Target Information

Target General Infomation
Target ID
T43189
Former ID
TTDS00271
Target Name
Tubulin
Gene Name
TUBB3
Synonyms
Tubulin beta-4 chain; Tubulin beta-III; TUBB3
Target Type
Successful
Disease Actinic keratosis [ICD9: 702; ICD10: L57.0]
Advanced sarcomar [ICD10: C96.4]
Advanced breast cancer [ICD9: 174, 175; ICD10: C50]
Acute gouty arthritis [ICD9: 274; ICD10: M10]
Breast cancer; Ovarian cancer [ICD9: 174, 175, 183; ICD10: C50, C56]
Breast cancer [ICD9: 174, 175; ICD10: C50]
Breast cancer; Prostate cancer [ICD9:174, 175, 185; ICD10: C50, C61]
Central nervous system disease [ICD10: G00-G99]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Immuno-suppressant [ICD10: T86.0]
Ovarian cancer [ICD9: 183; ICD10: C56]
Pancreatic cancer; Bladder cancer [ICD9: 188; ICD10: C25, C67]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
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 non-exchangeable site on the alpha chain. TUBB3 plays a critical role in proper axon guidance and mantainance.
BioChemical Class
Tubulin family
Target Validation
T43189
UniProt ID
Q13509
Sequence
MREIVHIQAGQCGNQIGAKFWEVISDEHGIDPSGNYVGDSDLQLERISVYYNEASSHKYV
PRAILVDLEPGTMDSVRSGAFGHLFRPDNFIFGQSGAGNNWAKGHYTEGAELVDSVLDVV
RKECENCDCLQGFQLTHSLGGGTGSGMGTLLISKVREEYPDRIMNTFSVVPSPKVSDTVV
EPYNATLSIHQLVENTDETYCIDNEALYDICFRTLKLATPTYGDLNHLVSATMSGVTTSL
RFPGQLNADLRKLAVNMVPFPRLHFFMPGFAPLTARGSQQYRALTVPELTQQMFDAKNMM
AACDPRHGRYLTVATVFRGRMSMKEVDEQMLAIQSKNSSYFVEWIPNNVKVAVCDIPPRG
LKMSSTFIGNSTAIQELFKRISEQFTAMFRRKAFLHWYTGEGMDEMEFTEAESNMNDLVS
EYQQYQDATAEEEGEMYEDDEEESEAQGPK
Drugs and Mode of Action
Drug(s) Cabazitaxel Drug Info Approved Breast cancer; Prostate cancer [531351], [541879]
Colchicine Drug Info Approved Acute gouty arthritis [538354], [542532], [551871]
Docetaxel Drug Info Approved Cancer [536361], [541891]
Eribulin Drug Info Approved Breast cancer [531351], [541895]
Ixabepilone Drug Info Approved Advanced breast cancer [529282], [531351], [541906]
Vinorelbine Drug Info Approved Cancer [536361], [542112]
Epothilon Drug Info Phase 3 Breast cancer; Ovarian cancer [536839]
BMS-184476 Drug Info Phase 2 Cancer [527405]
BMS-188797 Drug Info Phase 2 Cancer [521476], [527913]
BMS-275183 Drug Info Phase 2 Cancer [521864]
Cabazitaxel Drug Info Phase 2 Solid tumours [531351], [541879]
CRYPTOPHYCIN 52 Drug Info Phase 2 Cancer [526539]
DOLASTATIN-10 Drug Info Phase 2 Cancer [521453]
Indibulin Drug Info Phase 2 Advanced sarcomar [551789]
Milataxel Drug Info Phase 2 Cancer [522328]
Soblidotin Drug Info Phase 2 Cancer [521565]
E 7974 Drug Info Phase 1 Ovarian cancer [536839]
SDZ-LAV-694 Drug Info Phase 1 Actinic keratosis [530311]
ABI-013 Drug Info Preclinical Cancer [549895]
Epothilone B Drug Info Discontinued in Phase 3 Cancer [546007]
Larotaxel Drug Info Discontinued in Phase 3 Pancreatic cancer; Bladder cancer [546774]
ATX-201 Drug Info Discontinued in Phase 2 Actinic keratosis [548552]
Cryptophycin Drug Info Discontinued in Phase 2 Discovery agent [545698]
ERBULOZOLE Drug Info Discontinued in Phase 2 Cancer [545429]
RHIZOXIN Drug Info Discontinued in Phase 2 Breast cancer [544988]
ABJ-879 Drug Info Discontinued in Phase 1 Cancer [547922]
Discodermolide Drug Info Discontinued in Phase 1 Immuno-suppressant [546438]
FCE-28161 Drug Info Discontinued in Phase 1 Cancer [546352]
TALTOBULIN Drug Info Discontinued in Phase 1 Cancer [547769]
21-AMINOEPOTHILONE B Drug Info Terminated Cancer [547539]
Docetaxel Drug Info Investigative Cancer [536155]
Inhibitor 2-(3-Chloro-phenyl)-1H-[1,8]naphthyridin-4-one Drug Info [534469]
2-(4-Methoxy-phenyl)-1H-indole-3-carbaldehyde Drug Info [534765]
2-Furan-2-yl-7-methyl-1H-[1,8]naphthyridin-4-one Drug Info [525604]
2-m-Tolyl-1H-[1,8]naphthyridin-4-one Drug Info [534469]
2-Methoxy-5-(3,4,5-trimethoxy-benzyl)-phenol Drug Info [527276]
2-Methoxy-5-(3,4,5-trimethoxy-phenoxy)-phenol Drug Info [525946]
2-Methoxy-5-(5,6,7-trimethoxy-indan-1-yl)-phenol Drug Info [525450]
2-Naphthalen-1-yl-1H-[1,8]naphthyridin-4-one Drug Info [534469]
2-Naphthalen-2-yl-1H-[1,8]naphthyridin-4-one Drug Info [534469]
21-AMINOEPOTHILONE B Drug Info [544107], [551871]
5,7-Dimethyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one Drug Info [534469]
5-Methyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one Drug Info [534469]
6-Methyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one Drug Info [534469]
7-Methyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one Drug Info [534469]
ATX-201 Drug Info [551080]
BMS-184476 Drug Info [544055], [551871]
BMS-188797 Drug Info [526881], [551871]
BMS-275183 Drug Info [531077]
Cabazitaxel Drug Info [531351]
CENTAUREIDIN Drug Info [534652]
COLCHINOL Drug Info [527777]
COMBETASTATIN Drug Info [534795]
CRYPTOPHYCIN 52 Drug Info [526539], [551871]
Docetaxel Drug Info [536155]
DOLASTATIN-10 Drug Info [534612]
E 7974 Drug Info [536839]
Epothilone B Drug Info [537114]
Eribulin Drug Info [531351]
GNF-PF-117 Drug Info [534009]
Isopropyl 3-(phenylthio)-1H-indole-2-carboxylate Drug Info [527999]
Larotaxel Drug Info [549823]
Milataxel Drug Info [549708]
MR-22388 Drug Info [526982]
MYOSEVERIN Drug Info [526222]
NSC-106970 Drug Info [534652]
NSC-664171 Drug Info [534600]
NSC-679036 Drug Info [534469]
PHENSTATIN Drug Info [526346]
RHIZOXIN Drug Info [528337]
SDZ-LAV-694 Drug Info [551570], [551871]
TALTOBULIN Drug Info [530691], [551871]
THIOCOLCHICINE Drug Info [534060]
Vinorelbine Drug Info [536782]
WR85915 Drug Info [535074]
Modulator ABJ-879 Drug Info [528961]
AL-209 Drug Info [531541]
AL-309 Drug Info [531541]
Discodermolide Drug Info [534515]
ERBULOZOLE Drug Info [533220], [551871]
FCE-28161 Drug Info [550854], [551871]
Soblidotin Drug Info [528298]
Binder Colchicine Drug Info [537471]
Inducer Cryptophycin Drug Info [536415]
Eleutherobin Drug Info [538088]
Sarcodictyin A Drug Info [534859]
Stablizer Epothilon Drug Info [536839]
Indibulin Drug Info [551789]
Ixabepilone Drug Info [531351]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
References
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Ref 527913A phase I and pharmacokinetic study of novel taxane BMS-188797 and cisplatin in patients with advanced solid tumours. Br J Cancer. 2006 Jan 16;94(1):79-84.
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Ref 542112(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: 7105).
Ref 542532(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: 7526).
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Ref 526346J Med Chem. 2002 Jun 6;45(12):2534-42.Antineoplastic agents. 465. Structural modification of resveratrol: sodium resverastatin phosphate.
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Ref 527276J Med Chem. 1992 Mar 20;35(6):1058-67.Synthesis of alkoxy-substituted diaryl compounds and correlation of ring separation with inhibition of tubulin polymerization: differential enhancement of inhibitory effects under suboptimal polymerization reaction conditions.
Ref 527777Bioorg Med Chem Lett. 2005 Dec 1;15(23):5154-9. Epub 2005 Sep 28.Synthesis and structure-activity relationships of 1,2,4-triazoles as a novel class of potent tubulin polymerization inhibitors.
Ref 527999J Med Chem. 2006 Feb 9;49(3):947-54.New arylthioindoles: potent inhibitors of tubulin polymerization. 2. Structure-activity relationships and molecular modeling studies.
Ref 528298Antitumor activity of TZT-1027 (Soblidotin). Anticancer Res. 2006 May-Jun;26(3A):1973-81.
Ref 528337Bioorg Med Chem Lett. 2006 Sep 15;16(18):4748-51. Epub 2006 Jul 25.Tubulin polymerization inhibitors with a fluorinated phthalimide skeleton derived from thalidomide.
Ref 528961Novel tubulin-targeting agents: anticancer activity and pharmacologic profile of epothilones and related analogues. Ann Oncol. 2007 Jul;18 Suppl 5:v9-15.
Ref 530691Absolute configurations of tubulin inhibitors taltobulin (HTI-286) and HTI-042 characterized by X-ray diffraction analysis and NMR studies. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1535-8.
Ref 531077A phase 1 study of BMS-275183, a novel oral analogue of paclitaxel given on a daily schedule to patients with advanced malignancies. Invest New Drugs. 2011 Dec;29(6):1426-31.
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Ref 537114Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
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Ref 551080Clinical pipeline report, company report or official report of Kythera Biopharmaceuticals.
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Ref 5517892011 Pipeline of ZioPharm.
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