Target Information
Target General Information | Top | |||||
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Target ID |
T71536
(Former ID: TTDI01205)
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Target Name |
Human Deoxyribonucleic acid minor groove (hDNA min)
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Gene Name |
NO-GeName
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 1 Target-related Diseases | + | ||||
1 | Lung cancer [ICD-11: 2C25] | |||||
UniProt ID |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
1 | Lurbinectedin | Drug Info | Approved | Small-cell lung cancer | [2] | |
Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
1 | Brostallicin | Drug Info | Phase 2 | Breast cancer | [3] | |
Mode of Action | [+] 3 Modes of Action | + | ||||
Inhibitor | [+] 2 Inhibitor drugs | + | ||||
1 | Lurbinectedin | Drug Info | [2] | |||
2 | Brostallicin | Drug Info | [1] | |||
Binder (minor groove binder) | [+] 3 Binder (minor groove binder) drugs | + | ||||
1 | Di-imidazole lexitropsin | Drug Info | [4] | |||
2 | Distamycin A | Drug Info | [5] | |||
3 | Netropsin | Drug Info | [7] | |||
Breaker | [+] 1 Breaker drugs | + | ||||
1 | Duocarmycin | Drug Info | [6] |
Drug Property Profile of Target | Top | |
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(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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"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 |
References | Top | |||||
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REF 1 | Brostallicin (PNU-166196), a new minor groove DNA binder: preclinical and clinical activity. Expert Opin Investig Drugs. 2009 Dec;18(12):1939-46. | |||||
REF 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020 | |||||
REF 3 | ClinicalTrials.gov (NCT00633165) Brostallicin Clinical Trial for Myxoid Liposarcoma. U.S. National Institutes of Health. | |||||
REF 4 | Defining GC-specificity in the minor groove: side-by-side binding of the di-imidazole lexitropsin to C-A-T-G-G-C-C-A-T-G. Structure. 1997 Aug 15;5(8):1033-46. | |||||
REF 5 | Development of distamycin-related DNA binding anticancer drugs. Expert Opin Investig Drugs. 2001 Sep;10(9):1703-14. | |||||
REF 6 | Structural studies of atom-specific anticancer drugs acting on DNA. Pharmacol Ther. 1999 Sep;83(3):181-215. | |||||
REF 7 | Drug-DNA binding specificity: binding of netropsin and distamycin to poly(d2NH2A-dT). Biopolymers. 1990;30(1-2):223-7. |
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