Target Information
| Target General Information | Top | |||||
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| Target ID |
T65116
(Former ID: TTDR01229)
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| Target Name |
Ecto-5'-nucleotidase (CD73)
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| Synonyms |
NT5; CD73 antigen; 5'-nucleotidase; 5'-NT
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| Gene Name |
NT5E
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Pancreatic cancer [ICD-11: 2C10] | |||||
| 2 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||||
| Function |
Exhibits AMP-, NAD-, and NMN-nucleosidase activities. Hydrolyzes extracellular nucleotides into membrane permeable nucleosides.
Click to Show/Hide
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| BioChemical Class |
Phosphoric monoester hydrolase
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| UniProt ID | ||||||
| EC Number |
EC 3.1.3.5
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| Sequence |
MCPRAARAPATLLLALGAVLWPAAGAWELTILHTNDVHSRLEQTSEDSSKCVNASRCMGG
VARLFTKVQQIRRAEPNVLLLDAGDQYQGTIWFTVYKGAEVAHFMNALRYDAMALGNHEF DNGVEGLIEPLLKEAKFPILSANIKAKGPLASQISGLYLPYKVLPVGDEVVGIVGYTSKE TPFLSNPGTNLVFEDEITALQPEVDKLKTLNVNKIIALGHSGFEMDKLIAQKVRGVDVVV GGHSNTFLYTGNPPSKEVPAGKYPFIVTSDDGRKVPVVQAYAFGKYLGYLKIEFDERGNV ISSHGNPILLNSSIPEDPSIKADINKWRIKLDNYSTQELGKTIVYLDGSSQSCRFRECNM GNLICDAMINNNLRHTDEMFWNHVSMCILNGGGIRSPIDERNNGTITWENLAAVLPFGGT FDLVQLKGSTLKKAFEHSVHRYGQSTGEFLQVGGIHVVYDLSRKPGDRVVKLDVLCTKCR VPSYDPLKMDEVYKVILPNFLANGGDGFQMIKDELLRHDSGDQDINVVSTYISKMKVIYP AVEGRIKFSTGSHCHGSFSLIFLSLWAVIFVLYQ Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| HIT2.0 ID | T56TFE | |||||
| Drugs and Modes of Action | Top | |||||
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| Clinical Trial Drug(s) | [+] 7 Clinical Trial Drugs | + | ||||
| 1 | AB680 | Drug Info | Phase 1 | Pancreatic cancer | [2] | |
| 2 | CPI-006 | Drug Info | Phase 1 | Advanced cancer | [1] | |
| 3 | GS-1423 | Drug Info | Phase 1 | Solid tumour/cancer | [3] | |
| 4 | LY3475070 | Drug Info | Phase 1 | Solid tumour/cancer | [4] | |
| 5 | NZV930 | Drug Info | Phase 1 | Solid tumour/cancer | [5] | |
| 6 | Oleclumab | Drug Info | Phase 1 | Solid tumour/cancer | [1] | |
| 7 | TJ4309 | Drug Info | Phase 1 | Solid tumour/cancer | [6] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 43 Inhibitor drugs | + | ||||
| 1 | AB680 | Drug Info | [7] | |||
| 2 | LY3475070 | Drug Info | [10] | |||
| 3 | NZV930 | Drug Info | [11] | |||
| 4 | Oleclumab | Drug Info | [1] | |||
| 5 | PMID28870136-Compound-36 | Drug Info | [12] | |||
| 6 | PMID28870136-Compound-37 | Drug Info | [12] | |||
| 7 | PMID28870136-Compound-38 | Drug Info | [12] | |||
| 8 | PMID28870136-Compound-39 | Drug Info | [12] | |||
| 9 | PMID28870136-Compound-40 | Drug Info | [12] | |||
| 10 | PMID28870136-Compound-41 | Drug Info | [12] | |||
| 11 | PMID28870136-Compound-42 | Drug Info | [12] | |||
| 12 | PMID28870136-Compound-43 | Drug Info | [12] | |||
| 13 | PMID28870136-Compound-44 | Drug Info | [12] | |||
| 14 | PMID28870136-Compound-45 | Drug Info | [12] | |||
| 15 | PMID28870136-Compound-46 | Drug Info | [12] | |||
| 16 | PMID28870136-Compound-47 | Drug Info | [12] | |||
| 17 | PMID28870136-Compound-48 | Drug Info | [12] | |||
| 18 | PMID28870136-Compound-49 | Drug Info | [12] | |||
| 19 | PMID28870136-Compound-50 | Drug Info | [12] | |||
| 20 | PMID28870136-Compound-51 | Drug Info | [12] | |||
| 21 | PMID28870136-Compound-52 | Drug Info | [12] | |||
| 22 | PMID28870136-Compound-53 | Drug Info | [12] | |||
| 23 | PMID28870136-Compound-54 | Drug Info | [12] | |||
| 24 | PMID28870136-Compound-55 | Drug Info | [12] | |||
| 25 | PMID28870136-Compound-56 | Drug Info | [12] | |||
| 26 | PMID28870136-Compound-57 | Drug Info | [12] | |||
| 27 | PMID28870136-Compound-58 | Drug Info | [12] | |||
| 28 | PMID28870136-Compound-59 | Drug Info | [12] | |||
| 29 | PMID28870136-Compound-60 | Drug Info | [12] | |||
| 30 | PMID28870136-Compound-61 | Drug Info | [12] | |||
| 31 | PMID28870136-Compound-62 | Drug Info | [12] | |||
| 32 | PMID28870136-Compound-63 | Drug Info | [12] | |||
| 33 | PMID28870136-Compound-64 | Drug Info | [12] | |||
| 34 | PMID28870136-Compound-65 | Drug Info | [12] | |||
| 35 | PMID28870136-Compound-67 | Drug Info | [12] | |||
| 36 | PMID28870136-Compound-68 | Drug Info | [12] | |||
| 37 | PMID28870136-Compound-69 | Drug Info | [12] | |||
| 38 | PMID29166791-Compound-AMPCP | Drug Info | [13] | |||
| 39 | Acid blue 25 | Drug Info | [14] | |||
| 40 | alphabeta-methyleneADP | Drug Info | [15] | |||
| 41 | PSB-0952 | Drug Info | [14] | |||
| 42 | PSB-0963 | Drug Info | [14] | |||
| 43 | RB 2 | Drug Info | [14] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-regulating microRNAs | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| BioCyc | [+] 3 BioCyc Pathways | + | ||||
| 1 | Purine nucleotides degradation | |||||
| 2 | Urate biosynthesis/inosine 5'-phosphate degradation | |||||
| 3 | Adenosine nucleotides degradation | |||||
| KEGG Pathway | [+] 4 KEGG Pathways | + | ||||
| 1 | Purine metabolism | |||||
| 2 | Pyrimidine metabolism | |||||
| 3 | Nicotinate and nicotinamide metabolism | |||||
| 4 | Metabolic pathways | |||||
| Panther Pathway | [+] 2 Panther Pathways | + | ||||
| 1 | Purine metabolism | |||||
| 2 | Pyrimidine Metabolism | |||||
| PID Pathway | [+] 1 PID Pathways | + | ||||
| 1 | HIF-1-alpha transcription factor network | |||||
| Reactome | [+] 1 Reactome Pathways | + | ||||
| 1 | Purine catabolism | |||||
| WikiPathways | [+] 5 WikiPathways | + | ||||
| 1 | Differentiation Pathway | |||||
| 2 | miR-targeted genes in muscle cell - TarBase | |||||
| 3 | miR-targeted genes in lymphocytes - TarBase | |||||
| 4 | miR-targeted genes in epithelium - TarBase | |||||
| 5 | Metabolism of nucleotides | |||||
| 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 (NCT04104672) A Study to Evaluate the Safety and Tolerability of AB680 in Participants With Gastrointestinal Malignancies. U.S. National Institutes of Health. | |||||
| REF 3 | ClinicalTrials.gov (NCT03954704) Study of GS-1423 in Participants With Advanced Solid Tumors. U.S. National Institutes of Health. | |||||
| REF 4 | ClinicalTrials.gov (NCT04148937) A Study of the CD73 Inhibitor LY3475070 Alone or in Combination With Pembrolizumab in Participants With Advanced Cancer. U.S. National Institutes of Health. | |||||
| REF 5 | ClinicalTrials.gov (NCT03549000) A Phase I/Ib Study of NZV930 Alone and in Combination With PDR001 and /or NIR178 in Patients With Advanced Malignancies.. U.S. National Institutes of Health. | |||||
| REF 6 | ClinicalTrials.gov (NCT04322006) A Phase I/II Study of TJ004309 for Advanced Solid Tumor. U.S. National Institutes of Health. | |||||
| REF 7 | Discovery of AB680: A Potent and Selective Inhibitor of CD73. J Med Chem. 2020 Oct 22;63(20):11448-11468. | |||||
| REF 8 | Clinical pipeline report, company report or official report of Corvus Pharmaceuticals. | |||||
| REF 9 | Clinical pipeline report, company report or official report of Agenus. | |||||
| REF 10 | CD73's Potential as an Immunotherapy Target in Gastrointestinal Cancers. Front Immunol. 2020 Apr 15;11:508. | |||||
| REF 11 | Clinical pipeline report, company report or official report of Surface oncology. | |||||
| REF 12 | Ectonucleotidase inhibitors: a patent review (2011-2016).Expert Opin Ther Pat. 2017 Dec;27(12):1291-1304. | |||||
| REF 13 | Evaluation of WO2017098421: GSK's benzothiazine compounds as CD73 inhibitor filings.Expert Opin Ther Pat. 2018 Feb;28(2):167-171. | |||||
| REF 14 | Development of potent and selective inhibitors of ecto-5'-nucleotidase based on an anthraquinone scaffold. J Med Chem. 2010 Mar 11;53(5):2076-86. | |||||
| REF 15 | 5'-Nucleotidase from smooth muscle of small intestine and from brain. Inhibition of nucleotides. Biochemistry. 1975 Jun 3;14(11):2362-6. | |||||
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