Target General Infomation
Target ID
T43189 (Former ID: TTDS00271)
Target Name
Tubulin (TUB)
Synonyms
Human tubulin
Gene Name
NO-GeName
Target Type
Successful target
[1]
Disease [+] 3 Target-related Diseases +
1 Breast cancer [ICD-11: 2C60-2C6Y]
2 Gout [ICD-11: FA25]
3 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
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.
UniProt ID
NOUNIPROTAC
Drugs and Modes of Action
Approved Drug(s) [+] 6 Approved Drugs +
1 Cabazitaxel Drug Info Approved Breast cancer [1], [2]
2 Colchicine Drug Info Approved Acute gouty arthritis [3], [4], [5]
3 Docetaxel Drug Info Approved Solid tumour/cancer [6], [7]
4 Eribulin Drug Info Approved Breast cancer [8], [1]
5 Ixabepilone Drug Info Approved Breast cancer [1], [9], [10]
6 Vinorelbine Drug Info Approved Solid tumour/cancer [11], [7]
Clinical Trial Drug(s) [+] 12 Clinical Trial Drugs +
1 Epothilon Drug Info Phase 3 Ovarian cancer [12]
2 BMS-184476 Drug Info Phase 2 Solid tumour/cancer [13]
3 BMS-188797 Drug Info Phase 2 Solid tumour/cancer [14], [15]
4 BMS-275183 Drug Info Phase 2 Solid tumour/cancer [16]
5 CRYPTOPHYCIN 52 Drug Info Phase 2 Solid tumour/cancer [17]
6 DOLASTATIN-10 Drug Info Phase 2 Solid tumour/cancer [18]
7 Indibulin Drug Info Phase 2 Advanced sarcoma [19]
8 Milataxel Drug Info Phase 2 Solid tumour/cancer [20]
9 Soblidotin Drug Info Phase 2 Solid tumour/cancer [21]
10 BAL-101553 Drug Info Phase 1/2 Solid tumour/cancer [22]
11 E 7974 Drug Info Phase 1 Ovarian cancer [12]
12 SDZ-LAV-694 Drug Info Phase 1 Actinic keratosis [23]
Discontinued Drug(s) [+] 10 Discontinued Drugs +
1 Epothilone B Drug Info Discontinued in Phase 3 Solid tumour/cancer [24]
2 Larotaxel Drug Info Discontinued in Phase 3 Bladder cancer [25]
3 ATX-201 Drug Info Discontinued in Phase 2 Actinic keratosis [26]
4 ERBULOZOLE Drug Info Discontinued in Phase 2 Solid tumour/cancer [27]
5 RHIZOXIN Drug Info Discontinued in Phase 2 Breast cancer [28]
6 ABJ-879 Drug Info Discontinued in Phase 1 Solid tumour/cancer [29]
7 Discodermolide Drug Info Discontinued in Phase 1 Immune System disease [30]
8 FCE-28161 Drug Info Discontinued in Phase 1 Solid tumour/cancer [31]
9 TALTOBULIN Drug Info Discontinued in Phase 1 Solid tumour/cancer [32]
10 21-AMINOEPOTHILONE B Drug Info Terminated Solid tumour/cancer [34]
Preclinical Drug(s) [+] 1 Preclinical Drugs +
1 ABI-013 Drug Info Preclinical Solid tumour/cancer [33]
Mode of Action [+] 5 Modes of Action +
Inhibitor [+] 45 Inhibitor drugs +
1 Cabazitaxel Drug Info [1]
2 Docetaxel Drug Info [36]
3 Eribulin Drug Info [1]
4 Vinorelbine Drug Info [37]
5 BMS-184476 Drug Info [4], [38]
6 BMS-188797 Drug Info [4], [39]
7 BMS-275183 Drug Info [40]
8 CRYPTOPHYCIN 52 Drug Info [4], [17]
9 DOLASTATIN-10 Drug Info [41]
10 Milataxel Drug Info [42]
11 BAL-101553 Drug Info [44]
12 E 7974 Drug Info [12]
13 SDZ-LAV-694 Drug Info [4], [45]
14 Epothilone B Drug Info [46]
15 Larotaxel Drug Info [47]
16 ATX-201 Drug Info [48]
17 RHIZOXIN Drug Info [51]
18 TALTOBULIN Drug Info [4], [55]
19 21-AMINOEPOTHILONE B Drug Info [4], [57]
20 2-(3-Chloro-phenyl)-1H-[1,8]naphthyridin-4-one Drug Info [58]
21 2-(4-Methoxy-phenyl)-1H-indole-3-carbaldehyde Drug Info [59]
22 2-Furan-2-yl-7-methyl-1H-[1,8]naphthyridin-4-one Drug Info [60]
23 2-m-Tolyl-1H-[1,8]naphthyridin-4-one Drug Info [58]
24 2-Methoxy-5-(3,4,5-trimethoxy-benzyl)-phenol Drug Info [61]
25 2-Methoxy-5-(3,4,5-trimethoxy-phenoxy)-phenol Drug Info [62]
26 2-Methoxy-5-(5,6,7-trimethoxy-indan-1-yl)-phenol Drug Info [63]
27 2-Naphthalen-1-yl-1H-[1,8]naphthyridin-4-one Drug Info [58]
28 2-Naphthalen-2-yl-1H-[1,8]naphthyridin-4-one Drug Info [58]
29 5,7-Dimethyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one Drug Info [58]
30 5-Methyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one Drug Info [58]
31 6-Methyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one Drug Info [58]
32 7-Methyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one Drug Info [58]
33 CENTAUREIDIN Drug Info [65]
34 COLCHINOL Drug Info [66]
35 COMBETASTATIN Drug Info [67]
36 GNF-PF-117 Drug Info [69]
37 Isopropyl 3-(phenylthio)-1H-indole-2-carboxylate Drug Info [70]
38 MR-22388 Drug Info [71]
39 MYOSEVERIN Drug Info [72]
40 NSC-106970 Drug Info [65]
41 NSC-664171 Drug Info [73]
42 NSC-679036 Drug Info [58]
43 PHENSTATIN Drug Info [74]
44 THIOCOLCHICINE Drug Info [76]
45 WR85915 Drug Info [77]
Binder [+] 1 Binder drugs +
1 Colchicine Drug Info [35]
Stablizer [+] 3 Stablizer drugs +
1 Ixabepilone Drug Info [1]
2 Epothilon Drug Info [12]
3 Indibulin Drug Info [19]
Modulator [+] 7 Modulator drugs +
1 Soblidotin Drug Info [43]
2 ERBULOZOLE Drug Info [4], [50]
3 ABJ-879 Drug Info [52]
4 Discodermolide Drug Info [53]
5 FCE-28161 Drug Info [4], [54]
6 AL-209 Drug Info [64]
7 AL-309 Drug Info [64]
Inducer [+] 3 Inducer drugs +
1 Cryptophycin Drug Info [49]
2 Eleutherobin Drug Info [68]
3 Sarcodictyin A Drug Info [75]
Target Regulators
Target-regulating microRNAs
Target Profiles in Patients
Target Expression
 Profile (TEP)
Target-Related Models and Studies
Target Validation
References
REF 1 Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
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: 6798).
REF 3 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: 7526).
REF 4 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 5 FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 084279.
REF 6 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: 6809).
REF 7 Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.
REF 8 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: 6813).
REF 9 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: 6824).
REF 10 2007 FDA drug approvals: a year of flux. Nat Rev Drug Discov. 2008 Feb;7(2):107-9.
REF 11 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: 7105).
REF 12 Emerging drugs for ovarian cancer. Expert Opin Emerg Drugs. 2008 Sep;13(3):523-36.
REF 13 Phase II trial of the novel taxane BMS-184476 as second-line in non-small-cell lung cancer. Ann Oncol. 2005 Apr;16(4):597-601.
REF 14 A 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.
REF 15 ClinicalTrials.gov (NCT00006086) BMS-188797 and Carboplatin in Treating Patients With Advanced Nonhematologic Cancer. U.S. National Institutes of Health.
REF 16 ClinicalTrials.gov (NCT00359450) Study of BMS-275183 in Patients With Pretreated Locally Advanced or Metastatic NSCLC (Non Small Cell Lung Cancer). U.S. National Institutes of Health.
REF 17 Phase 2 study of cryptophycin 52 (LY355703) in patients previously treated with platinum based chemotherapy for advanced non-small cell lung cancer. Lung Cancer. 2003 Feb;39(2):197-9.
REF 18 ClinicalTrials.gov (NCT00003677) Dolastatin 10 in Treating Patients With Metastatic Pancreatic Cancer. U.S. National Institutes of Health.
REF 19 2011 Pipeline of ZioPharm.
REF 20 ClinicalTrials.gov (NCT00685204) An Efficacy Study of Milataxel (TL139) Administered Orally for Malignant Mesothelioma. U.S. National Institutes of Health.
REF 21 ClinicalTrials.gov (NCT00064220) Soblidotin in Treating Patients With Advanced or Metastatic Soft Tissue Sarcoma. U.S. National Institutes of Health.
REF 22 ClinicalTrials.gov (NCT02490800) Phase 1/2a Study of Oral BAL101553 in Adult Patients With Solid Tumors.
REF 23 Recent patents reveal microtubules as persistent promising target for novel drug development for cancers. Recent Pat Antiinfect Drug Discov. 2009 Nov;4(3):164-82.
REF 24 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005849)
REF 25 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010227)
REF 26 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026557)
REF 27 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003227)
REF 28 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001808)
REF 29 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020424)
REF 30 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008133)
REF 31 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007669)
REF 32 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019128)
REF 33 Clinical pipeline report, company report or official report of Celgene Corporation.
REF 34 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017146)
REF 35 Vitamin K3 disrupts the microtubule networks by binding to tubulin: a novel mechanism of its antiproliferative activity. Biochemistry. 2009 Jul 28;48(29):6963-74.
REF 36 Docetaxel: a review of its use in metastatic breast cancer. Drugs. 2005;65(17):2513-31.
REF 37 Vinca alkaloid and MDR1. Gan To Kagaku Ryoho. 2008 Jul;35(7):1086-9.
REF 38 Phase I trial of the novel taxane BMS-184476 administered in combination with carboplatin every 21 days. Br J Cancer. 2004 July 19; 91(2): 213-218.
REF 39 Phase I and pharmacokinetic study of BMS-188797, a new taxane analog, administered on a weekly schedule in patients with advanced malignancies. Clin Cancer Res. 2003 Nov 1;9(14):5187-94.
REF 40 A 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.
REF 41 Synthesis and biological activity of chimeric structures derived from the cytotoxic natural compounds dolastatin 10 and dolastatin 15. J Med Chem. 1998 Apr 23;41(9):1524-30.
REF 42 J Clin Oncol 28, 2010 (suppl; abstr e13075).
REF 43 Antitumor activity of TZT-1027 (Soblidotin). Anticancer Res. 2006 May-Jun;26(3A):1973-81.
REF 44 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
REF 45 Recent Patents Reveal Microtubules as Persistent Promising Target for Novel Drug Development for Cancers. Recent Patents on Anti-Infective Drug Discovery 12/2009; 4(3):164-82.
REF 46 Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
REF 47 Pharma & Vaccines. Product Development Pipeline. April 29 2009.
REF 48 Clinical pipeline report, company report or official report of Kythera Biopharmaceuticals.
REF 49 Single-walled tubulin ring polymers. Biopolymers. 2007 Aug 5-15;86(5-6):424-36.
REF 50 Influence of the synthetic microtubule inhibitor erbulozole (P.I.N.N.) (R 55 104), a new tubulozole congener, and gamma irradiation on murine tumors in vivo. Eur J Cancer Clin Oncol. 1989 Oct;25(10):1499-504.
REF 51 Tubulin polymerization inhibitors with a fluorinated phthalimide skeleton derived from thalidomide. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4748-51.
REF 52 Novel tubulin-targeting agents: anticancer activity and pharmacologic profile of epothilones and related analogues. Ann Oncol. 2007 Jul;18 Suppl 5:v9-15.
REF 53 The microtubule-stabilizing agent discodermolide competitively inhibits the binding of paclitaxel (Taxol) to tubulin polymers, enhances tubulin nucleation reactions more potently than paclitaxel, andinhibits the growth of paclitaxel-resistant cells. Mol Pharmacol. 1997 Oct;52(4):613-22.
REF 54 CN patent application no. 101065129, A combination of n-(3-metoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulphonamide and an anti-mitotic agent for the treatment of cancer.
REF 55 Absolute 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 56 Cardiovascular and CNS safety profile of ABI-013, a novel nanoparticle albumin-bound (nab) analog of docetaxel. Cancer Research. 01/2011; 70(8 Supplement):2617-2617.
REF 57 Tubulin-Interactive Natural Products as Anticancer Agents. Correction in: J Nat Prod. 2011 May 27; 74(5): 1352.
REF 58 Antitumor agents. 178. Synthesis and biological evaluation of substituted 2-aryl-1,8-naphthyridin-4(1H)-ones as antitumor agents that inhibit tubul... J Med Chem. 1997 Sep 12;40(19):3049-56.
REF 59 Methoxy-substituted 3-formyl-2-phenylindoles inhibit tubulin polymerization. J Med Chem. 1998 Dec 3;41(25):4965-72.
REF 60 Antitumor agents. 196. Substituted 2-thienyl-1,8-naphthyridin-4-ones: their synthesis, cytotoxicity, and inhibition of tubulin polymerization. J Med Chem. 1999 Oct 7;42(20):4081-7.
REF 61 Synthesis of alkoxy-substituted diaryl compounds and correlation of ring separation with inhibition of tubulin polymerization: differential enhance... J Med Chem. 1992 Mar 20;35(6):1058-67.
REF 62 Antimitotic and cell growth inhibitory properties of combretastatin A-4-like ethers. Bioorg Med Chem Lett. 2001 Jan 8;11(1):51-4.
REF 63 The synthesis and evaluation of temperature sensitive tubulin toxins. Bioorg Med Chem Lett. 1999 Feb 8;9(3):407-12.
REF 64 Protection against tauopathy by the drug candidates NAP (davunetide) and D-SAL: biochemical, cellular and behavioral aspects. Curr Pharm Des. 2011;17(25):2603-12.
REF 65 Structure-activity requirements for flavone cytotoxicity and binding to tubulin. J Med Chem. 1998 Jun 18;41(13):2333-8.
REF 66 Synthesis and structure-activity relationships of 1,2,4-triazoles as a novel class of potent tubulin polymerization inhibitors. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5154-9.
REF 67 Asymmetric synthesis of antimitotic combretadioxolane with potent antitumor activity against multi-drug resistant cells. Bioorg Med Chem Lett. 1998 Aug 4;8(15):1997-2000.
REF 68 Eleutherobin, a novel cytotoxic agent that induces tubulin polymerization, is similar to paclitaxel (Taxol). Cancer Res. 1998 Mar 15;58(6):1111-5.
REF 69 Synthesis and cytotoxicity of 1,6,7,8-substituted 2-(4'-substituted phenyl)-4-quinolones and related compounds: identification as antimitotic agent... J Med Chem. 1993 Apr 30;36(9):1146-56.
REF 70 New arylthioindoles: potent inhibitors of tubulin polymerization. 2. Structure-activity relationships and molecular modeling studies. J Med Chem. 2006 Feb 9;49(3):947-54.
REF 71 Design, synthesis, and evaluation of novel thienopyrrolizinones as antitubulin agents. J Med Chem. 2004 Mar 11;47(6):1448-64.
REF 72 Synthesis and biological evaluation of myoseverin derivatives: microtubule assembly inhibitors. J Med Chem. 2001 Dec 20;44(26):4497-500.
REF 73 Antitumor agents. 181. Synthesis and biological evaluation of 6,7,2',3',4'-substituted-1,2,3,4-tetrahydro-2-phenyl-4-quinolones as a new class of a... J Med Chem. 1998 Mar 26;41(7):1155-62.
REF 74 Antineoplastic agents. 465. Structural modification of resveratrol: sodium resverastatin phosphate. J Med Chem. 2002 Jun 6;45(12):2534-42.
REF 75 The coral-derived natural products eleutherobin and sarcodictyins A and B: effects on the assembly of purified tubulin with and without microtubule-associated proteins and binding at the polymer taxoid site. Biochemistry. 1999 Apr 27;38(17):5490-8.
REF 76 Antitumor agents. 139. Synthesis and biological evaluation of thiocolchicine analogs 5,6-dihydro-6(S)-(acyloxy)- and 5,6-dihydro-6(S)-[(aroyloxy)me... J Med Chem. 1993 Mar 5;36(5):544-51.
REF 77 Cellular effects of leishmanial tubulin inhibitors on L. donovani. Mol Biochem Parasitol. 2000 Oct;110(2):223-36.

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