Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T06273
(Former ID: TTDS00191)
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| Target Name |
Poly [ADP-ribose] polymerase 1 (PARP1)
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| Synonyms |
Protein poly-ADP-ribosyltransferase PARP1; Poly[ADP-ribose] synthetase-1; Poly[ADP-ribose] synthase 1; Poly(ADP-ribose)polymerase-1; PPOL; PARP-1; NAD(+)Poly [ADP-ribose] polymerase-1 ADP-ribosyltransferase-1; NAD(+) ADP-ribosyltransferase-1; NAD(+) ADP-ribosyltransferase 1; DNA ADP-ribosyltransferase PARP1; ARTD1; ADPRT 1; ADPRT; ADP-ribosyltransferase diphtheria toxin-like 1
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| Gene Name |
PARP1
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 4 Target-related Diseases | + | ||||
| 1 | Acquired cutaneous blood vessel malformation [ICD-11: EF20] | |||||
| 2 | Fallopian tube cancer [ICD-11: 2C74] | |||||
| 3 | Ovarian cancer [ICD-11: 2C73] | |||||
| 4 | Peritoneal cancer [ICD-11: 2C51] | |||||
| Function |
Mainly mediates glutamate and aspartate ADP-ribosylation of target proteins: the ADP-D-ribosyl group of NAD(+) is transferred to the acceptor carboxyl group of glutamate and aspartate residues and further ADP-ribosyl groups are transferred to the 2'-position of the terminal adenosine moiety, building up a polymer with an average chain length of 20-30 units. Mediates the poly(ADP-ribosyl)ation of a number of proteins, including itself, APLF and CHFR. Also mediates serine ADP-ribosylation of target proteins following interaction with HPF1; HPF1 conferring serine specificity. Probably also catalyzes tyrosine ADP-ribosylation of target proteins following interaction with HPF1. Catalyzes the poly-ADP-ribosylation of histones in a HPF1-dependent manner. Involved in the base excision repair (BER) pathway by catalyzing the poly-ADP-ribosylation of a limited number of acceptor proteins involved in chromatin architecture and in DNA metabolism. ADP-ribosylation follows DNA damage and appears as an obligatory step in a detection/signaling pathway leading to the reparation of DNA strand breaks. In addition to base excision repair (BER) pathway, also involved in double-strand breaks (DSBs) repair: together with TIMELESS, accumulates at DNA damage sites and promotes homologous recombination repair by mediating poly-ADP-ribosylation. In addition to proteins, also able to ADP-ribosylate DNA: catalyzes ADP-ribosylation of DNA strand break termini containing terminal phosphates and a 2'-OH group in single- and double-stranded DNA, respectively. Required for PARP9 and DTX3L recruitment to DNA damage sites. PARP1-dependent PARP9-DTX3L-mediated ubiquitination promotes the rapid and specific recruitment of 53BP1/TP53BP1, UIMC1/RAP80, and BRCA1 to DNA damage sites. Acts as a regulator of transcription: positively regulates the transcription of MTUS1 and negatively regulates the transcription of MTUS2/TIP150. With EEF1A1 and TXK, forms a complex that acts as a T-helper 1 (Th1) cell-specific transcription factor and binds the promoter of IFN-gamma to directly regulate its transcription, and is thus involved importantly in Th1 cytokine production. Involved in the synthesis of ATP in the nucleus, together with NMNAT1, PARG and NUDT5. Nuclear ATP generation is required for extensive chromatin remodeling events that are energy-consuming. Poly-ADP-ribosyltransferase that mediates poly-ADP-ribosylation of proteins and plays a key role in DNA repair.
Click to Show/Hide
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| BioChemical Class |
Glycosyltransferases
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| UniProt ID | ||||||
| EC Number |
EC 2.4.2.30
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| Sequence |
MAESSDKLYRVEYAKSGRASCKKCSESIPKDSLRMAIMVQSPMFDGKVPHWYHFSCFWKV
GHSIRHPDVEVDGFSELRWDDQQKVKKTAEAGGVTGKGQDGIGSKAEKTLGDFAAEYAKS NRSTCKGCMEKIEKGQVRLSKKMVDPEKPQLGMIDRWYHPGCFVKNREELGFRPEYSASQ LKGFSLLATEDKEALKKQLPGVKSEGKRKGDEVDGVDEVAKKKSKKEKDKDSKLEKALKA QNDLIWNIKDELKKVCSTNDLKELLIFNKQQVPSGESAILDRVADGMVFGALLPCEECSG QLVFKSDAYYCTGDVTAWTKCMVKTQTPNRKEWVTPKEFREISYLKKLKVKKQDRIFPPE TSASVAATPPPSTASAPAAVNSSASADKPLSNMKILTLGKLSRNKDEVKAMIEKLGGKLT GTANKASLCISTKKEVEKMNKKMEEVKEANIRVVSEDFLQDVSASTKSLQELFLAHILSP WGAEVKAEPVEVVAPRGKSGAALSKKSKGQVKEEGINKSEKRMKLTLKGGAAVDPDSGLE HSAHVLEKGGKVFSATLGLVDIVKGTNSYYKLQLLEDDKENRYWIFRSWGRVGTVIGSNK LEQMPSKEDAIEHFMKLYEEKTGNAWHSKNFTKYPKKFYPLEIDYGQDEEAVKKLTVNPG TKSKLPKPVQDLIKMIFDVESMKKAMVEYEIDLQKMPLGKLSKRQIQAAYSILSEVQQAV SQGSSDSQILDLSNRFYTLIPHDFGMKKPPLLNNADSVQAKVEMLDNLLDIEVAYSLLRG GSDDSSKDPIDVNYEKLKTDIKVVDRDSEEAEIIRKYVKNTHATTHNAYDLEVIDIFKIE REGECQRYKPFKQLHNRRLLWHGSRTTNFAGILSQGLRIAPPEAPVTGYMFGKGIYFADM VSKSANYCHTSQGDPIGLILLGEVALGNMYELKHASHISKLPKGKHSVKGLGKTTPDPSA NISLDGVDVPLGTGISSGVNDTSLLYNEYIVYDIAQVNLKYLLKLKFNFKTSLW Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| ADReCS ID | BADD_A04698 | |||||
| HIT2.0 ID | T73LPO | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 3 Approved Drugs | + | ||||
| 1 | KU-0058948 | Drug Info | Approved | Ovarian cancer | [2] | |
| 2 | Nicotinamide | Drug Info | Approved | Inflammatory skin condition | [3], [4] | |
| 3 | Niraparib Tosylate | Drug Info | Approved | Peritoneal cancer | [5], [6] | |
| Clinical Trial Drug(s) | [+] 7 Clinical Trial Drugs | + | ||||
| 1 | CC-486 | Drug Info | Phase 3 | Myelodysplastic syndrome | [7] | |
| 2 | Nicaraven | Drug Info | Phase 3 | Cerebrovascular disease | [8] | |
| 3 | AG140699 | Drug Info | Phase 2 | Melanoma | [9] | |
| 4 | PMID27841036-Compound-37 | Drug Info | Phase 2 | Ovarian cancer | [10] | |
| 5 | Stenoparib | Drug Info | Phase 2 | Ovarian cancer | [11] | |
| 6 | AMXI 5001 | Drug Info | Phase 1/2 | Solid tumour/cancer | [12] | |
| 7 | NMS-03305293 | Drug Info | Phase 1 | Solid tumour/cancer | [13] | |
| Preclinical Drug(s) | [+] 2 Preclinical Drugs | + | ||||
| 1 | CPH-102 | Drug Info | Preclinical | Solid tumour/cancer | [14] | |
| 2 | PJ34 | Drug Info | Preclinical | Coronavirus infection | [15] | |
| Mode of Action | [+] 3 Modes of Action | + | ||||
| Inhibitor | [+] 127 Inhibitor drugs | + | ||||
| 1 | KU-0058948 | Drug Info | [16] | |||
| 2 | CC-486 | Drug Info | [18] | |||
| 3 | AG140699 | Drug Info | [19] | |||
| 4 | PMID27841036-Compound-37 | Drug Info | [20] | |||
| 5 | Stenoparib | Drug Info | [11] | |||
| 6 | AMXI 5001 | Drug Info | [21] | |||
| 7 | NMS-03305293 | Drug Info | [22] | |||
| 8 | 3-oxo-2,3-dihydro-1H-indazole-4-carboxamide derivative 1 | Drug Info | [20] | |||
| 9 | 3-oxo-2,3-dihydro-1H-indazole-4-carboxamide derivative 2 | Drug Info | [20] | |||
| 10 | 3-oxo-2,3-dihydro-1H-indazole-4-carboxamide derivative 3 | Drug Info | [20] | |||
| 11 | 3-oxo-2,3-dihydro-1H-indazole-4-carboxamide derivative 4 | Drug Info | [20] | |||
| 12 | 3-oxo-2,3-dihydro-1H-indazole-4-carboxamide derivative 5 | Drug Info | [20] | |||
| 13 | 3-phenyl isoquinolin-1(2H) derivative 1 | Drug Info | [20] | |||
| 14 | 3-phenyl isoquinolin-1(2H) derivative 2 | Drug Info | [20] | |||
| 15 | 4-Carboxamido-isoindolinone derivative 1 | Drug Info | [20] | |||
| 16 | 4-Carboxamido-isoindolinone derivative 2 | Drug Info | [20] | |||
| 17 | 4-Carboxamido-isoindolinone derivative 3 | Drug Info | [20] | |||
| 18 | 4-Carboxamido-isoindolinone derivative 4 | Drug Info | [20] | |||
| 19 | 4-Carboxamido-isoindolinone derivative 5 | Drug Info | [20] | |||
| 20 | 7-azaindole derivative 8 | Drug Info | [20] | |||
| 21 | Benzimidazole carboxamide derivative 1 | Drug Info | [20] | |||
| 22 | Dihydrodiazepinocarbazolone derivative 1 | Drug Info | [20] | |||
| 23 | Dihydropyrido phthalazinone derivative 1 | Drug Info | [20] | |||
| 24 | Dihydropyrido phthalazinone derivative 2 | Drug Info | [20] | |||
| 25 | Phthalazine derivative 3 | Drug Info | [20] | |||
| 26 | Phthalazine ketone derivative 1 | Drug Info | [20] | |||
| 27 | Phthalazine ketone derivative 2 | Drug Info | [20] | |||
| 28 | Phthalazine ketone derivative 3 | Drug Info | [20] | |||
| 29 | PMID27841036-Compound-33 | Drug Info | [20] | |||
| 30 | Quinazolinedione derivative 1 | Drug Info | [20] | |||
| 31 | Quinazolinedione derivative 2 | Drug Info | [20] | |||
| 32 | Quinazolinedione derivative 3 | Drug Info | [20] | |||
| 33 | Tetra-cyclic pyridophthalazinone derivative 1 | Drug Info | [20] | |||
| 34 | Tetra-hydro-quinoline derivative 1 | Drug Info | [20] | |||
| 35 | Tricyclic indole compound 13 | Drug Info | [20] | |||
| 36 | CPH-102 | Drug Info | [23] | |||
| 37 | PJ34 | Drug Info | [24] | |||
| 38 | NU1025 | Drug Info | [25] | |||
| 39 | (E)-N-(4-Phenylthiazol-2-yl) cinnamamide | Drug Info | [26] | |||
| 40 | 1,2,3,4,4a,5-hexahydrophenanthridin-6(10bH)-one | Drug Info | [26] | |||
| 41 | 1,7,8,9-tetrahydro-1,5-diaza-trindene-4,6-dione | Drug Info | [27] | |||
| 42 | 2,3-dihydro-1H-benzo[de]isoquinolin-1-one | Drug Info | [28] | |||
| 43 | 2,8-Dimethyl-3H-quinazolin-4-one | Drug Info | [29] | |||
| 44 | 2-(2-Chlorophenyl)-2H-indazole-7-carboxamide | Drug Info | [30] | |||
| 45 | 2-(3'-Methoxyphenyl) Benzimidazole-4-Carboxamide | Drug Info | [25] | |||
| 46 | 2-(3-Chlorophenyl)-2H-indazole-7-carboxamide | Drug Info | [30] | |||
| 47 | 2-(3-Piperidin-1-yl-propyl)-3H-quinazolin-4-one | Drug Info | [31] | |||
| 48 | 2-(4-Amino-phenyl)-8-hydroxy-3H-quinazolin-4-one | Drug Info | [29] | |||
| 49 | 2-(4-Amino-phenyl)-8-methyl-3H-quinazolin-4-one | Drug Info | [29] | |||
| 50 | 2-(4-Azido-phenyl)-8-methoxy-3H-quinazolin-4-one | Drug Info | [29] | |||
| 51 | 2-(4-Chlorophenyl)-2H-indazole-7-carboxamide | Drug Info | [30] | |||
| 52 | 2-(4-Chlorophenyl)-5-Quinoxalinecarboxamide | Drug Info | [32] | |||
| 53 | 2-(4-Hydroxy-phenyl)-8-methyl-3H-quinazolin-4-one | Drug Info | [29] | |||
| 54 | 2-(4-Methoxy-phenyl)-8-methyl-3H-quinazolin-4-one | Drug Info | [29] | |||
| 55 | 2-(4-methoxyphenyl)quinoline-8-carboxamide | Drug Info | [33] | |||
| 56 | 2-Benzyl-2H-indazole-7-carboxamide | Drug Info | [30] | |||
| 57 | 2-ethylquinoline-8-carboxamide | Drug Info | [33] | |||
| 58 | 2-Methylquinoline-8-carboxamide | Drug Info | [33] | |||
| 59 | 2-phenyl-2H-benzo[d][1,2,3]triazole-4-carboxamide | Drug Info | [30] | |||
| 60 | 2-phenyl-2H-indazole-7-carboxamide | Drug Info | [30] | |||
| 61 | 2-phenylpyrazolo-[1,5-a]pyridine-7-carboxamide | Drug Info | [30] | |||
| 62 | 2-phenylquinoline-8-carboxamide | Drug Info | [33] | |||
| 63 | 2H-Isoquinolin-1-one | Drug Info | [29] | |||
| 64 | 3-(4-aminophenyl)quinoxaline-5-carboxamide | Drug Info | [26] | |||
| 65 | 3-(4-cyanophenyl)quinoxaline-5-carboxamide | Drug Info | [26] | |||
| 66 | 3-(4-methoxyphenyl)quinoxaline-5-carboxamide | Drug Info | [26] | |||
| 67 | 3-aminobenzamide | Drug Info | [24], [29] | |||
| 68 | 3-aminobenzo[c][1,5]naphthyridin-6(5H)-one | Drug Info | [26] | |||
| 69 | 3-Ethenylquinoline-8-carboxamide | Drug Info | [33] | |||
| 70 | 3-Ethylquinoline-8-carboxamide | Drug Info | [33] | |||
| 71 | 3-Ethynylquinoline-8-carboxamide | Drug Info | [33] | |||
| 72 | 3-Hydroxy-benzamide | Drug Info | [29] | |||
| 73 | 3-Methoxybenzamide | Drug Info | [32] | |||
| 74 | 3-Methylquinoline-8-carboxamide | Drug Info | [33] | |||
| 75 | 3-Morpholin-4-ylmethyl-5H-phenanthridin-6-one | Drug Info | [34] | |||
| 76 | 3-Phenylquinoline-8-carboxamide | Drug Info | [33] | |||
| 77 | 3-Prop-1-ynylquinoline-8-carboxamide | Drug Info | [33] | |||
| 78 | 4-(4-Morpholin-4-yl-butyl)-2H-phthalazin-1-one | Drug Info | [34] | |||
| 79 | 4-(5-Morpholin-4-yl-pentyl)-2H-phthalazin-1-one | Drug Info | [34] | |||
| 80 | 4-amino-1,8-naphthalimide | Drug Info | [25], [27] | |||
| 81 | 4-benzylphthalazin-1(2H)-one | Drug Info | [26] | |||
| 82 | 4-methylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione | Drug Info | [27] | |||
| 83 | 5-amino-3,4-dihydroisoquinolin-1(2H)-one | Drug Info | [28] | |||
| 84 | 5-aminoisoquinolin-1(2H)-one | Drug Info | [33] | |||
| 85 | 5-Chloro-2-methyl-3H-quinazolin-4-one | Drug Info | [31] | |||
| 86 | 5-methylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione | Drug Info | [27] | |||
| 87 | 8-Amino-6H,11H-indeno[1,2-c]isoquinolin-5-one | Drug Info | [35] | |||
| 88 | 8-Fluoro-6H,11H-indeno[1,2-c]isoquinolin-5-one | Drug Info | [35] | |||
| 89 | 8-Hydroxy-2-(4-nitro-phenyl)-3H-quinazolin-4-one | Drug Info | [29] | |||
| 90 | 8-Hydroxy-2-phenyl-3H-quinazolin-4-one | Drug Info | [29] | |||
| 91 | 8-Methoxy-2-(4-nitro-phenyl)-3H-quinazolin-4-one | Drug Info | [29] | |||
| 92 | 8-Methoxy-2-methyl-3H-quinazolin-4-one | Drug Info | [29] | |||
| 93 | 8-Methoxy-2-phenyl-3H-quinazolin-4-one | Drug Info | [29] | |||
| 94 | 8-Methyl-2-(4-nitro-phenyl)-3H-quinazolin-4-one | Drug Info | [29] | |||
| 95 | 8-Methyl-2-phenyl-3H-quinazolin-4-one | Drug Info | [29] | |||
| 96 | 8-Nitro-6H,11H-indeno[1,2-c]isoquinolin-5-one | Drug Info | [35] | |||
| 97 | 9-Amino-6H,11H-indeno[1,2-c]isoquinolin-5-one | Drug Info | [35] | |||
| 98 | 9-Fluoro-6H,11H-indeno[1,2-c]isoquinolin-5-one | Drug Info | [35] | |||
| 99 | A-620223 | Drug Info | [23] | |||
| 100 | AG-014376 | Drug Info | [36] | |||
| 101 | ANG-2684 | Drug Info | [23] | |||
| 102 | ANG-2864 | Drug Info | [23] | |||
| 103 | Benzo[c][1,5]naphthyridin-6(5H)-one | Drug Info | [26] | |||
| 104 | BPI-704001 | Drug Info | [23] | |||
| 105 | BZ3 | Drug Info | [37] | |||
| 106 | BZ5 | Drug Info | [37] | |||
| 107 | BZ6 | Drug Info | [37] | |||
| 108 | Carba-Nicotinamide-Adenine-Dinucleotide | Drug Info | [32] | |||
| 109 | CEP-6800 | Drug Info | [38] | |||
| 110 | DR2313 | Drug Info | [19] | |||
| 111 | EB-47 | Drug Info | [19] | |||
| 112 | HYDAMTIQ | Drug Info | [23] | |||
| 113 | INO-1002 | Drug Info | [23] | |||
| 114 | KR-33889 | Drug Info | [23] | |||
| 115 | KU-58684 | Drug Info | [26] | |||
| 116 | ME0328 | Drug Info | [39] | |||
| 117 | N-(4-Phenylthiazol-2-yl)isonicotinamide | Drug Info | [26] | |||
| 118 | PD-128763 | Drug Info | [29], [32] | |||
| 119 | Pyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione | Drug Info | [27] | |||
| 120 | Pyrrolo[3,4-e]indole-1,3(2H,6H)-dione | Drug Info | [27] | |||
| 121 | Quinoline-8-carboxamide | Drug Info | [33] | |||
| 122 | S-070 | Drug Info | [23] | |||
| 123 | S-111 | Drug Info | [23] | |||
| 124 | Thieno-phenanthridin-6-one | Drug Info | [19] | |||
| 125 | TI3 | Drug Info | [37] | |||
| 126 | TI4 | Drug Info | [37] | |||
| 127 | [2(R,S)-2-Sulfanylheptanoyl]-Phe-Ala | Drug Info | [37] | |||
| Binder | [+] 1 Binder drugs | + | ||||
| 1 | Nicotinamide | Drug Info | [1] | |||
| Modulator | [+] 2 Modulator drugs | + | ||||
| 1 | Niraparib Tosylate | Drug Info | [17] | |||
| 2 | Nicaraven | Drug Info | [8] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| 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 | ||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-regulating microRNAs | ||||||
| Target-interacting Proteins | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 2 KEGG Pathways | + | ||||
| 1 | Base excision repair | |||||
| 2 | NF-kappa B signaling pathway | |||||
| Panther Pathway | [+] 1 Panther Pathways | + | ||||
| 1 | FAS signaling pathway | |||||
| PID Pathway | [+] 3 PID Pathways | + | ||||
| 1 | Integrin-linked kinase signaling | |||||
| 2 | Caspase Cascade in Apoptosis | |||||
| 3 | Notch-mediated HES/HEY network | |||||
| Reactome | [+] 1 Reactome Pathways | + | ||||
| 1 | Dual Incision in GG-NER | |||||
| WikiPathways | [+] 4 WikiPathways | + | ||||
| 1 | FAS pathway and Stress induction of HSP regulation | |||||
| 2 | Transcriptional activity of SMAD2/SMAD3:SMAD4 heterotrimer | |||||
| 3 | Nanoparticle triggered regulated necrosis | |||||
| 4 | Corticotropin-releasing hormone | |||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | beta-1,2,3-Triazolyl-nucleosides as nicotinamide riboside mimics. Nucleosides Nucleotides Nucleic Acids. 2009 Mar;28(3):238-59. | |||||
| REF 2 | 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81. | |||||
| REF 3 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1588). | |||||
| REF 4 | Drug information of Nicotinamide. United States Environmental Protection Agency. 2015 | |||||
| REF 5 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2018 | |||||
| REF 6 | 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85. | |||||
| REF 7 | J Clin Oncol 33, 2015 (suppl, abstr TPS7097). | |||||
| REF 8 | Inhibition of poly (ADP-ribose) polymerase as a protective effect of nicaraven in ionizing radiation- and ara-C-induced cell death. Anticancer Res. 2006 Sep-Oct;26(5A):3421-7. | |||||
| REF 9 | Critical Care Nephrology, Claudio Ronco,Rinaldo Bellomo,John A. Kellum. Page(444). | |||||
| REF 10 | ClinicalTrials.gov (NCT03878849) Investigation of 2X-121 in Patients With Advanced Ovarian Cancer Selected by the 2X-121 DRP (PREDICT 2X-121). U.S. National Institutes of Health. | |||||
| REF 11 | Clinical pipeline report, company report or official report of Allarity Therapeutics. | |||||
| REF 12 | ClinicalTrials.gov (NCT04503265) A Trial of AMXI-5001 for Treatment in Patients With Advanced Malignancies. U.S. National Institutes of Health. | |||||
| REF 13 | ClinicalTrials.gov (NCT04182516) Study of NMS-03305293 in Pts With Selected Advanced/Metastatic Solid Tumors. U.S. National Institutes of Health. | |||||
| REF 14 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006586) | |||||
| REF 15 | Coronaviruses - drug discovery and therapeutic options. Nat Rev Drug Discov. 2016 May;15(5):327-47. | |||||
| REF 16 | Structural basis for inhibitor specificity in human poly(ADP-ribose) polymerase-3. J Med Chem. 2009 May 14;52(9):3108-11. | |||||
| REF 17 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
| REF 18 | Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors. J Med Chem. 2003 Jan 16;46(2):210-3. | |||||
| REF 19 | Poly(ADP-ribose) polymerase and the therapeutic effects of its inhibitors. Nat Rev Drug Discov. 2005 May;4(5):421-40. | |||||
| REF 20 | PARP inhibitors as antitumor agents: a patent update (2013-2015).Expert Opin Ther Pat. 2017 Mar;27(3):363-382. | |||||
| REF 21 | AMXI-5001, a novel dual parp1/2 and microtubule polymerization inhibitor for the treatment of human cancers. Am J Cancer Res. 2020 Aug 1;10(8):2649-2676. | |||||
| REF 22 | NMS-P293, a PARP-1 selective inhibitor with no trapping activity and high CNS penetration, possesses potent in vivo efficacy and represents a novel therapeutic option for brain localized metastases and glioblastoma. Cancer Res 2018;78(13 Suppl):Abstract nr 4843. | |||||
| REF 23 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2771). | |||||
| REF 24 | Diabetic endothelial dysfunction: the role of poly(ADP-ribose) polymerase activation. Nat Med. 2001 Jan;7(1):108-13. | |||||
| REF 25 | The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. | |||||
| REF 26 | Design, synthesis, and cytoprotective effect of 2-aminothiazole analogues as potent poly(ADP-ribose) polymerase-1 inhibitors. J Med Chem. 2009 Feb 12;52(3):718-25. | |||||
| REF 27 | Synthesis and structure-activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors. Bioorg Med Chem Lett. 2006 Feb 15;16(4):938-42. | |||||
| REF 28 | Discovery and SAR of novel, potent and selective hexahydrobenzonaphthyridinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1). Bioorg Med Chem Lett. 2010 Jan 15;20(2):448-52. | |||||
| REF 29 | Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymeras... J Med Chem. 1998 Dec 17;41(26):5247-56. | |||||
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