Target Information

Target General Infomation
Target ID
T28661
Former ID
TTDS00389
Target Name
Tubulin beta-2 chain
Gene Name
TUBB4B
Synonyms
Beta(II) isotype of Tubulin; Beta(II)-Tubulin; BetaII-Tubulin; TUBB4B
Target Type
Successful
Disease Cancer [ICD9: 140-229; ICD10: C00-C96]
Function
Tubulin is the major constituent of microtubules. It binds two moles of gtp, one at an exchangeable site on the beta chain and one at a nonexchangeable site on the alpha-chain.
Target Validation
T28661
UniProt ID
P68371
Sequence
MREIVHLQAGQCGNQIGAKFWEVISDEHGIDPTGTYHGDSDLQLERINVYYNEATGGKYV
PRAVLVDLEPGTMDSVRSGPFGQIFRPDNFVFGQSGAGNNWAKGHYTEGAELVDSVLDVV
RKEAESCDCLQGFQLTHSLGGGTGSGMGTLLISKIREEYPDRIMNTFSVVPSPKVSDTVV
EPYNATLSVHQLVENTDETYCIDNEALYDICFRTLKLTTPTYGDLNHLVSATMSGVTTCL
RFPGQLNADLRKLAVNMVPFPRLHFFMPGFAPLTSRGSQQYRALTVPELTQQMFDAKNMM
AACDPRHGRYLTVAAVFRGRMSMKEVDEQMLNVQNKNSSYFVEWIPNNVKTAVCDIPPRG
LKMSATFIGNSTAIQELFKRISEQFTAMFRRKAFLHWYTGEGMDEMEFTEAESNMNDLVS
EYQQYQDATAEEEGEFEEEAEEEVA
Drugs and Mode of Action
Drug(s) Vinblastine Drug Info Approved Cancer [541931], [551871]
DOLASTATIN-10 Drug Info Phase 2 Cancer [521453]
Inhibitor 2'-amino-3,4,4',5-tetramethoxy-(Z)-stillbene Drug Info [528474]
2,3'-diamino-3,4,4',5-tetramethoxy-(Z)-stillbene Drug Info [528474]
2-amino-3,4',5-trimethoxy-(Z)-stillbene Drug Info [528474]
3,4',5-trimethoxy-(Z)-stilbene Drug Info [528474]
3,4,4',5-tetramethoxy-(Z)-stilbene Drug Info [528474]
3-bromo-4,4',5-trimethoxy-(Z)-stilbene Drug Info [528474]
6-ile-ustiloxin Drug Info [528306]
DOLASTATIN-10 Drug Info [528306]
N-(4-(3-(pyridin-2-yl)acryloyl)phenyl)acetamide Drug Info [528428]
USTILOXIN A Drug Info [528306]
Ustiloxin D Drug Info [528306]
Ustiloxin F Drug Info [528306]
Vinblastine Drug Info [535740]
References
Ref 521453ClinicalTrials.gov (NCT00003677) Dolastatin 10 in Treating Patients With Metastatic Pancreatic Cancer. U.S. National Institutes of Health.
Ref 541931(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 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 528306Bioorg Med Chem Lett. 2006 Sep 15;16(18):4804-7. Epub 2006 Jul 11.Total synthesis and biological evaluation of ustiloxin natural products and two analogs.
Ref 528428J Med Chem. 2006 Sep 21;49(19):5664-70.Design and biological evaluation of novel tubulin inhibitors as antimitotic agents using a pharmacophore binding model with tubulin.
Ref 528474J Med Chem. 2006 Oct 19;49(21):6412-5.2-amino and 2'-aminocombretastatin derivatives as potent antimitotic agents.
Ref 535740Effect of the antitumor drug vinblastine on nuclear betaII-tubulin in cultured rat kidney mesangial cells. Invest New Drugs. 2003 Feb;21(1):15-20.

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