Target Information

General Information of This Target
Target ID
PATR0JHCHU
Target Name
DNA topoisomerase 2-alpha (TOP2A)
Gene Name
TOP2A
Gene ID
7153
Synonym
TOP2A; TOP2; DNA topoisomerase II, alpha isozyme
Sequence
MEVSPLQPVNENMQVNKIKKNEDAKKRLSVERIYQKKTQLEHILLRPDTYIGSVELVTQQ
MWVYDEDVGINYREVTFVPGLYKIFDEILVNAADNKQRDPKMSCIRVTIDPENNLISIWN
NGKGIPVVEHKVEKMYVPALIFGQLLTSSNYDDDEKKVTGGRNGYGAKLCNIFSTKFTVE
TASREYKKMFKQTWMDNMGRAGEMELKPFNGEDYTCITFQPDLSKFKMQSLDKDIVALMV
RRAYDIAGSTKDVKVFLNGNKLPVKGFRSYVDMYLKDKLDETGNSLKVIHEQVNHRWEVC
LTMSEKGFQQISFVNSIATSKGGRHVDYVADQIVTKLVDVVKKKNKGGVAVKAHQVKNHM
WIFVNALIENPTFDSQTKENMTLQPKSFGSTCQLSEKFIKAAIGCGIVESILNWVKFKAQ
VQLNKKCSAVKHNRIKGIPKLDDANDAGGRNSTECTLILTEGDSAKTLAVSGLGVVGRDK
YGVFPLRGKILNVREASHKQIMENAEINNIIKIVGLQYKKNYEDEDSLKTLRYGKIMIMT
DQDQDGSHIKGLLINFIHHNWPSLLRHRFLEEFITPIVKVSKNKQEMAFYSLPEFEEWKS
STPNHKKWKVKYYKGLGTSTSKEAKEYFADMKRHRIQFKYSGPEDDAAISLAFSKKQIDD
RKEWLTNFMEDRRQRKLLGLPEDYLYGQTTTYLTYNDFINKELILFSNSDNERSIPSMVD
GLKPGQRKVLFTCFKRNDKREVKVAQLAGSVAEMSSYHHGEMSLMMTIINLAQNFVGSNN
LNLLQPIGQFGTRLHGGKDSASPRYIFTMLSSLARLLFPPKDDHTLKFLYDDNQRVEPEW
YIPIIPMVLINGAEGIGTGWSCKIPNFDVREIVNNIRRLMDGEEPLPMLPSYKNFKGTIE
ELAPNQYVISGEVAILNSTTIEISELPVRTWTQTYKEQVLEPMLNGTEKTPPLITDYREY
HTDTTVKFVVKMTEEKLAEAERVGLHKVFKLQTSLTCNSMVLFDHVGCLKKYDTVLDILR
DFFELRLKYYGLRKEWLLGMLGAESAKLNNQARFILEKIDGKIIIENKPKKELIKVLIQR
GYDSDPVKAWKEAQQKVPDEEENEESDNEKETEKSDSVTDSGPTFNYLLDMPLWYLTKEK
KDELCRLRNEKEQELDTLKRKSPSDLWKEDLATFIEELEAVEAKEKQDEQVGLPGKGGKA
KGKKTQMAEVLPSPRGQRVIPRITIEMKAEAEKKNKKKIKNENTEGSPQEDGVELEGLKQ
RLEKKQKREPGTKTKKQTTLAFKPIKKGKKRNPWSDSESDRSSDESNFDVPPRETEPRRA
ATKTKFTMDLDSDEDFSDFDEKTDDEDFVPSDASPPKTKTSPKLSNKELKPQKSVVSDLE
ADDVKGSVPLSSSPPATHFPDETEITNPVPKKNVTVKKTAAKSQSSTSTTGAKKRAAPKG
TKRDPALNSGVSQKPDPAKTKNRRKRKPSTSDDSDSNFEKIVSKAVTSKKSKGESDDFHM
DFDSAVAPRAKSVRAKKPIKYLEESDEDDLF

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Family
the type II topoisomerase family
Function
Key decatenating enzyme that alters DNA topology by binding to two double-stranded DNA molecules, generating a double-stranded break in one of the strands, passing the intact strand through the broken strand, and religating the broken strand. May play a role in regulating the period length of BMAL1 transcriptional oscillation.

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Uniprot Entry
TOP2A_HUMAN
HGNC ID
HGNC:11989
KEGG ID
hsa:7153
Full List of The ADC Related to This Target
Phase 2
Click To Hide/Show 2 ADC Related to This Stage
ADC Info ADC Name Antibody Antigen Payload Linker Ref
 ADC Info 
NBE-002
Anti-ROR1 mAb huXBR1-402
ROR1
PNU-159682
LPETG-Gly5-EDA
 [1]
 ADC Info 
SOT-102
Undisclosed
CLDN18.2
PNU-159682
Undisclosed
 [2]
Phase 1
Click To Hide/Show 1 ADC Related to This Stage
ADC Info ADC Name Antibody Antigen Payload Linker Ref
 ADC Info 
EGFR-EDV-RRM1
Undisclosed
EGFR
Doxorubicin
Undisclosed
 [3]
Clinical candidate
Click To Hide/Show 6 ADC Related to This Stage
ADC Info ADC Name Antibody Antigen Payload Linker Ref
 ADC Info 
HuXBR1-402-G5-PNU
Anti-ROR1 mAb huXBR1-402
ROR1
PNU-159682
Gly5-FITC
 [4]
 ADC Info 
Trastuzumab-PNU-159682 Antibody-Drug Conjugate
Trastuzumab
ERBB2
PNU-159682
Undisclosed
 [5]
 ADC Info 
Anti-CD8-idarubicin conjugate
Anti-CD8 (Ly-2.1) mAb
CD8A; CD8A
Idarubicin
Undisclosed
 [6]
 ADC Info 
NV102
Undisclosed
CD19
Doxorubicin
Undisclosed
 [7]
 ADC Info 
NV101
Undisclosed
CD99
Doxorubicin
Undisclosed
 [8]
 ADC Info 
CytSCA208
CA208
PSG2
Cytorhodin S
Undisclosed
 [9]
Investigative
Click To Hide/Show 28 ADC Related to This Stage
ADC Info ADC Name Antibody Antigen Payload Linker Ref
 ADC Info 
Tras-Gly5-EDA-Pnu
Trastuzumab
ERBB2
PNU-159682
Gly5-EDA
 [10]
 ADC Info 
Tras-Gly5-EDA-Dox
Trastuzumab
ERBB2
Doxorubicin
Gly5-EDA
 [10]
 ADC Info 
Tras-Gly5-EDA-Nemo
Trastuzumab
ERBB2
Nemorubicin
Gly5-EDA
 [10]
 ADC Info 
Tras-Gly3-Vakl-Cit-PAB-PNU-159682
Trastuzumab
ERBB2
PNU-159682
Gly3-vcPAB
 [10]
 ADC Info 
Alb-DMBA-SIL-DOX
Alb
ALB
Doxorubicin
DMBA-SIL
 [11]
 ADC Info 
Trastuzumab-BCN-HydraSpace-Val-Cit-PABC-PNU-159682
Trastuzumab
ERBB2
PNU-159682
BCN-HydraSpace-Val-Cit-PABC
 [12]
 ADC Info 
Anti-CD22-NMS249
Pinatuzumab
CD22
PNU-159682
Mc-Val-Cit-PAB-DEA
 [13]
 ADC Info 
MAb-DMBA-SIL-Dox
Cetuximab
EGFR
Doxorubicin
DMBA-SIL
 [11]
 ADC Info 
Cetuximab-Val-Cit-Dox
Cetuximab
EGFR
Doxorubicin
Mc-Val-Cit-PABC
 [14]
 ADC Info 
Trastuzumab-PNUEDAGly5
Trastuzumab
ERBB2
PNU-159682
LPETG-Gly5-EDA
 [15]
 ADC Info 
Brentuximab-PNUEDAGly5
Brentuximab
TNFRSF8
PNU-159682
LPETG-Gly5-EDA
 [15]
 ADC Info 
CAC10-Gly5-PNU
Brentuximab
TNFRSF8
PNU-159682
Gly5
 [10]
 ADC Info 
Trastuzumab-G5-PNU
Trastuzumab
ERBB2
PNU-159682
Gly5-FITC
 [10]
 ADC Info 
Trastuzumab-PC4AP-DOX
Trastuzumab
ERBB2
Doxorubicin
Photocaged C4AP
 [16]
 ADC Info 
WO2007011968A2 cAC10-17
Brentuximab
TNFRSF8
Doxorubicin
WO2007011968A2_cAC10-17 linker
 [17]
 ADC Info 
WO2007011968A2 c1F6-17
Anti-CD70 mAb c1F6
CD70
Doxorubicin
WO2007011968A2_c1F6-17 linker
 [17]
 ADC Info 
PDL1-Dox ADC
Atezolizumab
CD274
Doxorubicin
Undisclosed
 [18]
 ADC Info 
hCD46-19
Anti-CD46 mAb
CD46
PNU-159682
Hydrophilic cleavable linker 19
 [19]
 ADC Info 
HuIgG1-19
Undisclosed
EGFR; ERBB3
PNU-159682
Hydrophilic cleavable linker 19
 [19]
 ADC Info 
hCD46-25
Anti-CD46 mAb
CD46
PNU-159682
Alternative linker without basic amines linker 25
 [19]
 ADC Info 
HuIgG1-25
Undisclosed
EGFR; ERBB3
PNU-159682
Alternative linker without basic amines linker 25
 [19]
 ADC Info 
hCD46-26
Anti-CD46 mAb
CD46
PNU-159682
Maleimide based noncleavable linker 26
 [19]
 ADC Info 
HuIgG1-26
Undisclosed
EGFR; ERBB3
PNU-159682
Maleimide based noncleavable linker 26
 [19]
 ADC Info 
hCD46-29
Anti-CD46 mAb
CD46
PNU-159682
PNU-thiazole cleavable linker 29
 [19]
 ADC Info 
HuIgG1-29
Undisclosed
EGFR; ERBB3
PNU-159682
PNU-thiazole cleavable linker 29
 [19]
 ADC Info 
B12-PEG-G2-DOX
B12
env
Cis-aconityl-doxorubicin
B12-PEG-G2-DOX linker
 [20]
 ADC Info 
B12-PEG-G4-DOX
B12
env
Cis-aconityl-doxorubicin
B12-PEG-G4-DOX linker
 [20]
 ADC Info 
B12-PEG-G5-DOX
B12
env
Cis-aconityl-doxorubicin
B12-PEG-G5-DOX linker
 [20]
Terminated in phase 2
Click To Hide/Show 2 ADC Related to This Stage
ADC Info ADC Name Antibody Antigen Payload Linker Ref
 ADC Info 
Milatuzumab doxorubicin
Milatuzumab
CD74
Doxorubicin
Mcc-hydrazide
 [21]
 ADC Info 
SGN-15
Anti-Lewis-Y mAb cBR96
Undisclosed
Doxorubicin
Undisclosed
 [22]
Terminated
Click To Hide/Show 2 ADC Related to This Stage
ADC Info ADC Name Antibody Antigen Payload Linker Ref
 ADC Info 
Monoclonal antibody 1H10-doxorubicin conjugate
IH10
TUBA1B
Doxorubicin
Dextran
 [23]
 ADC Info 
Anti-Laminin receptor monoclonal antibody-liposomal doxorubicin conjugate
Anti-laminin receptor IgM
RPSA
Doxorubicin
Disulfide bond linker
 [24]
References
Ref 1 NBE-002: A novel anthracycline-based antibody-drug conjugate (ADC) targeting ROR1 for the treatment of advanced solid tumorsA phase 1/2 clinical trial. Journal of Clinical Oncology 39, no. 15_suppl.
Ref 2 SOT102, a novel CLDN18.2-targeting antibody-drug conjugate for gastric and pancreatic cancer with a wide range of the tumor target expression. ESMO OPEN 2023 Mar; 8(1):supplement 101196.
Ref 3 Introduction to basic information on antibody-drug nanocell conjugates(EnGeneIC Pty Ltd.).
Ref 4 The ROR1 antibody-drug conjugate huXBR1-402-G5-PNU effectively targets ROR1+ leukemia. Blood Adv. 2021 Aug 24;5(16):3152-3162.
Ref 5 A novel anti-HER2 anthracycline-based antibody-drug conjugate induces adaptive anti-tumor immunity and potentiates PD-1 blockade in breast cancer. J Immunother Cancer. 2019 Jan 21;7(1):16. doi: 10.1186/s40425-018-0464-1.
Ref 6 Evidence that an anthracycline-anti-CD8 immunoconjugate, idarubicin-anti-Ly-2.1, prolongs heart allograft survival in mice. Transplantation. 1993 Mar;55(3):484-90. doi: 10.1097/00007890-199303000-00006.
Ref 7 ADC review: basic information about NV102 (Doxorubicin-Anti-CD19).
Ref 8 ADC review NV101
Ref 9 Selective killing of carcinoembryonic-antigen (CEA)-producing cells in vitro by the immunoconjugate cytorhodin-S and CEA-reactive cytorhodin-S antibody CA208. Cancer Immunol Immunother. 1989;30(4):239-46. doi: 10.1007/BF01665011.
Ref 10 Highly Potent, Anthracycline-based Antibody-Drug Conjugates Generated by Enzymatic, Site-specific Conjugation. Mol Cancer Ther. 2017 May;16(5):879-892.
Ref 11 Radiation Cleaved Drug-Conjugate Linkers Enable Local Payload Release. Bioconjug Chem. 2022 Aug 17;33(8):1474-1484.
Ref 12 Non-Genetic Generation of Antibody Conjugates Based on Chemoenzymatic Tyrosine Click Chemistry. Bioconjug Chem. 2021 Oct 20;32(10):2167-2172. doi: 10.1021/acs.bioconjchem.1c00351. Epub 2021 Sep 14.
Ref 13 A Novel Anti-CD22 Anthracycline-Based Antibody-Drug Conjugate (ADC) That Overcomes Resistance to Auristatin-Based ADCs. Clin Cancer Res. 2015 Jul 15;21(14):3298-306. doi: 10.1158/1078-0432.CCR-14-2035. Epub 2015 Apr 3.
Ref 14 EGFR Targeted Cetuximab-Valine-Citrulline (vc)-Doxorubicin Immunoconjugates- Loaded Bovine Serum Albumin (BSA) Nanoparticles for Colorectal Tumor Therapy. Int J Nanomedicine. 2021 Mar 26;16:2443-2459. doi: 10.2147/IJN.S289228. eCollection 2021.
Ref 15 Binding protein drug conjugates comprising anthracycline derivatives; 2016-06-30.
Ref 16 A light-responsive, self-immolative linker for controlled drug delivery via peptide- and protein-drug conjugates. Chem Sci. 2019 Aug 19;10(39):8973-8980. doi: 10.1039/c9sc03016f. eCollection 2019 Oct 21.
Ref 17 Beta-glucuronide-linker drug conjugates; 2007-10-25.
Ref 18 PDL-1 Antibody Drug Conjugate for Selective Chemo-Guided Immune Modulation of Cancer. Cancers (Basel). 2019 Feb 16;11(2):232. doi: 10.3390/cancers11020232.
Ref 19 Evaluation of PNU-159682 antibody drug conjugates (ADCs). Bioorg Med Chem Lett. 2020 Dec 15;30(24):127640. doi: 10.1016/j.bmcl.2020.127640. Epub 2020 Oct 28.
Ref 20 Immune conjugate having dendron conjugated to antibody and use thereof.
Ref 21 Anti-CD74 antibody-doxorubicin conjugate, IMMU-110, in a human multiple myeloma xenograft and in monkeys. Clin Cancer Res. 2005 Jul 15;11(14):5257-64.
Ref 22 A randomized, multicenter study to determine the safety and efficacy of the immunoconjugate SGN-15 plus docetaxel for the treatment of non-small cell lung carcinoma. Lung Cancer. 2006 Oct;54(1):69-77. doi: 10.1016/j.lungcan.2006.05.020. Epub 2006 Aug 28.
Ref 23 Doxorubicin: monoclonal antibody conjugate for therapy of human cervical carcinoma. Int J Cancer. 1992 May 8;51(2):274-82. doi: 10.1002/ijc.2910510217.
Ref 24 Anti-laminin receptor antibody targeting of liposomes with encapsulated doxorubicin to human breast cancer cells in vitro. J Natl Cancer Inst. 1989 Dec 6;81(23):1794-800. doi: 10.1093/jnci/81.23.1794.

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