLTTAKMPSVPLSSDPLPTHTTAFSPA
STFERENDFSETTTSLSPDNTSTQVSPDSLDNASAFNTTGVSSVQTPHLPTHADSQTPSA GTDTQTFSGSAANAKLNPTPGSNAISDVPGERSTASTFPTDPVSPLTTTLSLAHHSSAAL PARTSNTTITANTSDAYLNASETTTLSPSGSAVISTTTIATTPSKPTCDEKYANITVDYL YNKETKLFTAKLNVNENVECGNNTCTNNEVHNLTECKNASVSISHNSCTAPDKTLILDVP PGVEKFQLHDCTQVEKADTTICLKWKNIETFTCDTQNITYRFQCGNMIFDNKEIKLENLE PEHEYKCDSEILYNNHKFTNASKIIKTDFGSPGEPQIIFCRSEAAHQGVITWNPPQRSFH NFTLCYIKETEKDCLNLDKNLIKYDLQNLKPYTKYVLSLHAYIIAKVQRNGSAAMCHFTT KSAPPSQVWNMTVSMTSDNSMHVKCRPPRDRNGPHERYHLEVEAGNTLVRNESHKNCDFR VKDLQYSTDYTFKAYFHNGDYPGEPFILHHSTSYNSKALIAFLAFLIIVTSIALLVVLYK IYDLHKKRSCNLDEQQELVERDDEKQLMNVEPIHADILLETYKRKIADEGRLFLAEFQSI PRVFSKFPIKEARKPFNQNKNRYVDILPYDYNRVELSEINGDAGSNYINASYIDGFKEPR KYIAAQGPRDETVDDFWRMIWEQKATVIVMVTRCEEGNRNKCAEYWPSMEEGTRAFGDVV VKINQHKRCPDYIIQKLNIVNKKEKATGREVTHIQFTSWPDHGVPEDPHLLLKLRRRVNA FSNFFSGPIVVHCSAGVGRTGTYIGIDAMLEGLEAENKVDVYGYVVKLRRQRCLMVQVEA QYILIHQALVEYNQFGETEVNLSELHPYLHNMKKRDPPSEPSPLEAEFQRLPSYRSWRTQ HIGNQEENKSKNRNSNVIPYDYNRVPLKHELEMSKESEHDSDESSDDDSDSEEPSKYINA SFIMSYWKPEVMIAAQGPLKETIGDFWQMIFQRKVKVIVMLTELKHGDQEICAQYWGEGK QTYGDIEVDLKDTDKSSTYTLRVFELRHSKRKDSRTVYQYQYTNWSVEQLPAEPKELISM IQVVKQKLPQKNSSEGNKHHKSTPLLIHCRDGSQQTGIFCALLNLLESAETEEVVDIFQV VKALRKARPGMVSTFEQYQFLYDVIASTYPAQNGQVKKNNHQEDKIEFDNEVDKVKQDAN CVNPLGAPEKLPEAKEQAEGSEPTSGTEGPEHSVNGPASPALNQGS 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 | |||||
|---|---|---|---|---|---|---|
| Clinical Trial Drug(s) | [+] 6 Clinical Trial Drugs | + | ||||
| 1 | 131I-labelled aCD45 | Drug Info | Phase 3 | Acute myeloid leukaemia | [2] | |
| 2 | Iomab-B | Drug Info | Phase 3 | Bone marrow transplantation | [3] | |
| 3 | [131I]-BC8 | Drug Info | Phase 2 | leukaemia | [4] | |
| 4 | Anti-CD45 mabs | Drug Info | Phase 1 | Lymphoma | [5] | |
| 5 | Iomab-ACT | Drug Info | Phase 1 | Diffuse large B-cell lymphoma | [6] | |
| 6 | LM-CD45 | Drug Info | Phase 1 | Transplant rejection | [7] | |
| Discontinued Drug(s) | [+] 1 Discontinued Drugs | + | ||||
| 1 | OX-30 | Drug Info | Terminated | Pain | [8] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 2 Inhibitor drugs | + | ||||
| 1 | Iomab-ACT | Drug Info | [12] | |||
| 2 | Asp-BrPmp-Leu | Drug Info | [15] | |||
| Chemical Structure based Activity Landscape of Target | Top |
|---|---|
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-interacting Proteins | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 4 KEGG Pathways | + | ||||
| 1 | Cell adhesion molecules (CAMs) | |||||
| 2 | T cell receptor signaling pathway | |||||
| 3 | Fc gamma R-mediated phagocytosis | |||||
| 4 | Primary immunodeficiency | |||||
| NetPath Pathway | [+] 2 NetPath Pathways | + | ||||
| 1 | TCR Signaling Pathway | |||||
| 2 | IL2 Signaling Pathway | |||||
| Panther Pathway | [+] 3 Panther Pathways | + | ||||
| 1 | B cell activation | |||||
| 2 | JAK/STAT signaling pathway | |||||
| 3 | T cell activation | |||||
| PID Pathway | [+] 6 PID Pathways | + | ||||
| 1 | BCR signaling pathway | |||||
| 2 | TCR signaling in naï | |||||
| 3 | ||||||
| 4 | TCR signaling in naï | |||||
| 5 | ||||||
| 6 | CXCR4-mediated signaling events | |||||
| Reactome | [+] 2 Reactome Pathways | + | ||||
| 1 | Phosphorylation of CD3 and TCR zeta chains | |||||
| 2 | Other semaphorin interactions | |||||
| WikiPathways | [+] 5 WikiPathways | + | ||||
| 1 | Interferon type I signaling pathways | |||||
| 2 | EPO Receptor Signaling | |||||
| 3 | B Cell Receptor Signaling Pathway | |||||
| 4 | TCR signaling | |||||
| 5 | Semaphorin interactions | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | Clinical pipeline report, company report or official report of Actinium Pharmaceuticals. | |||||
| REF 2 | ClinicalTrials.gov (NCT02665065) Study of Iomab-B vs. Conventional Care in Older Subjects With Active, Relapsed or Refractory Acute Myeloid Leukemia (SIERRA). U.S. National Institutes of Health. | |||||
| REF 3 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 4 | Development of a marrow transplant regimen for acute leukemia using targeted hematopoietic irradiation delivered by 131I-labeled anti-CD45 antibody, combined with cyclophosphamide and total body irradiation. Blood. 1995 Feb 15;85(4):1122-31. | |||||
| REF 5 | ClinicalTrials.gov (NCT00078546) EBV-Specific CTLs Following CD45 Antibody to Patients With Epstein-Barr Virus (EBV) + Nasopharyngeal Carcinoma (NPC). U.S. National Institutes of Health. | |||||
| REF 6 | ClinicalTrials.gov (NCT04512716) Iomab-ACT: A Pilot Study of 131-I Apamistamab Followed by CD19-Targeted CAR T-Cell Therapy for Patients With Relapsed or Refractory B-Cell Acute Lymphoblastic Leukemia or Diffuse Large B-Cell Lymphoma. U.S. National Institutes of Health. | |||||
| REF 7 | ClinicalTrials.gov (NCT01678443) Monoclonal Antibody Therapy Before Stem Cell Transplant in Treating Patients With Relapsed or Refractory Lymphoid Malignancies. U.S. National Institutes of Health. | |||||
| REF 8 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027164) | |||||
| REF 9 | 131I-anti-CD45 antibody plus busulfan and cyclophosphamide before allogeneic hematopoietic cell transplantation for treatment of acute myeloid leukemia in first remission. Blood. 2006 Mar 1;107(5):2184-91. | |||||
| REF 10 | Therapeutic target database update 2012: a resource for facilitating target-oriented drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1128-36. | |||||
| REF 11 | CD45 monoclonal antibody-mediated cytolysis of human NK and T lymphoma cells. Haematologica. 2006 Jul;91(7):886-94. | |||||
| REF 12 | Clinical pipeline report, company report or official report of Actinium Pharmaceuticals. | |||||
| REF 13 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002932) | |||||
| REF 14 | CD45 / PTPRC Antibody, Biotin conjugate (OX-30). | |||||
| REF 15 | A protected l-bromophosphonomethylphenylalanine amino acid derivative (BrPmp) for synthesis of irreversible protein tyrosine phosphatase inhibitors. Bioorg Med Chem. 2010 Dec 15;18(24):8679-86. | |||||
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