Target Information

Target General Information

Top

Target ID

T86836 (Former ID: TTDI01911)

Target Name

Human Deoxyribonucleic acid (hDNA)

Gene Name

NO-GeName

Target Type

Successful target

[1]

Disease

[+] 21 Target-related Diseases

Acute myeloid leukaemia [ICD-11: 2A60]

Brain cancer [ICD-11: 2A00]

Breast cancer [ICD-11: 2C60-2C6Y]

Colorectal cancer [ICD-11: 2B91]

Cystic fibrosis [ICD-11: CA25]

Hodgkin lymphoma [ICD-11: 2B30]

Kaposi sarcoma [ICD-11: 2B57]

Leukaemia [ICD-11: 2A60-2B33]

Liver cancer [ICD-11: 2C12]

Lung cancer [ICD-11: 2C25]

Malignant digestive organ neoplasm [ICD-11: 2C11]

Mature T-cell lymphoma [ICD-11: 2A90]

Melanoma [ICD-11: 2C30]

Multiple myeloma [ICD-11: 2A83]

Myelodysplastic syndrome [ICD-11: 2A37]

Myeloproliferative neoplasm [ICD-11: 2A20]

Nutritional deficiency [ICD-11: 5B50-5B71]

Ovarian cancer [ICD-11: 2C73]

Pancreatic cancer [ICD-11: 2C10]

Prostate cancer [ICD-11: 2C82]

Solid tumour/cancer [ICD-11: 2A00-2F9Z]

UniProt ID

NOUNIPROTAC

Drugs and Modes of Action

Top

Approved Drug(s)

[+] 25 Approved Drugs

Adenine

Drug Info

Approved

Malnutrition

[15], [16]

Altretamine

Drug Info

Approved

Ovarian cancer

[17], [18]

Bendamustine hydrochloride

Drug Info

Approved

leukaemia

[19]

Bleomycin

Drug Info

Approved

Hodgkin lymphoma

[4]

Busulfan

Drug Info

Approved

Myeloproliferative syndrome

[20], [21]

Cyclophosphamide

Drug Info

Approved

Solid tumour/cancer

[22], [23]

Dactinomycin

Drug Info

Approved

Solid tumour/cancer

[24]

Daunorubicin

Drug Info

Approved

Acute myeloid leukaemia

[25], [4]

Dornase Alfa

Drug Info

Approved

Cystic fibrosis

[4]

DTI-015

Drug Info

Approved

Liver cancer

[1]

Ifosfamide

Drug Info

Approved

Solid tumour/cancer

[26], [27]

Lomustine

Drug Info

Approved

Brain cancer

[6], [28], [29]

Mechlorethamine

Drug Info

Approved

T-cell lymphoma

[6]

Melphalan

Drug Info

Approved

Multiple myeloma

[30], [31]

Melphalan flufenamide

Drug Info

Approved

Multiple myeloma

[32]

Mitomycin A

Drug Info

Approved

Solid tumour/cancer

[4]

Neocarzinostatin

Drug Info

Approved

Solid tumour/cancer

[6]

Pipobroman

Drug Info

Approved

Refractory chronic myeloid leukaemia

[6], [33], [34]

Pirarubicin

Drug Info

Approved

Breast cancer

[6], [35]

Procarbazine

Drug Info

Approved

Hodgkin lymphoma

[36], [37]

Radium-223-Dichloride

Drug Info

Approved

Prostate cancer

[38]

Streptozocin

Drug Info

Approved

Pancreatic cancer

[4]

Temozolomide

Drug Info

Approved

Grade IV astrocytoma

[39], [4]

Uracil mustard

Drug Info

Approved

Acute myeloid leukaemia

[4], [6], [40]

Dicycloplatin

Drug Info

Registered

Prostate cancer

[41]

Clinical Trial Drug(s)

[+] 34 Clinical Trial Drugs

Apaziquone

Drug Info

Phase 3

Non-muscle invasive bladder cancer

[42]

Glufosfamide

Drug Info

Phase 3

Pancreatic cancer

[43]

Laromustine

Drug Info

Phase 3

Solid tumour/cancer

[44]

Pafuramidine

Drug Info

Phase 3

Malaria

[45]

Taxol/Paraplatin/Herceptin

Drug Info

Phase 3

Breast cancer

[46]

VAL-083

Drug Info

Phase 3

Recurrent glioblastoma

[47]

13-DEOXYADRIAMYCIN HYDROCHLORIDE

Drug Info

Phase 2

Solid tumour/cancer

[52]

CGC-11047

Drug Info

Phase 2

Prostate cancer

[53]

CYSTEMUSTINE

Drug Info

Phase 2

Solid tumour/cancer

[54]

DM-CHOC-PEN

Drug Info

Phase 2

Brain cancer

[55]

JM216

Drug Info

Phase 2

Solid tumour/cancer

[56]

LADIRUBICIN

Drug Info

Phase 2

Breast cancer

[57]

NDDP

Drug Info

Phase 2

Solid tumour/cancer

[58]

PM-00104

Drug Info

Phase 2

Solid tumour/cancer

[59]

TETRAPLATIN TETRANITRATE

Drug Info

Phase 2

Solid tumour/cancer

[60]

TH-302

Drug Info

Phase 2

Soft tissue sarcoma

[61], [62]

TOL-3021

Drug Info

Phase 2

leukaemia

[63]

TROXACITABINE

Drug Info

Phase 2

Solid tumour/cancer

[64]

BN-2629

Drug Info

Phase 1/2

Solid tumour/cancer

[65]

GTU-TB vaccine

Drug Info

Phase 1/2

Mycobacterium infection

[66]

MBO7133

Drug Info

Phase 1/2

Liver cancer

[67]

SECTA belomycin

Drug Info

Phase 1/2

Solid tumour/cancer

[68]

5-FP

Drug Info

Phase 1

Solid tumour/cancer

[73]

BIZELESIN

Drug Info

Phase 1

Skin disease

[74]

DABIS MALEATE

Drug Info

Phase 1

Solid tumour/cancer

[75]

FFC-14A

Drug Info

Phase 1

Solid tumour/cancer

[76]

GALAMUSTINE HYDROCHLORIDE

Drug Info

Phase 1

Solid tumour/cancer

[77]

INO-3401

Drug Info

Phase 1

Influenza A virus H5N1 infection

[78]

INO-3510

Drug Info

Phase 1

Influenza A virus H1N1/H5N1 infection

[78]

LY-2334737

Drug Info

Phase 1

Solid tumour/cancer

[79]

NC-4016

Drug Info

Phase 1

Solid tumour/cancer

[80]

PENCLOMEDINE

Drug Info

Phase 1

Solid tumour/cancer

[81]

Pennvax-B

Drug Info

Phase 1

Human immunodeficiency virus infection

[82]

RH 1

Drug Info

Phase 1

Discovery agent

[83]

Discontinued Drug(s)

[+] 21 Discontinued Drugs

ARANOSE

Drug Info

Discontinued in Phase 3

Solid tumour/cancer

[85]

KW-2149

Drug Info

Discontinued in Phase 3

Solid tumour/cancer

[86]

AP-5346

Drug Info

Discontinued in Phase 2

Head and neck cancer

[88]

BBR-3438

Drug Info

Discontinued in Phase 2

Gastric adenocarcinoma

[89]

BISNAFIDE MESILATE

Drug Info

Discontinued in Phase 2

Solid tumour/cancer

[90]

CARZELESIN

Drug Info

Discontinued in Phase 2

Solid tumour/cancer

[91]

NB-506

Drug Info

Discontinued in Phase 2

Solid tumour/cancer

[92]

PIBROZELESIN HYDROCHLORIDE

Drug Info

Discontinued in Phase 2

Solid tumour/cancer

[93]

Tallimustine

Drug Info

Discontinued in Phase 2

Solid tumour/cancer

[94]

TOPIXANTRONE HYDROCHLORIDE

Drug Info

Discontinued in Phase 2

Gastric adenocarcinoma

[95]

TV-4710

Drug Info

Discontinued in Phase 2

Systemic lupus erythematosus

[84]

FK-973

Drug Info

Discontinued in Phase 1

Solid tumour/cancer

[97]

PLD-147

Drug Info

Discontinued in Phase 1

Solid tumour/cancer

[98]

RB-6145

Drug Info

Discontinued in Phase 1

Solid tumour/cancer

[99]

S-23906-1

Drug Info

Discontinued in Phase 1

Solid tumour/cancer

[100]

SR-271425

Drug Info

Discontinued in Phase 1

Solid tumour/cancer

[101]

SW-33377

Drug Info

Discontinued in Phase 1

Solid tumour/cancer

[102]

ZD-2767

Drug Info

Discontinued in Phase 1

Solid tumour/cancer

[103]

Bisbenzimide (Hoechst 33258)

Drug Info

Terminated

Solid tumour/cancer

[105]

BW-A502U

Drug Info

Terminated

Solid tumour/cancer

[106]

Doxorubicin-CEA conjugate

Drug Info

Terminated

Breast cancer

[107]

Preclinical Drug(s)

[+] 1 Preclinical Drugs

Indol-3-carbinol

Drug Info

Preclinical

Fungal infection

[104]

Mode of Action

[+] 7 Modes of Action

Binder

[+] 32 Binder drugs

Adenine

Drug Info

[108], [109]

DTI-015

Drug Info

[1]

Melphalan flufenamide

Drug Info

[32]

Pipobroman

Drug Info

[123]

Laromustine

Drug Info

[131]

Taxol/Paraplatin/Herceptin

Drug Info

[46]

CYSTEMUSTINE

Drug Info

[136]

LADIRUBICIN

Drug Info

[138]

NDDP

Drug Info

[139]

TETRAPLATIN TETRANITRATE

Drug Info

[141]

TROXACITABINE

Drug Info

[144]

BN-2629

Drug Info

[145]

MBO7133

Drug Info

[147]

SECTA belomycin

Drug Info

[148]

5-FP

Drug Info

[149]

DABIS MALEATE

Drug Info

[151]

FFC-14A

Drug Info

[152]

ARANOSE

Drug Info

[161]

KW-2149

Drug Info

[162]

BBR-3438

Drug Info

[164]

CARZELESIN

Drug Info

[166]

PIBROZELESIN HYDROCHLORIDE

Drug Info

[168]

FK-973

Drug Info

[171]

PLD-147

Drug Info

[172]

RB-6145

Drug Info

[173]

S-23906-1

Drug Info

[174]

SR-271425

Drug Info

[175]

SW-33377

Drug Info

[176]

ZD-2767

Drug Info

[177]

Indol-3-carbinol

Drug Info

[104]

BW-A502U

Drug Info

[179]

AMBAZONE

Drug Info

[181]

Breaker

[+] 7 Breaker drugs

Altretamine

Drug Info

[110]

Bleomycin

Drug Info

[111]

Dactinomycin

Drug Info

[115]

Dornase Alfa

Drug Info

[117]

Streptozocin

Drug Info

[125]

Talisomycin

Drug Info

[111]

Nitracrine

Drug Info

[183]

Modulator

[+] 28 Modulator drugs

Bendamustine hydrochloride

Drug Info

[19]

Busulfan

Drug Info

[112]

Cyclophosphamide

Drug Info

[113], [114]

Ifosfamide

Drug Info

[118]

Melphalan

Drug Info

[121]

Neocarzinostatin

Drug Info

[4]

Pirarubicin

Drug Info

[4]

Radium-223-Dichloride

Drug Info

[38]

Temozolomide

Drug Info

[126]

Uracil mustard

Drug Info

[127]

Apaziquone

Drug Info

[129]

Glufosfamide

Drug Info

[130]

Pafuramidine

Drug Info

[132]

VAL-083

Drug Info

[133]

13-DEOXYADRIAMYCIN HYDROCHLORIDE

Drug Info

[134]

CGC-11047

Drug Info

[135]

DM-CHOC-PEN

Drug Info

[137]

JM216

Drug Info

[134]

PM-00104

Drug Info

[140]

TH-302

Drug Info

[142]

TOL-3021

Drug Info

[143]

LY-2334737

Drug Info

[156], [157]

PENCLOMEDINE

Drug Info

[159]

RH 1

Drug Info

[83]

Tallimustine

Drug Info

[169]

Doxorubicin-CEA conjugate

Drug Info

[126]

doxorubicin-LL2 conjugate

Drug Info

[182]

doxorubicin-peptide-PEG conjugate

Drug Info

[182]

Intercalator

[+] 3 Intercalator drugs

Daunorubicin

Drug Info

[116]

Mechlorethamine

Drug Info

[120]

Ethidium

Drug Info

[116]

Inhibitor

[+] 14 Inhibitor drugs

Lomustine

Drug Info

[119]

Dicycloplatin

Drug Info

[128]

BIZELESIN

Drug Info

[150]

NC-4016

Drug Info

[158]

AP-5346

Drug Info

[163]

BISNAFIDE MESILATE

Drug Info

[165]

NB-506

Drug Info

[167]

TOPIXANTRONE HYDROCHLORIDE

Drug Info

[170]

TV-4710

Drug Info

[84]

2-(3,4-Dihydroxyphenyl)Acetic Acid

Drug Info

[180]

alphabeta-methyleneADP

Drug Info

[180]

Beta-D-Glucose

Drug Info

[180]

Lipid Fragment

Drug Info

[180]

Thiamin Diphosphate

Drug Info

[180]

Antagonist

[+] 1 Antagonist drugs

GALAMUSTINE HYDROCHLORIDE

Drug Info

[153]

Binder (minor groove binder)

[+] 1 Binder (minor groove binder) drugs

Bisbenzimide (Hoechst 33258)

Drug Info

[178]

Drug Property Profile of Target

Top

(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Co-Targets

Top

Co-Targets

Co-Targets Info

References

Top

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FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 016245.

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ClinicalTrials.gov (NCT01746992) CTOP/ITE/MTX Compared With CHOP as the First-line Therapy for Newly Diagnosed Young Patients With T Cell Lymphoma. U.S. National Institutes of Health.

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FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 016785.

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Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.

REF 39

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Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031375)

REF 42

ClinicalTrials.gov (NCT00598806) Phase 3 Trial of Single-Dose Intravesical EOquin as a Surgical Adjuvant for Noninvasive Bladder Cancer. U.S. National Institutes of Health.

REF 43

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 44

ClinicalTrials.gov (NCT00112554) Cytarabine With or Without VNP40101M in Treating Patients With Relapsed Acute Myeloid Leukemia. U.S. National Institutes of Health.

REF 45

ClinicalTrials.gov (NCT00302341) DB289 Versus TMP-SMX for the Treatment of Acute Pneumocystis Jiroveci Pneumonia (PCP). U.S. National Institutes of Health.

REF 46

Randomized phase III study of trastuzumab, paclitaxel, and carboplatin compared with trastuzumab and paclitaxel in women with HER-2-overexpressing metastatic breast cancer. J Clin Oncol. 2006 Jun 20;24(18):2786-92.

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Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

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ClinicalTrials.gov (NCT04315324) Study to Test AKR1C3-Activated Prodrug OBI-3424 (OBI-3424) in Patients With Relapsed/Refractory T-Cell Acute Lymphoblastic Leukemia (T-ALL). U.S. National Institutes of Health.

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ClinicalTrials.gov (NCT01233375) Study to Evaluate Efficacy of CO-1.01 as Second Line Therapy for Gemcitabine-Refractory Stage IV Pancreatic Adenocarcinoma. U.S. National Institutes of Health.

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ClinicalTrials.gov (NCT00123877) Study of GPX-100 in the Treatment of Metastatic Breast Cancer. U.S. National Institutes of Health.

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ClinicalTrials.gov (NCT00585416) Study of CGC-11047 in Patients With Metastatic Hormone Refractory Prostate Cancer. U.S. National Institutes of Health.

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ClinicalTrials.gov (NCT00004033) Liposomal-Cisplatin Analogue (L-NDDP) in Treating Patients With Malignant Pleural Mesothelioma. U.S. National Institutes of Health.

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ClinicalTrials.gov (NCT00900562) Clinical Trial of PM00104 (Zalypsis) in Patients With Advanced and/or Metastatic Endometrial or Cervical Cancer Previously Treated With One Line of Systemic Chemotherapy. U.S. National Institutes of Health.

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ClinicalTrials.gov (NCT00014547) BBR 3464 in Treating Patients With Metastatic Small Cell Lung Cancer That Has Not Responded to Previous Treatment. U.S. National Institutes of Health.

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ClinicalTrials.gov (NCT01403610) Safety and Efficacy Study of TH-302 CNS Penetration in Recurrent High Grade Astrocytoma Following Bevacizumab. U.S. National Institutes of Health.

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ClinicalTrials.gov (NCT00129948) Study for Patients With Relapsed or Refractory Acute Myeloid Leukemia (AML). U.S. National Institutes of Health.

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DNA damage and sequence specificity of DNA binding of the new anti-cancer agent 1,4-bis(2'-chloroethyl)-1,4-diazabicyclo-[2.2.1] heptane dimaleate (Dabis maleate)Broggini M1, Hartley JA, Mattes WB, Ponti M, Kohn KW, D'Incalci M.Author information1Laboratory of Cancer Chemotherapy, Istituto di Ricerche Farmacologiche Mario Negri, Milan, Italy.Erratum inBr J Cancer 1990 Jul;62(1):172. AbstractThe DNA damage and the sequence specificity of guanine-N7 alkylation produced by the novel, positively charged, antineoplastic agent 1,4-bis(2'-chloroethyl)-1,4-diazabicyclo-[2.2.1] heptane dimaleate (Dabis maleate) and its uncharged tertiary amine analogue 1,4-bis(2'-chloroethyl)-1,4-diazacyclohexane (Dabis analogue) were investigated in L1210 cells and isolated DNA. Both compounds are cytotoxic in vitro causing an arrest of L1210 cells in G2/M phase of the cell cycle. In isolated DNA, Dabis maleate alkylates guanine at the N7-position with some differences in specificity compared to other alkylating agents (e.g. nitrogen mustard). Significant differences are also evident between Dabis maleate and Dabis analogue, suggesting that Dabis analogue is not the sole alkylating species of Dabis maleate. Using the alkaline elution technique a moderate number of DNA interstrand cross-links were detected in L1210 cells treated with both compounds, which were completely repaired within 24 h. Dabis maleate and Dabis analogue do not cause DNA single strand breaks or DNA protein cross-links at the doses at which DNA interstrand cross-links were detected.PMID: 2393411 [PubMed - indexed for MEDLINE] PMCID: PMC1971404 Free PMC ArticleSharePublication Types, MeSH Terms, SubstancesPublication TypesResearch Support, Non-U.S. Gov'tMeSH TermsAnimalsAntineoplastic Agents/pharmacology*Base SequenceBicycloCompounds/pharmacology*Bicyclo Compounds, Heterocyclic*Bridged Compounds/pharmacology*Cell Survival/drug effectsDNA Damage*DNA, Neoplasm/drug effects*Dose-Response Relationship, DrugHumansInterphase/drug effectsLeukemia L1210/pathologyTumor Cells, Cultured/drug effectsSubstancesAntineoplastic AgentsBicyclo CompoundsBicyclo Compounds, HeterocyclicBridged CompoundsDNA, Neoplasm1,4-bis(2'-chloroethyl)-1,4-diazabicyclo(2.2.1)heptaneLinkOut - more resourcesFull Text SourcesEurope PubMed CentralPubMed CentralPubMed Central CanadaOther Literature SourcesCOS Scholar UniverseAccess more work from the authors - ResearchGateMiscellaneousNCI CPTAC Assay PortalPubMed Commons home Br J Cancer. 1990 Feb;61(2):285-9.

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