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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