Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T92308
(Former ID: TTDS00312)
|
|||||
| Target Name |
DNA [cytosine-5]-methyltransferase (DNMT)
|
|||||
| Synonyms |
DNA MTase
Click to Show/Hide
|
|||||
| Gene Name |
NO-GeName
|
|||||
| Target Type |
Successful target
|
[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Myelodysplastic syndrome [ICD-11: 2A37] | |||||
| Function |
This methylase recognizes the double-stranded sequence ccwgg, causes specific methylation on c-2 on both strands.
Click to Show/Hide
|
|||||
| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | Azacitidine | Drug Info | Approved | Myelodysplastic syndrome | [1], [2] | |
| Clinical Trial Drug(s) | [+] 3 Clinical Trial Drugs | + | ||||
| 1 | ASTX727 | Drug Info | Phase 3 | Chronic myelogenous leukaemia | [3] | |
| 2 | Curcumin | Drug Info | Phase 3 | Solid tumour/cancer | [4], [5] | |
| 3 | S-110 | Drug Info | Phase 3 | Acute myeloid leukaemia | [3], [6] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 25 Inhibitor drugs | + | ||||
| 1 | Azacitidine | Drug Info | [1] | |||
| 2 | ASTX727 | Drug Info | [3] | |||
| 3 | Curcumin | Drug Info | [7] | |||
| 4 | S-110 | Drug Info | [8] | |||
| 5 | PMID27376512-Compound-CROs | Drug Info | [9] | |||
| 6 | PMID27376512-Compound-MTC-434 | Drug Info | [9] | |||
| 7 | PMID27376512-Compound-PG-11047 | Drug Info | [9] | |||
| 8 | PMID27376512-Compound-PG-11048 | Drug Info | [9] | |||
| 9 | (L-)-S-adenosyl-L-homocysteine | Drug Info | [7], [10] | |||
| 10 | NSC-106084 | Drug Info | [7] | |||
| 11 | NSC-137546 | Drug Info | [7] | |||
| 12 | NSC-138419 | Drug Info | [7] | |||
| 13 | NSC-154957 | Drug Info | [7] | |||
| 14 | NSC-158324 | Drug Info | [7] | |||
| 15 | NSC-319745 | Drug Info | [7] | |||
| 16 | NSC-345763 | Drug Info | [7] | |||
| 17 | NSC-348926 | Drug Info | [7] | |||
| 18 | NSC-401077 | Drug Info | [7] | |||
| 19 | NSC-54162 | Drug Info | [7] | |||
| 20 | NSC-56071 | Drug Info | [7] | |||
| 21 | NSC-57893 | Drug Info | [7] | |||
| 22 | NSC-622444 | Drug Info | [7] | |||
| 23 | NSC-622445 | Drug Info | [7] | |||
| 24 | NSC-623548 | Drug Info | [7] | |||
| 25 | S-tubercidinylhomocysteine | Drug Info | [11] | |||
| Drug Property Profile of Target | Top | |
|---|---|---|
| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
|
|
||
| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
|
|
||
| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
|
|
||
| "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 | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | The DNA methyltransferase inhibitors azacitidine, decitabine and zebularine exert differential effects on cancer gene expression in acute myeloid l... Leukemia. 2009 Jun;23(6):1019-28. | |||||
| REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6796). | |||||
| REF 3 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 4 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7000). | |||||
| REF 5 | Nanocurcumin: a promising therapeutic advancement over native curcumin. Crit Rev Ther Drug Carrier Syst. 2013;30(4):331-68. | |||||
| REF 6 | ClinicalTrials.gov (NCT02348489) SGI-110 in Adults With Untreated Acute Myeloid Leukemia (AML), Not Considered Candidates for Intensive Remission Induction. U.S. National Institutes of Health. | |||||
| REF 7 | Novel and selective DNA methyltransferase inhibitors: Docking-based virtual screening and experimental evaluation. Bioorg Med Chem. 2010 Jan 15;18(2):822-9. | |||||
| REF 8 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 9 | DNA methyltransferase inhibitors: an updated patent review (2012-2015).Expert Opin Ther Pat. 2016 Sep;26(9):1017-30. | |||||
| REF 10 | Constrained (l-)-S-adenosyl-l-homocysteine (SAH) analogues as DNA methyltransferase inhibitors. Bioorg Med Chem Lett. 2009 May 15;19(10):2742-6. | |||||
| REF 11 | SAR around (l)-S-adenosyl-l-homocysteine, an inhibitor of human DNA methyltransferase (DNMT) enzymes. Bioorg Med Chem Lett. 2009 May 15;19(10):2747-51. | |||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.