Target Information
| Target General Information | Top | |||||
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| Target ID |
T28661
(Former ID: TTDS00389)
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| Target Name |
Tubulin beta-2 chain (TUBB2)
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| Synonyms |
Tubulin beta-2A chain; Tubulin beta class IIa; TUBB4B; BetaII-Tubulin; Beta(II)-Tubulin; Beta(II) isotype of Tubulin
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| Gene Name |
TUBB2A
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||||
| Function |
It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain. Tubulin is the major constituent of microtubules.
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| UniProt ID | ||||||
| Sequence |
MREIVHIQAGQCGNQIGAKFWEVISDEHGIDPTGSYHGDSDLQLERINVYYNEAAGNKYV
PRAILVDLEPGTMDSVRSGPFGQIFRPDNFVFGQSGAGNNWAKGHYTEGAELVDSVLDVV RKESESCDCLQGFQLTHSLGGGTGSGMGTLLISKIREEYPDRIMNTFSVMPSPKVSDTVV EPYNATLSVHQLVENTDETYSIDNEALYDICFRTLKLTTPTYGDLNHLVSATMSGVTTCL RFPGQLNADLRKLAVNMVPFPRLHFFMPGFAPLTSRGSQQYRALTVPELTQQMFDSKNMM AACDPRHGRYLTVAAIFRGRMSMKEVDEQMLNVQNKNSSYFVEWIPNNVKTAVCDIPPRG LKMSATFIGNSTAIQELFKRISEQFTAMFRRKAFLHWYTGEGMDEMEFTEAESNMNDLVS EYQQYQDATADEQGEFEEEEGEDEA Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| Drugs and Modes of Action | Top | |||||
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| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | Vinblastine | Drug Info | Approved | Solid tumour/cancer | [2], [3] | |
| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | DOLASTATIN-10 | Drug Info | Phase 2 | Solid tumour/cancer | [4] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 13 Inhibitor drugs | + | ||||
| 1 | Vinblastine | Drug Info | [1] | |||
| 2 | DOLASTATIN-10 | Drug Info | [5] | |||
| 3 | 2'-amino-3,4,4',5-tetramethoxy-(Z)-stillbene | Drug Info | [6] | |||
| 4 | 2,3'-diamino-3,4,4',5-tetramethoxy-(Z)-stillbene | Drug Info | [6] | |||
| 5 | 2-amino-3,4',5-trimethoxy-(Z)-stillbene | Drug Info | [6] | |||
| 6 | 3,4',5-trimethoxy-(Z)-stilbene | Drug Info | [6] | |||
| 7 | 3,4,4',5-tetramethoxy-(Z)-stilbene | Drug Info | [6] | |||
| 8 | 3-bromo-4,4',5-trimethoxy-(Z)-stilbene | Drug Info | [6] | |||
| 9 | 6-ile-ustiloxin | Drug Info | [5] | |||
| 10 | N-(4-(3-(pyridin-2-yl)acryloyl)phenyl)acetamide | Drug Info | [7] | |||
| 11 | USTILOXIN A | Drug Info | [5] | |||
| 12 | Ustiloxin D | Drug Info | [5] | |||
| 13 | Ustiloxin F | Drug Info | [5] | |||
| 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 | ||
| Co-Targets | Top | |||||
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| Co-Targets | ||||||
| Target Regulators | Top | |||||
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| Target-regulating microRNAs | ||||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | Effect of the antitumor drug vinblastine on nuclear betaII-tubulin in cultured rat kidney mesangial cells. Invest New Drugs. 2003 Feb;21(1):15-20. | |||||
| 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: 6851). | |||||
| REF 3 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 4 | ClinicalTrials.gov (NCT00003677) Dolastatin 10 in Treating Patients With Metastatic Pancreatic Cancer. U.S. National Institutes of Health. | |||||
| REF 5 | Total synthesis and biological evaluation of ustiloxin natural products and two analogs. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4804-7. | |||||
| REF 6 | 2-amino and 2'-aminocombretastatin derivatives as potent antimitotic agents. J Med Chem. 2006 Oct 19;49(21):6412-5. | |||||
| REF 7 | Design and biological evaluation of novel tubulin inhibitors as antimitotic agents using a pharmacophore binding model with tubulin. J Med Chem. 2006 Sep 21;49(19):5664-70. | |||||
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