General Information of This Target
Target ID
PATR0TYCUL
Target Name
kinesin spindle protein (KSP)
Gene Name
KIF11
Gene ID
3832
Synonym
EG5; KNSL1; TRIP5; Kinesin-like protein 1; Kinesin-like spindle protein HKSP; Kinesin-related motor protein Eg5; Thyroid receptor-interacting protein 5
Sequence
MASQPNSSAKKKEEKGKNIQVVVRCRPFNLAERKASAHSIVECDPVRKEVSVRTGGLADK
SSRKTYTFDMVFGASTKQIDVYRSVVCPILDEVIMGYNCTIFAYGQTGTGKTFTMEGERS
PNEEYTWEEDPLAGIIPRTLHQIFEKLTDNGTEFSVKVSLLEIYNEELFDLLNPSSDVSE
RLQMFDDPRNKRGVIIKGLEEITVHNKDEVYQILEKGAAKRTTAATLMNAYSSRSHSVFS
VTIHMKETTIDGEELVKIGKLNLVDLAGSENIGRSGAVDKRAREAGNINQSLLTLGRVIT
ALVERTPHVPYRESKLTRILQDSLGGRTRTSIIATISPASLNLEETLSTLEYAHRAKNIL
NKPEVNQKLTKKALIKEYTEEIERLKRDLAAAREKNGVYISEENFRVMSGKLTVQEEQIV
ELIEKIGAVEEELNRVTELFMDNKNELDQCKSDLQNKTQELETTQKHLQETKLQLVKEEY
ITSALESTEEKLHDAASKLLNTVEETTKDVSGLHSKLDRKKAVDQHNAEAQDIFGKNLNS
LFNNMEELIKDGSSKQKAMLEVHKTLFGNLLSSSVSALDTITTVALGSLTSIPENVSTHV
SQIFNMILKEQSLAAESKTVLQELINVLKTDLLSSLEMILSPTVVSILKINSQLKHIFKT
SLTVADKIEDQKKELDGFLSILCNNLHELQENTICSLVESQKQCGNLTEDLKTIKQTHSQ
ELCKLMNLWTERFCALEEKCENIQKPLSSVQENIQQKSKDIVNKMTFHSQKFCADSDGFS
QELRNFNQEGTKLVEESVKHSDKLNGNLEKISQETEQRCESLNTRTVYFSEQWVSSLNER
EQELHNLLEVVSQCCEASSSDITEKSDGRKAAHEKQHNIFLDQMTIDEDKLIAQNLELNE
TIKIGLTKLNCFLEQDLKLDIPTGTTPQRKSYLYPSTLVRTEPREHLLDQLKRKQPELLM
MLNCSENNKEETIPDVDVEEAVLGQYTEEPLSQEPSVDAGVDCSSIGGVPFFQHKKSHGK
DKENRGINTLERSKVEETTEHLVTKSRLPLRAQINL

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Family
the TRAFAC class myosin-kinesin ATPas
Function
Motor protein required for establishing a bipolar spindle during mitosis. Required in non-mitotic cells for transport of secretory proteins from the Golgi complex to the cell surface.

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Uniprot Entry
KIF11_HUMAN
HGNC ID
HGNC:6388
KEGG ID
hsa:3832
Full List of The ADC Related to This Target
Phase 1
Click To Hide/Show 25 ADC Related to This Stage
ADC Info ADC Name Antibody Antigen Payload Linker Ref
BAY-943
Anti-CD123 antibody
CD123
Proprietary BAY-943 spindle protein inhibitor
Lysine-linked legumain-cleavable linker
[1]
BAY-924
Anti-CXCR5 IgG1 mAb
C-X-C chemokine receptor type 5 (CXCR5)
KSP inhibitor
Undisclosed
[2]
TWEAKR-KSPi-ADC2
BAY-356
Tumor necrosis factor receptor superfamily member 12A (TNFRSF12A)
KSP inhibitor
Mc-peptide-based linker
[3]
TWEAKR-KSPi-ADC1
BAY-356
Tumor necrosis factor receptor superfamily member 12A (TNFRSF12A)
KSP inhibitor
Glutaricacid-peptide-based linker
[3]
TWEAKR ADC 3a
BAY-356
Tumor necrosis factor receptor superfamily member 12A (TNFRSF12A)
Kinesin spindle protein (KSP) inhibitor 3a
Open-chain glycine maleimide
[4]
TWEAKR ADC 3b
BAY-356
Tumor necrosis factor receptor superfamily member 12A (TNFRSF12A)
Kinesin spindle protein (KSP) inhibitor 3b
Open-chain glycine maleimide
[4]
TWEAKR ADC 3c
BAY-356
Tumor necrosis factor receptor superfamily member 12A (TNFRSF12A)
Kinesin spindle protein (KSP) inhibitor 3c
Open-chain glycine maleimide
[4]
TWEAKR ADC 3d
BAY-356
Tumor necrosis factor receptor superfamily member 12A (TNFRSF12A)
Kinesin spindle protein (KSP) inhibitor 3d
Open-chain glycine maleimide
[4]
TWEAKR ADC 3e
BAY-356
Tumor necrosis factor receptor superfamily member 12A (TNFRSF12A)
Kinesin spindle protein (KSP) inhibitor 3e
Open-chain glycine maleimide
[4]
TWEAKR ADC 3f
BAY-356
Tumor necrosis factor receptor superfamily member 12A (TNFRSF12A)
Kinesin spindle protein (KSP) inhibitor 3f
Open-chain glycine maleimide
[4]
TWEAKR ADC 3g
BAY-356
Tumor necrosis factor receptor superfamily member 12A (TNFRSF12A)
Kinesin spindle protein (KSP) inhibitor 3g
Open-chain glycine maleimide
[4]
Anti-B7H3 APDC 3f
TPP-8567
CD276 antigen (CD276)
Kinesin spindle protein (KSP) inhibitor 3f
Open-chain glycine maleimide
[4]
Anti-B7H3 APDC 3g
TPP-8567
CD276 antigen (CD276)
Kinesin spindle protein (KSP) inhibitor 3g
Open-chain glycine maleimide
[4]
TWEAKR-KSP-ADC 1.1
Anti-TWEAKR mAb
Tumor necrosis factor receptor superfamily member 12A (TNFRSF12A)
Pyrrole based kinesin spindle protein inhibitor
Kinesin spindle protein inhibitor (KSPi)-ADC linker 1
[5]
TWEAKR-KSP-ADC 1.2
Anti-TWEAKR mAb
Tumor necrosis factor receptor superfamily member 12A (TNFRSF12A)
Pyrrole based kinesin spindle protein inhibitor
Kinesin spindle protein inhibitor (KSPi)-ADC linker 2
[5]
TWEAKR-KSP-ADC 1.3
Anti-TWEAKR mAb
Tumor necrosis factor receptor superfamily member 12A (TNFRSF12A)
Pyrrole based kinesin spindle protein inhibitor
Kinesin spindle protein inhibitor (KSPi)-ADC linker 3
[5]
TWEAKR-KSP-ADC 1.4
Anti-TWEAKR mAb
Tumor necrosis factor receptor superfamily member 12A (TNFRSF12A)
Pyrrole based kinesin spindle protein inhibitor
Kinesin spindle protein inhibitor (KSPi)-ADC linker 4
[5]
TWEAKR-KSP-ADC 2.1
Anti-TWEAKR mAb
Tumor necrosis factor receptor superfamily member 12A (TNFRSF12A)
Pyrrole based kinesin spindle protein inhibitor
Kinesin spindle protein inhibitor (KSPi)-ADC linker 5
[5]
TWEAKR-KSP-ADC 2.2
Anti-TWEAKR mAb
Tumor necrosis factor receptor superfamily member 12A (TNFRSF12A)
Pyrrole based kinesin spindle protein inhibitor
Kinesin spindle protein inhibitor (KSPi)-ADC linker 6
[5]
HER2 KSP-ADC 1.1
BAY-865
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
Pyrrole based kinesin spindle protein inhibitor
Kinesin spindle protein inhibitor (KSPi)-ADC linker 1
[5]
HER2 KSP-ADC 1.2
BAY-865
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
Pyrrole based kinesin spindle protein inhibitor
Kinesin spindle protein inhibitor (KSPi)-ADC linker 2
[5]
HER2 KSP-ADC 1.3
BAY-865
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
Pyrrole based kinesin spindle protein inhibitor
Kinesin spindle protein inhibitor (KSPi)-ADC linker 3
[5]
HER2 KSP-ADC 1.4
BAY-865
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
Pyrrole based kinesin spindle protein inhibitor
Kinesin spindle protein inhibitor (KSPi)-ADC linker 4
[5]
HER2 KSP-ADC 2.1
BAY-865
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
Pyrrole based kinesin spindle protein inhibitor
Kinesin spindle protein inhibitor (KSPi)-ADC linker 5
[5]
HER2 KSP-ADC 2.2
BAY-865
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
Pyrrole based kinesin spindle protein inhibitor
Kinesin spindle protein inhibitor (KSPi)-ADC linker 6
[5]
Investigative
Click To Hide/Show 13 ADC Related to This Stage
ADC Info ADC Name Antibody Antigen Payload Linker Ref
H2-921
Trastuzumab
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
SB743921
CN118987256A, H2-921, Linker
[6]
CN110072556B 1c-8987
TPP-8987
Interleukin-3 receptor subunit alpha (IL3RA)
KSP Inhbitor
CN110072556B+Conjugate1+Linker
[7]
CN110072556B 1c-8988
TPP-8988
Interleukin-3 receptor subunit alpha (IL3RA)
KSP Inhbitor
CN110072556B+Conjugate1+Linker
[7]
CN110072556B 1c-9476
TPP-9476
Interleukin-3 receptor subunit alpha (IL3RA)
KSP Inhbitor
CN110072556B+Conjugate1+Linker
[7]
CN110072556B 1x-9024
TPP-9024
C-X-C chemokine receptor type 5 (CXCR5)
KSP Inhbitor
CN110072556B+Conjugate1+Linker
[7]
CN110072556B 1x-9574
TPP-9574
C-X-C chemokine receptor type 5 (CXCR5)
KSP Inhbitor
CN110072556B+Conjugate1+Linker
[7]
CN110072556B 1x-9580
TPP-9580
C-X-C chemokine receptor type 5 (CXCR5)
KSP Inhbitor
CN110072556B+Conjugate1+Linker
[7]
R1c-8987
TPP-8987
Interleukin-3 receptor subunit alpha (IL3RA)
KSP Inhbitor
CN110072556B+ConjugateR1+Linker
[7]
R1c-8988
TPP-8988
Interleukin-3 receptor subunit alpha (IL3RA)
KSP Inhbitor
CN110072556B+ConjugateR1+Linker
[7]
R1c-9476
TPP-9476
Interleukin-3 receptor subunit alpha (IL3RA)
KSP Inhbitor
CN110072556B+ConjugateR1+Linker
[7]
R1x-9024
TPP-9024
C-X-C chemokine receptor type 5 (CXCR5)
KSP Inhbitor
CN110072556B+ConjugateR1+Linker
[7]
R1x-9574
TPP-9574
C-X-C chemokine receptor type 5 (CXCR5)
KSP Inhbitor
CN110072556B+ConjugateR1+Linker
[7]
R1x-9580
TPP-9580
C-X-C chemokine receptor type 5 (CXCR5)
KSP Inhbitor
CN110072556B+ConjugateR1+Linker
[7]
References
Ref 1 IL3RA-Targeting Antibody-Drug Conjugate BAY-943 with a Kinesin Spindle Protein Inhibitor Payload Shows Efficacy in Preclinical Models of Hematologic Malignancies. Cancers (Basel). 2020 Nov 20;12(11):3464. doi: 10.3390/cancers12113464.
Ref 2 Preclinical characterization of BAY-924, a first in class ADC targeting CXCR5-positive B-cell malignancies, with a KSP inhibitor as novel payload. Cancer Res (2019) 79 (13_Supplement): 4825.
Ref 3 Antibody-drug conjugates harboring a kinesin spindle protein inhibitor with immunostimulatory properties. Oncoimmunology. 2022 Feb 9;11(1):2037216. doi: 10.1080/2162402X.2022.2037216. eCollection 2022.
Ref 4 Antibody-Prodrug Conjugates with KSP Inhibitors and Legumain-Mediated Metabolite Formation. Chemistry. 2019 Jun 21;25(35):8208-8213. doi: 10.1002/chem.201900441. Epub 2019 Apr 15.
Ref 5 Antibody-Drug Conjugates with Pyrrole-Based KSP Inhibitors as the Payload Class. Angew Chem Int Ed Engl. 2018 Nov 12;57(46):15243-15247. doi: 10.1002/anie.201807619. Epub 2018 Oct 15.
Ref 6 Antibody-drug conjugates and their preparation methods and uses
Ref 7 Specific antibody-drug conjugates (ADCs) having KSP inhibitors