Target Information
| Target General Information | Top | |||||
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| Target ID |
T05387
(Former ID: TTDC00120)
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| Target Name |
Tissue transglutaminase (TG2)
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| Synonyms |
Transglutaminase-2; Transglutaminase H; Transglutaminase C; Transglutaminase 2; Tranglutaminase 2; TTg; TGase-H; TGase-2; TGase H; TGase C; TGC; TG(C)Protein-glutamine gamma-glutamyltransferase; TG(C); Protein-glutamine gamma-glutamyltransferase 2
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| Gene Name |
TGM2
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| Target Type |
Preclinical target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Kidney fibrosis [ICD-11: GC01] | |||||
| Function |
Catalyzes the cross-linking of proteins and the conjugation of polyamines to proteins.
Click to Show/Hide
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| BioChemical Class |
Acyltransferase
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| UniProt ID | ||||||
| EC Number |
EC 2.3.2.13
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| Sequence |
MAEELVLERCDLELETNGRDHHTADLCREKLVVRRGQPFWLTLHFEGRNYEASVDSLTFS
VVTGPAPSQEAGTKARFPLRDAVEEGDWTATVVDQQDCTLSLQLTTPANAPIGLYRLSLE ASTGYQGSSFVLGHFILLFNAWCPADAVYLDSEEERQEYVLTQQGFIYQGSAKFIKNIPW NFGQFEDGILDICLILLDVNPKFLKNAGRDCSRRSSPVYVGRVVSGMVNCNDDQGVLLGR WDNNYGDGVSPMSWIGSVDILRRWKNHGCQRVKYGQCWVFAAVACTVLRCLGIPTRVVTN YNSAHDQNSNLLIEYFRNEFGEIQGDKSEMIWNFHCWVESWMTRPDLQPGYEGWQALDPT PQEKSEGTYCCGPVPVRAIKEGDLSTKYDAPFVFAEVNADVVDWIQQDDGSVHKSINRSL IVGLKISTKSVGRDEREDITHTYKYPEGSSEEREAFTRANHLNKLAEKEETGMAMRIRVG QSMNMGSDFDVFAHITNNTAEEYVCRLLLCARTVSYNGILGPECGTKYLLNLNLEPFSEK SVPLCILYEKYRDCLTESNLIKVRALLVEPVINSYLLAERDLYLENPEIKIRILGEPKQK RKLVAEVSLQNPLPVALEGCTFTVEGAGLTEEQKTVEIPDPVEAGEEVKVRMDLLPLHMG LHKLVVNFESDKLKAVKGFRNVIIGPA Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| HIT2.0 ID | T26FBV | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Preclinical Drug(s) | [+] 1 Preclinical Drugs | + | ||||
| 1 | NTU281 | Drug Info | Preclinical | Renal fibrosis | [2] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 55 Inhibitor drugs | + | ||||
| 1 | 2-alkyloxy-3-phenylethynyl-4a,5-dihydropyrido[2,3-b]pyrazine derivative 1 | Drug Info | [1] | |||
| 2 | 3-acylidene-2-oxoindole derivative 1 | Drug Info | [1] | |||
| 3 | 3-acylidene-2-oxoindole derivative 2 | Drug Info | [1] | |||
| 4 | Acyl piperidine derivative 2 | Drug Info | [1] | |||
| 5 | Acyl piperidine derivative 3 | Drug Info | [1] | |||
| 6 | Azachalcone derivative 1 | Drug Info | [1] | |||
| 7 | Benzotriazole derivative 1 | Drug Info | [1] | |||
| 8 | Chalcone derivative 5 | Drug Info | [1] | |||
| 9 | Chloroacetyl ester derivative 1 | Drug Info | [1] | |||
| 10 | Dihydroisoxazole derivative 1 | Drug Info | [1] | |||
| 11 | Dihydroisoxazole derivative 2 | Drug Info | [1] | |||
| 12 | Dipeptide analog 2 | Drug Info | [1] | |||
| 13 | Dipeptide analog 3 | Drug Info | [1] | |||
| 14 | Dipeptide analog 4 | Drug Info | [1] | |||
| 15 | Isothiocyanate derivative 1 | Drug Info | [1] | |||
| 16 | Peptide analog 52 | Drug Info | [1] | |||
| 17 | Peptide analog 53 | Drug Info | [1] | |||
| 18 | Peptide analog 54 | Drug Info | [1] | |||
| 19 | PMID26560530-Compound-1 | Drug Info | [1] | |||
| 20 | PMID26560530-Compound-11 | Drug Info | [1] | |||
| 21 | PMID26560530-Compound-12 | Drug Info | [1] | |||
| 22 | PMID26560530-Compound-13 | Drug Info | [1] | |||
| 23 | PMID26560530-Compound-14 | Drug Info | [1] | |||
| 24 | PMID26560530-Compound-15 | Drug Info | [1] | |||
| 25 | PMID26560530-Compound-16 | Drug Info | [1] | |||
| 26 | PMID26560530-Compound-17 | Drug Info | [1] | |||
| 27 | PMID26560530-Compound-18 | Drug Info | [1] | |||
| 28 | PMID26560530-Compound-2 | Drug Info | [1] | |||
| 29 | PMID26560530-Compound-23 | Drug Info | [1] | |||
| 30 | PMID26560530-Compound-24 | Drug Info | [1] | |||
| 31 | PMID26560530-Compound-25 | Drug Info | [1] | |||
| 32 | PMID26560530-Compound-26 | Drug Info | [1] | |||
| 33 | PMID26560530-Compound-27 | Drug Info | [1] | |||
| 34 | PMID26560530-Compound-3 | Drug Info | [1] | |||
| 35 | PMID26560530-Compound-31 | Drug Info | [1] | |||
| 36 | PMID26560530-Compound-32 | Drug Info | [1] | |||
| 37 | PMID26560530-Compound-33 | Drug Info | [1] | |||
| 38 | PMID26560530-Compound-34 | Drug Info | [1] | |||
| 39 | PMID26560530-Compound-35 | Drug Info | [1] | |||
| 40 | PMID26560530-Compound-4 | Drug Info | [1] | |||
| 41 | PMID26560530-Compound-46 | Drug Info | [1] | |||
| 42 | PMID26560530-Compound-47 | Drug Info | [1] | |||
| 43 | PMID26560530-Compound-48 | Drug Info | [1] | |||
| 44 | PMID26560530-Compound-49 | Drug Info | [1] | |||
| 45 | PMID26560530-Compound-5 | Drug Info | [1] | |||
| 46 | PMID26560530-Compound-50 | Drug Info | [1] | |||
| 47 | PMID26560530-Compound-54 | Drug Info | [1] | |||
| 48 | PMID26560530-Compound-6 | Drug Info | [1] | |||
| 49 | PMID26560530-Compound-7 | Drug Info | [1] | |||
| 50 | PMID26560530-Compound-8 | Drug Info | [1] | |||
| 51 | Pyrazolodiazepine derivative 1 | Drug Info | [1] | |||
| 52 | Sulfonamide derivative 9 | Drug Info | [1] | |||
| 53 | Triazole derivative 1 | Drug Info | [1] | |||
| 54 | NTU281 | Drug Info | [2] | |||
| 55 | Guanosine-5'-Diphosphate | Drug Info | [3] | |||
| 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 | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-interacting Proteins | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 1 KEGG Pathways | + | ||||
| 1 | Huntington's disease | |||||
| PID Pathway | [+] 3 PID Pathways | + | ||||
| 1 | Beta1 integrin cell surface interactions | |||||
| 2 | Thromboxane A2 receptor signaling | |||||
| 3 | Alpha9 beta1 integrin signaling events | |||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | Transglutaminase inhibitors: a patent review.Expert Opin Ther Pat. 2016;26(1):49-63. | |||||
| REF 2 | Drugs and Targets in Fibrosis. Front Pharmacol. 2017 Nov 23;8:855. | |||||
| REF 3 | How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | |||||
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