Details of the Drug-Related molecule(s) Interaction Atlas

General Information of DTT (ID: TTYFKSZ)

• DTT Name: Tubulin beta (TUBB) DTT Info
• Gene Name: TUBB

Molecule-Related Drug & Molecule List

5 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Albendazole	DMYZ57N	Echinococcus granulosus infectious disease		Approved	[1]
Mebendazole	DMO14SG	Ascariasis	1F62	Approved	[1]
Taxol	DMUOT9V	Breast cancer	2C60-2C65	Approved	[2]
Vincristine	DMINOX3	Acute lymphoblastic leukaemia	2A85	Approved	[3]
Vindesine	DMVR628	Acute lymphoblastic leukaemia	2A85	Approved	[4]

19 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Plinabulin	DMD7L48	Non-small-cell lung cancer	2C25.Y	Phase 3	[5]
Batabulin	DMHWE5R	Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[6]
ABT-751	DMNG35S	Solid tumour/cancer	2A00-2F9Z	Phase 2	[7]
BNC-105	DMJC8DR	Mesothelioma	2C51.2	Phase 2	[8]
DOLASTATIN-10	DMDUV1S	Solid tumour/cancer	2A00-2F9Z	Phase 2	[9]
Lexibulin	DMLEX1D	Glioblastoma multiforme	2A00.0	Phase 2	[10]
T-607	DM5C70M	Solid tumour/cancer	2A00-2F9Z	Phase 2	[11]
Verubulin	DMBQC3L	Brain metastases	2D50	Phase 2	[12]
ZD-6126	DMH85M0	Solid tumour/cancer	2A00-2F9Z	Phase 2	[13]
BAL-101553	DMPFGL8	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[14]
1069C	DMSMRC1	Solid tumour/cancer	2A00-2F9Z	Phase 1	[15]
ABI-011	DM1KD7U	Lymphoma	2A80-2A86	Phase 1	[16]
ALB-109564(a)	DMHD615	Solid tumour/cancer	2A00-2F9Z	Phase 1	[17]
CKD-516	DMGSEB0	Solid tumour/cancer	2A00-2F9Z	Phase 1	[18]
DAVLB-HYDRAZIDE	DM4A3U7	Solid tumour/cancer	2A00-2F9Z	Phase 1	[19]
NSC-639829	DMTYGWV	Solid tumour/cancer	2A00-2F9Z	Phase 1	[20]
Simotaxel	DMFK7UR	Solid tumour/cancer	2A00-2F9Z	Phase 1	[21]
STA-5312	DMGPIV0	Solid tumour/cancer	2A00-2F9Z	Phase 1	[22]
Tasidotin hydrochloride	DMKW4AJ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[23]

5 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CEMADOTIN HYDROCHLORIDE	DMIR4FB	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 2	[24]
Epothilone D	DM1WGUT	Breast cancer	2C60-2C65	Discontinued in Phase 2	[25]
RHIZOXIN	DMQ4IKZ	Breast cancer	2C60-2C65	Discontinued in Phase 2	[26]
S-12363	DMS6NAK	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 2	[27]
Denibulin	DM5G43H	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 1	[19]

1 Preclinical Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
KOS-1803	DMFLIC0	Solid tumour/cancer	2A00-2F9Z	Preclinical	[21]

43 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
2'-amino-3,4,4',5-tetramethoxy-(Z)-stillbene	DMUYZA8	Discovery agent	N.A.	Investigative	[28]
2,3'-diamino-3,4,4',5-tetramethoxy-(Z)-stillbene	DM2UWDR	Discovery agent	N.A.	Investigative	[28]
2-(3-Chloro-phenyl)-1H-[1,8]naphthyridin-4-one	DMK6CD9	Discovery agent	N.A.	Investigative	[29]
2-(4-Methoxy-phenyl)-1H-indole-3-carbaldehyde	DMTEQU8	Discovery agent	N.A.	Investigative	[30]
2-amino-3,4',5-trimethoxy-(Z)-stillbene	DMMZ2LI	Discovery agent	N.A.	Investigative	[28]
2-Furan-2-yl-7-methyl-1H-[1,8]naphthyridin-4-one	DMD8ZUH	Discovery agent	N.A.	Investigative	[31]
2-m-Tolyl-1H-[1,8]naphthyridin-4-one	DM9ZVHJ	Discovery agent	N.A.	Investigative	[29]
2-Methoxy-5-(3,4,5-trimethoxy-benzyl)-phenol	DMCGID6	Discovery agent	N.A.	Investigative	[32]
2-Methoxy-5-(3,4,5-trimethoxy-phenoxy)-phenol	DM6CAYV	Discovery agent	N.A.	Investigative	[33]
2-Methoxy-5-(5,6,7-trimethoxy-indan-1-yl)-phenol	DM9LY0Z	Discovery agent	N.A.	Investigative	[34]
2-Naphthalen-1-yl-1H-[1,8]naphthyridin-4-one	DMTSF6A	Discovery agent	N.A.	Investigative	[29]
2-Naphthalen-2-yl-1H-[1,8]naphthyridin-4-one	DM12YH4	Discovery agent	N.A.	Investigative	[29]
3,4',5-trimethoxy-(Z)-stilbene	DMYHC3S	Discovery agent	N.A.	Investigative	[28]
3,4,4',5-tetramethoxy-(Z)-stilbene	DMSN814	Discovery agent	N.A.	Investigative	[28]
3-bromo-4,4',5-trimethoxy-(Z)-stilbene	DMPZ4M8	Discovery agent	N.A.	Investigative	[28]
5,7-Dimethyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one	DMU618S	Discovery agent	N.A.	Investigative	[29]
5-Methyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one	DMH1IVN	Discovery agent	N.A.	Investigative	[29]
6-ile-ustiloxin	DMQF8JG	Discovery agent	N.A.	Investigative	[9]
6-Methyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one	DMAQGZR	Discovery agent	N.A.	Investigative	[29]
7-Methyl-2-m-tolyl-1H-[1,8]naphthyridin-4-one	DM7LGDC	Discovery agent	N.A.	Investigative	[29]
APH-0911	DMYGKW7	Solid tumour/cancer	2A00-2F9Z	Investigative	[21]
ARC-200	DMAZV5D	Solid tumour/cancer	2A00-2F9Z	Investigative	[21]
CENTAUREIDIN	DMCLXO0	Discovery agent	N.A.	Investigative	[35]
COLCHINOL	DM326VN	Discovery agent	N.A.	Investigative	[36]
COMBETASTATIN	DMIKD8X	Discovery agent	N.A.	Investigative	[37]
GNF-PF-117	DM3INUK	Discovery agent	N.A.	Investigative	[38]
IDN-5390	DM1OMSW	Solid tumour/cancer	2A00-2F9Z	Investigative	[21]
Isopropyl 3-(phenylthio)-1H-indole-2-carboxylate	DMS8MBI	Discovery agent	N.A.	Investigative	[39]
MR-22388	DMIQ8GL	Discovery agent	N.A.	Investigative	[40]
MYOSEVERIN	DMX1POR	Discovery agent	N.A.	Investigative	[41]
N-(4-(3-(pyridin-2-yl)acryloyl)phenyl)acetamide	DMRH987	Discovery agent	N.A.	Investigative	[42]
NSC-106970	DMHK0F6	Discovery agent	N.A.	Investigative	[35]
NSC-664171	DMEF603	Discovery agent	N.A.	Investigative	[43]
NSC-679036	DMPO2RU	Discovery agent	N.A.	Investigative	[29]
ON-24160	DMSFQHO	Solid tumour/cancer	2A00-2F9Z	Investigative	[21]
PHENSTATIN	DMJ5GY7	Discovery agent	N.A.	Investigative	[44]
RTA-301	DMLY4C9	Solid tumour/cancer	2A00-2F9Z	Investigative	[21]
Thiocolchicine	DMJSKIP	Discovery agent	N.A.	Investigative	[45]
TL-1892	DMAHG9E	Solid tumour/cancer	2A00-2F9Z	Investigative	[21]
USTILOXIN A	DMZP32O	Discovery agent	N.A.	Investigative	[9]
Ustiloxin D	DMA8JH7	Discovery agent	N.A.	Investigative	[9]
Ustiloxin F	DMT1LS0	Discovery agent	N.A.	Investigative	[9]
XN-0502	DMXH6DL	Solid tumour/cancer	2A00-2F9Z	Investigative	[21]

References

• [1] Flubendazole interferes with a wide spectrum of cell homeostatic mechanisms in Echinococcus granulosus protoscoleces. Parasitol Int. 2009 Sep;58(3):270-7.
• [2] Paclitaxel directly binds to Bcl-2 and functionally mimics activity of Nur77. Cancer Res. 2009 Sep 1;69(17):6906-14.
• [3] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [4] Antiproliferating activity of the mitotic inhibitor pironetin against vindesine- and paclitaxel-resistant human small cell lung cancer H69 cells. Anticancer Res. 2007 Mar-Apr;27(2):729-36.
• [5] NPI-2358 is a tubulin-depolymerizing agent: in-vitro evidence for activity as a tumor vascular-disrupting agent. Anticancer Drugs. 2006 Jan;17(1):25-31.
• [6] Hydrophilic, pro-drug analogues of T138067 are efficacious in controlling tumor growth in vivo and show a decreased ability to cross the blood brain barrier. J Med Chem. 2001 Oct 25;44(22):3599-605.
• [7] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [8] The vascular disrupting agent BNC105 potentiates the efficacy of VEGF and mTOR inhibitors in renal and breast cancer.Cancer Biol Ther.2014;15(11):1552-60.
• [9] Total synthesis and biological evaluation of ustiloxin natural products and two analogs. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4804-7.
• [10] National Cancer Institute Drug Dictionary (drug id 598799).
• [11] Nucleophilic reactions of N-ethoxycarbonyliminopyridinium ylide with alpha,beta-unsaturated carbonyl compounds. Volume 28, Issue 6, 1972, Pages 1469-1476.
• [12] Effects of the tumor-vasculature-disrupting agent verubulin and two heteroaryl analogues on cancer cells, endothelial cells, and blood vessels.ChemMedChem.2014 Apr;9(4):847-54.
• [13] Phase I clinical evaluation of ZD6126, a novel vascular-targeting agent, in patients with solid tumors. Invest New Drugs. 2008 Apr;26(2):159-67.
• [14] Initial testing (stage 1) of BAL101553, a novel tubulin binding agent, by the pediatric preclinical testing program. Pediatr Blood Cancer. 2015 Jun;62(6):1106-9.
• [15] Patent WO2005108424 A1.
• [16] Company report (Indena)
• [17] 2010 ASCO Annual Meeting
• [18] CKD-516 displays vascular disrupting properties and enhances anti-tumor activity in combination with chemotherapy in a murine tumor model. Invest New Drugs. 2014 Jun;32(3):400-11.
• [19] An Overview of Tubulin Inhibitors That Interact with the Colchicine Binding Site. Pharm Res. 2012 November; 29(11): 2943-2971.
• [20] Solubilization of NSC-639829. Int J Pharm. 2001 Aug 28;225(1-2):41-7.
• [21] 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. (Target id: 2640).
• [22] Conjugated indole-imidazole derivatives displaying cytotoxicity against multidrug resistant cancer cell lines. Bioorganic & Medicinal Chemistry Letters. 11/2006; 16(19):5164-8.
• [23] Intracellular activation and deactivation of tasidotin, an analog of dolastatin 15: correlation with cytotoxicity. Mol Pharmacol. 2009 Jan;75(1):218-26.
• [24] Suppression of microtubule dynamics by binding of cemadotin to tubulin: possible mechanism for its antitumor action. Biochemistry. 1998 Dec 15;37(50):17571-8.
• [25] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [26] Tubulin polymerization inhibitors with a fluorinated phthalimide skeleton derived from thalidomide. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4748-51.
• [27] Microtubule assembly protects the region 28-38 of the beta- tubulin subunit. Article first published online: 4 FEB 2005.
• [28] 2-amino and 2'-aminocombretastatin derivatives as potent antimitotic agents. J Med Chem. 2006 Oct 19;49(21):6412-5.
• [29] 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.
• [30] Methoxy-substituted 3-formyl-2-phenylindoles inhibit tubulin polymerization. J Med Chem. 1998 Dec 3;41(25):4965-72.
• [31] 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.
• [32] 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.
• [33] Antimitotic and cell growth inhibitory properties of combretastatin A-4-like ethers. Bioorg Med Chem Lett. 2001 Jan 8;11(1):51-4.
• [34] The synthesis and evaluation of temperature sensitive tubulin toxins. Bioorg Med Chem Lett. 1999 Feb 8;9(3):407-12.
• [35] Structure-activity requirements for flavone cytotoxicity and binding to tubulin. J Med Chem. 1998 Jun 18;41(13):2333-8.
• [36] 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.
• [37] 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.
• [38] 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.
• [39] 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.
• [40] Design, synthesis, and evaluation of novel thienopyrrolizinones as antitubulin agents. J Med Chem. 2004 Mar 11;47(6):1448-64.
• [41] Synthesis and biological evaluation of myoseverin derivatives: microtubule assembly inhibitors. J Med Chem. 2001 Dec 20;44(26):4497-500.
• [42] 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.
• [43] 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.
• [44] Antineoplastic agents. 465. Structural modification of resveratrol: sodium resverastatin phosphate. J Med Chem. 2002 Jun 6;45(12):2534-42.
• [45] 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.