Target Information
| Target General Information | Top | |||||
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| Target ID |
T13057
(Former ID: TTDR01263)
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| Target Name |
Protein-tyrosine phosphatase SHP-2 (PTPN11)
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| Synonyms |
Tyrosine-protein phosphatase non-receptor type 11; SHPTP2; SHP2; SHP-2; SH-PTP3; SH-PTP2; Protein-tyrosine phosphatase SHP2; Protein-tyrosine phosphatase 2C; Protein-tyrosine phosphatase 1D; PTP2C; PTP-2C; PTP-1D
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| Gene Name |
PTPN11
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||||
| Function |
Positively regulates MAPK signal transduction pathway. Dephosphorylates GAB1, ARHGAP35 and EGFR. Dephosphorylates ROCK2 at 'Tyr-722' resulting in stimulatation of its RhoA binding activity. Dephosphorylates CDC73. Acts downstream of various receptor and cytoplasmic protein tyrosine kinases to participate in the signal transduction from the cell surface to the nucleus.
Click to Show/Hide
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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 |
MTSRRWFHPNITGVEAENLLLTRGVDGSFLARPSKSNPGDFTLSVRRNGAVTHIKIQNTG
DYYDLYGGEKFATLAELVQYYMEHHGQLKEKNGDVIELKYPLNCADPTSERWFHGHLSGK EAEKLLTEKGKHGSFLVRESQSHPGDFVLSVRTGDDKGESNDGKSKVTHVMIRCQELKYD VGGGERFDSLTDLVEHYKKNPMVETLGTVLQLKQPLNTTRINAAEIESRVRELSKLAETT DKVKQGFWEEFETLQQQECKLLYSRKEGQRQENKNKNRYKNILPFDHTRVVLHDGDPNEP VSDYINANIIMPEFETKCNNSKPKKSYIATQGCLQNTVNDFWRMVFQENSRVIVMTTKEV ERGKSKCVKYWPDEYALKEYGVMRVRNVKESAAHDYTLRELKLSKVGQGNTERTVWQYHF RTWPDHGVPSDPGGVLDFLEEVHHKQESIMDAGPVVVHCSAGIGRTGTFIVIDILIDIIR EKGVDCDIDVPKTIQMVRSQRSGMVQTEAQYRFIYMAVQHYIETLQRRIEEEQKSKRKGH EYTNIKYSLADQTSGDQSPLPPCTPTPPCAEMREDSARVYENVGLMQQQKSFR Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| HIT2.0 ID | T51K6D | |||||
| Drugs and Modes of Action | Top | |||||
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| Clinical Trial Drug(s) | [+] 6 Clinical Trial Drugs | + | ||||
| 1 | JAB-3312 | Drug Info | Phase 1/2 | Solid tumour/cancer | [2] | |
| 2 | BBP-398 | Drug Info | Phase 1 | Solid tumour/cancer | [3] | |
| 3 | JAB-3068 | Drug Info | Phase 1 | Solid tumour/cancer | [4] | |
| 4 | RLY-1971 | Drug Info | Phase 1 | Solid tumour/cancer | [5] | |
| 5 | SAR442720 | Drug Info | Phase 1 | Solid tumour/cancer | [6] | |
| 6 | TNO155 | Drug Info | Phase 1 | Solid tumour/cancer | [1] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 8 Inhibitor drugs | + | ||||
| 1 | JAB-3312 | Drug Info | [7] | |||
| 2 | BBP-398 | Drug Info | [3] | |||
| 3 | JAB-3068 | Drug Info | [7] | |||
| 4 | RLY-1971 | Drug Info | [8] | |||
| 5 | SAR442720 | Drug Info | [9] | |||
| 6 | TNO155 | Drug Info | [1] | |||
| 7 | NSC-87877 | Drug Info | [10] | |||
| 8 | Dodecane-Trimethylamine | Drug Info | [11] | |||
| Chemical Structure based Activity Landscape of Target | Top |
|---|---|
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
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| Target-regulating microRNAs | ||||||
| Target-interacting Proteins | ||||||
| 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 the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 2 | ClinicalTrials.gov (NCT04720976) JAB-3312 Activity in Adult Patients With Advanced Solid Tumors. U.S. National Institutes of Health. | |||||
| REF 3 | ClinicalTrials.gov (NCT04528836) First-in-Human Study of the SHP2 Inhibitor BBP-398 in Patients With Advanced Solid Tumors. U.S. National Institutes of Health. | |||||
| REF 4 | ClinicalTrials.gov (NCT03518554) A First in Human, Dose Escalation Study of JAB-3068 (SHP2 Inhibitor) in Adult Patients With Advanced Solid Tumors. U.S. National Institutes of Health. | |||||
| REF 5 | ClinicalTrials.gov (NCT04252339) RLY-1971 in Subjects With Advanced or Metastatic Solid Tumors. U.S. National Institutes of Health. | |||||
| REF 6 | ClinicalTrials.gov (NCT04418661) Safety Study of SAR442720 in Combination With Pembrolizumab in Patients With Advanced Malignancies. U.S. National Institutes of Health. | |||||
| REF 7 | Clinical pipeline report, company report or official report of AbbVie. | |||||
| REF 8 | Clinical pipeline report, company report or official report of Relay Therapeutics. | |||||
| REF 9 | Clinical pipeline report, company report or official report of Revolution Medicines. | |||||
| REF 10 | Inhibitors of Src homology-2 domain containing protein tyrosine phosphatase-2 (Shp2) based on oxindole scaffolds. J Med Chem. 2008 Aug 28;51(16):4948-56. | |||||
| REF 11 | How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | |||||
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