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 | |||||
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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 | |||||
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Target Poor or Non Binders |
Target Regulators | Top | |||||
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Target-interacting Proteins |
Target Affiliated Biological Pathways | Top | |||||
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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 | |||||
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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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