Therapeutic Targets Database
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TTD Target ID: TTDS00271

Target Information
NameTubulin    
Type of targetSuccessful target    
DiseaseCancer, unspecific    [1][2]
Helminth infection    [3]
Leishmania infections    [4][5]
Parasitic diseases    [3]
Drug(s)CabazitaxelApprovedProstate cancer[6]
ColchicineApprovedAcute gouty arthritis[7]
DocetaxelApprovedCancers[8]
EribulinApprovedBreast cancer[6]
IxabepiloneApprovedAggressive metastatic or locally advanced breast cancer no longer responding to currently available chemotherapies[6]
VincristineApprovedAcute lymphoblastic leukemia and nephroblastoma [9][10]
VinorelbineApprovedCancers[11]
EpothilonPhase III completedBreast Cancer, Ovarian cancer[12]
LarotaxelPhase IIIPancreatic K, Bladder K[13]
BNC105Phase IIAdvanced solid tumours[14]
CabazitaxelPhase IISolid Cancer[13]
IndibulinPhase IIAdvanced sarcomar[15]
E 7974Phase IOvarian cancer[12]
PathwayGap junction
Pathogenic Escherichia coli infection
Pathogenic Escherichia coli infection
Target ValidationClick to Find Target Validation Information.    
Inhibitor2- (3-Chloro-phenyl)-1H-[1,8]naphthyridin-4-one[16]
2- (4-Methoxy-phenyl)-1H-indole-3-carbaldehyde[17]
2-Furan-2-yl-7-methyl-1H-[1,8]naphthyridin-4-one[18]
2-Methoxy-5- (3,4,5-trimethoxy-benzyl)-phenol[19]
2-Methoxy-5- (3,4,5-trimethoxy-phenoxy)-phenol[20]
2-Methoxy-5- (5,6,7-trimethoxy-indan-1-yl)-phenol[21]
2-Naphthalen-1-yl-1H-[1,8]naphthyridin-4-one[16]
2-Naphthalen-2-yl-1H-[1,8]naphthyridin-4-one[16]
2-m-Tolyl-1H-[1,8]naphthyridin-4-one[16]
5,7-Dimethyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one[16]
5-Methyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one[16]
6-Methyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one[16]
7-Methyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one[16]
ABT-751[22]
BNC105[14]
CENTAUREIDIN[23]
COLCHINOL[24]
COMBETASTATIN[25]
COMBRETASTATIN[26]
Cabazitaxel[13]
Cabazitaxel[6]
DOLASTATIN-10[27]
Docetaxel[8]
E 7974[12]
Epothilone B[28]
Eribulin[6]
GNF-PF-117[29]
Larotaxel[13]
MR-22388[30]
MYOSEVERIN[31]
NSC-106970[23]
NSC-664171[32]
NSC-679036[16]
PHENSTATIN[33]
RHIZOXIN[34]
THIOCOLCHICINE[35]
Vinorelbine[11]
WR85915[5]
isopropyl 3- (phenylthio)-1H-indole-2-carboxylate[36]
InducerCryptophycin[37]
Eleutherobin[38]
Sarcodictyin A[39]
Taxol[38]
BinderColchicine[7]
Vincristine[9][10]
StablizerEpothilon[12]
Indibulin[15]
Ixabepilone[6]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Tubulin as a target for anticancer drugs: agents which interact with the mitotic spindle. Med Res Rev. 1998 Jul;18(4):259-96. To Reference
Ref 2Characterization of nuclear betaII-tubulin in tumor cells: a possible novel target for taxol. Cell Motil Cytoskeleton. 2002 Sep;53(1):39-52. To Reference
Ref 3Tubulin as an antiprotozoal drug target. Mini Rev Med Chem. 2002 Dec;2(6):519-29. To Reference
Ref 4Purification, characterization, and drug susceptibility of tubulin from Leishmania. Mol Biochem Parasitol. 1999 Jan 5;98(1):53-65. To Reference
Ref 5Cellular effects of leishmanial tubulin inhibitors on L. donovani. Mol Biochem Parasitol. 2000 Oct;110(2):223-36. To Reference
Ref 6Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5. To Reference
Ref 7Vitamin K3 disrupts the microtubule networks by binding to tubulin: a novel mechanism of its antiproliferative activity. Biochemistry. 2009 Jul 28;48(29):6963-74. To Reference
Ref 8Docetaxel: a review of its use in metastatic breast cancer. Drugs. 2005;65(17):2513-31. To Reference
Ref 9Bone marrow CFU-GM and human tumor xenograft efficacy of three tubulin binding agents. Cancer Chemother Pharmacol. 2009 Mar 10. [Epub ahead of print] To Reference
Ref 10Vinflunine, a novel microtubule inhibitor, suppresses calmodulin interaction with the microtubule-associated protein STOP. Biochemistry. 2007 Dec 25;46(51):14899-906. Epub 2007 Dec 4. To Reference
Ref 11Vinca alkaloid and MDR1. Gan To Kagaku Ryoho. 2008 Jul;35(7):1086-9. To Reference
Ref 12Emerging drugs for ovarian cancer. Expert Opin Emerg Drugs. 2008 Sep;13(3):523-36. To Reference
Ref 13Pharma & Vaccines. Product Development Pipeline. April 29 2009. To Reference
Ref 142011 Pipeline of Bionomics Limited. To Reference
Ref 152011 Pipeline of ZioPharm. To Reference
Ref 16J Med Chem. 1997 Sep 12;40(19):3049-56.Antitumor agents. 178. Synthesis and biological evaluation of substituted 2-aryl-1,8-naphthyridin-4(1H)-ones as antitumor agents that inhibit tubulin polymerization. To Reference
Ref 17J Med Chem. 1998 Dec 3;41(25):4965-72.Methoxy-substituted 3-formyl-2-phenylindoles inhibit tubulin polymerization. To Reference
Ref 18J Med Chem. 1999 Oct 7;42(20):4081-7.Antitumor agents. 196. Substituted 2-thienyl-1,8-naphthyridin-4-ones: their synthesis, cytotoxicity, and inhibition of tubulin polymerization. To Reference
Ref 19J 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. To Reference
Ref 20Bioorg Med Chem Lett. 2001 Jan 8;11(1):51-4.Antimitotic and cell growth inhibitory properties of combretastatin A-4-like ethers. To Reference
Ref 21Bioorg Med Chem Lett. 1999 Feb 8;9(3):407-12.The synthesis and evaluation of temperature sensitive tubulin toxins. To Reference
Ref 22J Med Chem. 2002 Oct 24;45(22):4913-22.Array-based structure and gene expression relationship study of antitumor sulfonamides including N-[2-[(4-hydroxyphenyl)amino]-3-pyridinyl]-4-methoxybenzenesulfonamide and N-(3-chloro-7-indolyl)-1,4-benzenedisulfonamide. To Reference
Ref 23J Med Chem. 1998 Jun 18;41(13):2333-8.Structure-activity requirements for flavone cytotoxicity and binding to tubulin. To Reference
Ref 24Bioorg 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. To Reference
Ref 25Bioorg Med Chem Lett. 1998 Aug 4;8(15):1997-2000.Asymmetric synthesis of antimitotic combretadioxolane with potent antitumor activity against multi-drug resistant cells. To Reference
Ref 26J Med Chem. 2006 Jun 29;49(13):3906-15.Synthesis and biological evaluation of 2-amino-3-(3',4',5'-trimethoxybenzoyl)-5-aryl thiophenes as a new class of potent antitubulin agents. To Reference
Ref 27J Med Chem. 1998 Apr 23;41(9):1524-30.Synthesis and biological activity of chimeric structures derived from the cytotoxic natural compounds dolastatin 10 and dolastatin 15. To Reference
Ref 28Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127. To Reference
Ref 29J Med Chem. 1993 Apr 30;36(9):1146-56.Synthesis and cytotoxicity of 1,6,7,8-substituted 2-(4'-substituted phenyl)-4-quinolones and related compounds: identification as antimitotic agents interacting with tubulin. To Reference
Ref 30J Med Chem. 2004 Mar 11;47(6):1448-64.Design, synthesis, and evaluation of novel thienopyrrolizinones as antitubulin agents. To Reference
Ref 31J Med Chem. 2001 Dec 20;44(26):4497-500.Synthesis and biological evaluation of myoseverin derivatives: microtubule assembly inhibitors. To Reference
Ref 32J Med Chem. 1998 Mar 26;41(7):1155-62.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 antimitotic antitumor agents. To Reference
Ref 33J Med Chem. 2002 Jun 6;45(12):2534-42.Antineoplastic agents. 465. Structural modification of resveratrol: sodium resverastatin phosphate. To Reference
Ref 34Bioorg 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. To Reference
Ref 35J Med Chem. 1993 Mar 5;36(5):544-51.Antitumor agents. 139. Synthesis and biological evaluation of thiocolchicine analogs 5,6-dihydro-6(S)-(acyloxy)- and 5,6-dihydro-6(S)-[(aroyloxy)methyl]-1,2,3-trimethoxy-9-(methylthio)-8H- cyclohepta[a]naphthalen-8-ones as novel cytotoxic and antimitotic agents. To Reference
Ref 36J Med Chem. 2006 Feb 9;49(3):947-54.New arylthioindoles: potent inhibitors of tubulin polymerization. 2. Structure-activity relationships and molecular modeling studies. To Reference
Ref 37Single-walled tubulin ring polymers. Biopolymers. 2007 Aug 5-15;86(5-6):424-36. To Reference
Ref 38Eleutherobin, a novel cytotoxic agent that induces tubulin polymerization, is similar to paclitaxel (Taxol). Cancer Res. 1998 Mar 15;58(6):1111-5. To Reference
Ref 39The 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. To Reference



 

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