Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTBGTCW)

• DTT Name: Kinesin spindle messenger RNA (KIF11 mRNA)
• Synonyms: Thyroid receptor-interacting protein 5 (mRNA); TRIP5 (mRNA); TRIP-5 (mRNA); TR-interacting protein 5 (mRNA); Kinesin-related motor protein Eg5 (mRNA); Kinesin-like spindle protein HKSP (mRNA); Kinesin-like protein KIF11 (mRNA); Kinesin-like protein 1 (mRNA); KNSL1 (mRNA); EG5 (mRNA)
• Gene Name: KIF11
• DTT Type: Clinical trial target; [1]
• BioChemical Class: mRNA target
• UniProt ID: KIF11_HUMAN
• TTD ID: T63986
• Sequence:
  MASQPNSSAKKKEEKGKNIQVVVRCRPFNLAERKASAHSIVECDPVRKEVSVRTGGLADK
  SSRKTYTFDMVFGASTKQIDVYRSVVCPILDEVIMGYNCTIFAYGQTGTGKTFTMEGERS
  PNEEYTWEEDPLAGIIPRTLHQIFEKLTDNGTEFSVKVSLLEIYNEELFDLLNPSSDVSE
  RLQMFDDPRNKRGVIIKGLEEITVHNKDEVYQILEKGAAKRTTAATLMNAYSSRSHSVFS
  VTIHMKETTIDGEELVKIGKLNLVDLAGSENIGRSGAVDKRAREAGNINQSLLTLGRVIT
  ALVERTPHVPYRESKLTRILQDSLGGRTRTSIIATISPASLNLEETLSTLEYAHRAKNIL
  NKPEVNQKLTKKALIKEYTEEIERLKRDLAAAREKNGVYISEENFRVMSGKLTVQEEQIV
  ELIEKIGAVEEELNRVTELFMDNKNELDQCKSDLQNKTQELETTQKHLQETKLQLVKEEY
  ITSALESTEEKLHDAASKLLNTVEETTKDVSGLHSKLDRKKAVDQHNAEAQDIFGKNLNS
  LFNNMEELIKDGSSKQKAMLEVHKTLFGNLLSSSVSALDTITTVALGSLTSIPENVSTHV
  SQIFNMILKEQSLAAESKTVLQELINVLKTDLLSSLEMILSPTVVSILKINSQLKHIFKT
  SLTVADKIEDQKKELDGFLSILCNNLHELQENTICSLVESQKQCGNLTEDLKTIKQTHSQ
  ELCKLMNLWTERFCALEEKCENIQKPLSSVQENIQQKSKDIVNKMTFHSQKFCADSDGFS
  QELRNFNQEGTKLVEESVKHSDKLNGNLEKISQETEQRCESLNTRTVYFSEQWVSSLNER
  EQELHNLLEVVSQCCEASSSDITEKSDGRKAAHEKQHNIFLDQMTIDEDKLIAQNLELNE
  TIKIGLTKLNCFLEQDLKLDIPTGTTPQRKSYLYPSTLVRTEPREHLLDQLKRKQPELLM
  MLNCSENNKEETIPDVDVEEAVLGQYTEEPLSQEPSVDAGVDCSSIGGVPFFQHKKSHGK
  DKENRGINTLERSKVEETTEHLVTKSRLPLRAQINL
• Function: Required in non-mitotic cells for transport of secretory proteins from the Golgi complex to the cell surface. Motor protein required for establishing a bipolar spindle during mitosis.
• Reactome Pathway:
  Kinesins (R-HSA-983189)
  MHC class II antigen presentation (R-HSA-2132295)

Molecular Interaction Atlas (MIA) of This DTT

2 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ALN-VSP	DM89DHO	Liver cancer	2C12	Phase 1	[1]
EMD-534085	DMQ6YAZ	Haematological malignancy	2B33.Y	Phase 1	[2]

57 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(S)-dimethylenastron	DM0SEYN	Discovery agent	N.A.	Investigative	[3]
(S)-enastron	DMWNEA1	Discovery agent	N.A.	Investigative	[3]
1-(7-methyl-9H-carbazol-3-yl)ethanone	DMKHJBI	Discovery agent	N.A.	Investigative	[4]
1-(trifluoromethyl)-9H-carbazole	DMD6CHB	Discovery agent	N.A.	Investigative	[4]
1-tert-butyl-9H-carbazole	DMPSM4O	Discovery agent	N.A.	Investigative	[4]
11H-benzo[a]carbazole	DMK41DJ	Discovery agent	N.A.	Investigative	[4]
2,3,4,11-tetrahydro-1H-benzo[a]carbazole	DMV1CX0	Discovery agent	N.A.	Investigative	[4]
2-(difluoromethyl)-9H-carbazole	DMZVMDO	Discovery agent	N.A.	Investigative	[4]
2-(trifluoromethoxy)-9H-carbazole	DMDL8KY	Discovery agent	N.A.	Investigative	[4]
2-(trifluoromethyl)-9H-carbazole	DM7M6T3	Discovery agent	N.A.	Investigative	[4]
2-ethyl-9H-carbazole	DMN8W1H	Discovery agent	N.A.	Investigative	[4]
2-isopropyl-9H-carbazole	DMSLMAN	Discovery agent	N.A.	Investigative	[4]
2-methyl-6-(trifluoromethyl)-9H-carbazole	DMJYSF3	Discovery agent	N.A.	Investigative	[4]
2-methyl-9H-carbazole	DM06TZN	Discovery agent	N.A.	Investigative	[4]
2-tert-butoxy-9H-carbazole	DM26NKG	Discovery agent	N.A.	Investigative	[4]
2-tert-butyl-7-(trifluoromethyl)-9H-carbazole	DMJBQD8	Discovery agent	N.A.	Investigative	[4]
2-tert-butyl-9H-carbazole	DM6M8Y3	Discovery agent	N.A.	Investigative	[4]
3-(trifluoromethyl)-9H-carbazole	DMWX4L5	Discovery agent	N.A.	Investigative	[4]
3-methyl-6-(trifluoromethyl)-9H-carbazole	DM3BL45	Discovery agent	N.A.	Investigative	[4]
3-tert-butyl-9H-carbazole	DMY57CV	Discovery agent	N.A.	Investigative	[4]
4'-(trifluoromethyl)-4-biphenylol	DMMWZLC	Discovery agent	N.A.	Investigative	[5]
4'-(trifluoromethyl)-4-biphenylsulfonamide	DMLP67R	Discovery agent	N.A.	Investigative	[5]
4'-(trifluoromethyl)-4-biphenylyl carbamate	DMT3BX9	Discovery agent	N.A.	Investigative	[5]
4'-(trifluoromethyl)-4-biphenylyl sulfamate	DM8PTNR	Discovery agent	N.A.	Investigative	[5]
4'-trifluoromethyl-biphenyl-4-ylamine	DMT81SD	Discovery agent	N.A.	Investigative	[5]
4-(trifluoromethyl)biphenyl	DMZ0AKP	Discovery agent	N.A.	Investigative	[5]
6-fluoro-2-methyl-9H-carbazole	DM2DTHV	Discovery agent	N.A.	Investigative	[4]
7-tert-butyl-9H-carbazole-3-carboxylic acid	DMD7Q1R	Discovery agent	N.A.	Investigative	[4]
9-methyl-2-(trifluoromethyl)-9H-carbazole	DMKLTD5	Discovery agent	N.A.	Investigative	[4]
9H-carbazole-2-carbaldehyde	DM6WHIA	Discovery agent	N.A.	Investigative	[4]
9H-carbazole-3-carbaldehyde	DM0HNU3	Discovery agent	N.A.	Investigative	[4]
Adociasulfate-2	DM6MRSC	Discovery agent	N.A.	Investigative	[6]
ISIS 183881	DMOU9EP	Discovery agent	N.A.	Investigative	[7]
ISIS 183882	DMT3YI5	Discovery agent	N.A.	Investigative	[8]
ISIS 183883	DMA46S1	Discovery agent	N.A.	Investigative	[8]
ISIS 183897	DMS172K	Discovery agent	N.A.	Investigative	[8]
ISIS 183901	DMSEJZK	Discovery agent	N.A.	Investigative	[8]
ISIS 183910	DMMQ2L7	Discovery agent	N.A.	Investigative	[8]
ISIS 183911	DMTB350	Discovery agent	N.A.	Investigative	[8]
ISIS 183912	DM5QWED	Discovery agent	N.A.	Investigative	[8]
Methyl 7-tert-butyl-9H-carbazole-3-carboxylate	DM9HLXD	Discovery agent	N.A.	Investigative	[4]
Methyl 9H-carbazole-2-carboxylate	DM4DIS3	Discovery agent	N.A.	Investigative	[4]
Methyl[4'-(trifluoromethyl)-4-biphenylyl]amine	DMZVBLT	Discovery agent	N.A.	Investigative	[5]
N-(4'-bromo-3,3'-difluoro-4-biphenylyl)urea	DMWHYOJ	Discovery agent	N.A.	Investigative	[5]
N-(4'-chloro-4-biphenylyl)methanesulfonamide	DM0ARP8	Discovery agent	N.A.	Investigative	[5]
N-(4'-isopropyl-4-biphenylyl)urea	DM2MGSO	Discovery agent	N.A.	Investigative	[5]
N-(4'-methyl-4-biphenylyl)urea	DMO8L57	Discovery agent	N.A.	Investigative	[5]
N-(4'-t-butyl-4-biphenylyl)urea	DMHX4F2	Discovery agent	N.A.	Investigative	[5]
N-[3'-(trifluoromethyl)-4-biphenylyl]urea	DM7OA4R	Discovery agent	N.A.	Investigative	[5]
N-[4'-(ethylsulfonyl)-3-fluoro-4-biphenylyl]urea	DMD5F6Z	Discovery agent	N.A.	Investigative	[5]
N-[4'-(trifluoromethyl)-4-biphenylyl]sulfamide	DMCTZFP	Discovery agent	N.A.	Investigative	[5]
N-[4'-(trifluoromethyl)-4-biphenylyl]thiourea	DMPVKWG	Discovery agent	N.A.	Investigative	[5]
N-[4'-(trifluoromethyl)-4-biphenylyl]urea	DMMHQRT	Discovery agent	N.A.	Investigative	[5]
N-[4-(1,3-benzodioxol-5-yl)phenyl]sulfamide	DMITN82	Discovery agent	N.A.	Investigative	[5]
N-{4'-[(trifluoromethyl)sulfonyl]-4-biphenyl}urea	DM90U5P	Discovery agent	N.A.	Investigative	[5]
N-{4'-[(trifluoromethyl)thio]-4-biphenyl}urea	DMEIB69	Discovery agent	N.A.	Investigative	[5]
SB-731489	DMO2EXW	Discovery agent	N.A.	Investigative	[5]

References

• [1] Clinical pipeline report, company report or official report of Alnylam Pharmaceuticals, Inc (2011).
• [2] The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1491-5.
• [3] Structural basis for inhibition of Eg5 by dihydropyrimidines: stereoselectivity of antimitotic inhibitors enastron, dimethylenastron and fluorastrol. J Med Chem. 2010 Aug 12;53(15):5676-83.
• [4] Kinesin spindle protein (KSP) inhibitors with 2,3-fused indole scaffolds. J Med Chem. 2010 Jul 8;53(13):5054-8.
• [5] Novel ATP-competitive kinesin spindle protein inhibitors. J Med Chem. 2007 Oct 4;50(20):4939-52.
• [6] Inhibition of kinesin motor proteins by adociasulfate-2. J Med Chem. 2006 Aug 10;49(16):4857-60.
• [7] US patent application no. 7,407,943, Antisense modulation of apolipoprotein B expression.
• [8] US patent application no. 7,163,927, Antisense modulation of kinesin-like 1 expression.