Target Information
General Information of This Target
| Target ID |
TAR10002
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|---|---|---|---|---|---|---|
| Target Name |
DNA topoisomerase 2-alpha (TOP2A)
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| Gene Name |
TOP2A
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| Gene ID | ||||||
| Synonym |
TOP2; DNA topoisomerase II, alpha isozyme
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| 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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| 3D Structure | ||||||
| Family |
the type II topoisomerase family
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| 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 (By similarity).
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| Uniprot Entry | ||||||
| HGNC ID | ||||||
| KEGG ID | ||||||
Full List of The PDC Related to This Target
Preclinical
| PDC Info | PDC Name | Peptide | Receptor | Drug | Linker |
|---|---|---|---|---|---|
|
TH1904
|
TH19P01
|
Sortilin (SORT1)
|
Doxorubicin
|
3,3-Dimethylglutaric acid
|
Investigative
| PDC Info | PDC Name | Peptide | Receptor | Drug | Linker |
|---|---|---|---|---|---|
|
pHLIP-SS-DOX
|
pHLIP (AEQ)
|
DNA topoisomerase 2-alpha (TOP2A)
|
Doxorubicin
|
Disulfide bond
|
|
|
BP9a-DOX
|
BP9a
|
Transferrin receptor protein 1 (TFRC)
|
Doxorubicin
|
N-succinimidyl-3-maleimidopropionate
|
|
|
BP9a-SS-DOX
|
BP9a
|
Transferrin receptor protein 1 (TFRC)
|
Doxorubicin
|
Disulfide bond
|
|
|
(DOX-S)2-S-Pep
|
CCKIGLFRWR
|
72 kDa type IV collagenase (MMP2)
|
Doxorubicin
|
2,2-Dipyridyl disulfide
|
|
|
DOX-ApoA-1 mimic peptide
|
ApoA-1 mimic peptide
|
Undisclosed
|
Doxorubicin
|
3-Disulfanylpropanoic Acid
|
|
|
DOXoxmCPPamph
|
oxmCPPamph
|
Undisclosed
|
Doxorubicin
|
Disulfide bond
|
|
|
99mTc-HYNIC-CLB-c(NGR)
|
Cyclic NGR
|
Undisclosed
|
Chlorambucil
|
Amide bond
|
|
|
DOXoxmCPP
|
oxmCPP
|
Undisclosed
|
Doxorubicin
|
Disulfide bond
|
|
|
Peptide-drug conjugate 10
|
oxmCPP
|
Undisclosed
|
Doxorubicin
|
Disulfide bond
|
|
|
[d-Cys6-des-Gly10-Pro9-α-azaGly-NH2]-GnRH-Dox
|
GnRH analogs 3
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Doxorubicin
|
N-succinimidyl-3-maleimidopropionate
|
|
|
[d-Cys6-des-Gly10-Pro9-NH2]-GnRH-Dox
|
GnRH analogs 1
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Doxorubicin
|
N-succinimidyl-3-maleimidopropionate
|
|
|
[d-Cys6-des-Gly10-Pro9-NHEt]-GnRH-Dox
|
GnRH analogs 2
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Doxorubicin
|
N-succinimidyl-3-maleimidopropionate
|
|
|
PNS-SS-DOX
|
Fmoc-FKKGSHC
|
Undisclosed
|
Doxorubicin
|
2-Aminothiolane
|
|
|
DOX-EMCH-fMLFC
|
DEF
|
fMet-Leu-Phe receptor (FPR1)
|
Doxorubicin
|
N-ε-maleimidocaproic acid hydrazide
|
|
|
E1-3 doxorubicin
|
E1-3
|
Undisclosed
|
Doxorubicin
|
Glutaric acid
|
|
|
RGD-GFLG-DOX
|
GFLG
|
Integrin alpha-V; Integrin beta-3 (ITGAV; ITGB3)
|
Doxorubicin
|
GFLG
|
|
|
PDC-G3
|
GFLG-fQWAV-β-Ala-H-Aib-Nle
|
Gastrin-releasing peptide receptor (GRPR)
|
Daunorubicin
|
GFLG
|
|
|
PDC-G4
|
GFLG-fQWAV-β-Ala-H-N-Me-Ala-Nle
|
Gastrin-releasing peptide receptor (GRPR)
|
Daunorubicin
|
GFLG
|
|
|
PDC-G2
|
GFLG-fQWAVGHL-Nle
|
Gastrin-releasing peptide receptor (GRPR)
|
Daunorubicin
|
GFLG
|
|
|
PDC-G5
|
GFLG-fQWAVGH-Sta-L
|
Gastrin-releasing peptide receptor (GRPR)
|
Daunorubicin
|
GFLG
|
|
|
PDC-G1
|
GFLG-QWAVGHL-Nle
|
Gastrin-releasing peptide receptor (GRPR)
|
Daunorubicin
|
GFLG
|
|
|
Dox-GLRKRLRKFRNK
|
GLRKRLRKFRNK
|
Cell membrane
|
Doxorubicin
|
S-(1-(2-carboxyethyl)-2,5-dioxopyrrolidin-3-yl)cysteine
|
|
|
Dox-GLRKRLRKFRNKIKEK
|
GLRKRLRKFRNKIKEK
|
Cell membrane
|
Doxorubicin
|
S-(1-(2-carboxyethyl)-2,5-dioxopyrrolidin-3-yl)cysteine
|
|
|
Dox-GLRKRLRKFRNKIKK
|
GLRKRLRKFRNKIKK
|
Cell membrane
|
Doxorubicin
|
S-(1-(2-carboxyethyl)-2,5-dioxopyrrolidin-3-yl)cysteine
|
|
|
pHLIP-M-DOX
|
pHLIP (GGEQ)
|
Undisclosed
|
Doxorubicin
|
Sulfo-SMCC
|
|
|
pHLIP-PAMAM-DOX
|
pHLIP (GGEQ)
|
Undisclosed
|
Doxorubicin
|
PAMAM linker
|
|
|
pHLIP-S-S-DOX
|
pHLIP (GGEQ)
|
Undisclosed
|
Doxorubicin
|
Disulfide bond
|
|
|
P4-chlorambucil
|
p4
|
Undisclosed
|
Chlorambucil
|
Gamma-Aminobutyric Acid
|
|
|
P4-Chlor-PEG-AuNP
|
p4
|
Undisclosed
|
Chlorambucil
|
Gamma-Aminobutyric Acid
|
|
|
DOXKGFRWR
|
KGFRWR
|
Undisclosed
|
Doxorubicin
|
Succinic Acid
|
|
|
Dox-S-S-GFLG-C6-[KTVRTSADE]
|
KTVRTSADE
|
Fibronectin (FN1)
|
Doxorubicin
|
S-S-GFLG-C6
|
|
|
DauQ=AoaGFLGD4G5HbPG
|
D4
|
Pro-epidermal growth factor (EGF)
|
Daunorubicin
|
GFLG
|
|
|
DauQ=AoaGFLGD4G5PEG
|
D4
|
Pro-epidermal growth factor (EGF)
|
Daunorubicin
|
GFLG
|
|
|
DauQ=AoaGFLGD4HbPG
|
D4
|
Pro-epidermal growth factor (EGF)
|
Daunorubicin
|
GFLG
|
|
|
DauQ=AoaGFLGD4PEG
|
D4
|
Pro-epidermal growth factor (EGF)
|
Daunorubicin
|
GFLG
|
|
|
PDC-L3
|
LRRY-fQWAV-β-Ala-H-Aib-Nle
|
Gastrin-releasing peptide receptor (GRPR)
|
Daunorubicin
|
LRRY
|
|
|
PDC-L4
|
LRRY-fQWAV-β-Ala-H-N-Me-Ala-Nle
|
Gastrin-releasing peptide receptor (GRPR)
|
Daunorubicin
|
LRRY
|
|
|
PDC-L6
|
LRRYFQWAVAH-Sta-Nle
|
Gastrin-releasing peptide receptor (GRPR)
|
Daunorubicin
|
LRRY
|
|
|
PDC-L2
|
LRRY-fQWAVGHL-Nle
|
Gastrin-releasing peptide receptor (GRPR)
|
Daunorubicin
|
LRRY
|
|
|
PDC-L5
|
LRRY-fQWAVGH-Sta-L
|
Gastrin-releasing peptide receptor (GRPR)
|
Daunorubicin
|
LRRY
|
|
|
Dau=Aoa-LRRYfQWAVGHStaL-NH2
|
LRRYfQWAVGHStaL-NH2
|
Bombesin receptor
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
Dau=Aoa-LRRYfQWAVβAlaHStaNle-NH2
|
LRRYfQWAVβAlaHStaNle-NH2
|
Bombesin receptor
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
PDC-L1
|
LRRY-QWAVGHL-Nle
|
Gastrin-releasing peptide receptor (GRPR)
|
Daunorubicin
|
LRRY
|
|
|
Dau=Aoa-LRRYQWAVGHLNle-NH2
|
LRRYQWAVGHLNle-NH2
|
Bombesin receptor
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
ABD-RGDK-DOXO
|
ABD-RGDK
|
Undisclosed
|
Doxorubicin
|
(6-maleimidocaproyl) hydrazone derivative
|
|
|
ABD-RPARPAR-DOXO
|
ABD-RPARPAR
|
Undisclosed
|
Doxorubicin
|
(6-maleimidocaproyl) hydrazone derivative
|
|
|
P6-chlorambucil
|
p6
|
Undisclosed
|
Chlorambucil
|
Gamma-Aminobutyric Acid
|
|
|
Cyclic NGR peptidedaunomycin conjugates 1
|
Cyclic NGR
|
Aminopeptidase N (ANPEP)
|
Daunorubicin
|
GFLG
|
|
|
GE11-DOX conjugate
|
GE11 peptide
|
Epidermal growth factor receptor (EGFR)
|
Doxorubicin
|
Disulfide bond
|
|
|
Ac-NleEHfRWGK(Dau=Aoa)-NH2
|
Ac-NleEHfRWGK-NH2
|
Melanocyte-stimulating hormone receptor (MC1R)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
pHA-AHX-VAP-DOX
|
DVAP
|
Endoplasmic reticulum chaperone BiP; D(2) dopamine receptor (HSPA5; DRD2)
|
Doxorubicin
|
AHX
|
|
|
pHA-AOHX-VAP-DOX
|
DVAP
|
Endoplasmic reticulum chaperone BiP; D(2) dopamine receptor (HSPA5; DRD2)
|
Doxorubicin
|
AOHX
|
|
|
Conjugates 1a
|
c(RGDfK)
|
Integrin alpha-V; Integrin beta-3 (ITGAV; ITGB3)
|
Chlorambucil
|
Amide bond
|
|
|
Conjugates 1c
|
c(RGDfK)
|
Integrin alpha-V; Integrin beta-3 (ITGAV; ITGB3)
|
Chlorambucil
|
Amide; Ester
|
|
|
Conjugates 8a
|
c(RGDfK)
|
Integrin alpha-V; Integrin beta-3 (ITGAV; ITGB3)
|
Chlorambucil
|
Amide bond
|
|
|
Conjugates 8b
|
c(RGDfK)
|
Integrin alpha-V; Integrin beta-3 (ITGAV; ITGB3)
|
Chlorambucil
|
Ester bond
|
|
|
DOXO-EMCH-(RNWELRLK-PEG4)2
|
RNWELRLK
|
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
|
Doxorubicin
|
EMCH
|
|
|
Ac-SYSNleEHFRWGK(Dau=Aoa)PV-NH2
|
Ac-SYSNleEHFRWGKPV-NH2
|
Melanocyte-stimulating hormone receptor (MC1R)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
Dau=Aoa-SYSNleEHFRWGK(Dau=Aoa)PV-NH2
|
Ac-SYSNleEHFRWGKPV-NH2
|
Melanocyte-stimulating hormone receptor (MC1R)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
Dau=Aoa-SYSNleEHFRWGKPV-NH2
|
Ac-SYSNleEHFRWGKPV-NH2
|
Melanocyte-stimulating hormone receptor (MC1R)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
E1-7 doxorubicin
|
E1-7
|
Undisclosed
|
Doxorubicin
|
Glutaric acid
|
|
|
rL-A9-DOX
|
rL-A9
|
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
|
Doxorubicin
|
Sulfo-SMCC
|
|
|
DauQ=AoaGFLGGE11G5HbPG
|
GE11
|
Pro-epidermal growth factor (EGF)
|
Daunorubicin
|
GFLG
|
|
|
DauQ=AoaGFLGGE11G5PEG
|
GE11
|
Pro-epidermal growth factor (EGF)
|
Daunorubicin
|
GFLG
|
|
|
DauQ=AoaGFLGGE11HbPG
|
GE11
|
Pro-epidermal growth factor (EGF)
|
Daunorubicin
|
GFLG
|
|
|
DauQ=AoaGFLGGE11PEG
|
GE11
|
Pro-epidermal growth factor (EGF)
|
Daunorubicin
|
GFLG
|
|
|
Peptide 18-4-doxorubicin
|
Peptide 18-4
|
Keratin, type II cytoskeletal 1 (KRT1)
|
Doxorubicin
|
Sulfo-SMCC
|
|
|
Peptide-Dox hydrazone
|
Peptide 18-4
|
Keratin, type II cytoskeletal 1 (KRT1)
|
Doxorubicin
|
(Z)-N'-(2-hydroxyethylidene)-6-(3-mercapto-2,5-dioxopyrrolidin-1-yl)hexanehydrazide
|
|
|
Dau=Aoa-TFFYGGSRGK(Dau=Aoa)RNNFK(Dau=Aoa)TEEY-OH
|
Angiopep-2
|
Prolow-density lipoprotein receptor-related protein 1; Low-density lipoprotein receptor-related protein 2 (LRP1; LRP2)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
Dau=Aoa-TFFYGGSRGK(Dau=Aoa)RNNFKTEEY-OH
|
Angiopep-2
|
Prolow-density lipoprotein receptor-related protein 1; Low-density lipoprotein receptor-related protein 2 (LRP1; LRP2)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
Dau=Aoa-TFFYGGSRGKRNNFK(Dau=Aoa)TEEY-OH
|
Angiopep-2
|
Prolow-density lipoprotein receptor-related protein 1; Low-density lipoprotein receptor-related protein 2 (LRP1; LRP2)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
Dau=Aoa-TFFYGGSRGKRNNFKTEEY-OH
|
Angiopep-2
|
Prolow-density lipoprotein receptor-related protein 1; Low-density lipoprotein receptor-related protein 2 (LRP1; LRP2)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
H-TFFYGGSRGK(Dau=Aoa)RNNFK(Dau=Aoa)TEEY-OH
|
Angiopep-2
|
Prolow-density lipoprotein receptor-related protein 1; Low-density lipoprotein receptor-related protein 2 (LRP1; LRP2)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
H-TFFYGGSRGK(Dau=Aoa)RNNFKTEEY-OH
|
Angiopep-2
|
Prolow-density lipoprotein receptor-related protein 1; Low-density lipoprotein receptor-related protein 2 (LRP1; LRP2)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
H-TFFYGGSRGK(Dau=Aoa-GFLG)RNNFKTEEY-OH
|
Angiopep-2
|
Prolow-density lipoprotein receptor-related protein 1; Low-density lipoprotein receptor-related protein 2 (LRP1; LRP2)
|
Daunorubicin
|
GFLG
|
|
|
H-TFFYGGSRGK(Dau=Aoa-VA)RNNFKTEEY-OH
|
Angiopep-2
|
Prolow-density lipoprotein receptor-related protein 1; Low-density lipoprotein receptor-related protein 2 (LRP1; LRP2)
|
Daunorubicin
|
2-(aminooxy)acetic acid-VA
|
|
|
H-TFFYGGSRGK(Dau=Aoa-VAGG)RNNFKTEEY-OH
|
Angiopep-2
|
Prolow-density lipoprotein receptor-related protein 1; Low-density lipoprotein receptor-related protein 2 (LRP1; LRP2)
|
Daunorubicin
|
2-(aminooxy)acetic acid-VAGG
|
|
|
H-TFFYGGSRGKRNNFK(Dau=Aoa)TEEY-OH
|
Angiopep-2
|
Prolow-density lipoprotein receptor-related protein 1; Low-density lipoprotein receptor-related protein 2 (LRP1; LRP2)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
c[DKP-RGD]-PEG4-Aoa=dau
|
c[DKP-RGD]
|
Indoleamine 2,3-dioxygenase 1 (IDO1)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
Dau=Aoa-GFLG-c[DKP-RGD]
|
c[DKP-RGD]
|
Indoleamine 2,3-dioxygenase 1 (IDO1)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
c[DKP-RGD]-PEG4-sC18(dau=Aoa-GFLG-Lys8)
|
c[DKP-RGD]-PEG4-sC18
|
Undisclosed
|
Daunorubicin
|
GFLG
|
|
|
c[DKP-RGD]-PEG4-sC18(dau=Aoa-Lys8)
|
c[DKP-RGD]-PEG4-sC18
|
Undisclosed
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
DT7-SS-DOX
|
DT7
|
Transferrin receptor protein 1 (TFRC)
|
Doxorubicin
|
SPDP
|
|
|
LT7-SS-DOX
|
DT7
|
Transferrin receptor protein 1 (TFRC)
|
Doxorubicin
|
SPDP
|
|
|
[4Lys(Ac),8Lys(Dau=Aoa)]-GnRH-III
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
[4Lys(Dau=Aoa),8Lys(Dau=Aoa)]-GnRH-III
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
[8Lys(Dau=Aoa-GFLG)]-GnRH-III
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
[8Lys(Dau=Aoa-K(Dau=Aoa))]GnRH-III
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
[8Lys(Dau=Aoa-LRRY)]-GnRH-III
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
[8Lys(Dox-O-glut)]-GnRH-III
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Doxorubicin
|
Glutaric acid
|
|
|
GnRH-III-[2ΔHis, 3D-Tic, 4Lys(Bu), 7D-Trp 8Lys(Dau=Aoa)]
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
GnRH-III-[2ΔHis, 3D-Tic, 4Lys(Bu), 8Lys(Dau=Aoa)]
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
GnRH-III-[2ΔHis, 3D-Tic, 7D-Trp 8Lys(Dau=Aoa)]
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
GnRH-III-[2ΔHis, 3D-Tic, 8Lys(Dau=Aoa)]
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
GnRH-III-[2ΔHis-3D-Tic, 8Lys(glutaryl-Val-Ala-PABC-Dau conjugate
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Val-Ala
|
|
|
GnRH-III-[2ΔHis-3D-Tic,8Lys(glutaryl-Val-Cit-PABC-Dau)] conjugate
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Val-Cit
|
|
|
GnRH-III-[2ΔHis-3D-Tic,8Lys(glutaryl-Val-Cit-PABC-diamine-PTX)] conjugate
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Glutaric acid
|
|
|
GnRH-III-[2His-3Trp,8Lys(glutaryl-Val-Ala-PABC-Dau)] conjugate
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Val-Ala
|
|
|
GnRH-III-[2His-3Trp,8Lys(glutaryl-Val-Cit-PABC-Dau)]
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Val-Cit
|
|
|
GnRH-III-[2His-3Trp,8Lys(glutaryl-Val-Cit-PABC-diamine-PTX)] conjugate
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Glutaric acid
|
|
|
GnRH-III-[3D-Tic, 4Lys(Bu), 7D-Trp 8Lys(Dau=Aoa)]
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
GnRH-III-[3D-Tic, 4Lys(Bu), 8Lys(Dau=Aoa)]
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
GnRH-III-[3D-Tic, 7D-Trp 8Lys(Dau=Aoa)]
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
GnRH-III-[3D-Tic, 8Lys(Dau=Aoa)]
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
GnRH-III-[3D-Trp, 4Lys(Bu), 8Lys(Dau=Aoa)]
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
GnRH-III-[3D-Trp, 8Lys(Dau=Aoa)]
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
GnRH-III-[4Lys(Bu), 6Asp(OMe), 8Lys(Dau=Aoa)]
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
GnRH-III-[4Lys(Bu), 8Lys(Dau=Aoa), 10ΔGly-NH-Et]
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
GnRH-III-[4Lys(Bu), 8Lys(Dau=Aoa)]
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
GnRH-III-[6Asp(OMe), 8Lys(Dau=Aoa)]
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
GnRH-III-[8Lys(Dau=Aoa), 10ΔGly-NH-Et]
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
GnRH-III-[8Lys(Dau=Aoa)]
|
GnRH-III
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
CRB-FFE-YSV
|
YSV
|
Undisclosed
|
Chlorambucil
|
FFE
|
|
|
Cyclic NGR peptidedaunomycin conjugates 2
|
Cyclic NGR 2
|
Aminopeptidase N (ANPEP)
|
Daunorubicin
|
GFLG
|
|
|
GFLG - Doxorubicin conjugate
|
GFLG
|
Integrin alpha-V; Integrin beta-3 (ITGAV; ITGB3)
|
Doxorubicin
|
Undisclosed
|
|
|
GFLG - Doxorubicine conjugate
|
GFLG
|
Integrin alpha-V; Integrin beta-3 (ITGAV; ITGB3)
|
Doxorubicin
|
Undisclosed
|
|
|
TPP-DOX-AP2H
|
AP2H
|
Mitochondria-eating protein (SPATA18)
|
Doxorubicin
|
Hydrazone bond
|
|
|
MPD1
|
DEVD
|
Caspase-3 (CASP3)
|
Doxorubicin
|
Amide bond
|
|
|
Cyclic NGR peptidedaunomycin conjugates 4
|
Cyclic NGR 4
|
Aminopeptidase N (ANPEP)
|
Daunorubicin
|
GFLG
|
|
|
Cyclic NGR peptidedaunomycin conjugates 3
|
Cyclic NGR 3
|
Aminopeptidase N (ANPEP)
|
Daunorubicin
|
GFLG
|
|
|
Cyclic NGR peptidedaunomycin conjugates 6
|
Cyclic NGR 6
|
Aminopeptidase N (ANPEP)
|
Daunorubicin
|
GFLG
|
|
|
Cyclic NGR peptidedaunomycin conjugates 5
|
Cyclic NGR 5
|
Aminopeptidase N (ANPEP)
|
Daunorubicin
|
GFLG
|
|
|
Octreotide doxorubicin conjugate
|
Octreotide
|
Somatostatin receptor type 1 (SSTR1)
|
Doxorubicin
|
Aminooxyacetic acid
|
|
|
[D-Lys6]-LH-RH - Doxorubicin conjugate
|
[D-Lys6]-LH-RH
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Doxorubicin
|
Glutaric acid
|
|
|
XHWSYKLRPG - Doxorubicin conjugate
|
[D-Lys6]-LH-RH
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Doxorubicin
|
Glutaric acid
|
|
|
Peptide 18-4 doxorubicin conjugate 1
|
Peptide 18-4
|
Keratin, type II cytoskeletal 1 (KRT1)
|
Doxorubicin
|
Glutaric acid
|
|
|
Peptide 18-4 doxorubicin conjugate 2
|
Peptide 18-4
|
Keratin, type II cytoskeletal 1 (KRT1)
|
Doxorubicin
|
Glutaric acid
|
|
|
ANG1009
|
Angiopep-2
|
Prolow-density lipoprotein receptor-related protein 1; Low-density lipoprotein receptor-related protein 2 (LRP1; LRP2)
|
Etoposide
|
Succinic Acid
|
|
|
sC18(dau-Aoa-Lys8)
|
c[DKP-RGD]-PEG4-sC18
|
Undisclosed
|
Daunorubicin
|
Aminooxyacetic acid
|
|
|
RWRWRWRW - Doxorubicin conjugate
|
RWRWRWRW
|
Undisclosed
|
Doxorubicin
|
Glutaric acid
|
|
|
WRWRWRWRWK - Doxorubicin conjugate
|
WRWRWRWRWK
|
Undisclosed
|
Doxorubicin
|
Glutaric acid
|
|
|
CGRKKRRQRRRPPQ - Doxorubicin conjugate
|
CGRKKRRQRRRPPQ
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
CGRKKRRQRRPPQ - Doxorubicin conjugate
|
CGRKKRRQRRPPQ
|
Undisclosed
|
Doxorubicin
|
Succinimide
|
|
|
CRRRRRRRRGGGPKKKKKK - Doxorubicin conjugate
|
CRRRRRRRRGGGPKKKKKK
|
Undisclosed
|
Doxorubicin
|
Succinimide
|
|
|
HAIYPRHGGCGMPKKKPTPIQLNP - Doxorubicin conjugate
|
HAIYPRHGGCGMPKKKPTPIQLNP
|
Undisclosed
|
Doxorubicin
|
Succinimide
|
|
|
CPRGGSVC - Doxorubicin conjugate 1
|
CPRGGSVC
|
Undisclosed
|
Doxorubicin
|
PEG
|
|
|
CPRGGSVC - Doxorubicin conjugate 2
|
CPRGGSVC
|
Undisclosed
|
Doxorubicin
|
PEG
|
|
|
GPLGIAGQ - Doxorubicin conjugate
|
GPLGIAGQ
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
CTVALPGGYVRVCVXVX - Doxorubicin conjugate
|
CTVALPGGYVRVCVXVX
|
Undisclosed
|
Doxorubicin
|
Benzyl
|
|
|
GKRKKKGKLGKKRPRSRC - Doxorubicin conjugate 1
|
GKRKKKGKLGKKRPRSRC
|
Undisclosed
|
Doxorubicin
|
4-Maleimidobutyric acid
|
|
|
GKRKKKGKLGKKRPRSRC - Doxorubicin conjugate
|
GKRKKKGKLGKKRPRSRC
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
SRRARRSPRHLGSGC - Doxorubicin conjugate 1
|
SRRARRSPRHLGSGC
|
Undisclosed
|
Doxorubicin
|
4-Maleimidobutyric acid
|
|
|
SRRARRSPRHLGSGC - Doxorubicin conjugate 2
|
SRRARRSPRHLGSGC
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
SRRARRSPRHLGSGC - Doxorubicin conjugate 3
|
SRRARRSPRHLGSGC
|
Undisclosed
|
Doxorubicin
|
4-Maleimidobutyric acid
|
|
|
CVKRGLKLRHVRPRVTRMDV - Doxorubicin conjugate
|
CVKRGLKLRHVRPRVTRMDV
|
Undisclosed
|
Doxorubicin
|
4-Maleimidobutyric acid
|
|
|
GPLGPAG - Doxorubicin conjugate 1
|
GPLGPAG
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
GPLGPAG - Doxorubicin conjugate
|
GPLGPAG
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
GPLGV - Doxorubicin conjugate 1
|
GPLGV
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
GPLGV - Doxorubicin conjugate 2
|
GPLGV
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
GPLG - Doxorubicin conjugate 1
|
GPLG
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
GPLG - Doxorubicin conjugate 2
|
GPLG
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
XASXQSL - Doxorubicin conjugate 1
|
XASXQSL
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
XASXQSL - Doxorubicin conjugate 2
|
XASXQSL
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
XASXQSL - Doxorubicin conjugate 3
|
XASXQSL
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
XASXQSL - Doxorubicin conjugate 4
|
XASXQSL
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
XASXQSL - Doxorubicin conjugate 5
|
XASXQSL
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
XASXQSL - Doxorubicin conjugate 6
|
XASXQSL
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
XASXQSL - Doxorubicin conjugate 7
|
XASXQSL
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
XASXQSL - Doxorubicin conjugate 8
|
XASXQSL
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
XASXQSL - Doxorubicin conjugate 9
|
XASXQSL
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
XASXQSL - Doxorubicin conjugate 10
|
XASXQSL
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
XASXQSL - Doxorubicin conjugate 11
|
XASXQSL
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
PASXQSL - Doxorubicin conjugate
|
PASXQSL
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
KASXQSL - Doxorubicin conjugate
|
KASXQSL
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
XASYQSL - Doxorubicin conjugate 1
|
XASYQSL
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
XASYQSL - Doxorubicin conjugate 2
|
XASYQSL
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
KASYQSL - Doxorubicin conjugate
|
KASYQSL
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
XYQSSSL - Doxorubicin conjugate
|
XYQSSSL
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
KYQSSSL - Doxorubicin conjugate
|
KYQSSSL
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
ANKASYQSSL - Doxorubicin conjugate
|
ANKASYQSSL
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
ANKASYQSSSL - Doxorubicin conjugate
|
ANKASYQSSSL
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
ANKASYQSASL - Doxorubicin conjugate
|
ANKASYQSASL
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
[C(WR)4K2(b-A)] - Doxorubicin & Curcumine conjugate
|
[C(WR)4K2(b-A)]
|
Undisclosed
|
Doxorubicin
|
Propanamide
|
|
|
[C(WR)4K2(b-A)] - Doxorubicin conjugate
|
[C(WR)4K2(b-A)]
|
Undisclosed
|
Doxorubicin
|
Propanamide
|
|
|
Activable cell-penetrating peptide (ACCP) - Doxorubicin conjugate
|
Activable cell-penetrating peptide (ACCP)
|
Undisclosed
|
Doxorubicin
|
Succinimide
|
|
|
Dipeptide 24 - Doxorubicin conjugate
|
Dipeptide 24
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
Dipeptide 46 - Chlorambucil conjugate
|
Dipeptide 46
|
Undisclosed
|
Chlorambucil
|
Undisclosed
|
|
|
EGFR-binding peptide (EBP) - Doxorubicin conjugate
|
EGFR-binding peptide (EBP)
|
Undisclosed
|
Doxorubicin
|
Glutaric acid
|
|
|
ErbB-2-binding peptide - Daunorubicin conjugate
|
ErbB-2-binding peptide
|
Undisclosed
|
Daunorubicin
|
Glutaric acid
|
|
|
High-affinity DNA binding peptide HyM10 - Chlorambucil conjugate
|
High-affinity DNA binding peptide HyM10
|
Undisclosed
|
Chlorambucil
|
Undisclosed
|
|
|
High-affinity DNA binding peptide HyQ10 - Chlorambucil conjugate
|
High-affinity DNA binding peptide HyQ10
|
Undisclosed
|
Chlorambucil
|
Undisclosed
|
|
|
Polyarginin 1 - Daunorubicine conjugate
|
Polyarginin 1
|
Undisclosed
|
Daunorubicin
|
Succinic Acid
|
|
|
Polyarginin 2 - Daunorubicine conjugate
|
Polyarginin 2
|
Undisclosed
|
Daunorubicin
|
Succinic Acid
|
|
|
Polyarginin 3 - Daunorubicine conjugate
|
Polyarginin 3
|
Undisclosed
|
Daunorubicin
|
Succinic Acid
|
|
|
Somatostatin backbone cyclic analog - Chlorambucil conjugate
|
Somatostatin backbone cyclic analog
|
Undisclosed
|
Chlorambucil
|
Butyramide
|
|
|
TAT-analogue 1 - Doxorubicin conjugate
|
TAT-analogue 1
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
TAT-analogue 3 - Doxorubicin conjugate
|
TAT-analogue 3
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
Tetrapeptide 19 - Doxorubicin conjugate
|
Tetrapeptide 19
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
Tetrapeptide 53 - Doxorubicin conjugate
|
Tetrapeptide 53
|
Undisclosed
|
Doxorubicin
|
Undisclosed
|
|
|
Tripeptide 93 - Chlorambucil conjugate 1
|
Tripeptide 93
|
Undisclosed
|
Chlorambucil
|
Undisclosed
|
|
|
Tripeptide 93 - Chlorambucil conjugate 2
|
Tripeptide 93
|
Undisclosed
|
Chlorambucil
|
Undisclosed
|
|
|
CRB-FFFK-cyclen
|
FFFK
|
Undisclosed
|
Chlorambucil
|
Amide bond
|
|
|
PDC-DOX2
|
KIGLFRWR
|
Undisclosed
|
Doxorubicin
|
Adipic acid
|
|
|
HA@PDC-DOX2
|
KIGLFRWR
|
Undisclosed
|
Doxorubicin
|
Adipic acid
|
|
|
FDPC-NPs
|
KIGLFRWR
|
Undisclosed
|
Doxorubicin
|
Succinic Acid
|
|
|
SMAC-FRRG-DOX
|
SMAC-FRRG
|
Undisclosed
|
Doxorubicin
|
Amide bond
|
|
|
DPV1047-E-Dox
|
DPV1047
|
Undisclosed
|
Doxorubicin
|
4-(3-((2-Amino-2-carboxyethyl)thio)-2,5-dioxopyrrolidin-1-yl)butanoic acid
|
|
|
DPV1047-A-Dox
|
DPV1047
|
Undisclosed
|
Doxorubicin
|
4-(3-((2-Amino-2-carboxyethyl)thio)-2,5-dioxopyrrolidin-1-yl)butanoic acid
|
|
|
DPV10-E-Dox
|
DPV10
|
Undisclosed
|
Doxorubicin
|
4-(3-((2-Amino-2-carboxyethyl)thio)-2,5-dioxopyrrolidin-1-yl)butanoic acid
|
|
|
DPV10-TE-Dox
|
DPV10
|
Undisclosed
|
Doxorubicin
|
S-(carboxymethyl)cysteine
|
|
|
DPV10-A-Dox
|
DPV10
|
Undisclosed
|
Doxorubicin
|
4-(3-((2-Amino-2-carboxyethyl)thio)-2,5-dioxopyrrolidin-1-yl)butanoic acid
|
|
|
DPV7b-E-Dox
|
DPV7b
|
Undisclosed
|
Doxorubicin
|
4-(3-((2-Amino-2-carboxyethyl)thio)-2,5-dioxopyrrolidin-1-yl)butanoic acid
|
|
|
DPV7b-TE-Dox
|
DPV7b
|
Undisclosed
|
Doxorubicin
|
S-(carboxymethyl)cysteine
|
|
|
[C15]-NPY-Dauno-MBS
|
[C15]-NPY
|
Undisclosed
|
Daunorubicin
|
2-(4-(3-mercapto-2,5-dioxopyrrolidin-1-yl)phenyl)acetic acid
|
|
|
[C15]-NPY-Dauno-HYD
|
[C15]-NPY
|
Undisclosed
|
Daunorubicin
|
2-(4-(3-mercapto-2,5-dioxopyrrolidin-1-yl)phenyl)acetic acid
|
|
|
[C15]-NPY-Doxo-MBS
|
[C15]-NPY
|
Undisclosed
|
Doxorubicin
|
2-(4-(3-mercapto-2,5-dioxopyrrolidin-1-yl)phenyl)acetic acid
|
|
|
NH2-GCKSYR-PC4AP-DOX
|
GCKSYR
|
Undisclosed
|
Doxorubicin
|
PC4AP
|
|
|
Ac-NH-GCKSYR-PC4AP-DOX
|
GCKSYR
|
Undisclosed
|
Doxorubicin
|
PC4AP
|
|
|
NH2-GCKSYR-C4AP-DOX
|
GCKSYR
|
Undisclosed
|
Doxorubicin
|
C4AP
|
|
|
Ac-NH-GCKSYR-C4AP-DOX
|
GCKSYR
|
Undisclosed
|
Doxorubicin
|
C4AP
|
|
|
Ac-NH-GCASYR-PC4AP-DOX
|
GCASYR
|
Undisclosed
|
Doxorubicin
|
PC4AP
|
|
|
NH2-GCASYR-PC4AP-DOX
|
GCASYR
|
Undisclosed
|
Doxorubicin
|
PC4AP
|
|
|
Ac-NH-GCASYR-C4AP-DOX
|
GCASYR
|
Undisclosed
|
Doxorubicin
|
C4AP
|
|
|
NH2-GCASYR-C4AP-DOX
|
GCASYR
|
Undisclosed
|
Doxorubicin
|
C4AP
|
|
|
NH2-GRDWQSCMEYKTHN-PC4AP-DOX
|
GRDWQSCMEYKTHN
|
Undisclosed
|
Doxorubicin
|
PC4AP
|
|
|
NH2-GRDWQSCMEYKTHN-C4AP-DOX
|
GRDWQSCMEYKTHN
|
Undisclosed
|
Doxorubicin
|
C4AP
|
|
|
Peptide 18-4 analog doxorubicin conjugate
|
Peptide 18-4 analog
|
Keratin, type II cytoskeletal 1 (KRT1)
|
Doxorubicin
|
4-yl 6-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexanoate
|
|
|
MAHNP-Dox conjugate
|
AHNP
|
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
|
Doxorubicin
|
Glutaric acid
|
Terminated in Phase 3
| PDC Info | PDC Name | Peptide | Receptor | Drug | Linker |
|---|---|---|---|---|---|
|
AEZS-108
|
[D-Lys6]-LH-RH
|
Gonadotropin-releasing hormone receptor (GNRHR)
|
Doxorubicin
|
Glutaric acid
|